In vitroeffects of standardized extract ofBacopa monnieraand its five individual active constituents on human P-glycoprotein activity

Abstract

1. For centuries Bacopa monniera (BM) has been used as an herbal drug for the treatment of various mental ailments. A chemically standardized alcoholic extract of BM is clinically available over the counter herbal remedy for memory enhancement in children and adults. Consumption of herbal preparations has been reported to alter the function of membrane transporters, especially P-glycoprotein (P-gp), ATP-dependent drug efflux transporter responsible for the development of herb-drug interactions. 2. In the present study, we evaluated the in vitro effect of BM extract and its five individual active constituents (namely, bacopaside I, bacopaside II and bacopasaponin C, bacoside A and bacoside A3) on P-gp function using luminescent P-gp ATPase assay and Rh123 transport assay across human MDR1 gene transfected LLC-GA5-COL150 cell line. 3. It was observed that BM extract and its five individual constituents inhibited both basal activity as well as verapamil-stimulated ATPase activity, suggesting their affinity towards P-gp. Further, BM and its five active constituents inhibited the rhodamine 123 (Rh123) transport across LLC-GA5-COL150 cell monolayer with bacopaside II being the most potent inhibitor of P-gp, which decreased P-gp efflux ratio of Rh123 by fourfold in comparison to control. 4. Our finding may prove beneficial in predicting the potential herb-drug interactions of BM on concomitant medication with P-gp substrate drugs in clinical settings.

The Purified Extract from the Medicinal Plant Bacopa monnieri, Bacopaside II, Inhibits Growth of Colon Cancer Cells In Vitro by Inducing Cell Cycle Arrest and Apoptosis

“…However, at this point, we cannot rule out that the effects on cell growth and migration are mediated by other targets, either independently or in conjunction with AQP1. For example, bacopaside II inhibits the activity of P-glycoprotein, an ATP-dependent efflux pump involved in transporting a broad range of xenobiotics across extra- and intracellular membranes [ 21 ]. Furthermore, HT-29 harbors an activating BRAF mutation (BRAF V600E ) and developed from a serrated polyp, in contrast to the remaining three cell lines.…”

Measurement of Rhodamine 123 in Three‐Dimensional Organoids: A Novel Model for P‐Glycoprotein Inhibitor Screening

“…Three‐dimensional organoids were counted on the third cultured day before incubating with Rh123, the substrate of P‐gp. The concentration of Rh123 was 10 μM according to the previous studies . The studies were divided into four groups, including control (Rh123 alone), averapamil, quinidine and mitotane together with Rh123, respectively.…”

A Novel Model of P‐Glycoprotein Inhibitor Screening Using Human Small Intestinal Organoids

“…In contrast, the NBD is relatively hydrophilic and considered as the sites for ATP binding and hydrolysis [3,4]. P-gp is found in a variety of normal tissues and organs extremely in which involved in drug pharmacokinetics such as the brain-blood barrier, liver, kidney and small intestine [5,6]. It functions as an efflux pump to transport a broad spectrum of substrates including endogenous (e.g.…”