The activity of platinum, iridium and rhodium drug complexes against Leishmania donovani.
The activities of twenty seven Platinum, Rhodium and Iridium drug complexes were determined against Leishmania donovani amastigotes in mouse peritoneal macrophages in vitro. Eight compounds showed antileishmanial activity of which only three, Rh(III)-mepacrine, Ir(III) pyrrolidine dithiocarbamate and Ir(III) diethyl dithiocarbamate had ED50 values of less than 1 microM. The two Iridium complexes produced, respectively, a 50% and 39% suppression of L. donovani amastigotes in the liver of BALB/c mice following the subcutaneous administration of 200 mg/kg for 5 consecutive days. Ultrastructural studies suggest that the amastigote kinetoplast-mitochondrion complex is the primary site of action of the Ir and Rh complexes.
Croft
S L
SL
Department of Medical Parasitology, London School of Hygiene, UK.
Neal
R A
RA
Craciunescu
D G
DG
Certad-Fombona
G
G
D000818:Animals; D007495:Iridium / Q000494:pharmacology* / Q000627:therapeutic use; D007893:Leishmania donovani / Q000187:drug effects* / Q000648:ultrastructure; D007898:Leishmaniasis, Visceral / Q000188:drug therapy*; D008297:Male; D051379:Mice; D008854:Microscopy, Electron; D009942:Organometallic Compounds / Q000494:pharmacology / Q000627:therapeutic use; D009944:Organoplatinum Compounds / Q000494:pharmacology* / Q000627:therapeutic use; D012238:Rhodium / Q000494:pharmacology* / Q000627:therapeutic use
D009942:Organometallic Compounds; D009944:Organoplatinum Compounds; D007495:Iridium; D012238:Rhodium