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.
Highlights
Bacopa monnieri (Linn.) Pennell (Scrophulariaceae), known as brahmi in Ayurvedic medicine, has been used in traditional and Ayurvedic medicine for centuries as a brain tonic to enhance learning and memory and to improve concentration [1]
Inhibition of a cytochrome P450 (CYP) enzyme causes an increase in drug plasma levels through decreased drug metabolism, which could result in significant adverse reactions or toxicity
The pharmacokinetic parameters (IC50, Ki values) show that B. monnieri extract most strongly inhibits CYP2C19 followed by CYP2C9, CYP1A2, and CYP3A4 and most weakly inhibits CYP2D6
Summary
Bacopa monnieri (Linn.) Pennell (Scrophulariaceae), known as brahmi in Ayurvedic medicine, has been used in traditional and Ayurvedic medicine for centuries as a brain tonic to enhance learning and memory and to improve concentration [1]. These traditional claims have been supported by several preclinical and clinical studies [2,3,4,5], and the observed cognitive effects have been attributed to bacoside. Drug interactions can lead to serious adverse events or decreased drug efficacy These interactions may occur through the inhibition or induction of hepatic and intestinal drug-metabolizing enzymes (e.g., CYPs) and transporters (e.g., p-glycoprotein) [12]. Inhibition-based drug interactions are a primary cause of clinically significant drug interactions [14]
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