Antitrypanosomal action of cis-diamminedichloroplatinum (II) analogs.
The present report deals with the alterations produced by cis-diamminedichloroplatinum (II) (DDP), and 2 of its analogs: cis-Pt(II)(tranylcypromine)2Cl2 and cis-Pt(II)(benzothiazole)2Cl2 in cultured epimastigote forms of Trypanosoma cruzi. Studies have been performed at the ultrastructural level and the inhibitory effect of these complexes on macromolecule synthesis, evaluated by 3H-thymidine, 3H-uridine, and 3H-leucine incorporation, has been investigated. DDP at concentrations of 50 and 100 micrograms/ml does not inhibit significantly the incorporation of radioactive precursors, but a clear decrease was observed with the 2 analogs. Eight hours of treatment at a concentration of 10 micrograms/ml rendered in all 3 cases an increase in autophagic vacuoles and lipids as well as an abnormal condensation of the nucleus chromatin.
D000818:Animals; D052160:Benzothiazoles; D002467:Cell Nucleus / Q000648:ultrastructure; D002945:Cisplatin / Q000031:analogs & derivatives* / Q000494:pharmacology*; D004247:DNA / Q000096:biosynthesis / Q000187:drug effects; D007930:Leucine / Q000378:metabolism; D008854:Microscopy, Electron; D009940:Organoids / Q000648:ultrastructure; D014176:Protein Biosynthesis; D012313:RNA / Q000096:biosynthesis; D013844:Thiazoles / Q000494:pharmacology*; D013936:Thymidine / Q000378:metabolism; D014191:Tranylcypromine / Q000031:analogs & derivatives* / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000378:metabolism / Q000648:ultrastructure; D014529:Uridine / Q000378:metabolism; D014617:Vacuoles / Q000648:ultrastructure
D052160:Benzothiazoles; D013844:Thiazoles; D014191:Tranylcypromine; C052860:dichlorbis(benzothiazole)platinum(II); D012313:RNA; C052859:dichlorobis(tranylcypromine)platinum(II); D004247:DNA; D007930:Leucine; D002945:Cisplatin; D013936:Thymidine; D014529:Uridine