Bromoacetyl-L-carnitine: biochemical and antitrypanosomal actions against Trypanosoma brucei brucei.
One of the causative agents of the African Trypanosamiases, Trypanosoma brucei brucei is able to use high intracellular carnitine concentrations and a high carnitine acetyl transferase (CAT) activity to stimulate ATP production. This paper reports that a carnitine analogue, bromoacetyl-L-carnitine, is an irreversible inhibitor of CAT from T.brucei, non-competitively inhibits carnitine uptake by T.brucei and has a potent in vitro effect against T.brucei motility and infectivity. An in vivo action in T.brucei infected mice is also reported. These results represent a new area of investigation in the important search for new antitrypanosomal agents.
D000108:Acetylcarnitine / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D000123:Acetyltransferases / Q000037:antagonists & inhibitors*; D000818:Animals; D002331:Carnitine / Q000031:analogs & derivatives* / Q000378:metabolism; D002332:Carnitine O-Acetyltransferase / Q000037:antagonists & inhibitors*; D051379:Mice; D009068:Movement / Q000187:drug effects; D014346:Trypanosoma brucei brucei / Q000187:drug effects* / Q000472:pathogenicity / Q000502:physiology; D014353:Trypanosomiasis, African / Q000188:drug therapy
C033813:bromoacetylcarnitine; D000108:Acetylcarnitine; D000123:Acetyltransferases; D002332:Carnitine O-Acetyltransferase; D002331:Carnitine