Screening of in vitro inhibitory effects of 15 herbal medicines on CYP3A4-catalyzed midazo-lam hydroxylation

Y. R. Yoon, M. J. Kim, J. H. Shon, J. Y. Park, B. H. Chun, J. G. Shin

    Research output: Contribution to journalArticlepeer-review


    Traditional herbal medicine (HM) is frequently taken in combination with conventional medications in Korea, but few reports have been addressed to herb-drug interaction. We assessed the inhibitory potential of 15 commonly used HMs in Korea on CYP3A4-catalyzed midazolam hydroxylation. Up to 1000 μg/ml of freeze-dried water extracts (extraction ratio: 15∼25%) of following HMs were tested for the inhibition of 1-hydroxymidazolam formation after 30 min incubations in human liver microsomes: Radix Glycyrrhizae, Radix Ginseng, Radix Dioscoreae, Fructus Lycii, Herba Leonuri, Radix Salviae Miltiorrhizae, Radix Angelicas, Semen Persicae, Rhizoma Atractylodis, Radix Morindae, Radix Rehmanniae, Tuber Liriopis, Herba Epimedii, Poria Cocos, and Eucommia Ulmoides. Among 15 HMs, Herba Eppimedii, a herb prescribing for the symptoms of amnesia, fatigue, and impotence and as diuretics, strongly inhibited CYP3A4-catalyzed medazolam hydroxylation (IC50=92.4±25.4 μg/ml). Herba Leonuri, a herb for managing endometriosis, dysmenorrhea, and hypertension, showed relatively weak inhibition (IC50=578.5±337.5 μg/ml). Other 13 HMs had no significant inhibition on midazolam hydroxylation. These results suggest that some of HMs have inhibitory potentials on CYP3A4 activity in their usual dose range (grams of dried herb) and the possible herb-drug interaction should be considered when HMs used with CYP3A4 substrate drugs.

    Original languageEnglish
    Pages (from-to)P88
    JournalClinical Pharmacology and Therapeutics
    Issue number2
    Publication statusPublished - 2001

    ASJC Scopus subject areas

    • Pharmacology
    • Pharmacology (medical)


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