Effect of several Chinese natural health products of human cytochrome P450 metabolism

J Pharm Pharm Sci. 2002 May-Aug;5(2):185-9.

Abstract

Purpose: Traditional Chinese medicines (TCM) are believed by many to be safe and used for self-medication without supervision. Although the risk appears to be low, certain TCM have been associated with a number of serious adverse reactions. A preliminary study was undertaken with 12 products using a human cytochrome P450 (CYP450) isozyme assay to determine if these products could affect human drug metabolism.

Methods: Aliquots of samples were analyzed directly or as extracts for their potential to affect CYP450 2C9, 2C19, 2D6, and 3A4 mediated-metabolism of marker substrates using an in vitro fluorometric microtiter plate assay.

Results: One product was found to be a Chinese Proprietary Medicine (CPM). Most aqueous extracts inhibited CYP450 mediated-metabolism of at least 3 isozymes (ranging from 25-100%). All liquid samples markedly inhibited the metabolism of all 4 isozymes. De le ke chuan kang and Rensheng dao were the strongest CYP450 inhibitors.

Conclusions: Our in vitro findings demonstrate that TCM can inhibit CYP450 2C9, 2C19, 2D6 and 3A4 mediated-metabolism. TCM need to be examined further under clinical settings to determine if potential interactions will occur that affect the safety and efficacy of conventional therapeutic products.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aryl Hydrocarbon Hydroxylases*
  • Cytochrome P-450 CYP2C19
  • Cytochrome P-450 CYP2D6 / metabolism
  • Cytochrome P-450 CYP2D6 Inhibitors
  • Cytochrome P-450 CYP3A
  • Cytochrome P-450 Enzyme Inhibitors*
  • Cytochrome P-450 Enzyme System / metabolism
  • Drugs, Chinese Herbal / pharmacology*
  • Humans
  • Medicine, Chinese Traditional*
  • Mixed Function Oxygenases / antagonists & inhibitors
  • Mixed Function Oxygenases / metabolism
  • Plants, Medicinal / chemistry
  • Steroid 16-alpha-Hydroxylase*
  • Steroid Hydroxylases / antagonists & inhibitors
  • Steroid Hydroxylases / metabolism

Substances

  • Cytochrome P-450 CYP2D6 Inhibitors
  • Cytochrome P-450 Enzyme Inhibitors
  • Drugs, Chinese Herbal
  • Cytochrome P-450 Enzyme System
  • Mixed Function Oxygenases
  • Steroid Hydroxylases
  • Aryl Hydrocarbon Hydroxylases
  • CYP2C19 protein, human
  • CYP3A protein, human
  • Cytochrome P-450 CYP2C19
  • Cytochrome P-450 CYP2D6
  • Cytochrome P-450 CYP3A
  • Steroid 16-alpha-Hydroxylase