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Molecules 2016, 21(9), 1158;

Icariin Metabolism by Human Intestinal Microflora

Metalloenzyme Research Group and Department of Integrative Plant Science, Chung-Ang University, Anseong 17546, Korea
Author to whom correspondence should be addressed.
Academic Editor: Marcello Iriti
Received: 4 August 2016 / Revised: 25 August 2016 / Accepted: 26 August 2016 / Published: 31 August 2016
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Icariin is a major bioactive compound of Epimedii Herba, a traditional oriental medicine exhibiting anti-cancer, anti-inflammatory and anti-osteoporosis activities. Recently, the estrogenic activities of icariin drew significant attention, but the published scientific data seemed not to be so consistent. To provide fundamental information for the study of the icaritin metabolism, the biotransformation of icariin by the human intestinal bacteria is reported for the first time. Together with human intestinal microflora, the three bacteria Streptococcus sp. MRG-ICA-B, Enterococcus sp. MRG-ICA-E, and Blautia sp. MRG-PMF-1 isolated from human intestine were reacted with icariin under anaerobic conditions. The metabolites including icariside II, icaritin, and desmethylicaritin, but not icariside I, were produced. The MRG-ICA-B and E strains hydrolyzed only the glucose moiety of icariin, and icariside II was the only metabolite. However, the MRG-PMF-1 strain metabolized icariin further to desmethylicaritin via icariside II and icaritin. From the results, along with the icariin metabolism by human microflora, it was evident that most icariin is quickly transformed to icariside II before absorption in the human intestine. We propose the pharmacokinetics of icariin should focus on metabolites such as icariside II, icaritin and desmethylicaritin to explain the discrepancy between the in vitro bioassay and pharmacological effects. View Full-Text
Keywords: biotransformation; desmethylicaritin; Epimedium koreanum; human intestinal bacteria; icariin; icariside II; icaritin biotransformation; desmethylicaritin; Epimedium koreanum; human intestinal bacteria; icariin; icariside II; icaritin

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Wu, H.; Kim, M.; Han, J. Icariin Metabolism by Human Intestinal Microflora. Molecules 2016, 21, 1158.

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