Lim, S.Y.M. and Alshagga, M.A. and Alshawsh, Mohammed Abdullah and Ong, C.E. and Pan, Y. (2021) In vitro effects of 95% khat ethanol extract (KEE) on human recombinant cytochrome P450 (CYP)1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C19, CYP2E1, CYP2J2 and CYP3A5. Drug Metabolism and Personalized Therapy, 37 (1). ISSN 2363-8907, DOI https://doi.org/10.1515/dmpt-2021-1000196.
Full text not available from this repository.Abstract
Abstract Objectives Khat, a natural amphetamine-like psychostimulant plant, are widely consumed globally. Concurrent intake of khat and xenobiotics may lead to herb-drug interactions and adverse drug reactions (ADRs). This study is a continuation of our previous study, targeted to evaluate the in vitro inhibitory effects of khat ethanol extract (KEE) on human cytochrome (CYP) 1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C19, CYP2E1, CYP2J2, and CYP3A5, major human drug metabolizing enzymes. Methods In vitro fluorescence enzyme assays were employed to assess CYPs inhibition with the presence and absence of various KEE concentrations. Results KEE reversibly inhibited CYP2A6, CYP2B6, CYP2C8, CYP2C19, CYP2E1, CYP2J2 and CYP3A5 but not CYP1A2 with IC50 values of 25.5, 99, 4.5, 21, 27, 17, and 10 μg/mL respectively. No irreversible inhibition of KEE on all the eight CYPs were identified. The Ki values of CYP2A6, CYP2B6, CYP2C8, CYP2C19, CYP2E1, CYP2J2 and CYP3A5 were 20.9, 85, 4.8, 18.3, 59.3, 3, and 21.7 μg/mL, respectively. KEE inhibited CYP2B6 via competitive or mixed inhibition; CYP2E1 via un-competitive or mixed inhibition; while CYP2A6, CYP2C8, CYP2C19, CYP2J2 and CYP3A5 via non-competitive or mixed inhibition. Conclusions Caution should be taken by khat users who are on medications metabolized by CYP2A6, CYP2B6, CYP2C8, CYP2C19, CYP2E1, CYP2J2, and CYP3A5. © 2021 Walter de Gruyter GmbH, Berlin/Boston
| Item Type: | Article |
|---|---|
| Funders: | University of Nottingham Malaysia Campus |
| Uncontrolled Keywords: | CYP; Herb-drug interaction; In vitro; Khat; Khat-drug interaction |
| Subjects: | R Medicine > RM Therapeutics. Pharmacology |
| Divisions: | Faculty of Medicine > Department of Pharmacology |
| Depositing User: | Ms Zaharah Ramly |
| Date Deposited: | 04 Jun 2025 01:42 |
| Last Modified: | 04 Jun 2025 07:25 |
| URI: | http://eprints.um.edu.my/id/eprint/36146 |
Actions (login required)
 |
View Item |
