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Icariin Metabolism by Human Intestinal Microflora

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 consis...

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Autores principales: Wu, Hailong, Kim, Mihyang, Han, Jaehong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273050/
https://www.ncbi.nlm.nih.gov/pubmed/27589718
http://dx.doi.org/10.3390/molecules21091158
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author Wu, Hailong
Kim, Mihyang
Han, Jaehong
author_facet Wu, Hailong
Kim, Mihyang
Han, Jaehong
author_sort Wu, Hailong
collection PubMed
description 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.
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spelling pubmed-62730502018-12-28 Icariin Metabolism by Human Intestinal Microflora Wu, Hailong Kim, Mihyang Han, Jaehong Molecules Article 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. MDPI 2016-08-31 /pmc/articles/PMC6273050/ /pubmed/27589718 http://dx.doi.org/10.3390/molecules21091158 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Wu, Hailong
Kim, Mihyang
Han, Jaehong
Icariin Metabolism by Human Intestinal Microflora
title Icariin Metabolism by Human Intestinal Microflora
title_full Icariin Metabolism by Human Intestinal Microflora
title_fullStr Icariin Metabolism by Human Intestinal Microflora
title_full_unstemmed Icariin Metabolism by Human Intestinal Microflora
title_short Icariin Metabolism by Human Intestinal Microflora
title_sort icariin metabolism by human intestinal microflora
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273050/
https://www.ncbi.nlm.nih.gov/pubmed/27589718
http://dx.doi.org/10.3390/molecules21091158
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