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1. Am J Chin Med. 2012;40(1):57-73.

Herb-Drug Interaction of 50 Chinese Herbal Medicines on CYP3A4 Activity in Vitro
and in Vivo.

Pao LH, Hu OY, Fan HY, Lin CC, Liu LC, Huang PW.

School of Pharmacy, National Defense Medical Center, Taipei, Taiwan.
paolh@ndmctsgh.edu.tw.

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 6β-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.

PMID: 22298448 [PubMed - in process]