Pharmacokinetic interactions of herbs with cytochrome p450 and p-glycoprotein.

Hyun-Jong Cho,In-Soo Yoon

doi:10.1155/2015/736431

Abstract

The concurrent use of drugs and herbal products is becoming increasingly prevalent over the last decade. Several herbal products have been known to modulate cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp) which are recognized as representative drug metabolizing enzymes and drug transporter, respectively. Thus, a summary of knowledge on the modulation of CYP and P-gp by commonly used herbs can provide robust fundamentals for optimizing CYP and/or P-gp substrate drug-based therapy. Herein, we review ten popular medicinal and/or dietary herbs as perpetrators of CYP- and P-gp-mediated pharmacokinetic herb-drug interactions. The main focus is placed on previous works on the ability of herbal extracts and their phytochemicals to modulate the expression and function of CYP and P-gp in several in vitro and in vivo animal and human systems.

Highlights

In the last decade, a number of herbal products have attracted growing interest as a complementary and alternative medicine for the prevention and treatment of various diseases [1]
Recent surveys have reported that the prevalence of herbal medicine use is approximately 20% and the concurrent use of herbal medicine occurs in 20–30% of prescription drug users in the United States [2,3,4]
Cytochrome P450 (CYP) monooxygenase is a superfamily of hemoproteins responsible for the phase I

Summary

Introduction

A number of herbal products have attracted growing interest as a complementary and alternative medicine for the prevention and treatment of various diseases [1]. Herbal products have been generally considered as natural and safe Some of their constituents can modulate various xenobiotic metabolism and transport systems which play a significant role in the absorption and disposition of prescription drugs. P-gp is highly expressed in the apical (luminal) membrane of intestinal epithelium, hepatocytes, kidney proximal tubule epithelium, and brain capillary endothelium, where it pumps a variety of xenobiotics into the intestinal lumen, bile duct, renal tubule, and brain capillary, respectively [11, 12] It plays an important role in the intestinal absorption, distribution to the central nervous system, and biliary/urinary excretion of drugs [13]. John’s Wort and grapefruit are not addressed in this paper, because they are welldocumented as CYP and P-gp modulators in many previous reviews

Herbal Modulations of CYP and P-gp

C R2 O

Conclusions