Cyclohex-1,2-ylenediamine

Basic toxicokinetics

Administrative data

Endpoint:

basic toxicokinetics in vitro / ex vivo

Type of information:

experimental study

Adequacy of study:

other information

Study period:

Published: 2010

Reliability:

3 (not reliable)

Rationale for reliability incl. deficiencies:

unsuitable test system

Data source

Reference

Reference Type:

publication

Title:

Cytotoxicity, cellular uptake, glutathione and DNA interactions of an antitumor large-ring PtII chelate complex incorporating the cis-1,4-diaminocyclohexane carrier ligand

Author:

Kasparkova, J.; Suchankova, T.; Halamikova, A.; Zerzankova, L.; Vrana, O.; Margiotta, N.; Natile, G.; Brabec, V

Year:

2010

Bibliographic source:

Biochemical Pharmacology, 79, 552-564

Materials and methods

Objective of study:

other: cellular uptake

Principles of method if other than guideline:

basic research experiment: Cellular uptake of PtCl2(cis-1,4-diaminocyclohexane) into A2780 cells (i.e. Human ovarian carcinoma cells, sensitive to cisplatin) was measured. Therefore, cells were seeded (in 60 mm cell culture dishes with 30 000 cells per cubic centimetre). After over night incubation the cells were exposed to medium containing the platinum compound at a concentration of 2.7 microM for either 4 or 24 hours. After the treatment period cells were washed twice with ice-cold phosphate buffered saline, harvested via trypsin-detachment, pelleted and stored at minus 80 °C. For the assay pellets wer digested with 12 M HCl and platinum content was determined via flameless atomic absorption spectrophotometry (FAAS). Cellular uptake measures were corrected for adsorption effects and experiments were performed in quadrudplicate.

GLP compliance:

not specified

Test material

Test material information

Constituent 1

Reference substance name:

PtCl2(cis-1,4-diaminocyclohexane)

IUPAC Name:

PtCl2(cis-1,4-diaminocyclohexane)

Test material form:

not specified

Details on test material:

- Name of test material (as cited in study report):
- Analytical purity: >95%

Radiolabelling:

not specified

Applicant's summary and conclusion

Conclusions:

PtCl2(cis-1,4-diaminocyclohexane) was taken up into human ovarian carcinoma cells (A2780). After 4 and 24 hours 4.7 and 38 pmol compund/10EXP6 cells was found respectively, i.e. 1.3 to 2fold the amount of cisplatin which was taken up by these cells within the same timeframe.