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  • Title: Identification of Quinone Methide Intermediate Resulting from Metabolic Activation of Icaritin in Vitro and in Vivo.
    Author: Chen Y, Guo X, Ma Y, Hu X, Peng Y, Zheng J.
    Journal: Chem Res Toxicol; 2019 Jun 17; 32(6):969-973. PubMed ID: 30938510.
    Abstract:
    Many herbal medicines such as epimedium have been reported to cause adverse effects, and icaritin is the common aglycone of many glucosides in epimedium. Our present work aimed at the clarification of the metabolic activation of icaritin possibly responsible for the adverse effects of epimedium. A quinone methide metabolite (M1) was detected in icaritin-fortified microsomal incubations. A glutathione (GSH) conjugate (M2) and N-acetyl-l-cysteine (NAC) conjugate (M3) derived from icaritin were observed in GSH/NAC-supplemented rat/human liver microsomal incubations. CYP3A family was the predominant enzyme catalyzing the bioactivation of icaritin. In conclusion, sufficient evidence indicates the metabolic activation of icaritin to quinone methide metabolite.
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