Thenoyltrifluoroacetone, a potent inhibitor of carboxylesterase activity.
Thenoyltrifluoroacetone (TTFA), a conventional mitochondrial complex II inhibitor, was found to inhibit purified porcine liver carboxylesterase non-competitively with a K(i) of 0.61x10(-6)M and an IC(50) of 0.54x10(-6)M. Both rat plasma and liver mitochondrial esterases were inhibited in a concentration-dependent fashion. Results indicate that TTFA is a potent inhibitor of carboxylesterase activity, in addition to its ability to inhibit mitochondrial complex II activity. Therefore, caution is warranted in using TTFA as a mitochondrial complex inhibitor in combination with esterase substrates, such as fluorescence probes or vitamin E esters.
Zhang
Jin Gang
JG
Department of Pharmaceutical Sciences, College of Pharmacy, Washington State University, Pullman, WA 99164-6534, USA. jgzhang@mail.wsu.edu
Fariss
Marc W
MW
D000818:Animals; D043182:Carboxylesterase; D002265:Carboxylic Ester Hydrolases / Q000037:antagonists & inhibitors* / Q000097:blood / Q000302:isolation & purification / Q000378:metabolism; D002614:Chelating Agents / Q000494:pharmacology; D042963:Electron Transport Complex II; D007700:Kinetics; D008297:Male; D008930:Mitochondria, Liver / Q000187:drug effects* / Q000201:enzymology; D009097:Multienzyme Complexes / Q000378:metabolism; D010088:Oxidoreductases / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D013385:Succinate Dehydrogenase / Q000378:metabolism; D013804:Thenoyltrifluoroacetone / Q000494:pharmacology*
D002614:Chelating Agents; D009097:Multienzyme Complexes; D013804:Thenoyltrifluoroacetone; D010088:Oxidoreductases; D042963:Electron Transport Complex II; D013385:Succinate Dehydrogenase; D002265:Carboxylic Ester Hydrolases; D043182:Carboxylesterase