In vitro trypanocidal activity of dibutyltin dichloride and its fatty acid derivatives.
Searching for new compounds against pathogenic trypanosomes has been substantially accelerated by the development of in vitro screening assays. In an attempt to explore the chemotherapeutic potential of organotin compounds and to broaden the search for newer trypanocides, fatty acid derivatives of dibutyltin dichloride were synthesized and their in vitro trypanocidal profiles studied on Trypanosoma brucei brucei, Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense. A 24-h time course experiment was conducted with various concentrations of the compounds using a 24-well microtiter plate technique. The compounds tested were trypanocidal in a dose-dependent fashion: inhibiting survival and growth, resulting in irreversible morphological deformation and the eventual death of the parasites. The minimum inhibitory concentrations of the tested diorganotins are at low micromolar ranges: from 0.15-0.75 microM for T. b. brucei, T. b. gambiense and T. b. rhodesiense. These observations suggest that organotin has chemotherapeutic potential.
Shuaibu
M N
MN
Protozoology Department, Institute of Tropical Medicine, Nagasaki University, 1-12-4 Sakamoto, Nagasaki-shi 852-8523, Japan.
Kanbara
H
H
Yanagi
T
T
Ichinose
A
A
Ameh
D A
DA
Bonire
J J
JJ
Nok
A J
AJ
D000818:Animals; D005227:Fatty Acids / Q000737:chemistry*; D051379:Mice; D008854:Microscopy, Electron; D008855:Microscopy, Electron, Scanning; D009947:Organotin Compounds / Q000737:chemistry / Q000494:pharmacology*; D021261:Parasitic Sensitivity Tests; D014344:Trypanocidal Agents / Q000494:pharmacology*; D014345:Trypanosoma / Q000187:drug effects* / Q000254:growth & development / Q000648:ultrastructure; D014346:Trypanosoma brucei brucei / Q000187:drug effects / Q000254:growth & development / Q000648:ultrastructure; D014347:Trypanosoma brucei gambiense / Q000187:drug effects / Q000254:growth & development / Q000648:ultrastructure; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects / Q000254:growth & development / Q000648:ultrastructure
D005227:Fatty Acids; D009947:Organotin Compounds; D014344:Trypanocidal Agents; C020735:dibutyldichlorotin; C010409:dibutyltin dilaurate