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 journalArticlepeer-review

54 Citations (Scopus)


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
Issue number1
Publication statusPublished - Feb 10 2012
Externally publishedYes


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

ASJC Scopus subject areas

  • Complementary and alternative medicine


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