[Antitumor activity and toxicity of the degradation products and the aquated species of cis-dichlorodiammineplatinum (II)].
Antitumor activity and mouse acute toxicity of the following degradation products and aquated species of cis-dichlorodiammineplatinum(II) (CDDP): trans-dichlorodiammineplatinum(II), trichloroamminepltinate(II), tetrachloroplatinate(II), produced by heat treatment of the saline solution of CDDP, mono- and di-aquocomplexes, hydroxo-bridged dimer and trimer of CDDP, have been studied. These degradation products did not show antitumor activity against mouse leukemia L1210 corresponding to their low anti-HeLa cell activity. Their acute toxicities were much milder than CDDP. On the other hand, all the aquated species possessed higher toxicities than CDDP. Among them, the dimer and trimer were less active against HeLa cells than CDDP, and did not show antitumor activity against L1210 leukemia. However, the mono- and di-aquo complexes showed about 2 approximately 4 times higher anti-HeLa cell activity and prolonged the survival time of mice bearing L1210 leukemia similarly to CDDP.
D000818:Animals; D001835:Body Weight / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D002945:Cisplatin / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D004351:Drug Resistance; D005260:Female; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D007939:Leukemia L1210 / Q000473:pathology*; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR
D002945:Cisplatin