Herb-drug interaction of 50 Chinese herbal medicines on CYP3A4 activity in vitro and in vivo

Li Heng Pao, Oliver Yoa Pu Hu, Hsien Yuan Fan, Chang Ching Lin, Liang Chun Liu, Pei Wei Huang

Research output: Contribution to journalArticle

33 Citations (Scopus)

Abstract

The purpose of this study is to evaluate the effects of Chinese herbal medicines on the enzymatic activity of CYP3A4 and the possible metabolism-based herb-drug interactions in human liver microsomes and in rats. Fifty single-herbal preparations were screened for the activity of CYP3A4 using human liver microsomes for an in vitro probe reaction study. The enzymatic activity of CYP3A4 was estimated by determing the 6-hydroxytestosterone metabolized from testosterone performed on a liquid chromatography-tandem mass spectrometry (LC-MS/MS). Huang Qin (Scutellaria baicalensis Geprgi), Mu Dan Pi (Paeonia suffruticosa Andr.), Ji Shiee Terng (Spatholobus suberectus Dunn.) and Huang Qi (Astragalus membranaceus [Fisch] Bge) have been demonstrated to have remarkable inhibiting effects on the metabolism of CYP3A4, whereas Xi Yi Hua (Magnolia biondii Pamp.) exhibited a moderate inhibition. These five single herbs were further investigated in an animal study using midazolam. Mu Dan Pi, Ji Shiee Terng and Huang Qi were observed to have greatly increased in the C max and AUC of midazolam. This study provides evidence of possible herb-drug interactions involved with certain single herbs.

Original languageEnglish
Pages (from-to)57-73
Number of pages17
JournalAmerican Journal of Chinese Medicine
Volume40
Issue number1
DOIs
Publication statusPublished - Feb 10 2012
Externally publishedYes

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Herb-Drug Interactions
Cytochrome P-450 CYP3A
Herbal Medicine
Scutellaria baicalensis
Midazolam
Liver Microsomes
Hydroxytestosterones
Astragalus membranaceus
Magnolia
Paeonia
Plant Preparations
Tandem Mass Spectrometry
Liquid Chromatography
Area Under Curve
Testosterone
In Vitro Techniques

Keywords

  • Chinese Herbal Medicine
  • CYP3A4
  • Herb-Drug Interaction
  • Pharmacokinetics

ASJC Scopus subject areas

  • Complementary and alternative medicine

Cite this

Herb-drug interaction of 50 Chinese herbal medicines on CYP3A4 activity in vitro and in vivo. / Pao, Li Heng; Hu, Oliver Yoa Pu; Fan, Hsien Yuan; Lin, Chang Ching; Liu, Liang Chun; Huang, Pei Wei.

In: American Journal of Chinese Medicine, Vol. 40, No. 1, 10.02.2012, p. 57-73.

Research output: Contribution to journalArticle

Pao, Li Heng ; Hu, Oliver Yoa Pu ; Fan, Hsien Yuan ; Lin, Chang Ching ; Liu, Liang Chun ; Huang, Pei Wei. / Herb-drug interaction of 50 Chinese herbal medicines on CYP3A4 activity in vitro and in vivo. In: American Journal of Chinese Medicine. 2012 ; Vol. 40, No. 1. pp. 57-73.
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