Trypanocidal and antitumour activity of platinum-metal and platinum-metal-drug dual-function complexes.
A number of antitumour platinum-metal complexes related to cis-platin showed trypanocidal activity against Trypanosoma rhodesiense in vitro but not in vivo. New platinum- and rhodium-metal complexes of diamidine and plenanthridinium trypanocides are described which showed higher therapeutic indices than the parent drugs, due to increased activity in the former drug type and decreased toxicity in the latter. Some evidence of potentiation of antitumour activity was noted in these drug complexes. At the ultrastructural level, complex-treated trypanosomes showed a number of nuclear effects and other lesions specifically attributable to platinum-metal action. Some of the lesions were similar to those induced by cis-platin in tumour cells.
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002945:Cisplatin / Q000031:analogs & derivatives* / Q000494:pharmacology; D004133:Diminazene / Q000031:analogs & derivatives / Q000494:pharmacology; D051379:Mice; D008815:Mice, Inbred Strains; D010984:Platinum / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000494:pharmacology* / Q000633:toxicity; D014345:Trypanosoma / Q000187:drug effects / Q000648:ultrastructure
D000970:Antineoplastic Agents; D014344:Trypanocidal Agents; D010984:Platinum; C003915:diminazene aceturate; D002945:Cisplatin; D004133:Diminazene