Mode of action of intercalating drug, cis-Pt(II)(DDH)Cl2, cis-Pt(II)(DDH) (metafluorobenzoic)2, and cis-Pt(II)(DDH)(mucubromic)2, on Trypanosoma cruzi.
The trypanocidal activity of three new compounds derived of the antineoplastic drug cis-diamminodichloroplatinum(II) (DDP) has been studied over epimastigote forms of Trypanosoma cruzi. The electron microscopy indicated that, in the treated animals, the nuclear chromatin is distributed in the nucleus in a lax form and that the number of lipidic vacuoles increases largely. This action is more significant when cis-Pt(II)1,2-diaminocyclohexane is used. In addition this compound causes a destabilization of the DNA double helix with a decrease of melting temperature. The three compounds inhibit the incorporation of leucine, uridine and thymidine, although the thymidine uptake is the most significantly affected.
Ruiz-Perez
L M
LM
Osuna
A
A
Lopez
M C
MC
Castanys
S
S
Gammaro
F
F
Craciunescu
D
D
Alonso
C
C
D000818:Animals; D008854:Microscopy, Electron; D009944:Organoplatinum Compounds / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000648:ultrastructure
D009944:Organoplatinum Compounds; D014344:Trypanocidal Agents; C052583:cis-Pt(II)(DDH)bis(mucobromic acid); C013933:dichloro-1,2-diaminocyclohexane platinum complex; C052582:cis-Pt(II)(DDH)bis(metafluorobenzoic acid)