Estrogenic/antiestrogenic activities of a Epimedium koreanum extract and its major components: in vitro and in vivo studies
► ICT and quercetin exhibited in vitro ER mediated estrogenic activity with a more potent interaction with ERβ. ► Prenylflavonoid glycosides did not show any in vitro estrogenic activities. ► The potency of in vitro estrogenic activity was in the order of ICT>Epi ext>ICA. ► ICA had the stronge...
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| Veröffentlicht in: | Food and chemical toxicology 2012-08, Vol.50 (8), p.2751-2759 |
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| creator | Kang, Hyun Ku Choi, Yun-Ho Kwon, Hyosuk Lee, Sang-Bum Kim, Dong-Hyun Sung, Chung Ki Park, Young In Dong, Mi-Sook |
| description | ► ICT and quercetin exhibited in vitro ER mediated estrogenic activity with a more potent interaction with ERβ. ► Prenylflavonoid glycosides did not show any in vitro estrogenic activities. ► The potency of in vitro estrogenic activity was in the order of ICT>Epi ext>ICA. ► ICA had the strongest estrogenic activity in ovariectomized rats.
The estrogenic and antiestrogenic activities of Epimedii Herba, which is a traditional medicinal herb used in Korea and China were investigated in this study. The in vitro estrogen receptor (ER) mediated estrogenic/antiestrogenic activities of an Epimedii Herba extract (Epi ext) and its major components were determined using an estrogen responsive element driven reporter gene assay in MCF-7/ERE and HEK293T cells. The Epi ext exhibited ERα- and ERβ-mediated estrogenic activity with an EC50 of 5.0 and 17.8μM in HEK293T cells, respectively. Prenylflavonoid glycosides such as icariin (ICA), epimedin A, B, and C did not show any in vitro estrogenic or antiestrogenic activities. Icaritin (ICT) and quercetin exhibited in vitro ER mediated estrogenic activity with a more potent interaction with ERβ. In vivo estrogenic activities of the Epi ext, ICA and ICT were compared using an uterotrophic assay. Although the potency of in vitro estrogenic activity was in the order of ICT>Epi ext>ICA, ICA had the strongest estrogenic activity and next ICT in ovariectomized rats. These results collectively suggest that phytoestrogens possess both estrogenic and antiestrogenic activity, and that the differential expression of these two compounds with opposing activities is dependent on the physiological environment in terms of estrogen level, which may be the case in humans. |
| doi_str_mv | 10.1016/j.fct.2012.05.017 |
| format | Article |
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The estrogenic and antiestrogenic activities of Epimedii Herba, which is a traditional medicinal herb used in Korea and China were investigated in this study. The in vitro estrogen receptor (ER) mediated estrogenic/antiestrogenic activities of an Epimedii Herba extract (Epi ext) and its major components were determined using an estrogen responsive element driven reporter gene assay in MCF-7/ERE and HEK293T cells. The Epi ext exhibited ERα- and ERβ-mediated estrogenic activity with an EC50 of 5.0 and 17.8μM in HEK293T cells, respectively. Prenylflavonoid glycosides such as icariin (ICA), epimedin A, B, and C did not show any in vitro estrogenic or antiestrogenic activities. Icaritin (ICT) and quercetin exhibited in vitro ER mediated estrogenic activity with a more potent interaction with ERβ. In vivo estrogenic activities of the Epi ext, ICA and ICT were compared using an uterotrophic assay. Although the potency of in vitro estrogenic activity was in the order of ICT>Epi ext>ICA, ICA had the strongest estrogenic activity and next ICT in ovariectomized rats. These results collectively suggest that phytoestrogens possess both estrogenic and antiestrogenic activity, and that the differential expression of these two compounds with opposing activities is dependent on the physiological environment in terms of estrogen level, which may be the case in humans.</description><identifier>ISSN: 0278-6915</identifier><identifier>EISSN: 1873-6351</identifier><identifier>DOI: 10.1016/j.fct.2012.05.017</identifier><identifier>PMID: 22613215</identifier><identifier>CODEN: FCTOD7</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Animals ; Biological and medical sciences ; Cell Line ; Epimedium ; Epimedium - chemistry ; Epimedium koreanum ; Estrogen Receptor Modulators - pharmacology ; estrogen receptors ; estrogenic properties ; Estrogenic/antiestrogenic activity ; Estrogens - pharmacology ; Female ; gene expression regulation ; glycosides ; Humans ; Icariin ; Icaritin ; In Vitro Techniques ; in vivo studies ; Medical sciences ; medicinal plants ; ovariectomy ; plant estrogens ; Plant Extracts - pharmacology ; quercetin ; Rats ; Rats, Sprague-Dawley ; Reporter gene assay ; reporter genes ; Toxicology ; Uterotrophic assay</subject><ispartof>Food and chemical toxicology, 2012-08, Vol.50 (8), p.2751-2759</ispartof><rights>2012 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2012 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c440t-ba4c8d838d37403865eb784e18c4edb1abbd3fe8033c64d60afc2d4be5825abd3</citedby><cites>FETCH-LOGICAL-c440t-ba4c8d838d37403865eb784e18c4edb1abbd3fe8033c64d60afc2d4be5825abd3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0278691512003584$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=26208001$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22613215$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kang, Hyun Ku</creatorcontrib><creatorcontrib>Choi, Yun-Ho</creatorcontrib><creatorcontrib>Kwon, Hyosuk</creatorcontrib><creatorcontrib>Lee, Sang-Bum</creatorcontrib><creatorcontrib>Kim, Dong-Hyun</creatorcontrib><creatorcontrib>Sung, Chung Ki</creatorcontrib><creatorcontrib>Park, Young In</creatorcontrib><creatorcontrib>Dong, Mi-Sook</creatorcontrib><title>Estrogenic/antiestrogenic activities of a Epimedium koreanum extract and its major components: in vitro and in vivo studies</title><title>Food and chemical toxicology</title><addtitle>Food Chem Toxicol</addtitle><description>► ICT and quercetin exhibited in vitro ER mediated estrogenic activity with a more potent interaction with ERβ. ► Prenylflavonoid glycosides did not show any in vitro estrogenic activities. ► The potency of in vitro estrogenic activity was in the order of ICT>Epi ext>ICA. ► ICA had the strongest estrogenic activity in ovariectomized rats.
The estrogenic and antiestrogenic activities of Epimedii Herba, which is a traditional medicinal herb used in Korea and China were investigated in this study. The in vitro estrogen receptor (ER) mediated estrogenic/antiestrogenic activities of an Epimedii Herba extract (Epi ext) and its major components were determined using an estrogen responsive element driven reporter gene assay in MCF-7/ERE and HEK293T cells. The Epi ext exhibited ERα- and ERβ-mediated estrogenic activity with an EC50 of 5.0 and 17.8μM in HEK293T cells, respectively. Prenylflavonoid glycosides such as icariin (ICA), epimedin A, B, and C did not show any in vitro estrogenic or antiestrogenic activities. Icaritin (ICT) and quercetin exhibited in vitro ER mediated estrogenic activity with a more potent interaction with ERβ. In vivo estrogenic activities of the Epi ext, ICA and ICT were compared using an uterotrophic assay. Although the potency of in vitro estrogenic activity was in the order of ICT>Epi ext>ICA, ICA had the strongest estrogenic activity and next ICT in ovariectomized rats. These results collectively suggest that phytoestrogens possess both estrogenic and antiestrogenic activity, and that the differential expression of these two compounds with opposing activities is dependent on the physiological environment in terms of estrogen level, which may be the case in humans.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cell Line</subject><subject>Epimedium</subject><subject>Epimedium - chemistry</subject><subject>Epimedium koreanum</subject><subject>Estrogen Receptor Modulators - pharmacology</subject><subject>estrogen receptors</subject><subject>estrogenic properties</subject><subject>Estrogenic/antiestrogenic activity</subject><subject>Estrogens - pharmacology</subject><subject>Female</subject><subject>gene expression regulation</subject><subject>glycosides</subject><subject>Humans</subject><subject>Icariin</subject><subject>Icaritin</subject><subject>In Vitro Techniques</subject><subject>in vivo studies</subject><subject>Medical sciences</subject><subject>medicinal plants</subject><subject>ovariectomy</subject><subject>plant estrogens</subject><subject>Plant Extracts - pharmacology</subject><subject>quercetin</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Reporter gene assay</subject><subject>reporter genes</subject><subject>Toxicology</subject><subject>Uterotrophic assay</subject><issn>0278-6915</issn><issn>1873-6351</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU1v1DAQhi0EokvhB3ABX5B6SWo7ie3CCVXLh1SJA_RsOfak8rKxFztZFfHnmShLucHJHs8z45n3JeQlZzVnXF7u6sFNtWBc1KyrGVePyIZr1VSy6fhjsmFC6Upe8e6MPCtlxxhTXMmn5EwIyRvBuw35tS1TTncQg7u0cQrwEFLrpnAMyxNNA7V0ewgj-DCP9HvKYCNe4H7KiFEbPQ1ToaPdpUxdGg8pQpzKWxoixR45rcgSHBMt0-yx7XPyZLD7Ai9O5zm5_bD9dv2puvny8fP1-5vKtS2bqt62TnvdaN-oljVadtAr3QLXrgXfc9v3vhlAs6ZxsvWS2cEJ3_bQadFZzJ2Ti7XvIacfM25oxlAc7Pc2QpqL4VKhYPqKy_-jKKnUKLhGlK-oy6mUDIM55DDa_BMhs9hjdgbtMYs9hnUG7cGaV6f2c49aPlT88QOBNyfAFmf3Q7bRhfKXk4Jpxjhyr1dusMnYu4zM7Vf8qcOkEpwtm7xbCUBljwGyKS5AdOhgBhzLp_CPQX8D7o64TQ</recordid><startdate>20120801</startdate><enddate>20120801</enddate><creator>Kang, Hyun Ku</creator><creator>Choi, Yun-Ho</creator><creator>Kwon, Hyosuk</creator><creator>Lee, Sang-Bum</creator><creator>Kim, Dong-Hyun</creator><creator>Sung, Chung Ki</creator><creator>Park, Young In</creator><creator>Dong, Mi-Sook</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>FBQ</scope><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>7U7</scope><scope>C1K</scope></search><sort><creationdate>20120801</creationdate><title>Estrogenic/antiestrogenic activities of a Epimedium koreanum extract and its major components: in vitro and in vivo studies</title><author>Kang, Hyun Ku ; Choi, Yun-Ho ; Kwon, Hyosuk ; Lee, Sang-Bum ; Kim, Dong-Hyun ; Sung, Chung Ki ; Park, Young In ; Dong, Mi-Sook</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c440t-ba4c8d838d37403865eb784e18c4edb1abbd3fe8033c64d60afc2d4be5825abd3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cell Line</topic><topic>Epimedium</topic><topic>Epimedium - chemistry</topic><topic>Epimedium koreanum</topic><topic>Estrogen Receptor Modulators - pharmacology</topic><topic>estrogen receptors</topic><topic>estrogenic properties</topic><topic>Estrogenic/antiestrogenic activity</topic><topic>Estrogens - pharmacology</topic><topic>Female</topic><topic>gene expression regulation</topic><topic>glycosides</topic><topic>Humans</topic><topic>Icariin</topic><topic>Icaritin</topic><topic>In Vitro Techniques</topic><topic>in vivo studies</topic><topic>Medical sciences</topic><topic>medicinal plants</topic><topic>ovariectomy</topic><topic>plant estrogens</topic><topic>Plant Extracts - pharmacology</topic><topic>quercetin</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Reporter gene assay</topic><topic>reporter genes</topic><topic>Toxicology</topic><topic>Uterotrophic assay</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kang, Hyun Ku</creatorcontrib><creatorcontrib>Choi, Yun-Ho</creatorcontrib><creatorcontrib>Kwon, Hyosuk</creatorcontrib><creatorcontrib>Lee, Sang-Bum</creatorcontrib><creatorcontrib>Kim, Dong-Hyun</creatorcontrib><creatorcontrib>Sung, Chung Ki</creatorcontrib><creatorcontrib>Park, Young In</creatorcontrib><creatorcontrib>Dong, Mi-Sook</creatorcontrib><collection>AGRIS</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Toxicology Abstracts</collection><collection>Environmental Sciences and Pollution Management</collection><jtitle>Food and chemical toxicology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kang, Hyun Ku</au><au>Choi, Yun-Ho</au><au>Kwon, Hyosuk</au><au>Lee, Sang-Bum</au><au>Kim, Dong-Hyun</au><au>Sung, Chung Ki</au><au>Park, Young In</au><au>Dong, Mi-Sook</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Estrogenic/antiestrogenic activities of a Epimedium koreanum extract and its major components: in vitro and in vivo studies</atitle><jtitle>Food and chemical toxicology</jtitle><addtitle>Food Chem Toxicol</addtitle><date>2012-08-01</date><risdate>2012</risdate><volume>50</volume><issue>8</issue><spage>2751</spage><epage>2759</epage><pages>2751-2759</pages><issn>0278-6915</issn><eissn>1873-6351</eissn><coden>FCTOD7</coden><abstract>► ICT and quercetin exhibited in vitro ER mediated estrogenic activity with a more potent interaction with ERβ. ► Prenylflavonoid glycosides did not show any in vitro estrogenic activities. ► The potency of in vitro estrogenic activity was in the order of ICT>Epi ext>ICA. ► ICA had the strongest estrogenic activity in ovariectomized rats.
The estrogenic and antiestrogenic activities of Epimedii Herba, which is a traditional medicinal herb used in Korea and China were investigated in this study. The in vitro estrogen receptor (ER) mediated estrogenic/antiestrogenic activities of an Epimedii Herba extract (Epi ext) and its major components were determined using an estrogen responsive element driven reporter gene assay in MCF-7/ERE and HEK293T cells. The Epi ext exhibited ERα- and ERβ-mediated estrogenic activity with an EC50 of 5.0 and 17.8μM in HEK293T cells, respectively. Prenylflavonoid glycosides such as icariin (ICA), epimedin A, B, and C did not show any in vitro estrogenic or antiestrogenic activities. Icaritin (ICT) and quercetin exhibited in vitro ER mediated estrogenic activity with a more potent interaction with ERβ. In vivo estrogenic activities of the Epi ext, ICA and ICT were compared using an uterotrophic assay. Although the potency of in vitro estrogenic activity was in the order of ICT>Epi ext>ICA, ICA had the strongest estrogenic activity and next ICT in ovariectomized rats. These results collectively suggest that phytoestrogens possess both estrogenic and antiestrogenic activity, and that the differential expression of these two compounds with opposing activities is dependent on the physiological environment in terms of estrogen level, which may be the case in humans.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>22613215</pmid><doi>10.1016/j.fct.2012.05.017</doi><tpages>9</tpages></addata></record> |
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| subjects | Animals Biological and medical sciences Cell Line Epimedium Epimedium - chemistry Epimedium koreanum Estrogen Receptor Modulators - pharmacology estrogen receptors estrogenic properties Estrogenic/antiestrogenic activity Estrogens - pharmacology Female gene expression regulation glycosides Humans Icariin Icaritin In Vitro Techniques in vivo studies Medical sciences medicinal plants ovariectomy plant estrogens Plant Extracts - pharmacology quercetin Rats Rats, Sprague-Dawley Reporter gene assay reporter genes Toxicology Uterotrophic assay |
| title | Estrogenic/antiestrogenic activities of a Epimedium koreanum extract and its major components: in vitro and in vivo studies |
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