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EC number: 295-253-9 | CAS number: 91994-95-5
- Life Cycle description
- Uses advised against
- Endpoint summary
- Appearance / physical state / colour
- Melting point / freezing point
- Boiling point
- Density
- Particle size distribution (Granulometry)
- Vapour pressure
- Partition coefficient
- Water solubility
- Solubility in organic solvents / fat solubility
- Surface tension
- Flash point
- Auto flammability
- Flammability
- Explosiveness
- Oxidising properties
- Oxidation reduction potential
- Stability in organic solvents and identity of relevant degradation products
- Storage stability and reactivity towards container material
- Stability: thermal, sunlight, metals
- pH
- Dissociation constant
- Viscosity
- Additional physico-chemical information
- Additional physico-chemical properties of nanomaterials
- Nanomaterial agglomeration / aggregation
- Nanomaterial crystalline phase
- Nanomaterial crystallite and grain size
- Nanomaterial aspect ratio / shape
- Nanomaterial specific surface area
- Nanomaterial Zeta potential
- Nanomaterial surface chemistry
- Nanomaterial dustiness
- Nanomaterial porosity
- Nanomaterial pour density
- Nanomaterial photocatalytic activity
- Nanomaterial radical formation potential
- Nanomaterial catalytic activity
- Endpoint summary
- Stability
- Biodegradation
- Bioaccumulation
- Transport and distribution
- Environmental data
- Additional information on environmental fate and behaviour
- Ecotoxicological Summary
- Aquatic toxicity
- Endpoint summary
- Short-term toxicity to fish
- Long-term toxicity to fish
- Short-term toxicity to aquatic invertebrates
- Long-term toxicity to aquatic invertebrates
- Toxicity to aquatic algae and cyanobacteria
- Toxicity to aquatic plants other than algae
- Toxicity to microorganisms
- Endocrine disrupter testing in aquatic vertebrates – in vivo
- Toxicity to other aquatic organisms
- Sediment toxicity
- Terrestrial toxicity
- Biological effects monitoring
- Biotransformation and kinetics
- Additional ecotoxological information
- Toxicological Summary
- Toxicokinetics, metabolism and distribution
- Acute Toxicity
- Irritation / corrosion
- Sensitisation
- Repeated dose toxicity
- Genetic toxicity
- Carcinogenicity
- Toxicity to reproduction
- Specific investigations
- Exposure related observations in humans
- Toxic effects on livestock and pets
- Additional toxicological data
Toxicity to reproduction
Administrative data
- Endpoint:
- screening for reproductive / developmental toxicity
- Type of information:
- experimental study
- Adequacy of study:
- key study
- Study period:
- 22 August 2013 - 17 October 2013
- Reliability:
- 1 (reliable without restriction)
- Rationale for reliability incl. deficiencies:
- other: The study is GLP compliant and follow the OECD 422 guideline. Acceptable with no restrictions.
- Justification for type of information:
- A discussion and report on the read across strategy is given as an attachment in Section 13.
Cross-referenceopen allclose all
- Reason / purpose for cross-reference:
- read-across: supporting information
Reference
- Endpoint:
- screening for reproductive / developmental toxicity
- Type of information:
- read-across based on grouping of substances (category approach)
- Adequacy of study:
- key study
- Study period:
- 22 August 2013 - 17 October 2013
- Reliability:
- 1 (reliable without restriction)
- Rationale for reliability incl. deficiencies:
- other: The study is GLP compliant and follow the OECD 422 guideline. Acceptable with no restrictions.
- Justification for type of information:
- A discussion and report on the read across strategy is given as an attachment in Section 13.
- Reason / purpose for cross-reference:
- read-across source
- Reason / purpose for cross-reference:
- other: Independent Analysis
- Reason / purpose for cross-reference:
- other: GLP Certificate
- Qualifier:
- according to guideline
- Guideline:
- OECD Guideline 422 (Combined Repeated Dose Toxicity Study with the Reproduction / Developmental Toxicity Screening Test)
- Deviations:
- no
- GLP compliance:
- yes (incl. QA statement)
- Specific details on test material used for the study:
- - Name of test material: Nonene, branched
- CAS No.:97280-95-0
- Substance type: UVCB
- Physical state: Clear colorless liquid
- Analytical purity: 100%
- Lot/batch No.: TQ-12-2003-23042013
- Data received: 29 April 2013
- Label: Nonene Sampling Date Apr 22.2013
- Expiration date of the lot/batch: 23 April2014
Nonene, branched, CAS# 97280-95-0 used in this study was a typical production sample, according to the details included in the boundary composition in IUCLID section 1.2. Nonene, branched was chosen in the Higher Olefins category testing strategy because it represents a substance with high tri-sub content (category range 1 – 65%), odd carbon number (C9 odd 90%). Please see the testing strategy attached in section 13 for further details. - Species:
- rat
- Strain:
- other: Wistar Han™:RccHan™:WIST strain rats
- Sex:
- male/female
- Details on test animals or test system and environmental conditions:
- TEST ANIMALS
- Source: Harlan Laboratories U.K. Ltd., Blackthorn, Bicester, Oxon, UK.
- Age at study initiation: 12 weeks old
- Weight at study initiation: (P) Males: 311 to 375 g; Females: 194 to 222 g.
- Housing: Pre-mating: groups of four animals were housed in solid floor polypropylene cages with stainless steel mesh lids and softwood flake bedding (Datesand Ltd., Cheshire, UK). Pairing phase: polypropylene grid floor cages suspended over trays lined with absorbent paper on a one male: one female basis within each dose group. Post mating: the males were returned to their original cages. Mated females were housed individually during gestation and lactation in solid floor polypropylene cages with stainless steel mesh lids and softwood flakes.
- Use of restrainers for preventing ingestion (if dermal): yes/no
- Diet (e.g. ad libitum): A pelleted diet (Rodent 2018C Teklad Global Certified Diet, Harlan Laboratories U.K. Ltd., Oxon, UK.)
- Water (e.g. ad libitum): free access to food and water
- Acclimation period: 5 days
ENVIRONMENTAL CONDITIONS
- Temperature (°C): 21 +/-2°C
- Humidity (%): 55 =/- 15%
- Air changes (per hr): at least 15 air changes per hour. The low intensity fluorescent lighting was controlled to give twelve hours continuous light
- Photoperiod (hrs dark / hrs light): 12 hr dark and 12 hr light
The study was performed between 10 June 2013 and 10 June 2014. The in-life phase of the study was conducted between 22 August 2013 (first day of treatment) and 17 October 2013 (final day of necropsy). - Route of administration:
- oral: gavage
- Vehicle:
- arachis oil
- Details on exposure:
- PREPARATION OF DOSING SOLUTIONS:
DIET PREPARATION
- Mixing appropriate amounts with (Type of food): Arachis oil BP
- Storage temperature of food: 4 C
VEHICLE
- Amount of vehicle (if gavage): 4 ml/kg
- Concentration in vehicle:
- Control: 0 ml/kg
- Low: 25 mg/ml
- Intermediate: 75 mg/ml
- High: 250 mg/ml
- Lot/batch no. (if required): 2018C-020713MA
- The volume of the test and control item administrated to each animal was based on the most recent scheduled body weight and was adjusted at weekly intervals. - Details on mating procedure:
- - M/F ratio per cage: 1/1
- Length of cohabitation:15 days
- Proof of pregnancy referred to as day 0 of pregnancy
- After successful mating each pregnant female was caged individually during gestation and lactation in solid floor polypropylene cages. - Analytical verification of doses or concentrations:
- yes
- Duration of treatment / exposure:
- 6 weeks
- Frequency of treatment:
- The test item was administrated daily by gavage using a stainless cannula attached to a disposable plastic syringe. Control animals were treated in an identical manner with 4 ml/kg of Arachis oil BP.
- Details on study schedule:
- i. Groups of twelve male and twelve female animals were treated daily at the appropriate dose level throughout the study (except for females during parturition where applicable). The first day of dosing was designated as Day 1 of the study.
ii. Prior to the start of treatment and once weekly thereafter, all animals were observed for signs of functional/behavioral toxicity.
iii. On Day 15, animals were paired on a 1 male: 1 female basis within each dose group for a maximum of fourteen days.
iv. Following evidence of mating (designated as Day 0 post coitum) the males were returned to their original cages and females were transferred to individual cages.
v. On completion of the pairing phase (during Week 6), five selected males per dose group were evaluated for functional/sensory responses to various stimuli.
vi. Pregnant females were allowed to give birth and maintain their offspring until Day 5 post partum. Litter size, offspring weight and sex, surface righting and clinical signs were also recorded during this period.
vii. At Day 4 post partum, five selected females per dose group were evaluated for functional/sensory responses to various stimuli.
viii. Blood samples were taken from five males from each dose group for hematological and blood chemical assessments on Day 42. The male dose groups were killed and examined macroscopically on Day 43.
ix. Blood samples were taken from five randomly selected females from each dose group for hematological and blood chemical assessment on Day 4 post partum. At Day 5 post partum, all females and surviving offspring were killed and examined macroscopically. Any female which did not produce a pregnancy was also killed and examined macroscopically. - Dose / conc.:
- 100 mg/kg bw/day (actual dose received)
- Remarks:
- Doses / Concentrations:
Basis: actual ingested 100 mg/kg bw/day - Dose / conc.:
- 300 mg/kg bw/day (actual dose received)
- Remarks:
- Doses / Concentrations:
Basis: actual ingested 300 mg/kg bw/day - Dose / conc.:
- 1 000 mg/kg bw/day (actual dose received)
- Remarks:
- Doses / Concentrations:
Basis: actual ingested 1000 mg/kg bw/day - No. of animals per sex per dose:
- Three groups, each of twelve males and twelve females
- Control animals:
- yes, concurrent vehicle
- Details on study design:
- - Dose selection rationale: Dose selected during the Range-finding experiment - Study Number 41301414
- Parental animals: Observations and examinations:
- Clinical Observations:
Signs of toxicity, ill-health and behavioural change immediately before dosing, soon after dosing, and one hour after dosing throughout the treatment period.
Functional Observations:
All animals were observed for signs of functional/behavioural toxicity prior to the start of treatment and at weekly intervals thereafter.
Functional performance tests were also performed on five selected males and females from each dose level, prior to termination, together with an assessment of sensory reactivity to various stimuli.
- behavioural assessment
- functional Performance Tests
- Sensory Reactivity
Body Weight:
Individual body weights: Day 1 (prior to dosing), weekly for surviving males until termination and weekly for females until mating was evident.
Female: Days 0, 7, 14 and 20 post coitum, and on Days 1, 4 post partum and terminal kill.
Food Consumption:
Pre-pairing period and after (male): weekly
Females showing evidence of mating: post coitum Days 0-7, 7-14 and 14-20.
Females with live litters: Days 1 and 4 post partum.
Food efficiency:
Males (throughout the study period-with the exception of the mating phase, and females during the pre-pairing phase
Water Consumption:
Daily- visual inspection of the water bottles
Reproductive Performance:
Presence of ejected copulation plugs and each female was examined for the presence of a copulation plug in the vagina.
A vaginal smear was prepared for each female and the stage of oestrus or the presence of sperm was recorded.
The presence of sperm within the vaginal smear and/or vaginal plug in situ was taken as positive evidence of mating (Day 0 of gestation).
Pregnancy and Parturition:
Pregnant females: observations at approximately 0830, 1230 and 1630 hours and around the period of expected parturition (08.30 and 12.30 hr at weekends and public holidays)
Female data collections:
i. Date of pairing
ii. Date of mating
iii. Date and time of observed start of parturition
iv. Date and time of observed completion of parturition
Laboratory Investigations:
- Haematology
- Blood Chemistry - Litter observations:
- Number of live and dead offspring
For each litter the following was recorded:
i. Number of offspring born
ii.Number of offspring alive recorded daily and reported on Days 1 and 4 post partum
iii. Sex of offspring on Days 1 and 4 post partum
iv. Clinical condition of offspring from birth to Day 5 post partum
v. Individual offspring weights on Days 1 and 4 post partum (litter weights were calculated retrospectively from this data)
All live offspring were assessed for surface righting reflex on Day 1 post partum. - Postmortem examinations (parental animals):
- Pathology Females: Uterus (for signs of implantation and the number of uterine implantations in each horn), the corpora lutea. All adult animals and offspring: full external and internal examination. All macroscopic abnormalities were recorded.
- Organ Weights- Histopathology: Tissues from 5 selected male and female animals/group were preserved. Histopathological examination was undertaken on tissues from control and high dost animals.
To clarify possible treatment-related changes, histopathological examination was extended to include similarly prepared sections of the liver, kidneys (males only), stomach, thyroid and pituitary from animals in the low and intermediate groups. In addition, male kidney tissue was subject to immunohistochemical examination to confirm the presence of alph-2-microglobulin. - Postmortem examinations (offspring):
- All adult animals and offspring, including those dying during the study, were subjected to a full external and internal examination, and any macroscopic abnormalities were recorded.
- Statistics:
- Please see "Any other information on materials and methods incl. tables" for information on statistics.
- Reproductive indices:
- - Pre-coital Interval
- Fertility Indices
- Gestation length
- Parturition Index - Offspring viability indices:
- - Implantation Losses (%)
- Live Birth and Viability Indices
- Sex Ratio (% males) - Clinical signs:
- effects observed, treatment-related
- Description (incidence and severity):
- 1000 and 300 mg/kg bw/day: Increasing salivation in males and females. No effects in animals of either sex treated with 100 mg/kg bw/day.
- Mortality:
- no mortality observed
- Description (incidence):
- There were no unscheduled deaths.
- Body weight and weight changes:
- effects observed, treatment-related
- Description (incidence and severity):
- Males treated with 1000 mg/kg bw/day showed a statistically significant reduction in body weight gain during Weeks 1 and 3 of treatment. Overall body weight gain was reduced for these males.
No such effects were detected in treated females or in males treated with 300 or 100 mg/kg bw/day.
Females treated with 300 mg/kg bw/day showed a statistically significant increase in cumulative body weight gain during the final week of gestation. An increase in body weight gain is considered not to represent an adverse effect oftreatment therefore the intergroup difference was considered not to be of toxicological importance. - Food consumption and compound intake (if feeding study):
- effects observed, treatment-related
- Description (incidence and severity):
- No adverse effect on food consumption was detected in treated animals when compared to control animals.
Females treated with 1000 mg/kg bw/day showed a statistically significant increase in food consumption during the second week of gestation. An increase in food consumption is considered not to represent an adverse effect of treatment therefore the intergroup difference was considered not to be of toxicological importance. - Food efficiency:
- no effects observed
- Description (incidence and severity):
- No adverse effect on food efficiency was detected in treated animals when compared to control animals.
- Water consumption and compound intake (if drinking water study):
- effects observed, treatment-related
- Description (incidence and severity):
- Daily measurements of water bottles revealed a marked increase in water consumption in males treated with 1000 mg/kg bw/day and a slight increase in males treated with 300 or 100 mg/kg bw/day throughout the treatment period. Females from all treatment groups also showed an increase in water consumption throughout the treatment period with statistical significance being achieved throughout gestation and lactation at 1000 mg/kg bw/day.
- Haematological findings:
- effects observed, treatment-related
- Description (incidence and severity):
- Males treated with 1000 mg/kg bw/day showed a reduction in hemoglobin. Three out of the five individual values were outside of the normal background range for this parameter.
No toxicologically significant effects were detected in females treated with 1000 mg/kg bw/day or animals of either sex treated with 300 or 100 mg/kg bw/day.
Males treated with 1000 mg/kg bw/day showed a reduction in mean corpuscular hemoglobin. Males treated with 1000 and 300 mg/kg bw/day showed a reduction in mean corpuscular hemoglobin concentration. Males from all treatment groups also showed a reduction in
prothrombin time. All of the individual values were within the normal background range for these parameters, therefore the intergroup differences were considered not to be of toxicological importance. Females from all treatment groups showed a statistically significant increase in neutrophil count. The majority of individual values were within the normal background range for these parameters and a true dose related response was not evident, therefore the intergroup differences were considered not to be of toxicological significance. - Clinical biochemistry findings:
- effects observed, treatment-related
- Description (incidence and severity):
- No toxicologically significant effects were detected in the blood chemical parameters examined.
Males treated with 1000 and 300 mg/kg bw/day showed a statistically significant increase in calcium concentration and a statistically significant reduction in alkaline phosphatase. Males treated with 1000 mg/kg bw/day also showed a reduction in cholesterol. All of the individual values were within the normal ranges for rats ofthe strain and age used and in the absence of a true dose related response or any associated histology correlates the intergroup differences were considered not to be of toxicological importance. - Behaviour (functional findings):
- effects observed, treatment-related
- Description (incidence and severity):
- Behavioral Assessments
Weekly open field arena observations did not reveal any treatment-related effects for treated animals when compared to controls.
Functional Performance Tests
There were no toxicologically significant changes in functional performance. Males from all treatment groups showed a statistically significant increase in fore limb grip strength. The statistically significant difference was confined to one out of the three tests and in the absence of a true dose related response or any supporting clinical observations to suggest an effect of neurotoxicity, the intergroup differences were considered to be of no toxicological significance.
Sensory Reactivity Assessments
There were no treatment-related changes in sensory reactivity. - Organ weight findings including organ / body weight ratios:
- effects observed, treatment-related
- Histopathological findings: non-neoplastic:
- effects observed, treatment-related
- Description (incidence and severity):
- The following treatment related microscopic findings were detected:
Liver:hepatocyte hypertrophy was evident in animals of either sex treated with 1000 and 300 mg/kg bw/day and in males treated with 100 mg/kg bw/day. No such effects were detected in females treated with 100 mg/kg bw/day.
Kidneys:proximal tubular basophilia and hyaline droplets were evident in males from all treatment groups. Tubular degeneration/debris was evident in males treated with 1000 and 300 mg/kg bw/day. These findings were demonstrated by immunohistochemical staining to be
due to alpha-2-microglobulin nephropathy. No such effects were detected in any treated female.
Stomach:epithelial hyperplasia was evident in the fore stomach of animals of either sex treated with 1000 mg/kg bw/day and in males treated with 300 mg/kg bw/day. No such effects were detected in females treated with 300 mg/kg bw/day or animals of either sex treated with 100 mg/kg bw/day.
Thyroid:follicular cell hypertrophy and hyperplasia was evident in animals of either sex treated with 1000 and 300 mg/kg bw/day and in males treated with 100 mg/kg bw/day. No such effects were detected in females treated with 100 mg/kg bw/day.
Pituitary:increased incidence and severity of hypertrophic/vacuolated cells in pars anterior was evident in males treated with 1000 and 300 mg/kg bw/day. No such effects were detected in any treated female or in males treated with 100 mg/kg bw/day. - Other effects:
- no effects observed
- Reproductive function: oestrous cycle:
- no effects observed
- Reproductive function: sperm measures:
- no effects observed
- Reproductive performance:
- effects observed, non-treatment-related
- Description (incidence and severity):
- Mating
There were no treatment-related effects on mating performance.
Fertility
No treatment-related effects on fertility were detected for treated animals, when compared to controls.
One control female and one female treated 100 mg/kg bw/day did not achieve pregnancy following evidence of mating. No histopathological correlates were evident in the female or male reproductive organs which could have been the cause of the infertility. One female treated with 1000 mg/kg bw/day failed to show any positive signs of mating and was non pregnant.
Gestation Length
There were no differences in gestation lengths. The distribution for treated females was comparable to controls. All animals showed gestation lengths of 22 to 24½ days. - Key result
- Dose descriptor:
- NOAEL
- Effect level:
- 1 000 mg/kg bw/day (actual dose received)
- Based on:
- test mat.
- Sex:
- male/female
- Basis for effect level:
- other: Systemic Toxicity
- Dose descriptor:
- NOEL
- Effect level:
- 300 mg/kg bw/day (actual dose received)
- Based on:
- test mat.
- Sex:
- male/female
- Basis for effect level:
- other: Reproductive Toxicity
- Key result
- Critical effects observed:
- no
- Clinical signs:
- effects observed, non-treatment-related
- Description (incidence and severity):
- No obvious clinical signs of toxicity were detected for offspring from treated females when compared to controls. The incidental clinical signs detected throughout the control and treated groups, consisting of small size, cold, weak, pale, no milk in stomach, physical injury, found dead or missing, were considered to be low incidence findings observed in offspring in studies of this type and were considered unrelated to test item toxicity.
- Mortality / viability:
- no mortality observed
- Body weight and weight changes:
- effects observed, treatment-related
- Description (incidence and severity):
- Litter weights on Day 4 post partum from females treated with 1000 mg/kg bw/day were reduced when compared to control litters however statistical significance was not achieved. Offspring body weight gain at 1000 mg/kg bw/day was also reduced between Days 1 and 4 post partum. Statistical significance was achieved for male off spring only. No such effects were detected in litters from females treated with 300 or 100 mg/kg bw/day.
- Sexual maturation:
- not examined
- Organ weight findings including organ / body weight ratios:
- no effects observed
- Gross pathological findings:
- effects observed, non-treatment-related
- Description (incidence and severity):
- No treatment-related macroscopic abnormalities were detected for interim death or terminal kill offspring. The incidental findings observed were those occasionally observed in reproductive studies of this type and were considered to be unrelated to toxicity of the test item.
- Histopathological findings:
- no effects observed
- Behaviour (functional findings):
- no effects observed
- Description (incidence and severity):
- Statistical analysis of surface righting reflex data did not reveal any significant intergroup differences.
- Key result
- Dose descriptor:
- NOEL
- Generation:
- F1
- Effect level:
- 300 mg/kg bw/day (actual dose received)
- Based on:
- test mat.
- Sex:
- male/female
- Basis for effect level:
- other: reduced post natal offspring viability, offspring body weight gain and litter size at 1000 mg/kg bw/day.
- Key result
- Critical effects observed:
- no
- Key result
- Reproductive effects observed:
- yes
- Lowest effective dose / conc.:
- 1 000 mg/kg bw/day (actual dose received)
- Treatment related:
- yes
- Relation to other toxic effects:
- reproductive effects occurring together with other toxic effects, but not as a secondary non-specific consequence of other toxic effects
- Dose response relationship:
- not specified
- Relevant for humans:
- not specified
- Conclusions:
- Oral administration of Nonene, branched to rats for 8 weeks, at levels of 100, 300 and 1000 mgk/kg/day, resulted in treatment related effects in both sexes and at all treatment levels. The effects seen were however either adaptive in nature or were not considered toxicologically relevant for man. The No Observed Adverse Effect Level (NOAEL) for systemic toxicity was therefore considered to be 1000 mg/kg bw/day.
The ‘No Observed Effect Level’ (NOEL) for reproductive toxicity was considered to be 300 mg/kg bw/day based on reduced offspring viability, offspring body weight gain, litter size and litter weigh at 1000 mg/kg bw/day. - Executive summary:
In a key Guideline (OECD 422) combined repeated dose reproductive/developmental toxicity study, the test material (Nonene, branched; CAS# 97280-95-0) was administered by gavage to three groups of Wistar Han™:RccHan™:WIST strain rats (12/sex/dose) for up to eight weeks (including a two week pre-pairing phase, pairing, gestation and early lactation for females), at dose levels of 100, 300 and 1000 mg/Kg bw/day. A control group of twelve males and twelve females was dosed with vehicle alone (Arachis oil BP).
Clinical signs, behavioral assessments, body weight change and food and water consumption were monitored during the study. Pairing of animals within each dose group was undertaken on a one male: one female basis within each treatment group on Day 15 of the study, with females subsequently being allowed to litter and rear their offspring to Day 5 of lactation. During the lactation phase, daily clinical observations were performed on all surviving offspring, together with litter size and offspring weights and assessment of surface righting reflex. Extensive functional observations were performed on five selected males from each dose group after the completion of the pairing phase, and for five selected parental females from each dose group on Day 4 post-partum. Hematology and blood chemistry were evaluated prior to termination on five selected males and females from each dose group.
Adult males were terminated on Day 43, followed by the termination of all females and offspring on Day 5 post-partum. Any female which did not produce a pregnancy was terminated on or after Day 25 post coitum. One female which did not show positive evidence of mating and did not produce a pregnancy was terminated on Day 57. All animals were subjected to a gross necropsy examination and histopathological evaluation of selected tissues was performed.
No test material related mortality was observed through the study period. Clinical signs were detected in animals of either sex treated with 300 and 1000 mg/Kg bw/day during the study. Episodes of increased salivation were reported from Day 8 onwards. The physical condition of males treated with 1000 mg/Kg bw/day was also affected with reductions in body weight development during Weeks 1 and 3 of treatment. Subsequently, a reduction in overall body weight gain in these males and a slight reduction in food efficiency during week 1, was evident. A reduction in haemoglobin was also observed in these males. Water consumption was also significantly increased for animals of either sex from all treatment groups throughout the treatment period. Observations of this nature are often reported when a test material formulation is unpalatable or irritant and can be associated with gastric irritancy rather than be attributable to systemic toxicity. This was supported microscopically with stomach changes identified as epithelial hyperplasia in the forestomach in animals of either sex treated with 1000 mg/Kg bw/day and in males treated with 300 mg/Kg bw/day. This finding was considered to be the result of local irritancy of the test material and therefore cannot be considered indicative of true systemic toxicity.
Although there were some statistically significant differences in treated animals from controls for the blood chemical parameters measured, these differences were considered not to be of toxicological significance. Macroscopic findings detected at necropsy were confined to enlarged, pale and mottled kidneys and a dark liver in a number of males treated with 1000 mg/Kg bw/day. One male treated with 300 mg/Kg bw/day also had enlarged kidneys.
Histopathological examination of the liver revealed hepatocellular hypertrophy in animals of either sex treated with 1000 and 300 mg/Kg bw/day and in males treated with 100 mg/Kg bw/day. Organ weight data supported this finding with increased absolute and relative liver weights observed in these animals. In the absence of any degenerative or inflammatory changes, this condition is considered to be adaptive in nature.
Microscopic examination of the thyroid revealed increased incidence and severity of follicular cell hypertrophy/hyperplasia in animals of either sex treated with 1000 and 300 mg/Kg bw/day and in males treated with 100 mg/Kg bw/day. Males treated with 1000 and 300 mg/Kg bw/day also showed hypertrophic/vacuolated cells in the pituitary. The thyroid, liver and pituitary changes are characteristic of a consequence of hepatocellular induction as a result of enhanced hepatic metabolism. As a side effect of hepatic induction an increased liver metabolism of thyroid hormones T3 and T4 can occur. This subsequently leads to an enhanced thyroid gland production of these hormones as a consequence of a negative feedback stimulation of TSH production. The appearance of thyroid follicular cell hypertrophy and hypertrophic/vacuolated cells in the pituitary are themselves considered to be a result of this process. The thyroid and pituitary changes were considered to be adaptive in nature.
Microscopic examination also revealed effects in the kidneys of males from all treatment groups. Tubular basophilia and hyaline droplets was present in males from all treated groups. These tubular findings were also accompanied by tubular degeneration/debris in males treated with 1000 and 300 mg/Kg bw/day. The hyaline droplets can be directly linked to accumulation of alpha 2u-globulin, which is unique to the male rat. This finding is commonly observed in male rats following treatment with some hydrocarbons and is not predictive of any adverse effect in humans. The remaining kidney findings consisting of tubular degeneration/debris may be considered to represent an adverse effect of the test item, however immunohistochemical staining demonstrated that these findings were correlated to the same condition as hyaline droplets.
Mating performance and fertility was unaffected by treatment. Offspring viability was however reduced in litters from females treated with 1000 mg/Kg bw/day on Day 4 post-partum. Subsequently reduced litter size and litter weights were evident in these litters on Day 4 post-partum when compared to controls. One female treated with 1000 mg/Kg bw/day also had a total litter loss between Days 2 and 4 post-partum. The mean offspring body weight gains for litters which survived to Day 5 post-partum were also reduced between Days 1 and 4 post-partum at this treatment level.
Based on the results observed, the No Observed Adverse Effect Level (NOAEL) for systemic toxicity was determined to be 1000 mg/Kg bw/day. The ‘No Observed Effect Level’ (NOEL) for reproductive toxicity was considered to be 300 mg/Kg bw/day, based on reduced offspring viability, offspring body weight gain, litter size and litter weights on Day 4 post-partum at 1000 mg/Kg bw/day.
1000 and 300 mg/kg bw/day: Increasing salivation in males and females. No effects in animals of either sex treated with 100 mg/kg bw/day.
Body Weight and Weight Changes:
Males treated with 1000 mg/kg bw/day showed a statistically significant reduction in body weight gain during Weeks 1 and 3 of treatment. Overall body weight gain was reduced for these males.
No such effects were detected in treated females or in males treated with 300 or 100 mg/kg bw/day.
Females treated with 300 mg/kg bw/day showed a statistically significant increase in cumulative body weight gain during the final week of gestation. An increase in body weight gain is considered not to represent an adverse effect oftreatment therefore the intergroup difference was considered not to be of toxicological importance.
Food consumption and Compound Intake:
No adverse effect on food consumption was detected in treated animals when compared to control animals.
Females treated with 1000 mg/kg bw/day showed a statistically significant increase in food consumption during the second week of gestation. An increase in food consumption is considered not to represent an adverse effect of treatment therefore the intergroup difference was considered not to be of toxicological importance.
Water Consumption:
Daily measurements of water bottles revealed a marked increase in water consumption in males treated with 1000 mg/kg bw/day and a slight increase in males treated with 300 or 100 mg/kg bw/day throughout the treatment period. Females from all treatment groups also showed an increase in water consumption throughout the treatment period with statistical significance being achieved throughout gestation and lactation at 1000 mg/kg bw/day.
Hematology:
Males treated with 1000 mg/kg bw/day showed a reduction in hemoglobin. Three out of the five individual values were outside of the normal background range for this parameter.
No toxicologically significant effects were detected in females treated with 1000 mg/kg bw/day or animals of either sex treated with 300 or 100 mg/kg bw/day.
Males treated with 1000 mg/kg bw/day showed a reduction in mean corpuscular hemoglobin. Males treated with 1000 and 300 mg/kg bw/day showed a reduction in mean corpuscular hemoglobin concentration. Males from all treatment groups also showed a reduction in
prothrombin time. All of the individual values were within the normal background range for these parameters, therefore the intergroup differences were considered not to be of toxicological importance. Females from all treatment groups showed a statistically significant increase in neutrophil count. The majority of individual values were within the normal background range for these parameters and a true dose related response was not evident, therefore the intergroup differences were considered not to be of toxicological significance.
Clinical Biochemistry:
No toxicologically significant effects were detected in the blood chemical parameters examined.
Males treated with 1000 and 300 mg/kg bw/day showed a statistically significant increase in calcium concentration and a statistically significant reduction in alkaline phosphatase. Males treated with 1000 mg/kg bw/day also showed a reduction in cholesterol. All of the individual values were within the normal ranges for rats ofthe strain and age used and in the absence of a true dose related response or any associated histology correlates the intergroup differences were considered not to be of toxicological importance.
Behaviour:
Functional Performance Tests - There were no toxicologically significant changes in functional performance. Males from all treatment groups showed a statistically significant increase in fore limb grip strength. The statistically significant difference was confined to one out of the three tests and in the absence of a true dose related response or any supporting clinical observations to suggest an effect of neurotoxicity, the intergroup differences were considered to be of no toxicological significance.
Organ Weight:
Animals of either sex treated with 1000 and 300 mg/kg bw/day and females treated with 100 mg/kg bw/day showed an increase in absolute and relative liver weight. Males treated with 1000 mg/kg bw/day also showed an increase in kidney weight both absolute and relative to terminal body weight. Males from all treatment groups showed an increase in absolute and relative thyroid weight whilst females treated with 1000 mg/kg bw/day showed a reduction in absolute and relative thyroid weight. All of the individual values were within the normal range for rats of the strain and age used and the effect on male thyroid weight also did not show a true dose related response. However with the associated microscopic thyroid changes observed in this study the intergroup differences detected in thyroid weights can not be excluded as an effect of treatment.
Females treated with 1000 mg/kg bw/day showed a reduction in pituitary weight and an increase in kidney weight both absolute and relative to terminal body weight. In the absence of any associated histopathological changes detected in the kidneys or pituitary of females the intergroup differences were considered not to be of toxicological importance.
Necropsy:
Nine males treated with 1000 mg/kg bw/day had enlarged kidneys at necropsy, eight of which had pale kidneys; four showed a mottled appearance to the kidneys and five of these males also had a dark liver at necropsy. One male treated with 300 mg/kg bw/day had enlarged kidneys at necropsy.
No toxicologically significant effects were detected in females from any treatment group or in males treated with 100 mg/kg bw/day.
One male treated with 100 mg/kg bw/day had small testes and epididymides. One female treated with 300 mg/kg bw/day and two females treated with 100 mg/kg bw/day had reddened lungs at necropsy. Histopathological examination of these tissues did reveal associated microscopic findings to the macroscopic abnormalities however in the absence of a similar effect seen at 1000 mg/kg bw/day, the intergroup differences were considered to be incidental and of no toxicological importance.
Histopathology:
Liver:hepatocyte hypertrophy was evident in animals of either sex treated with 1000 and 300 mg/kg bw/day and in males treated with 100 mg/kg bw/day. No such effects were detected in females treated with 100 mg/kg bw/day.
Kidneys:proximal tubular basophilia and hyaline droplets were evident in males from all treatment groups. Tubular degeneration/debris was evident in males treated with 1000 and 300 mg/kg bw/day. These findings were demonstrated by immunohistochemical staining to be
due to alpha-2-microglobulin nephropathy. No such effects were detected in any treated female.
Stomach:epithelial hyperplasia was evident in the fore stomach of animals of either sex treated with 1000 mg/kg bw/day and in males treated with 300 mg/kg bw/day. No such effects were detected in females treated with 300 mg/kg bw/day or animals of either sex treated with 100 mg/kg bw/day.
Thyroid:follicular cell hypertrophy and hyperplasia was evident in animals of either sex treated with 1000 and 300 mg/kg bw/day and in males treated with 100 mg/kg bw/day. No such effects were detected in females treated with 100 mg/kg bw/day.
Pituitary:increased incidence and severity of hypertrophic/vacuolated cells in pars anterior was evident in males treated with 1000 and 300 mg/kg bw/day. No such effects were detected in any treated female or in males treated with 100 mg/kg bw/day.
Reproductive Performance:
Fertility - No treatment-related effects on fertility were detected for treated animals, when compared to controls.
One control female and one female treated 100 mg/kg bw/day did not achieve pregnancy following evidence of mating. No histopathological correlates were evident in the female or male reproductive organs which could have been the cause of the infertility. One female treated with 1000 mg/kg bw/day failed to show any positive signs of mating and was non pregnant.
No significant differences were detected for corpora lutea, implantation counts or implantation losses for treated animals when compared to controls. Statistical analysis of the data did not reveal any significant intergroup differences.
Of the litters born, litter size at birth and subsequently on Day 1 post partumwere comparable to controls. Litter size on Day 4 post partumhowever was reduced in litters from females treated with 1000 mg/kg bw/day although statistical significance was not achieved. Offspring viability on Day 4 post partumwas statistically significantly reduced in these litters. A total litter loss was also observed for one female treated with 1000 mg/kg bw/day. No such effects were detected in litters from females treated with 300 or 100 mg/kg bw/day.
There were no intergroup differences in sex ratio (percentage male offspring) for litters from treated groups compared to controls. Statistical analysis of the data did not reveal any significant intergroup differences.
Offspring Growth and Development
Litter weights on Day 4 post partumfrom females treated with 1000 mg/kg bw/day were reduced when compared to control litters however statistical significance was not achieved. Offspring body weight gain at 1000 mg/kg bw/day was also reduced between Days 1 and 4 post partum. Statistical significance was achieved for male offspring only.
No such effects were detected in litters from females treated with 300 or 100 mg/kg bw/day. Statistical analysis of surface righting reflex data did not reveal any significant intergroup differences.
No obvious clinical signs of toxicity were detected for offspring from treated females when compared to controls. The incidental clinical signs detected throughout the control and treated groups, consisting of small size, cold, weak, pale, no milk in stomach, physical injury, found dead or missing, were considered to be low incidence findings observed in offspring in studies of this type and were considered unrelated to test item toxicity.
Table 2. Summary of Reproductive Performance - Groups Values |
||||
|
Dose Group (mg/Kg bw/day |
|||
0 (Control) |
100 |
300 |
1000 |
|
Males |
|
|||
Initial group size |
12 |
12 |
12 |
12 |
Paired |
12 |
12 |
12 |
12 |
Failed to mate |
0 |
0 |
0 |
1 |
Failed to induce pregnancy in female partner |
1 |
1 |
0 |
0 |
Induced pregnancy in female partner |
11 |
11 |
12 |
11 |
Surviving to terminal necropsy |
12 |
12 |
12 |
12 |
|
||||
Females |
|
|||
Initial group size |
12 |
12 |
12 |
12 |
Paired |
12 |
12 |
12 |
12 |
Failed to mate |
0 |
0 |
0 |
1 |
Non-pregnant |
1 |
1 |
0 |
0 |
Rearing young to Day 5 of age |
11 |
11 |
12 |
10 |
Total Litter Loss |
0 |
0 |
0 |
1 |
Table 3. Group Mean Functional Test Values and Standard Deviations - Males |
|||||||||||
Group (sex) |
|
Test 1 Forelimb (g) |
Test 1 Hindlimb (g) |
Test 2 Forelimb (g) |
Test 2 Hindlimb (g) |
Test 3 Forelimb (g) |
Test 3 Hindlimb (g) |
Overall Activity |
Overall Mobile |
Last 20% Activity |
Last 20% Mobile |
1 (M) |
Mean |
1143.2 |
422.6 |
1004.2 |
524.4 |
985.2 |
445.0 |
377.2 |
0.6 |
3.4 |
0.0n |
S.D. |
234.7 |
131.5 |
113.9 |
66.2 |
91.6 |
76.7 |
122.9 |
0.9 |
4.0 |
0.0 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||||
2 (M) |
Mean |
1176.8 |
510.2 |
1303.0* |
581.4 |
1084.8 |
628.2 |
384.0 |
0.6 |
8.2 |
0.0n |
S.D. |
237.0 |
140.4 |
313.6 |
105.2 |
146.7 |
157.4 |
214.5 |
0.5 |
9.5 |
0.0 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||||
3 (M) |
Mean |
1353.0 |
593.8 |
1450.4* |
472.0 |
1378.2 |
528.2 |
334.6 |
0.2 |
4.2 |
0.0n |
S.D. |
297.1 |
121.5 |
200.0 |
147.6 |
442.9 |
177.5 |
141.7 |
0.4 |
5.2 |
0.0 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||||
4 (M) |
Mean |
1071.2 |
620.8 |
1271.0* |
473.4 |
1118.6 |
555.0 |
250.8 |
0.2 |
36.2 |
0.0n |
S.D. |
257.2 |
184.4 |
250.8 |
230.9 |
185.2 |
151.8 |
118.6 |
0.4 |
58.3 |
0.0 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
General Footnote: Unit = Time (seconds) for Motor Activity Assessments
Dose Levels: Group 1 - 0(Control); Group 2 - 100 mg/kg bw/day; Group 3 - 300 mg/kg bw/day; Group 4 - 1000 mg/kg bw/day
* Significantly different from control group p<0.05
n Data not appropriate for statistical analysis
Table 4. Group Mean Body Weight Values - Males |
|||||||||||
Group (sex) |
|
Increase in Body Weight (g) |
|||||||||
|
Day Numbers Relative to Start Date |
Abs Gain |
% Gain |
||||||||
From: |
1 |
8 |
15 |
22 |
29 |
36 |
1 |
1 |
|||
To: |
8 |
15 |
22 |
29 |
36 |
43 |
43 |
43 |
|||
1 (M) |
Mean |
14.4 |
13.0 |
9.7 |
14.6 |
10.2 |
6.8 |
68.6 |
20.9 |
||
S.D. |
5,8 |
6.5 |
6.6 |
6.0 |
4.5 |
3.7 |
21.7 |
5.9 |
|||
N |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
|||
|
|
|
|||||||||
2 (M) |
Mean |
13.9 |
12.5 |
6.9 |
13.3 |
12.0 |
4.3 |
63.0 |
19.0 |
||
S.D. |
3.8 |
3.9 |
6.3 |
4.4 |
3.4 |
5.1 |
16.9 |
4.8 |
|||
N |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
|||
|
|
|
|||||||||
3 (M) |
Mean |
13.4 |
15.3 |
7.3 |
14.1 |
11.9 |
8.1 |
70.2 |
21.3 |
||
S.D. |
5.5 |
5.0 |
3.9 |
4.6 |
5.6 |
3.4 |
18.8 |
5.3 |
|||
N |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
|||
|
|
|
|||||||||
4 (M) |
Mean |
5.5** |
10.0 |
1.7** |
12.4 |
8.1 |
5.1 |
42.8 |
13.0 |
||
S.D. |
9.8 |
7.5 |
6.8 |
3.8 |
4.8 |
4.8 |
18.0 |
5.3 |
|||
N |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
|||
Dose Levels: Group 1 - 0(Control); Group 2 - 100 mg/kg bw/day; Group 3 - 300 mg/kg bw/day; Group 4 - 1000 mg/kg bw/day
** Significantly different from control group p<0.01
Table 5. Group Mean Body Weight Gains - Females |
|||||||
Group (sex) |
|
Increase in Body Weight (g) |
Cumulative Body Weight Change (g) |
||||
|
Days |
Days |
|||||
|
Gestation |
Lactation |
Gestation |
||||
From: |
0 |
7 |
14 |
1 |
0 |
0 |
|
To: |
7 |
14 |
20 |
4 |
14 |
20 |
|
1 (F) |
Mean |
29.8 |
28.9 |
60.4 |
7.9 |
58.7 |
119.1 |
S.D. |
4.4 |
3.9 |
13.0 |
5.4 |
7.3 |
16.3 |
|
N |
11 |
11 |
11 |
11 |
11 |
11 |
|
|
|||||||
2 (F) |
Mean |
27.4 |
28.3 |
60.8 |
11.8 |
55.6 |
116.5 |
S.D. |
4.8 |
5.0 |
12.5 |
10.3 |
6.1 |
14.9 |
|
N |
11 |
11 |
11 |
11 |
11 |
11 |
|
|
|||||||
3 (F) |
Mean |
33.3 |
33.1 |
69.1 |
12.8 |
66.4 |
135.5* |
S.D. |
5.2 |
5.2 |
10.9 |
7.1 |
7.8 |
15.2 |
|
N |
12 |
12 |
12 |
12 |
12 |
12 |
|
|
|||||||
4 (F) |
Mean |
29.8 |
27.9 |
57.3 |
6.4 |
57.7 |
115.0 |
S.D. |
6.8 |
6.5 |
11.7 |
12.2 |
11.4 |
17.1 |
|
N |
11 |
11 |
11 |
10 |
11 |
11 |
Dose Levels: Group 1 - 0(Control); Group 2 - 100 mg/kg bw/day; Group 3 - 300 mg/kg bw/day; Group 4 - 1000 mg/kg bw/day
* Significantly different from control group p<0.05
Table 6. Group Mean Food Consumptions - Females |
|||||
Group (sex) |
|
Day Numbers |
|||
Gestation |
Lactation |
||||
From |
0 |
7 |
14 |
1 |
|
To |
7 |
14 |
20 |
4 |
|
1 (F) |
Mean |
19.7 |
22.3 |
25.1 |
26.5 |
S.D. |
1.8 |
1.9 |
2.4 |
4.6 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
2 (F) |
Mean |
20.2 |
22.5 |
24.6 |
29.5 |
S.D. |
2.0 |
2.3 |
1.2 |
8.3 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
3 (F) |
Mean |
20.7 |
23.6 |
25.5 |
28.2 |
S.D. |
1.2 |
1.2 |
1.1 |
3.3 |
|
N |
12 |
12 |
12 |
12 |
|
|
|||||
4 (F) |
Mean |
20.9 |
24.2* |
26.8 |
25.4 |
S.D. |
1.6 |
2.2 |
2.3 |
6.2 |
|
N |
11 |
11 |
11 |
10 |
Dose Levels: Group 1 - 0(Control); Group 2 - 100 mg/kg bw/day; Group 3 - 300 mg/kg bw/day; Group 4 - 1000 mg/kg bw/day
* Significantly different from control group p<0.05
Table 7. Group Mean Water Consumption - Females |
|||||
Group (sex) |
|
Day Numbers |
|||
Gestation |
Lactation |
||||
From |
0 |
7 |
14 |
1 |
|
To |
7 |
14 |
20 |
4 |
|
1 (F) |
Mean |
27.6 |
31.0 |
36.0 |
39.9 |
S.D. |
3.8 |
5.1 |
6.8 |
4.3 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
2 (F) |
Mean |
32.1 |
36.9 |
39.9 |
44.2 |
S.D. |
5.3 |
5.9 |
4.8 |
10.6 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
3 (F) |
Mean |
36.5 |
42.9 |
44.8 |
45.8 |
S.D. |
2.2 |
13.9 |
10.7 |
7.1 |
|
N |
12 |
12 |
12 |
12 |
|
|
|||||
4 (F) |
Mean |
52.6*** |
67.8*** |
76.4*** |
54.1** |
S.D. |
20.4 |
22.5 |
34.1 |
12.5 |
|
N |
11 |
11 |
11 |
11 |
Dose Levels: Group 1 - 0(Control); Group 2 - 100 mg/kg bw/day; Group 3 - 300 mg/kg bw/day; Group 4 - 1000 mg/kg bw/day
** Significantly different from control group p<0.01
*** Significantly different from control group p<0.001
Table 8. Group Mean Hematological Values - Males |
|||||
Group |
|
Hb (g/dL) |
MCH (pg) |
MCHC (g/dL) |
CT (seconds) |
Group 1 (0 – Control) |
Mean |
16.92 |
18.86 |
35.66 |
9.92 |
S.D. |
0.44 |
0.44 |
1.49 |
0.47 |
|
N |
5 |
5 |
5 |
5 |
|
|
|||||
Group 2 (100 mg/Kg bw/day) |
Mean |
16.86 |
18.64 |
35.18 |
9.40* |
S.D. |
0.74 |
0.11 |
0.67 |
0.23 |
|
N |
5 |
5 |
5 |
5 |
|
|
|||||
Group 3 (300 mg/Kg bw/day) |
Mean |
16.08 |
18.36 |
34.12** |
9.34* |
S.D. |
0.31 |
0.48 |
0.53 |
0.26 |
|
N |
5 |
5 |
5 |
5 |
|
|
|||||
Group 4 (1000 mg/Kg bw/day) |
Mean |
14.94** |
17.58** |
33.72** |
9.34* |
S.D. |
1.56 |
0.63 |
0.28 |
0.36 |
|
N |
5 |
5 |
5 |
5 |
* Significantly different from control group p<0.05
** Significantly different from control group p<0.01
Table 9. Group Mean Hematological Values - Females |
||
Group |
|
Neut (109/L) |
Group 1 (0 – Control) |
Mean |
1.360 |
S.D. |
0.417 |
|
N |
5 |
|
|
||
Group 2 (100 mg/Kg bw/day) |
Mean |
2.500* |
S.D. |
0.568 |
|
N |
5 |
|
|
||
Group 3 (300 mg/Kg bw/day) |
Mean |
2.146* |
S.D. |
0.463 |
|
N |
5 |
|
|
||
Group 4 (1000 mg/Kg bw/day) |
Mean |
1.872* |
S.D. |
0.509 |
|
N |
5 |
* Significantly different from control group p<0.05
Table 10. Group Mean Blood Chemical Values - Males |
||||
Group |
|
Ca++(mmol/L) |
AP (IU/L) |
Chol (mg/dL) |
Group 1 (0 – Control) |
Mean |
2.448 |
234.0 |
95.2 |
S.D. |
0.258 |
52.1 |
5.3 |
|
N |
5 |
5 |
5 |
|
|
||||
Group 2 (100 mg/Kg bw/day) |
Mean |
2.522 |
201.6 |
102.6 |
S.D. |
0.146 |
26.1 |
14.4 |
|
N |
5 |
5 |
5 |
|
|
||||
Group 3 (300 mg/Kg bw/day) |
Mean |
2.730* |
150.6** |
99.4 |
S.D. |
0.077 |
10.8 |
10.7 |
|
N |
5 |
5 |
5 |
|
|
||||
Group 4 (1000 mg/Kg bw/day) |
Mean |
2.644* |
157.6** |
78.0* |
S.D. |
0.129 |
55.2 |
13.3 |
|
N |
5 |
5 |
5 |
* Significantly different from control group p<0.05
** Significantly different from control group p<0.01
Table 11. Summary Incidence of Necropsy Findings - Males |
||||
|
Males |
|||
0 Control |
100 mg/Kg bw/day |
300 mg/Kg bw/day |
1000 mg/Kg bw/day |
|
Number of animals examined |
12 |
12 |
12 |
12 |
Epididymides |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
11 |
12 |
12 |
Small; Left |
0 |
1 |
0 |
0 |
|
||||
Kidneys |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
12 |
11 |
3 |
Enlarged |
0 |
0 |
1 |
9 |
Mottled Appearance |
0 |
0 |
0 |
4 |
Pallor |
0 |
0 |
0 |
3 |
Pale |
0 |
0 |
0 |
6 |
|
||||
Liver |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
12 |
12 |
7 |
Dark |
0 |
0 |
0 |
5 |
|
||||
Testes |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
11 |
12 |
12 |
Small; Left |
0 |
1 |
0 |
0 |
Table 12. Summary Incidence of Necropsy Findings - Females |
||||
|
Females |
|||
0 Control |
100 mg/Kg bw/day |
300 mg/Kg bw/day |
1000 mg/Kg bw/day |
|
Number of animals examined |
12 |
12 |
12 |
12 |
Liver |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
12 |
12 |
11 |
Dark |
0 |
0 |
0 |
1 |
|
||||
Lungs (With Bronchi) |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
10 |
11 |
12 |
Reddened |
0 |
2 |
1 |
0 |
Table 13. Group Mean Organ Weights with Corresponding Relative (% of Body Weight) Organ Weights |
|||||||||
|
|
Males |
Females |
||||||
0 Control |
100 mg/Kg bw/day |
300 mg/Kg bw/day |
1000 mg/Kg bw/day |
0 Control |
100 mg/Kg bw/day |
300 mg/Kg bw/day |
1000 mg/Kg bw/day |
||
Kidneys |
Mean (g) |
2.29348 |
2.31240 |
2.38234 |
3.16702** |
1.54460 |
1.65510 |
1.66136 |
1.97002** |
S.D. |
0.32697 |
0.14310 |
0.16218 |
0.44018 |
0.14343 |
0.11476 |
0.20712 |
0.11782 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||
Mean (%) |
0.574 |
0.585 |
0.616 |
0.830** |
0.565 |
0.610 |
0.602 |
0.701** |
|
S.D. |
0.046 |
0.013 |
0.051 |
0.102 |
0.047 |
0.035 |
0.055 |
0.041 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||
Liver |
Mean (g) |
12.7830 |
13.2647 |
14.3898** |
19.3412** |
10.5429 |
11.7936* |
12.7876** |
16.1219** |
S.D. |
1.51792 |
0.98038 |
1.33119 |
1.23327 |
0.51191 |
0.52983 |
1.29755 |
1.61466 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||
Mean (%) |
3.203 |
3.355 |
3.710** |
5.070** |
3.857 |
4.353* |
4.638** |
5.742** |
|
S.D. |
0.125 |
0.111 |
0.164 |
0.230 |
0.149 |
0.194 |
0.424 |
0.639 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||
Pituitary |
Mean (g) |
|
|
|
|
0.01793 |
0.01529 |
0.01783 |
0.01467** |
S.D. |
|
|
|
|
0.00277 |
0.00241 |
0.00264 |
0.00180 |
|
N |
|
|
|
|
11 |
11 |
12 |
10 |
|
|
|
||||||||
Mean (%) |
|
|
|
|
0.006 |
0.006 |
0.006 |
0.005** |
|
S.D. |
|
|
|
|
0.001 |
0.001 |
0.001 |
0.001 |
|
N |
|
|
|
|
11 |
11 |
12 |
10 |
|
|
|||||||||
Thyroid/Parathyroid |
Mean (g) |
0.01552 |
0.02172** |
0.02162** |
0.02112** |
0.002238 |
0.01972 |
0.02046 |
0.01776* |
S.D. |
0.00377 |
0.00176 |
0.00140 |
0.00207 |
0.00395 |
0.00339 |
0.00202 |
0.00259 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||
Mean (%) |
0.004 |
0.005** |
0.006** |
0.006** |
0.008 |
0.007 |
0.007 |
0.006* |
|
S.D. |
0.001 |
0.000 |
0.000 |
0.000 |
0.002 |
0.001 |
0.001 |
0.001 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
* Significantly different from control group p<0.05
** Significantly different from control group p<0.01
Table 14. Histopathology – Treatment-related Findings |
||||||||
|
Male |
Female |
||||||
Dosage (mg/Kg bw/day) |
0 |
100 |
300 |
1000 |
0 |
100 |
300 |
1000 |
|
||||||||
Liver |
||||||||
Number Examined |
5 |
5 |
5 |
9 |
5 |
5 |
5 |
6 |
- Hypertrophy; hepatoc. |
0 |
5 (1.0) |
5 (1.0) |
9 (1.7) |
0 |
0 |
3 (1.0) |
6 (1.0) |
- Congestion |
0 |
0 |
0 |
5 (1.0) |
0 |
0 |
0 |
1(3.0) |
|
||||||||
Thyroid |
||||||||
Number Examined |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
- Hypertrophy / Hyperplasia; Follicular Cell |
2 (1.0) |
5 (1.4) |
5 (1.4) |
5 (1.8) |
2 (1.0) |
2 (1.0) |
3 (1.3) |
5 (1.2) |
|
||||||||
Pituitary Gland |
||||||||
Number Examined |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
10 |
-Hypertrophic / Vacuolated cells in Pars Anterior |
10 (1.0) |
9 (1.2) |
12 (1.4) |
9 (1.6) |
0 |
0 |
3 (1.0) |
0 |
|
||||||||
Kidney |
||||||||
Number Examined |
5 |
5 |
5 |
9 |
5 |
5 |
5 |
5 |
- Tubular Basophilia |
0 |
3 (1.0) |
4 (1.3) |
9 (2.0) |
0 |
0 |
0 |
1 (1.0) |
- Tubular Degeneration / Debris |
0 |
0 |
4 (1.0) |
7 (2.0) |
0 |
0 |
0 |
0 |
- Hyaline Droplets |
0 |
5 (1.0) |
5 (1.8) |
9 (2.1) |
0 |
0 |
0 |
0 |
|
||||||||
Kidney Immunohistochemistry |
||||||||
Number Examined |
3 |
3 |
3 |
3 |
0 |
0 |
0 |
0 |
- alpha-2-microglobulin |
3 (1.0) |
3 (2.0) |
3 (2.3) |
3 (2.7) |
0 |
0 |
0 |
0 |
|
||||||||
Stomach - Forestomach (microscopic changes recorded in the stomach) |
||||||||
Number Examined |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
- Hyperplasia, epithelial |
0 |
0 |
2 (1.0) |
2 (1.0) |
0 |
0 |
0 |
3 (1.0) |
(): Mean Severity
Findings in Bold were considered treatment-related
Table 15. Group Mean offspring Weights |
|||
Group |
|
Offspring Body Weight Change (g) – Days 1-4 |
|
Males |
Females |
||
Control (0 mg/Kg bw/day) |
Mean (g) |
3.18 |
3.07 |
S.D. |
0.90 |
0.82 |
|
N |
10 |
11 |
|
|
|||
100 mg/Kg bw/day |
Mean (g) |
3.07 |
3.02 |
S.D. |
0.67 |
0.61 |
|
N |
11 |
11 |
|
|
|||
300 mg/Kg bw/day |
Mean (g) |
2.60 |
2.54 |
S.D. |
0.62 |
0.48 |
|
N |
12 |
12 |
|
|
|||
1000 mg/Kg bw/day |
Mean (g) |
2.30* |
2.42 |
S.D. |
0.85 |
0.78 |
|
N |
10 |
9 |
* Significantly different from control group p<0.05
Table 16. Group Mean Implantation Losses and Survival Indices Values |
|||||
Group |
|
Pre-Implantation Loss (%) |
Post-Implantation Loss (%) |
Live Birth Index (%) |
Viability Index (%) |
Control (0 mg/Kg bw/day) |
Mean |
13.9 |
8.5 |
100.0 |
98.9 |
S.D. |
13.7 |
9.2 |
0.0 |
3.8 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
100 mg/Kg bw/day |
Mean |
7.9 |
12.6 |
100.0 |
99.2 |
S.D. |
16.2 |
15.3 |
0.0 |
2.5 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
300 mg/Kg bw/day |
Mean |
3.4 |
5.4 |
100.0 |
99.4 |
S.D. |
4.9 |
6.0 |
0.0 |
1.9 |
|
N |
12 |
12 |
12 |
12 |
|
|
|||||
1000 mg/Kg bw/day |
Mean |
12.2 |
12.1 |
97.1 |
91.9* |
S.D. |
18.6 |
8.2 |
7.2 |
9.5 |
|
N |
11 |
11 |
11 |
10 |
* Significantly different from control group p<0.05
- Reason / purpose for cross-reference:
- other: Independent Analysis
- Reason / purpose for cross-reference:
- other: GLP Certificate
Data source
Reference
- Reference Type:
- study report
- Title:
- Unnamed
- Year:
- 2 014
- Report date:
- 2014
Materials and methods
Test guideline
- Qualifier:
- according to guideline
- Guideline:
- OECD Guideline 422 (Combined Repeated Dose Toxicity Study with the Reproduction / Developmental Toxicity Screening Test)
- Deviations:
- no
- GLP compliance:
- yes (incl. QA statement)
Test material
- Reference substance name:
- Nonene, branched
- EC Number:
- 306-492-6
- EC Name:
- Nonene, branched
- Cas Number:
- 97280-95-0
- Molecular formula:
- C9H18
- IUPAC Name:
- Nonene, branched
- Test material form:
- other: Clear colorless liquid
- Details on test material:
- - Name of test material: Nonene, branched
- CAS No.:97280-95-0
- Substance type: UVCB
- Physical state: Clear colorless liquid
- Analytical purity: 100%
- Lot/batch No.: TQ-12-2003-23042013
- Data received: 29 April 2013
- Label: Nonene Sampling Date Apr 22.2013
- Expiration date of the lot/batch: 23 April2014
Constituent 1
- Specific details on test material used for the study:
- - Name of test material: Nonene, branched
- CAS No.:97280-95-0
- Substance type: UVCB
- Physical state: Clear colorless liquid
- Analytical purity: 100%
- Lot/batch No.: TQ-12-2003-23042013
- Data received: 29 April 2013
- Label: Nonene Sampling Date Apr 22.2013
- Expiration date of the lot/batch: 23 April2014
Nonene, branched, CAS# 97280-95-0 used in this study was a typical production sample, according to the details included in the boundary composition in IUCLID section 1.2. Nonene, branched was chosen in the Higher Olefins category testing strategy because it represents a substance with high tri-sub content (category range 1 – 65%), odd carbon number (C9 odd 90%). Please see the testing strategy attached in section 13 for further details.
Test animals
- Species:
- rat
- Strain:
- other: Wistar Han™:RccHan™:WIST strain rats
- Sex:
- male/female
- Details on test animals or test system and environmental conditions:
- TEST ANIMALS
- Source: Harlan Laboratories U.K. Ltd., Blackthorn, Bicester, Oxon, UK.
- Age at study initiation: 12 weeks old
- Weight at study initiation: (P) Males: 311 to 375 g; Females: 194 to 222 g.
- Housing: Pre-mating: groups of four animals were housed in solid floor polypropylene cages with stainless steel mesh lids and softwood flake bedding (Datesand Ltd., Cheshire, UK). Pairing phase: polypropylene grid floor cages suspended over trays lined with absorbent paper on a one male: one female basis within each dose group. Post mating: the males were returned to their original cages. Mated females were housed individually during gestation and lactation in solid floor polypropylene cages with stainless steel mesh lids and softwood flakes.
- Use of restrainers for preventing ingestion (if dermal): yes/no
- Diet (e.g. ad libitum): A pelleted diet (Rodent 2018C Teklad Global Certified Diet, Harlan Laboratories U.K. Ltd., Oxon, UK.)
- Water (e.g. ad libitum): free access to food and water
- Acclimation period: 5 days
ENVIRONMENTAL CONDITIONS
- Temperature (°C): 21 +/-2°C
- Humidity (%): 55 =/- 15%
- Air changes (per hr): at least 15 air changes per hour. The low intensity fluorescent lighting was controlled to give twelve hours continuous light
- Photoperiod (hrs dark / hrs light): 12 hr dark and 12 hr light
The study was performed between 10 June 2013 and 10 June 2014. The in-life phase of the study was conducted between 22 August 2013 (first day of treatment) and 17 October 2013 (final day of necropsy).
Administration / exposure
- Route of administration:
- oral: gavage
- Vehicle:
- arachis oil
- Details on exposure:
- PREPARATION OF DOSING SOLUTIONS:
DIET PREPARATION
- Mixing appropriate amounts with (Type of food): Arachis oil BP
- Storage temperature of food: 4 C
VEHICLE
- Amount of vehicle (if gavage): 4 ml/kg
- Concentration in vehicle:
- Control: 0 ml/kg
- Low: 25 mg/ml
- Intermediate: 75 mg/ml
- High: 250 mg/ml
- Lot/batch no. (if required): 2018C-020713MA
- The volume of the test and control item administrated to each animal was based on the most recent scheduled body weight and was adjusted at weekly intervals. - Details on mating procedure:
- - M/F ratio per cage: 1/1
- Length of cohabitation:15 days
- Proof of pregnancy referred to as day 0 of pregnancy
- After successful mating each pregnant female was caged individually during gestation and lactation in solid floor polypropylene cages. - Analytical verification of doses or concentrations:
- yes
- Duration of treatment / exposure:
- 6 weeks
- Frequency of treatment:
- The test item was administrated daily by gavage using a stainless cannula attached to a disposable plastic syringe. Control animals were treated in an identical manner with 4 ml/kg of Arachis oil BP.
- Details on study schedule:
- i. Groups of twelve male and twelve female animals were treated daily at the appropriate dose level throughout the study (except for females during parturition where applicable). The first day of dosing was designated as Day 1 of the study.
ii. Prior to the start of treatment and once weekly thereafter, all animals were observed for signs of functional/behavioral toxicity.
iii. On Day 15, animals were paired on a 1 male: 1 female basis within each dose group for a maximum of fourteen days.
iv. Following evidence of mating (designated as Day 0 post coitum) the males were returned to their original cages and females were transferred to individual cages.
v. On completion of the pairing phase (during Week 6), five selected males per dose group were evaluated for functional/sensory responses to various stimuli.
vi. Pregnant females were allowed to give birth and maintain their offspring until Day 5 post partum. Litter size, offspring weight and sex, surface righting and clinical signs were also recorded during this period.
vii. At Day 4 post partum, five selected females per dose group were evaluated for functional/sensory responses to various stimuli.
viii. Blood samples were taken from five males from each dose group for hematological and blood chemical assessments on Day 42. The male dose groups were killed and examined macroscopically on Day 43.
ix. Blood samples were taken from five randomly selected females from each dose group for hematological and blood chemical assessment on Day 4 post partum. At Day 5 post partum, all females and surviving offspring were killed and examined macroscopically. Any female which did not produce a pregnancy was also killed and examined macroscopically.
Doses / concentrationsopen allclose all
- Dose / conc.:
- 100 mg/kg bw/day (actual dose received)
- Remarks:
- Doses / Concentrations:
Basis: actual ingested 100 mg/kg bw/day
- Dose / conc.:
- 300 mg/kg bw/day (actual dose received)
- Remarks:
- Doses / Concentrations:
Basis: actual ingested 300 mg/kg bw/day
- Dose / conc.:
- 1 000 mg/kg bw/day (actual dose received)
- Remarks:
- Doses / Concentrations:
Basis: actual ingested 1000 mg/kg bw/day
- No. of animals per sex per dose:
- Three groups, each of twelve males and twelve females
- Control animals:
- yes, concurrent vehicle
- Details on study design:
- - Dose selection rationale: Dose selected during the Range-finding experiment - Study Number 41301414
Examinations
- Parental animals: Observations and examinations:
- Clinical Observations:
Signs of toxicity, ill-health and behavioural change immediately before dosing, soon after dosing, and one hour after dosing throughout the treatment period.
Functional Observations:
All animals were observed for signs of functional/behavioural toxicity prior to the start of treatment and at weekly intervals thereafter.
Functional performance tests were also performed on five selected males and females from each dose level, prior to termination, together with an assessment of sensory reactivity to various stimuli.
- behavioural assessment
- functional Performance Tests
- Sensory Reactivity
Body Weight:
Individual body weights: Day 1 (prior to dosing), weekly for surviving males until termination and weekly for females until mating was evident.
Female: Days 0, 7, 14 and 20 post coitum, and on Days 1, 4 post partum and terminal kill.
Food Consumption:
Pre-pairing period and after (male): weekly
Females showing evidence of mating: post coitum Days 0-7, 7-14 and 14-20.
Females with live litters: Days 1 and 4 post partum.
Food efficiency:
Males (throughout the study period-with the exception of the mating phase, and females during the pre-pairing phase
Water Consumption:
Daily- visual inspection of the water bottles
Reproductive Performance:
Presence of ejected copulation plugs and each female was examined for the presence of a copulation plug in the vagina.
A vaginal smear was prepared for each female and the stage of oestrus or the presence of sperm was recorded.
The presence of sperm within the vaginal smear and/or vaginal plug in situ was taken as positive evidence of mating (Day 0 of gestation).
Pregnancy and Parturition:
Pregnant females: observations at approximately 0830, 1230 and 1630 hours and around the period of expected parturition (08.30 and 12.30 hr at weekends and public holidays)
Female data collections:
i. Date of pairing
ii. Date of mating
iii. Date and time of observed start of parturition
iv. Date and time of observed completion of parturition
Laboratory Investigations:
- Haematology
- Blood Chemistry - Litter observations:
- Number of live and dead offspring
For each litter the following was recorded:
i. Number of offspring born
ii.Number of offspring alive recorded daily and reported on Days 1 and 4 post partum
iii. Sex of offspring on Days 1 and 4 post partum
iv. Clinical condition of offspring from birth to Day 5 post partum
v. Individual offspring weights on Days 1 and 4 post partum (litter weights were calculated retrospectively from this data)
All live offspring were assessed for surface righting reflex on Day 1 post partum. - Postmortem examinations (parental animals):
- Pathology Females: Uterus (for signs of implantation and the number of uterine implantations in each horn), the corpora lutea. All adult animals and offspring: full external and internal examination. All macroscopic abnormalities were recorded.
- Organ Weights- Histopathology: Tissues from 5 selected male and female animals/group were preserved. Histopathological examination was undertaken on tissues from control and high dost animals.
To clarify possible treatment-related changes, histopathological examination was extended to include similarly prepared sections of the liver, kidneys (males only), stomach, thyroid and pituitary from animals in the low and intermediate groups. In addition, male kidney tissue was subject to immunohistochemical examination to confirm the presence of alph-2-microglobulin. - Postmortem examinations (offspring):
- All adult animals and offspring, including those dying during the study, were subjected to a full external and internal examination, and any macroscopic abnormalities were recorded.
- Statistics:
- Please see "Any other information on materials and methods incl. tables" for information on statistics.
- Reproductive indices:
- - Pre-coital Interval
- Fertility Indices
- Gestation length
- Parturition Index - Offspring viability indices:
- - Implantation Losses (%)
- Live Birth and Viability Indices
- Sex Ratio (% males)
Results and discussion
Results: P0 (first parental generation)
General toxicity (P0)
- Clinical signs:
- effects observed, treatment-related
- Description (incidence and severity):
- 1000 and 300 mg/kg bw/day: Increasing salivation in males and females. No effects in animals of either sex treated with 100 mg/kg bw/day.
- Mortality:
- no mortality observed
- Description (incidence):
- There were no unscheduled deaths.
- Body weight and weight changes:
- effects observed, treatment-related
- Description (incidence and severity):
- Males treated with 1000 mg/kg bw/day showed a statistically significant reduction in body weight gain during Weeks 1 and 3 of treatment. Overall body weight gain was reduced for these males.
No such effects were detected in treated females or in males treated with 300 or 100 mg/kg bw/day.
Females treated with 300 mg/kg bw/day showed a statistically significant increase in cumulative body weight gain during the final week of gestation. An increase in body weight gain is considered not to represent an adverse effect oftreatment therefore the intergroup difference was considered not to be of toxicological importance. - Food consumption and compound intake (if feeding study):
- effects observed, treatment-related
- Description (incidence and severity):
- No adverse effect on food consumption was detected in treated animals when compared to control animals.
Females treated with 1000 mg/kg bw/day showed a statistically significant increase in food consumption during the second week of gestation. An increase in food consumption is considered not to represent an adverse effect of treatment therefore the intergroup difference was considered not to be of toxicological importance. - Food efficiency:
- no effects observed
- Description (incidence and severity):
- No adverse effect on food efficiency was detected in treated animals when compared to control animals.
- Water consumption and compound intake (if drinking water study):
- effects observed, treatment-related
- Description (incidence and severity):
- Daily measurements of water bottles revealed a marked increase in water consumption in males treated with 1000 mg/kg bw/day and a slight increase in males treated with 300 or 100 mg/kg bw/day throughout the treatment period. Females from all treatment groups also showed an increase in water consumption throughout the treatment period with statistical significance being achieved throughout gestation and lactation at 1000 mg/kg bw/day.
- Haematological findings:
- effects observed, treatment-related
- Description (incidence and severity):
- Males treated with 1000 mg/kg bw/day showed a reduction in hemoglobin. Three out of the five individual values were outside of the normal background range for this parameter.
No toxicologically significant effects were detected in females treated with 1000 mg/kg bw/day or animals of either sex treated with 300 or 100 mg/kg bw/day.
Males treated with 1000 mg/kg bw/day showed a reduction in mean corpuscular hemoglobin. Males treated with 1000 and 300 mg/kg bw/day showed a reduction in mean corpuscular hemoglobin concentration. Males from all treatment groups also showed a reduction in
prothrombin time. All of the individual values were within the normal background range for these parameters, therefore the intergroup differences were considered not to be of toxicological importance. Females from all treatment groups showed a statistically significant increase in neutrophil count. The majority of individual values were within the normal background range for these parameters and a true dose related response was not evident, therefore the intergroup differences were considered not to be of toxicological significance. - Clinical biochemistry findings:
- effects observed, treatment-related
- Description (incidence and severity):
- No toxicologically significant effects were detected in the blood chemical parameters examined.
Males treated with 1000 and 300 mg/kg bw/day showed a statistically significant increase in calcium concentration and a statistically significant reduction in alkaline phosphatase. Males treated with 1000 mg/kg bw/day also showed a reduction in cholesterol. All of the individual values were within the normal ranges for rats ofthe strain and age used and in the absence of a true dose related response or any associated histology correlates the intergroup differences were considered not to be of toxicological importance. - Behaviour (functional findings):
- effects observed, treatment-related
- Description (incidence and severity):
- Behavioral Assessments
Weekly open field arena observations did not reveal any treatment-related effects for treated animals when compared to controls.
Functional Performance Tests
There were no toxicologically significant changes in functional performance. Males from all treatment groups showed a statistically significant increase in fore limb grip strength. The statistically significant difference was confined to one out of the three tests and in the absence of a true dose related response or any supporting clinical observations to suggest an effect of neurotoxicity, the intergroup differences were considered to be of no toxicological significance.
Sensory Reactivity Assessments
There were no treatment-related changes in sensory reactivity. - Organ weight findings including organ / body weight ratios:
- effects observed, treatment-related
- Histopathological findings: non-neoplastic:
- effects observed, treatment-related
- Description (incidence and severity):
- The following treatment related microscopic findings were detected:
Liver:hepatocyte hypertrophy was evident in animals of either sex treated with 1000 and 300 mg/kg bw/day and in males treated with 100 mg/kg bw/day. No such effects were detected in females treated with 100 mg/kg bw/day.
Kidneys:proximal tubular basophilia and hyaline droplets were evident in males from all treatment groups. Tubular degeneration/debris was evident in males treated with 1000 and 300 mg/kg bw/day. These findings were demonstrated by immunohistochemical staining to be
due to alpha-2-microglobulin nephropathy. No such effects were detected in any treated female.
Stomach:epithelial hyperplasia was evident in the fore stomach of animals of either sex treated with 1000 mg/kg bw/day and in males treated with 300 mg/kg bw/day. No such effects were detected in females treated with 300 mg/kg bw/day or animals of either sex treated with 100 mg/kg bw/day.
Thyroid:follicular cell hypertrophy and hyperplasia was evident in animals of either sex treated with 1000 and 300 mg/kg bw/day and in males treated with 100 mg/kg bw/day. No such effects were detected in females treated with 100 mg/kg bw/day.
Pituitary:increased incidence and severity of hypertrophic/vacuolated cells in pars anterior was evident in males treated with 1000 and 300 mg/kg bw/day. No such effects were detected in any treated female or in males treated with 100 mg/kg bw/day. - Other effects:
- no effects observed
Reproductive function / performance (P0)
- Reproductive function: oestrous cycle:
- no effects observed
- Reproductive function: sperm measures:
- no effects observed
- Reproductive performance:
- effects observed, non-treatment-related
- Description (incidence and severity):
- Mating
There were no treatment-related effects on mating performance.
Fertility
No treatment-related effects on fertility were detected for treated animals, when compared to controls.
One control female and one female treated 100 mg/kg bw/day did not achieve pregnancy following evidence of mating. No histopathological correlates were evident in the female or male reproductive organs which could have been the cause of the infertility. One female treated with 1000 mg/kg bw/day failed to show any positive signs of mating and was non pregnant.
Gestation Length
There were no differences in gestation lengths. The distribution for treated females was comparable to controls. All animals showed gestation lengths of 22 to 24½ days.
Details on results (P0)
1000 and 300 mg/kg bw/day: Increasing salivation in males and females. No effects in animals of either sex treated with 100 mg/kg bw/day.
Body Weight and Weight Changes:
Males treated with 1000 mg/kg bw/day showed a statistically significant reduction in body weight gain during Weeks 1 and 3 of treatment. Overall body weight gain was reduced for these males.
No such effects were detected in treated females or in males treated with 300 or 100 mg/kg bw/day.
Females treated with 300 mg/kg bw/day showed a statistically significant increase in cumulative body weight gain during the final week of gestation. An increase in body weight gain is considered not to represent an adverse effect oftreatment therefore the intergroup difference was considered not to be of toxicological importance.
Food consumption and Compound Intake:
No adverse effect on food consumption was detected in treated animals when compared to control animals.
Females treated with 1000 mg/kg bw/day showed a statistically significant increase in food consumption during the second week of gestation. An increase in food consumption is considered not to represent an adverse effect of treatment therefore the intergroup difference was considered not to be of toxicological importance.
Water Consumption:
Daily measurements of water bottles revealed a marked increase in water consumption in males treated with 1000 mg/kg bw/day and a slight increase in males treated with 300 or 100 mg/kg bw/day throughout the treatment period. Females from all treatment groups also showed an increase in water consumption throughout the treatment period with statistical significance being achieved throughout gestation and lactation at 1000 mg/kg bw/day.
Hematology:
Males treated with 1000 mg/kg bw/day showed a reduction in hemoglobin. Three out of the five individual values were outside of the normal background range for this parameter.
No toxicologically significant effects were detected in females treated with 1000 mg/kg bw/day or animals of either sex treated with 300 or 100 mg/kg bw/day.
Males treated with 1000 mg/kg bw/day showed a reduction in mean corpuscular hemoglobin. Males treated with 1000 and 300 mg/kg bw/day showed a reduction in mean corpuscular hemoglobin concentration. Males from all treatment groups also showed a reduction in
prothrombin time. All of the individual values were within the normal background range for these parameters, therefore the intergroup differences were considered not to be of toxicological importance. Females from all treatment groups showed a statistically significant increase in neutrophil count. The majority of individual values were within the normal background range for these parameters and a true dose related response was not evident, therefore the intergroup differences were considered not to be of toxicological significance.
Clinical Biochemistry:
No toxicologically significant effects were detected in the blood chemical parameters examined.
Males treated with 1000 and 300 mg/kg bw/day showed a statistically significant increase in calcium concentration and a statistically significant reduction in alkaline phosphatase. Males treated with 1000 mg/kg bw/day also showed a reduction in cholesterol. All of the individual values were within the normal ranges for rats ofthe strain and age used and in the absence of a true dose related response or any associated histology correlates the intergroup differences were considered not to be of toxicological importance.
Behaviour:
Functional Performance Tests - There were no toxicologically significant changes in functional performance. Males from all treatment groups showed a statistically significant increase in fore limb grip strength. The statistically significant difference was confined to one out of the three tests and in the absence of a true dose related response or any supporting clinical observations to suggest an effect of neurotoxicity, the intergroup differences were considered to be of no toxicological significance.
Organ Weight:
Animals of either sex treated with 1000 and 300 mg/kg bw/day and females treated with 100 mg/kg bw/day showed an increase in absolute and relative liver weight. Males treated with 1000 mg/kg bw/day also showed an increase in kidney weight both absolute and relative to terminal body weight. Males from all treatment groups showed an increase in absolute and relative thyroid weight whilst females treated with 1000 mg/kg bw/day showed a reduction in absolute and relative thyroid weight. All of the individual values were within the normal range for rats of the strain and age used and the effect on male thyroid weight also did not show a true dose related response. However with the associated microscopic thyroid changes observed in this study the intergroup differences detected in thyroid weights can not be excluded as an effect of treatment.
Females treated with 1000 mg/kg bw/day showed a reduction in pituitary weight and an increase in kidney weight both absolute and relative to terminal body weight. In the absence of any associated histopathological changes detected in the kidneys or pituitary of females the intergroup differences were considered not to be of toxicological importance.
Necropsy:
Nine males treated with 1000 mg/kg bw/day had enlarged kidneys at necropsy, eight of which had pale kidneys; four showed a mottled appearance to the kidneys and five of these males also had a dark liver at necropsy. One male treated with 300 mg/kg bw/day had enlarged kidneys at necropsy.
No toxicologically significant effects were detected in females from any treatment group or in males treated with 100 mg/kg bw/day.
One male treated with 100 mg/kg bw/day had small testes and epididymides. One female treated with 300 mg/kg bw/day and two females treated with 100 mg/kg bw/day had reddened lungs at necropsy. Histopathological examination of these tissues did reveal associated microscopic findings to the macroscopic abnormalities however in the absence of a similar effect seen at 1000 mg/kg bw/day, the intergroup differences were considered to be incidental and of no toxicological importance.
Histopathology:
Liver:hepatocyte hypertrophy was evident in animals of either sex treated with 1000 and 300 mg/kg bw/day and in males treated with 100 mg/kg bw/day. No such effects were detected in females treated with 100 mg/kg bw/day.
Kidneys:proximal tubular basophilia and hyaline droplets were evident in males from all treatment groups. Tubular degeneration/debris was evident in males treated with 1000 and 300 mg/kg bw/day. These findings were demonstrated by immunohistochemical staining to be
due to alpha-2-microglobulin nephropathy. No such effects were detected in any treated female.
Stomach:epithelial hyperplasia was evident in the fore stomach of animals of either sex treated with 1000 mg/kg bw/day and in males treated with 300 mg/kg bw/day. No such effects were detected in females treated with 300 mg/kg bw/day or animals of either sex treated with 100 mg/kg bw/day.
Thyroid:follicular cell hypertrophy and hyperplasia was evident in animals of either sex treated with 1000 and 300 mg/kg bw/day and in males treated with 100 mg/kg bw/day. No such effects were detected in females treated with 100 mg/kg bw/day.
Pituitary:increased incidence and severity of hypertrophic/vacuolated cells in pars anterior was evident in males treated with 1000 and 300 mg/kg bw/day. No such effects were detected in any treated female or in males treated with 100 mg/kg bw/day.
Reproductive Performance:
Fertility - No treatment-related effects on fertility were detected for treated animals, when compared to controls.
One control female and one female treated 100 mg/kg bw/day did not achieve pregnancy following evidence of mating. No histopathological correlates were evident in the female or male reproductive organs which could have been the cause of the infertility. One female treated with 1000 mg/kg bw/day failed to show any positive signs of mating and was non pregnant.
Effect levels (P0)
open allclose all
- Key result
- Dose descriptor:
- NOAEL
- Effect level:
- 1 000 mg/kg bw/day (actual dose received)
- Based on:
- test mat.
- Sex:
- male/female
- Basis for effect level:
- other: Systemic Toxicity
- Dose descriptor:
- NOEL
- Effect level:
- 300 mg/kg bw/day (actual dose received)
- Based on:
- test mat.
- Sex:
- male/female
- Basis for effect level:
- other: Reproductive Toxicity
Target system / organ toxicity (P0)
- Key result
- Critical effects observed:
- no
Results: F1 generation
General toxicity (F1)
- Clinical signs:
- effects observed, non-treatment-related
- Description (incidence and severity):
- No obvious clinical signs of toxicity were detected for offspring from treated females when compared to controls. The incidental clinical signs detected throughout the control and treated groups, consisting of small size, cold, weak, pale, no milk in stomach, physical injury, found dead or missing, were considered to be low incidence findings observed in offspring in studies of this type and were considered unrelated to test item toxicity.
- Mortality / viability:
- no mortality observed
- Body weight and weight changes:
- effects observed, treatment-related
- Description (incidence and severity):
- Litter weights on Day 4 post partum from females treated with 1000 mg/kg bw/day were reduced when compared to control litters however statistical significance was not achieved. Offspring body weight gain at 1000 mg/kg bw/day was also reduced between Days 1 and 4 post partum. Statistical significance was achieved for male off spring only. No such effects were detected in litters from females treated with 300 or 100 mg/kg bw/day.
- Sexual maturation:
- not examined
- Organ weight findings including organ / body weight ratios:
- no effects observed
- Gross pathological findings:
- effects observed, non-treatment-related
- Description (incidence and severity):
- No treatment-related macroscopic abnormalities were detected for interim death or terminal kill offspring. The incidental findings observed were those occasionally observed in reproductive studies of this type and were considered to be unrelated to toxicity of the test item.
- Histopathological findings:
- no effects observed
Developmental neurotoxicity (F1)
- Behaviour (functional findings):
- no effects observed
- Description (incidence and severity):
- Statistical analysis of surface righting reflex data did not reveal any significant intergroup differences.
Details on results (F1)
No significant differences were detected for corpora lutea, implantation counts or implantation losses for treated animals when compared to controls. Statistical analysis of the data did not reveal any significant intergroup differences.
Of the litters born, litter size at birth and subsequently on Day 1 post partumwere comparable to controls. Litter size on Day 4 post partumhowever was reduced in litters from females treated with 1000 mg/kg bw/day although statistical significance was not achieved. Offspring viability on Day 4 post partumwas statistically significantly reduced in these litters. A total litter loss was also observed for one female treated with 1000 mg/kg bw/day. No such effects were detected in litters from females treated with 300 or 100 mg/kg bw/day.
There were no intergroup differences in sex ratio (percentage male offspring) for litters from treated groups compared to controls. Statistical analysis of the data did not reveal any significant intergroup differences.
Offspring Growth and Development
Litter weights on Day 4 post partumfrom females treated with 1000 mg/kg bw/day were reduced when compared to control litters however statistical significance was not achieved. Offspring body weight gain at 1000 mg/kg bw/day was also reduced between Days 1 and 4 post partum. Statistical significance was achieved for male offspring only.
No such effects were detected in litters from females treated with 300 or 100 mg/kg bw/day. Statistical analysis of surface righting reflex data did not reveal any significant intergroup differences.
No obvious clinical signs of toxicity were detected for offspring from treated females when compared to controls. The incidental clinical signs detected throughout the control and treated groups, consisting of small size, cold, weak, pale, no milk in stomach, physical injury, found dead or missing, were considered to be low incidence findings observed in offspring in studies of this type and were considered unrelated to test item toxicity.
Effect levels (F1)
- Key result
- Dose descriptor:
- NOEL
- Generation:
- F1
- Effect level:
- 300 mg/kg bw/day (actual dose received)
- Based on:
- test mat.
- Sex:
- male/female
- Basis for effect level:
- other: reduced post natal offspring viability, offspring body weight gain and litter size at 1000 mg/kg bw/day.
Target system / organ toxicity (F1)
- Key result
- Critical effects observed:
- no
Overall reproductive toxicity
- Key result
- Reproductive effects observed:
- yes
- Lowest effective dose / conc.:
- 1 000 mg/kg bw/day (actual dose received)
- Treatment related:
- yes
- Relation to other toxic effects:
- reproductive effects occurring together with other toxic effects, but not as a secondary non-specific consequence of other toxic effects
- Dose response relationship:
- not specified
- Relevant for humans:
- not specified
Any other information on results incl. tables
Table 2. Summary of Reproductive Performance - Groups Values |
||||
|
Dose Group (mg/Kg bw/day |
|||
0 (Control) |
100 |
300 |
1000 |
|
Males |
|
|||
Initial group size |
12 |
12 |
12 |
12 |
Paired |
12 |
12 |
12 |
12 |
Failed to mate |
0 |
0 |
0 |
1 |
Failed to induce pregnancy in female partner |
1 |
1 |
0 |
0 |
Induced pregnancy in female partner |
11 |
11 |
12 |
11 |
Surviving to terminal necropsy |
12 |
12 |
12 |
12 |
|
||||
Females |
|
|||
Initial group size |
12 |
12 |
12 |
12 |
Paired |
12 |
12 |
12 |
12 |
Failed to mate |
0 |
0 |
0 |
1 |
Non-pregnant |
1 |
1 |
0 |
0 |
Rearing young to Day 5 of age |
11 |
11 |
12 |
10 |
Total Litter Loss |
0 |
0 |
0 |
1 |
Table 3. Group Mean Functional Test Values and Standard Deviations - Males |
|||||||||||
Group (sex) |
|
Test 1 Forelimb (g) |
Test 1 Hindlimb (g) |
Test 2 Forelimb (g) |
Test 2 Hindlimb (g) |
Test 3 Forelimb (g) |
Test 3 Hindlimb (g) |
Overall Activity |
Overall Mobile |
Last 20% Activity |
Last 20% Mobile |
1 (M) |
Mean |
1143.2 |
422.6 |
1004.2 |
524.4 |
985.2 |
445.0 |
377.2 |
0.6 |
3.4 |
0.0n |
S.D. |
234.7 |
131.5 |
113.9 |
66.2 |
91.6 |
76.7 |
122.9 |
0.9 |
4.0 |
0.0 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||||
2 (M) |
Mean |
1176.8 |
510.2 |
1303.0* |
581.4 |
1084.8 |
628.2 |
384.0 |
0.6 |
8.2 |
0.0n |
S.D. |
237.0 |
140.4 |
313.6 |
105.2 |
146.7 |
157.4 |
214.5 |
0.5 |
9.5 |
0.0 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||||
3 (M) |
Mean |
1353.0 |
593.8 |
1450.4* |
472.0 |
1378.2 |
528.2 |
334.6 |
0.2 |
4.2 |
0.0n |
S.D. |
297.1 |
121.5 |
200.0 |
147.6 |
442.9 |
177.5 |
141.7 |
0.4 |
5.2 |
0.0 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||||
4 (M) |
Mean |
1071.2 |
620.8 |
1271.0* |
473.4 |
1118.6 |
555.0 |
250.8 |
0.2 |
36.2 |
0.0n |
S.D. |
257.2 |
184.4 |
250.8 |
230.9 |
185.2 |
151.8 |
118.6 |
0.4 |
58.3 |
0.0 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
General Footnote: Unit = Time (seconds) for Motor Activity Assessments
Dose Levels: Group 1 - 0(Control); Group 2 - 100 mg/kg bw/day; Group 3 - 300 mg/kg bw/day; Group 4 - 1000 mg/kg bw/day
* Significantly different from control group p<0.05
n Data not appropriate for statistical analysis
Table 4. Group Mean Body Weight Values - Males |
|||||||||||
Group (sex) |
|
Increase in Body Weight (g) |
|||||||||
|
Day Numbers Relative to Start Date |
Abs Gain |
% Gain |
||||||||
From: |
1 |
8 |
15 |
22 |
29 |
36 |
1 |
1 |
|||
To: |
8 |
15 |
22 |
29 |
36 |
43 |
43 |
43 |
|||
1 (M) |
Mean |
14.4 |
13.0 |
9.7 |
14.6 |
10.2 |
6.8 |
68.6 |
20.9 |
||
S.D. |
5,8 |
6.5 |
6.6 |
6.0 |
4.5 |
3.7 |
21.7 |
5.9 |
|||
N |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
|||
|
|
|
|||||||||
2 (M) |
Mean |
13.9 |
12.5 |
6.9 |
13.3 |
12.0 |
4.3 |
63.0 |
19.0 |
||
S.D. |
3.8 |
3.9 |
6.3 |
4.4 |
3.4 |
5.1 |
16.9 |
4.8 |
|||
N |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
|||
|
|
|
|||||||||
3 (M) |
Mean |
13.4 |
15.3 |
7.3 |
14.1 |
11.9 |
8.1 |
70.2 |
21.3 |
||
S.D. |
5.5 |
5.0 |
3.9 |
4.6 |
5.6 |
3.4 |
18.8 |
5.3 |
|||
N |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
|||
|
|
|
|||||||||
4 (M) |
Mean |
5.5** |
10.0 |
1.7** |
12.4 |
8.1 |
5.1 |
42.8 |
13.0 |
||
S.D. |
9.8 |
7.5 |
6.8 |
3.8 |
4.8 |
4.8 |
18.0 |
5.3 |
|||
N |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
|||
Dose Levels: Group 1 - 0(Control); Group 2 - 100 mg/kg bw/day; Group 3 - 300 mg/kg bw/day; Group 4 - 1000 mg/kg bw/day
** Significantly different from control group p<0.01
Table 5. Group Mean Body Weight Gains - Females |
|||||||
Group (sex) |
|
Increase in Body Weight (g) |
Cumulative Body Weight Change (g) |
||||
|
Days |
Days |
|||||
|
Gestation |
Lactation |
Gestation |
||||
From: |
0 |
7 |
14 |
1 |
0 |
0 |
|
To: |
7 |
14 |
20 |
4 |
14 |
20 |
|
1 (F) |
Mean |
29.8 |
28.9 |
60.4 |
7.9 |
58.7 |
119.1 |
S.D. |
4.4 |
3.9 |
13.0 |
5.4 |
7.3 |
16.3 |
|
N |
11 |
11 |
11 |
11 |
11 |
11 |
|
|
|||||||
2 (F) |
Mean |
27.4 |
28.3 |
60.8 |
11.8 |
55.6 |
116.5 |
S.D. |
4.8 |
5.0 |
12.5 |
10.3 |
6.1 |
14.9 |
|
N |
11 |
11 |
11 |
11 |
11 |
11 |
|
|
|||||||
3 (F) |
Mean |
33.3 |
33.1 |
69.1 |
12.8 |
66.4 |
135.5* |
S.D. |
5.2 |
5.2 |
10.9 |
7.1 |
7.8 |
15.2 |
|
N |
12 |
12 |
12 |
12 |
12 |
12 |
|
|
|||||||
4 (F) |
Mean |
29.8 |
27.9 |
57.3 |
6.4 |
57.7 |
115.0 |
S.D. |
6.8 |
6.5 |
11.7 |
12.2 |
11.4 |
17.1 |
|
N |
11 |
11 |
11 |
10 |
11 |
11 |
Dose Levels: Group 1 - 0(Control); Group 2 - 100 mg/kg bw/day; Group 3 - 300 mg/kg bw/day; Group 4 - 1000 mg/kg bw/day
* Significantly different from control group p<0.05
Table 6. Group Mean Food Consumptions - Females |
|||||
Group (sex) |
|
Day Numbers |
|||
Gestation |
Lactation |
||||
From |
0 |
7 |
14 |
1 |
|
To |
7 |
14 |
20 |
4 |
|
1 (F) |
Mean |
19.7 |
22.3 |
25.1 |
26.5 |
S.D. |
1.8 |
1.9 |
2.4 |
4.6 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
2 (F) |
Mean |
20.2 |
22.5 |
24.6 |
29.5 |
S.D. |
2.0 |
2.3 |
1.2 |
8.3 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
3 (F) |
Mean |
20.7 |
23.6 |
25.5 |
28.2 |
S.D. |
1.2 |
1.2 |
1.1 |
3.3 |
|
N |
12 |
12 |
12 |
12 |
|
|
|||||
4 (F) |
Mean |
20.9 |
24.2* |
26.8 |
25.4 |
S.D. |
1.6 |
2.2 |
2.3 |
6.2 |
|
N |
11 |
11 |
11 |
10 |
Dose Levels: Group 1 - 0(Control); Group 2 - 100 mg/kg bw/day; Group 3 - 300 mg/kg bw/day; Group 4 - 1000 mg/kg bw/day
* Significantly different from control group p<0.05
Table 7. Group Mean Water Consumption - Females |
|||||
Group (sex) |
|
Day Numbers |
|||
Gestation |
Lactation |
||||
From |
0 |
7 |
14 |
1 |
|
To |
7 |
14 |
20 |
4 |
|
1 (F) |
Mean |
27.6 |
31.0 |
36.0 |
39.9 |
S.D. |
3.8 |
5.1 |
6.8 |
4.3 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
2 (F) |
Mean |
32.1 |
36.9 |
39.9 |
44.2 |
S.D. |
5.3 |
5.9 |
4.8 |
10.6 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
3 (F) |
Mean |
36.5 |
42.9 |
44.8 |
45.8 |
S.D. |
2.2 |
13.9 |
10.7 |
7.1 |
|
N |
12 |
12 |
12 |
12 |
|
|
|||||
4 (F) |
Mean |
52.6*** |
67.8*** |
76.4*** |
54.1** |
S.D. |
20.4 |
22.5 |
34.1 |
12.5 |
|
N |
11 |
11 |
11 |
11 |
Dose Levels: Group 1 - 0(Control); Group 2 - 100 mg/kg bw/day; Group 3 - 300 mg/kg bw/day; Group 4 - 1000 mg/kg bw/day
** Significantly different from control group p<0.01
*** Significantly different from control group p<0.001
Table 8. Group Mean Hematological Values - Males |
|||||
Group |
|
Hb (g/dL) |
MCH (pg) |
MCHC (g/dL) |
CT (seconds) |
Group 1 (0 – Control) |
Mean |
16.92 |
18.86 |
35.66 |
9.92 |
S.D. |
0.44 |
0.44 |
1.49 |
0.47 |
|
N |
5 |
5 |
5 |
5 |
|
|
|||||
Group 2 (100 mg/Kg bw/day) |
Mean |
16.86 |
18.64 |
35.18 |
9.40* |
S.D. |
0.74 |
0.11 |
0.67 |
0.23 |
|
N |
5 |
5 |
5 |
5 |
|
|
|||||
Group 3 (300 mg/Kg bw/day) |
Mean |
16.08 |
18.36 |
34.12** |
9.34* |
S.D. |
0.31 |
0.48 |
0.53 |
0.26 |
|
N |
5 |
5 |
5 |
5 |
|
|
|||||
Group 4 (1000 mg/Kg bw/day) |
Mean |
14.94** |
17.58** |
33.72** |
9.34* |
S.D. |
1.56 |
0.63 |
0.28 |
0.36 |
|
N |
5 |
5 |
5 |
5 |
* Significantly different from control group p<0.05
** Significantly different from control group p<0.01
Table 9. Group Mean Hematological Values - Females |
||
Group |
|
Neut (109/L) |
Group 1 (0 – Control) |
Mean |
1.360 |
S.D. |
0.417 |
|
N |
5 |
|
|
||
Group 2 (100 mg/Kg bw/day) |
Mean |
2.500* |
S.D. |
0.568 |
|
N |
5 |
|
|
||
Group 3 (300 mg/Kg bw/day) |
Mean |
2.146* |
S.D. |
0.463 |
|
N |
5 |
|
|
||
Group 4 (1000 mg/Kg bw/day) |
Mean |
1.872* |
S.D. |
0.509 |
|
N |
5 |
* Significantly different from control group p<0.05
Table 10. Group Mean Blood Chemical Values - Males |
||||
Group |
|
Ca++(mmol/L) |
AP (IU/L) |
Chol (mg/dL) |
Group 1 (0 – Control) |
Mean |
2.448 |
234.0 |
95.2 |
S.D. |
0.258 |
52.1 |
5.3 |
|
N |
5 |
5 |
5 |
|
|
||||
Group 2 (100 mg/Kg bw/day) |
Mean |
2.522 |
201.6 |
102.6 |
S.D. |
0.146 |
26.1 |
14.4 |
|
N |
5 |
5 |
5 |
|
|
||||
Group 3 (300 mg/Kg bw/day) |
Mean |
2.730* |
150.6** |
99.4 |
S.D. |
0.077 |
10.8 |
10.7 |
|
N |
5 |
5 |
5 |
|
|
||||
Group 4 (1000 mg/Kg bw/day) |
Mean |
2.644* |
157.6** |
78.0* |
S.D. |
0.129 |
55.2 |
13.3 |
|
N |
5 |
5 |
5 |
* Significantly different from control group p<0.05
** Significantly different from control group p<0.01
Table 11. Summary Incidence of Necropsy Findings - Males |
||||
|
Males |
|||
0 Control |
100 mg/Kg bw/day |
300 mg/Kg bw/day |
1000 mg/Kg bw/day |
|
Number of animals examined |
12 |
12 |
12 |
12 |
Epididymides |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
11 |
12 |
12 |
Small; Left |
0 |
1 |
0 |
0 |
|
||||
Kidneys |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
12 |
11 |
3 |
Enlarged |
0 |
0 |
1 |
9 |
Mottled Appearance |
0 |
0 |
0 |
4 |
Pallor |
0 |
0 |
0 |
3 |
Pale |
0 |
0 |
0 |
6 |
|
||||
Liver |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
12 |
12 |
7 |
Dark |
0 |
0 |
0 |
5 |
|
||||
Testes |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
11 |
12 |
12 |
Small; Left |
0 |
1 |
0 |
0 |
Table 12. Summary Incidence of Necropsy Findings - Females |
||||
|
Females |
|||
0 Control |
100 mg/Kg bw/day |
300 mg/Kg bw/day |
1000 mg/Kg bw/day |
|
Number of animals examined |
12 |
12 |
12 |
12 |
Liver |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
12 |
12 |
11 |
Dark |
0 |
0 |
0 |
1 |
|
||||
Lungs (With Bronchi) |
|
|||
Submitted |
(12) |
(12) |
(12) |
(12) |
No Visible Lesions |
12 |
10 |
11 |
12 |
Reddened |
0 |
2 |
1 |
0 |
Table 13. Group Mean Organ Weights with Corresponding Relative (% of Body Weight) Organ Weights |
|||||||||
|
|
Males |
Females |
||||||
0 Control |
100 mg/Kg bw/day |
300 mg/Kg bw/day |
1000 mg/Kg bw/day |
0 Control |
100 mg/Kg bw/day |
300 mg/Kg bw/day |
1000 mg/Kg bw/day |
||
Kidneys |
Mean (g) |
2.29348 |
2.31240 |
2.38234 |
3.16702** |
1.54460 |
1.65510 |
1.66136 |
1.97002** |
S.D. |
0.32697 |
0.14310 |
0.16218 |
0.44018 |
0.14343 |
0.11476 |
0.20712 |
0.11782 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||
Mean (%) |
0.574 |
0.585 |
0.616 |
0.830** |
0.565 |
0.610 |
0.602 |
0.701** |
|
S.D. |
0.046 |
0.013 |
0.051 |
0.102 |
0.047 |
0.035 |
0.055 |
0.041 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||
Liver |
Mean (g) |
12.7830 |
13.2647 |
14.3898** |
19.3412** |
10.5429 |
11.7936* |
12.7876** |
16.1219** |
S.D. |
1.51792 |
0.98038 |
1.33119 |
1.23327 |
0.51191 |
0.52983 |
1.29755 |
1.61466 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||
Mean (%) |
3.203 |
3.355 |
3.710** |
5.070** |
3.857 |
4.353* |
4.638** |
5.742** |
|
S.D. |
0.125 |
0.111 |
0.164 |
0.230 |
0.149 |
0.194 |
0.424 |
0.639 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||
Pituitary |
Mean (g) |
|
|
|
|
0.01793 |
0.01529 |
0.01783 |
0.01467** |
S.D. |
|
|
|
|
0.00277 |
0.00241 |
0.00264 |
0.00180 |
|
N |
|
|
|
|
11 |
11 |
12 |
10 |
|
|
|
||||||||
Mean (%) |
|
|
|
|
0.006 |
0.006 |
0.006 |
0.005** |
|
S.D. |
|
|
|
|
0.001 |
0.001 |
0.001 |
0.001 |
|
N |
|
|
|
|
11 |
11 |
12 |
10 |
|
|
|||||||||
Thyroid/Parathyroid |
Mean (g) |
0.01552 |
0.02172** |
0.02162** |
0.02112** |
0.002238 |
0.01972 |
0.02046 |
0.01776* |
S.D. |
0.00377 |
0.00176 |
0.00140 |
0.00207 |
0.00395 |
0.00339 |
0.00202 |
0.00259 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
|
|
|||||||||
Mean (%) |
0.004 |
0.005** |
0.006** |
0.006** |
0.008 |
0.007 |
0.007 |
0.006* |
|
S.D. |
0.001 |
0.000 |
0.000 |
0.000 |
0.002 |
0.001 |
0.001 |
0.001 |
|
N |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
* Significantly different from control group p<0.05
** Significantly different from control group p<0.01
Table 14. Histopathology – Treatment-related Findings |
||||||||
|
Male |
Female |
||||||
Dosage (mg/Kg bw/day) |
0 |
100 |
300 |
1000 |
0 |
100 |
300 |
1000 |
|
||||||||
Liver |
||||||||
Number Examined |
5 |
5 |
5 |
9 |
5 |
5 |
5 |
6 |
- Hypertrophy; hepatoc. |
0 |
5 (1.0) |
5 (1.0) |
9 (1.7) |
0 |
0 |
3 (1.0) |
6 (1.0) |
- Congestion |
0 |
0 |
0 |
5 (1.0) |
0 |
0 |
0 |
1(3.0) |
|
||||||||
Thyroid |
||||||||
Number Examined |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
- Hypertrophy / Hyperplasia; Follicular Cell |
2 (1.0) |
5 (1.4) |
5 (1.4) |
5 (1.8) |
2 (1.0) |
2 (1.0) |
3 (1.3) |
5 (1.2) |
|
||||||||
Pituitary Gland |
||||||||
Number Examined |
12 |
12 |
12 |
12 |
12 |
12 |
12 |
10 |
-Hypertrophic / Vacuolated cells in Pars Anterior |
10 (1.0) |
9 (1.2) |
12 (1.4) |
9 (1.6) |
0 |
0 |
3 (1.0) |
0 |
|
||||||||
Kidney |
||||||||
Number Examined |
5 |
5 |
5 |
9 |
5 |
5 |
5 |
5 |
- Tubular Basophilia |
0 |
3 (1.0) |
4 (1.3) |
9 (2.0) |
0 |
0 |
0 |
1 (1.0) |
- Tubular Degeneration / Debris |
0 |
0 |
4 (1.0) |
7 (2.0) |
0 |
0 |
0 |
0 |
- Hyaline Droplets |
0 |
5 (1.0) |
5 (1.8) |
9 (2.1) |
0 |
0 |
0 |
0 |
|
||||||||
Kidney Immunohistochemistry |
||||||||
Number Examined |
3 |
3 |
3 |
3 |
0 |
0 |
0 |
0 |
- alpha-2-microglobulin |
3 (1.0) |
3 (2.0) |
3 (2.3) |
3 (2.7) |
0 |
0 |
0 |
0 |
|
||||||||
Stomach - Forestomach (microscopic changes recorded in the stomach) |
||||||||
Number Examined |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
5 |
- Hyperplasia, epithelial |
0 |
0 |
2 (1.0) |
2 (1.0) |
0 |
0 |
0 |
3 (1.0) |
(): Mean Severity
Findings in Bold were considered treatment-related
Table 15. Group Mean offspring Weights |
|||
Group |
|
Offspring Body Weight Change (g) – Days 1-4 |
|
Males |
Females |
||
Control (0 mg/Kg bw/day) |
Mean (g) |
3.18 |
3.07 |
S.D. |
0.90 |
0.82 |
|
N |
10 |
11 |
|
|
|||
100 mg/Kg bw/day |
Mean (g) |
3.07 |
3.02 |
S.D. |
0.67 |
0.61 |
|
N |
11 |
11 |
|
|
|||
300 mg/Kg bw/day |
Mean (g) |
2.60 |
2.54 |
S.D. |
0.62 |
0.48 |
|
N |
12 |
12 |
|
|
|||
1000 mg/Kg bw/day |
Mean (g) |
2.30* |
2.42 |
S.D. |
0.85 |
0.78 |
|
N |
10 |
9 |
* Significantly different from control group p<0.05
Table 16. Group Mean Implantation Losses and Survival Indices Values |
|||||
Group |
|
Pre-Implantation Loss (%) |
Post-Implantation Loss (%) |
Live Birth Index (%) |
Viability Index (%) |
Control (0 mg/Kg bw/day) |
Mean |
13.9 |
8.5 |
100.0 |
98.9 |
S.D. |
13.7 |
9.2 |
0.0 |
3.8 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
100 mg/Kg bw/day |
Mean |
7.9 |
12.6 |
100.0 |
99.2 |
S.D. |
16.2 |
15.3 |
0.0 |
2.5 |
|
N |
11 |
11 |
11 |
11 |
|
|
|||||
300 mg/Kg bw/day |
Mean |
3.4 |
5.4 |
100.0 |
99.4 |
S.D. |
4.9 |
6.0 |
0.0 |
1.9 |
|
N |
12 |
12 |
12 |
12 |
|
|
|||||
1000 mg/Kg bw/day |
Mean |
12.2 |
12.1 |
97.1 |
91.9* |
S.D. |
18.6 |
8.2 |
7.2 |
9.5 |
|
N |
11 |
11 |
11 |
10 |
* Significantly different from control group p<0.05
Applicant's summary and conclusion
- Conclusions:
- Oral administration of Nonene, branched to rats for 8 weeks, at levels of 100, 300 and 1000 mgk/kg/day, resulted in treatment related effects in both sexes and at all treatment levels. The effects seen were however either adaptive in nature or were not considered toxicologically relevant for man. The No Observed Adverse Effect Level (NOAEL) for systemic toxicity was therefore considered to be 1000 mg/kg bw/day.
The ‘No Observed Effect Level’ (NOEL) for reproductive toxicity was considered to be 300 mg/kg bw/day based on reduced offspring viability, offspring body weight gain, litter size and litter weigh at 1000 mg/kg bw/day. - Executive summary:
In a key Guideline (OECD 422) combined repeated dose reproductive/developmental toxicity study, the test material (Nonene, branched; CAS# 97280-95-0) was administered by gavage to three groups of Wistar Han™:RccHan™:WIST strain rats (12/sex/dose) for up to eight weeks (including a two week pre-pairing phase, pairing, gestation and early lactation for females), at dose levels of 100, 300 and 1000 mg/Kg bw/day. A control group of twelve males and twelve females was dosed with vehicle alone (Arachis oil BP).
Clinical signs, behavioral assessments, body weight change and food and water consumption were monitored during the study. Pairing of animals within each dose group was undertaken on a one male: one female basis within each treatment group on Day 15 of the study, with females subsequently being allowed to litter and rear their offspring to Day 5 of lactation. During the lactation phase, daily clinical observations were performed on all surviving offspring, together with litter size and offspring weights and assessment of surface righting reflex. Extensive functional observations were performed on five selected males from each dose group after the completion of the pairing phase, and for five selected parental females from each dose group on Day 4 post-partum. Hematology and blood chemistry were evaluated prior to termination on five selected males and females from each dose group.
Adult males were terminated on Day 43, followed by the termination of all females and offspring on Day 5 post-partum. Any female which did not produce a pregnancy was terminated on or after Day 25 post coitum. One female which did not show positive evidence of mating and did not produce a pregnancy was terminated on Day 57. All animals were subjected to a gross necropsy examination and histopathological evaluation of selected tissues was performed.
No test material related mortality was observed through the study period. Clinical signs were detected in animals of either sex treated with 300 and 1000 mg/Kg bw/day during the study. Episodes of increased salivation were reported from Day 8 onwards. The physical condition of males treated with 1000 mg/Kg bw/day was also affected with reductions in body weight development during Weeks 1 and 3 of treatment. Subsequently, a reduction in overall body weight gain in these males and a slight reduction in food efficiency during week 1, was evident. A reduction in haemoglobin was also observed in these males. Water consumption was also significantly increased for animals of either sex from all treatment groups throughout the treatment period. Observations of this nature are often reported when a test material formulation is unpalatable or irritant and can be associated with gastric irritancy rather than be attributable to systemic toxicity. This was supported microscopically with stomach changes identified as epithelial hyperplasia in the forestomach in animals of either sex treated with 1000 mg/Kg bw/day and in males treated with 300 mg/Kg bw/day. This finding was considered to be the result of local irritancy of the test material and therefore cannot be considered indicative of true systemic toxicity.
Although there were some statistically significant differences in treated animals from controls for the blood chemical parameters measured, these differences were considered not to be of toxicological significance. Macroscopic findings detected at necropsy were confined to enlarged, pale and mottled kidneys and a dark liver in a number of males treated with 1000 mg/Kg bw/day. One male treated with 300 mg/Kg bw/day also had enlarged kidneys.
Histopathological examination of the liver revealed hepatocellular hypertrophy in animals of either sex treated with 1000 and 300 mg/Kg bw/day and in males treated with 100 mg/Kg bw/day. Organ weight data supported this finding with increased absolute and relative liver weights observed in these animals. In the absence of any degenerative or inflammatory changes, this condition is considered to be adaptive in nature.
Microscopic examination of the thyroid revealed increased incidence and severity of follicular cell hypertrophy/hyperplasia in animals of either sex treated with 1000 and 300 mg/Kg bw/day and in males treated with 100 mg/Kg bw/day. Males treated with 1000 and 300 mg/Kg bw/day also showed hypertrophic/vacuolated cells in the pituitary. The thyroid, liver and pituitary changes are characteristic of a consequence of hepatocellular induction as a result of enhanced hepatic metabolism. As a side effect of hepatic induction an increased liver metabolism of thyroid hormones T3 and T4 can occur. This subsequently leads to an enhanced thyroid gland production of these hormones as a consequence of a negative feedback stimulation of TSH production. The appearance of thyroid follicular cell hypertrophy and hypertrophic/vacuolated cells in the pituitary are themselves considered to be a result of this process. The thyroid and pituitary changes were considered to be adaptive in nature.
Microscopic examination also revealed effects in the kidneys of males from all treatment groups. Tubular basophilia and hyaline droplets was present in males from all treated groups. These tubular findings were also accompanied by tubular degeneration/debris in males treated with 1000 and 300 mg/Kg bw/day. The hyaline droplets can be directly linked to accumulation of alpha 2u-globulin, which is unique to the male rat. This finding is commonly observed in male rats following treatment with some hydrocarbons and is not predictive of any adverse effect in humans. The remaining kidney findings consisting of tubular degeneration/debris may be considered to represent an adverse effect of the test item, however immunohistochemical staining demonstrated that these findings were correlated to the same condition as hyaline droplets.
Mating performance and fertility was unaffected by treatment. Offspring viability was however reduced in litters from females treated with 1000 mg/Kg bw/day on Day 4 post-partum. Subsequently reduced litter size and litter weights were evident in these litters on Day 4 post-partum when compared to controls. One female treated with 1000 mg/Kg bw/day also had a total litter loss between Days 2 and 4 post-partum. The mean offspring body weight gains for litters which survived to Day 5 post-partum were also reduced between Days 1 and 4 post-partum at this treatment level.
Based on the results observed, the No Observed Adverse Effect Level (NOAEL) for systemic toxicity was determined to be 1000 mg/Kg bw/day. The ‘No Observed Effect Level’ (NOEL) for reproductive toxicity was considered to be 300 mg/Kg bw/day, based on reduced offspring viability, offspring body weight gain, litter size and litter weights on Day 4 post-partum at 1000 mg/Kg bw/day.
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