Biochemical and molecular analysis of carboxylesterase-mediated hydrolysis of cocaine and heroin.

ABSTRACT:

Background and purpose

Carboxylesterases (CEs) metabolize a wide range of xenobiotic substrates including heroin, cocaine, meperidine and the anticancer agent CPT-11. In this study, we have purified to homogeneity human liver and intestinal CEs and compared their ability with hydrolyse heroin, cocaine and CPT-11.

Experimental approach

The hydrolysis of heroin and cocaine by recombinant human CEs was evaluated and the kinetic parameters determined. In addition, microsomal samples prepared from these tissues were subjected to chromatographic separation, and substrate hydrolysis and amounts of different CEs were determined.

Key results

In contrast to previous reports, cocaine was not hydrolysed by the human liver CE, hCE1 (CES1), either as highly active recombinant prote

SUBMITTER: Hatfield MJ 

PROVIDER: S-EPMC2958638 | biostudies-literature | 2010 Aug

REPOSITORIES: biostudies-literature