Molecules 2014, 19(2), 2588-2601; doi:10.3390/molecules19022588
Article

Inhibition of Human Cytochrome P450 Enzymes by Bacopa monnieri Standardized Extract and Constituents

1email, 2email and 1,* email
Received: 21 January 2014; in revised form: 19 February 2014 / Accepted: 19 February 2014 / Published: 24 February 2014
(This article belongs to the Section Metabolites)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: Bacopa monnieri and the constituents of this plant, especially bacosides, possess various neuropharmacological properties. Like drugs, some herbal extracts and the constituents of their extracts alter cytochrome P450 (CYP) enzymes, causing potential herb-drug interactions. The effects of Bacopa monnieri standardized extract and the bacosides from the extract on five major CYP isoforms in vitro were analyzed using a luminescent CYP recombinant human enzyme assay. B. monnieri extract exhibited non-competitive inhibition of CYP2C19 (IC50/Ki = 23.67/9.5 µg/mL), CYP2C9 (36.49/12.5 µg/mL), CYP1A2 (52.20/25.1 µg/mL); competitive inhibition of CYP3A4 (83.95/14.5 µg/mL) and weak inhibition of CYP2D6 (IC50 = 2061.50 µg/mL). However, the bacosides showed negligible inhibition of the same isoforms. B. monnieri, which is orally administered, has a higher concentration in the gut than the liver; therefore, this herb could exhibit stronger inhibition of intestinal CYPs than hepatic CYPs. At an estimated gut concentration of 600 µg/mL (based on a daily dosage of 300 mg/day), B. monnieri reduced the catalytic activities of CYP3A4, CYP2C9 and CYP2C19 to less than 10% compared to the total activity (without inhibitor = 100%). These findings suggest that B. monnieri extract could contribute to herb-drug interactions when orally co-administered with drugs metabolized by CYP1A2, CYP3A4, CYP2C9 and CYP2C19.
Keywords: Bacopa monnieri; bacoside; cytochrome P450 (CYP); herb-drug interactions; Scrophulariaceae
PDF Full-text Download PDF Full-Text [1637 KB, uploaded 18 June 2014 20:30 CEST]

Export to BibTeX |
EndNote


MDPI and ACS Style

Ramasamy, S.; Kiew, L.V.; Chung, L.Y. Inhibition of Human Cytochrome P450 Enzymes by Bacopa monnieri Standardized Extract and Constituents. Molecules 2014, 19, 2588-2601.

AMA Style

Ramasamy S, Kiew LV, Chung LY. Inhibition of Human Cytochrome P450 Enzymes by Bacopa monnieri Standardized Extract and Constituents. Molecules. 2014; 19(2):2588-2601.

Chicago/Turabian Style

Ramasamy, Seetha; Kiew, Lik V.; Chung, Lip Y. 2014. "Inhibition of Human Cytochrome P450 Enzymes by Bacopa monnieri Standardized Extract and Constituents." Molecules 19, no. 2: 2588-2601.

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert