Abstract Title:

Epicatechin gallate and epigallocatechin gallate are potent inhibitors of human arylacetamide deacetylase.

Abstract Source:

Drug Metab Pharmacokinet. 2021 Apr 20 ;39:100397. Epub 2021 Apr 20. PMID: 34171773

Abstract Author(s):

Kaori Yasuda, Kazuki Watanabe, Tatsuki Fukami, Shimon Nakashima, Shin-Ichi Ikushiro, Miki Nakajima, Toshiyuki Sakaki

Article Affiliation:

Kaori Yasuda


Recently, in addition to carboxylesterases (CESs), we found that arylacetamide deacetylase (AADAC) plays an important role in the metabolism of some clinical drugs. In this study, we screened for food-related natural compounds that could specifically inhibit human AADAC, CES1, or CES2. AADAC, CES1, and CES2 activities in human liver microsomes were measured using phenacetin, fenofibrate, and procaine as specific substrates, respectively. In total, 43 natural compounds were screened for their inhibitory effects on each of these enzymes. Curcumin and quercetin showed strong inhibitory effects against all three enzymes, whereas epicatechin, epicatechin gallate (ECg), and epigallocatechin gallate (EGCg) specifically inhibited AADAC. In particular, ECg and EGCg showed strong inhibitory effects on AADAC (ICvalues: 3.0 ± 0.5 and 2.2 ± 0.2 μM, respectively). ECg and EGCg also strongly inhibited AADAC-mediated rifampicin hydrolase activity in human liver microsomes with ICvalues of 2.2 ± 1.4 and 1.7 ± 0.4 μM, respectively, whereas it weakly inhibited p-nitrophenyl acetate hydrolase activity, which is catalyzed by AADAC, CES1, and CES2. Our results indicate that ECg and EGCg are potent inhibitors of AADAC.

Study Type : In Vitro Study

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