Korean J Physiol Pharmacol.
1998 Jun;2(3):395-401.
In vitro cytotoxicity of novel platinum(II) coordination complexes containing diaminocyclohexane and diphenylphosphines
- Affiliations
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- 1Department of Pharmacology, School of Medicine, Kyung Hee University, Seoul 130-701, Korea.
- 2Department of Urology, School of Medicine, Kyung Hee University, Seoul 130-701, Korea.
- 3Department of Biochemistry, College of Pharmacy, Kyung Hee University, Seoul 130-701, Korea.
- 4Department of Pharmacochemistry, College of Pharmacy, Kyung Hee University, Seoul 130-701, Korea.
Abstract
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We have synthesized new platinum(H) analogs containing
1,2-diaminocyclohexane (dach) as a carrier ligand,
1,3-bis(diphenylphosphino) propane (DPPP)
/1,2-bis(diphenylphosphino)ethane (DPPE) as a leaving group and
nitrates to improve solubility. In the present study, the cytotoxicity
of (Pt(trans-l-dach)(DPPP))cntdot2NO3 (KHPC-001) and
(Pt(trans-l-dach)(DPPE)) cntdot 2NO3 (KHPC-002) was evaluated and
compared on various P-388 cancer cell lines and porcine kidney cell
line (LLC-PK1). The new platinum complexes demonstrated high efficacy
on P-388 mouse leukemia cell line as well as cisplatin-resistant
(P-388/CDDP) and adriamycin-resistant (P-388/ADR) P-388 cell lines. The
intracellular platinum content was measured by a flame atomic
absorption spectrophotometer (FAAS), and it was comparable to the
results
of IC50 of the three complexes on LLC-PK1I and P-388/S cells, while only DPPE compound was accumulated in high volume in P-388/ADR and P-388/CDDP cells. While the DNA-interstrand cross-links of KHPC-001, KHPC-002 and cisplatin were similar on P-388/S leukemia cells, these new platinum complexes were much less DNA cross-linking to a kidney derived cell line, LLC-PK1. These results indicate that KHPC-001 and KHPC-002 are a third-generation platinum complexes with potent antitumor activity and low nephrotoxicity.
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