In vitro inhibition of carboxylesterase 1 by Kava (Piper methysticum) Kavalactones.

ABSTRACT: Kava refers to the extracts from the rhizome of the plant Piper methysticum which is of particular significance to various indigenous cultures in the South Pacific region. Kavalactones are the active constituents of kava products and are associated with sedative and anxiolytic effects. Kavalactones have been evaluated in vitro for their potential to alter the activity of various CYP450 enzymes but have undergone little systematic investigation as to their potential influence on esterases. This study investigated the inhibition effects of kava and its kavalactones on carboxylesterase 1 (CES1) in an in vitro system and established associated kinetic parameters. Kava and its kavalactones were found to produce reversible inhibition of CES1 to varying degrees. Kavain, dihydrokavain, and desmeth

SUBMITTER: Melchert PW 

PROVIDER: S-EPMC9244838 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature