Thenoyltrifluoroacetone, a potent inhibitor of carboxylesterase activity

  • Biochem Pharmacol. 2002 Feb 15;63(4):751-4. doi: 10.1016/s0006-2952(01)00871-1.
Jin Gang Zhang  1 ,  Marc W Fariss
Affiliations
  • 1. Department of Pharmaceutical Sciences, College of Pharmacy, Washington State University, Pullman, WA 99164-6534, USA. [email protected]
PMID: 11992644 DOI: 10.1016/s0006-2952(01)00871-1
Abstract

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.

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