Evaluation of Estrogenic Activity of Plant Extracts for the Potential Treatment of Menopausal Symptoms
Eight botanical preparations that are commonly used for the treatment of menopausal symptoms were tested for estrogenic activity. Methanol extracts of red clover (Trifolium pratense L.), chasteberry (Vitex agnus-castus L.), and hops (Humulus lupulus L.) showed significant competitive binding to estr...
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| Veröffentlicht in: | Journal of agricultural and food chemistry 2001-05, Vol.49 (5), p.2472-2479 |
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| creator | Liu, Jianghua Burdette, Joanna E Xu, Haiyan Gu, Chungang van Breemen, Richard B Bhat, Krishna P. L Booth, Nancy Constantinou, Andreas I Pezzuto, John M Fong, Harry H. S Farnsworth, Norman R Bolton, Judy L |
| description | Eight botanical preparations that are commonly used for the treatment of menopausal symptoms were tested for estrogenic activity. Methanol extracts of red clover (Trifolium pratense L.), chasteberry (Vitex agnus-castus L.), and hops (Humulus lupulus L.) showed significant competitive binding to estrogen receptors α (ERα) and β (ERβ). With cultured Ishikawa (endometrial) cells, red clover and hops exhibited estrogenic activity as indicated by induction of alkaline phosphatase (AP) activity and up-regulation of progesterone receptor (PR) mRNA. Chasteberry also stimulated PR expression, but no induction of AP activity was observed. In S30 breast cancer cells, pS2 (presenelin-2), another estrogen-inducible gene, was up-regulated in the presence of red clover, hops, and chasteberry. Interestingly, extracts of Asian ginseng (Panax ginseng C.A. Meyer) and North American ginseng (Panax quinquefolius L.) induced pS2 mRNA expression in S30 cells, but no significant ER binding affinity, AP induction, or PR expression was noted in Ishikawa cells. Dong quai [Angelica sinensis (Oliv.) Diels] and licorice (Glycyrrhiza glabra L.) showed only weak ER binding and PR and pS2 mRNA induction. Black cohosh [Cimicifuga racemosa (L.) Nutt.] showed no activity in any of the above in vitro assays. Bioassay-guided isolation utilizing ER competitive binding as a monitor and screening using ultrafiltration LC-MS revealed that genistein was the most active component of red clover. Consistent with this observation, genistein was found to be the most effective of four red clover isoflavones tested in the above in vitro assays. Therefore, estrogenic components of plant extracts can be identified using assays for estrogenic activity along with screening and identification of the active components using ultrafiltration LC-MS. These data suggest a potential use for some dietary supplements, ingested by human beings, in the treatment of menopausal symptoms. Keywords: Estrogen receptor; alkaline phosphatase; progesterone receptor; pS2; dietary supplement; phytoestrogens; isoflavones |
| doi_str_mv | 10.1021/jf0014157 |
| format | Article |
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L ; Booth, Nancy ; Constantinou, Andreas I ; Pezzuto, John M ; Fong, Harry H. S ; Farnsworth, Norman R ; Bolton, Judy L</creator><creatorcontrib>Liu, Jianghua ; Burdette, Joanna E ; Xu, Haiyan ; Gu, Chungang ; van Breemen, Richard B ; Bhat, Krishna P. L ; Booth, Nancy ; Constantinou, Andreas I ; Pezzuto, John M ; Fong, Harry H. S ; Farnsworth, Norman R ; Bolton, Judy L</creatorcontrib><description>Eight botanical preparations that are commonly used for the treatment of menopausal symptoms were tested for estrogenic activity. Methanol extracts of red clover (Trifolium pratense L.), chasteberry (Vitex agnus-castus L.), and hops (Humulus lupulus L.) showed significant competitive binding to estrogen receptors α (ERα) and β (ERβ). With cultured Ishikawa (endometrial) cells, red clover and hops exhibited estrogenic activity as indicated by induction of alkaline phosphatase (AP) activity and up-regulation of progesterone receptor (PR) mRNA. Chasteberry also stimulated PR expression, but no induction of AP activity was observed. In S30 breast cancer cells, pS2 (presenelin-2), another estrogen-inducible gene, was up-regulated in the presence of red clover, hops, and chasteberry. Interestingly, extracts of Asian ginseng (Panax ginseng C.A. Meyer) and North American ginseng (Panax quinquefolius L.) induced pS2 mRNA expression in S30 cells, but no significant ER binding affinity, AP induction, or PR expression was noted in Ishikawa cells. Dong quai [Angelica sinensis (Oliv.) Diels] and licorice (Glycyrrhiza glabra L.) showed only weak ER binding and PR and pS2 mRNA induction. Black cohosh [Cimicifuga racemosa (L.) Nutt.] showed no activity in any of the above in vitro assays. Bioassay-guided isolation utilizing ER competitive binding as a monitor and screening using ultrafiltration LC-MS revealed that genistein was the most active component of red clover. Consistent with this observation, genistein was found to be the most effective of four red clover isoflavones tested in the above in vitro assays. Therefore, estrogenic components of plant extracts can be identified using assays for estrogenic activity along with screening and identification of the active components using ultrafiltration LC-MS. These data suggest a potential use for some dietary supplements, ingested by human beings, in the treatment of menopausal symptoms. Keywords: Estrogen receptor; alkaline phosphatase; progesterone receptor; pS2; dietary supplement; phytoestrogens; isoflavones</description><identifier>ISSN: 0021-8561</identifier><identifier>EISSN: 1520-5118</identifier><identifier>DOI: 10.1021/jf0014157</identifier><identifier>PMID: 11368622</identifier><identifier>CODEN: JAFCAU</identifier><language>eng</language><publisher>Washington, DC: American Chemical Society</publisher><subject>Binding, Competitive ; Biological and medical sciences ; Cells, Cultured ; Dietary Supplements ; Estrogens - physiology ; Estrogens, Non-Steroidal - pharmacology ; General pharmacology ; Humans ; Isoflavones ; Medical sciences ; Menopause - drug effects ; Pharmacognosy. Homeopathy. Health food ; Pharmacology. Drug treatments ; Phytoestrogens ; Plant Extracts - chemistry ; Plant Preparations ; Receptors, Estrogen - metabolism ; Receptors, Progesterone - metabolism ; Up-Regulation</subject><ispartof>Journal of agricultural and food chemistry, 2001-05, Vol.49 (5), p.2472-2479</ispartof><rights>Copyright © 2001 American Chemical Society</rights><rights>2001 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-a445t-fa0a8e3ec7444d1067be203b8a9da9716d10cbf71704b74c29d7a8980eaa70f3</citedby><cites>FETCH-LOGICAL-a445t-fa0a8e3ec7444d1067be203b8a9da9716d10cbf71704b74c29d7a8980eaa70f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://pubs.acs.org/doi/pdf/10.1021/jf0014157$$EPDF$$P50$$Gacs$$H</linktopdf><linktohtml>$$Uhttps://pubs.acs.org/doi/10.1021/jf0014157$$EHTML$$P50$$Gacs$$H</linktohtml><link.rule.ids>314,776,780,2752,27053,27901,27902,56713,56763</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=998384$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11368622$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Liu, Jianghua</creatorcontrib><creatorcontrib>Burdette, Joanna E</creatorcontrib><creatorcontrib>Xu, Haiyan</creatorcontrib><creatorcontrib>Gu, Chungang</creatorcontrib><creatorcontrib>van Breemen, Richard B</creatorcontrib><creatorcontrib>Bhat, Krishna P. L</creatorcontrib><creatorcontrib>Booth, Nancy</creatorcontrib><creatorcontrib>Constantinou, Andreas I</creatorcontrib><creatorcontrib>Pezzuto, John M</creatorcontrib><creatorcontrib>Fong, Harry H. S</creatorcontrib><creatorcontrib>Farnsworth, Norman R</creatorcontrib><creatorcontrib>Bolton, Judy L</creatorcontrib><title>Evaluation of Estrogenic Activity of Plant Extracts for the Potential Treatment of Menopausal Symptoms</title><title>Journal of agricultural and food chemistry</title><addtitle>J. Agric. Food Chem</addtitle><description>Eight botanical preparations that are commonly used for the treatment of menopausal symptoms were tested for estrogenic activity. Methanol extracts of red clover (Trifolium pratense L.), chasteberry (Vitex agnus-castus L.), and hops (Humulus lupulus L.) showed significant competitive binding to estrogen receptors α (ERα) and β (ERβ). With cultured Ishikawa (endometrial) cells, red clover and hops exhibited estrogenic activity as indicated by induction of alkaline phosphatase (AP) activity and up-regulation of progesterone receptor (PR) mRNA. Chasteberry also stimulated PR expression, but no induction of AP activity was observed. In S30 breast cancer cells, pS2 (presenelin-2), another estrogen-inducible gene, was up-regulated in the presence of red clover, hops, and chasteberry. Interestingly, extracts of Asian ginseng (Panax ginseng C.A. Meyer) and North American ginseng (Panax quinquefolius L.) induced pS2 mRNA expression in S30 cells, but no significant ER binding affinity, AP induction, or PR expression was noted in Ishikawa cells. Dong quai [Angelica sinensis (Oliv.) Diels] and licorice (Glycyrrhiza glabra L.) showed only weak ER binding and PR and pS2 mRNA induction. Black cohosh [Cimicifuga racemosa (L.) Nutt.] showed no activity in any of the above in vitro assays. Bioassay-guided isolation utilizing ER competitive binding as a monitor and screening using ultrafiltration LC-MS revealed that genistein was the most active component of red clover. Consistent with this observation, genistein was found to be the most effective of four red clover isoflavones tested in the above in vitro assays. Therefore, estrogenic components of plant extracts can be identified using assays for estrogenic activity along with screening and identification of the active components using ultrafiltration LC-MS. These data suggest a potential use for some dietary supplements, ingested by human beings, in the treatment of menopausal symptoms. Keywords: Estrogen receptor; alkaline phosphatase; progesterone receptor; pS2; dietary supplement; phytoestrogens; isoflavones</description><subject>Binding, Competitive</subject><subject>Biological and medical sciences</subject><subject>Cells, Cultured</subject><subject>Dietary Supplements</subject><subject>Estrogens - physiology</subject><subject>Estrogens, Non-Steroidal - pharmacology</subject><subject>General pharmacology</subject><subject>Humans</subject><subject>Isoflavones</subject><subject>Medical sciences</subject><subject>Menopause - drug effects</subject><subject>Pharmacognosy. Homeopathy. Health food</subject><subject>Pharmacology. Drug treatments</subject><subject>Phytoestrogens</subject><subject>Plant Extracts - chemistry</subject><subject>Plant Preparations</subject><subject>Receptors, Estrogen - metabolism</subject><subject>Receptors, Progesterone - metabolism</subject><subject>Up-Regulation</subject><issn>0021-8561</issn><issn>1520-5118</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2001</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpt0EFr2zAUB3AxNta03aFfYBjGCj24fbJlSz52XdoO0i7Q0Kt4VqRNmW1lklyab1-FhOyyk9D__Xg8_oScUbikUNCrlQGgjFb8HZnQqoC8olS8JxNIw1xUNT0ixyGsAEBUHD6SI0rLWtRFMSFm-oLdiNG6IXMmm4bo3S89WJVdq2hfbNxs43mHQ8ymr9GjiiEzzmfxt87mLuohWuyyhdcY-_TZ6gc9uDWOIeVPm34dXR9OyQeDXdCf9u8JWdxOFzf3-ezn3Y-b61mOjFUxNwgodKkVZ4wtKdS81QWUrcBmiQ2ndcpUazjlwFrOVNEsOYpGgEbkYMoTcr5bu_bu76hDlL0NSnfpfO3GIDkIxouSJ3ixg8q7ELw2cu1tj34jKchtp_LQabKf90vHttfLf3JfYgJf9gCDws54HJQNB9c0ohQsqXynbIj69TBF_0fWvOSVXMyfZDP_9r0uZ4_yOfmvO48qyJUb_ZCK-895byIZmX8</recordid><startdate>20010501</startdate><enddate>20010501</enddate><creator>Liu, Jianghua</creator><creator>Burdette, Joanna E</creator><creator>Xu, Haiyan</creator><creator>Gu, Chungang</creator><creator>van Breemen, Richard B</creator><creator>Bhat, Krishna P. L</creator><creator>Booth, Nancy</creator><creator>Constantinou, Andreas I</creator><creator>Pezzuto, John M</creator><creator>Fong, Harry H. S</creator><creator>Farnsworth, Norman R</creator><creator>Bolton, Judy L</creator><general>American Chemical Society</general><scope>BSCLL</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></search><sort><creationdate>20010501</creationdate><title>Evaluation of Estrogenic Activity of Plant Extracts for the Potential Treatment of Menopausal Symptoms</title><author>Liu, Jianghua ; Burdette, Joanna E ; Xu, Haiyan ; Gu, Chungang ; van Breemen, Richard B ; Bhat, Krishna P. L ; Booth, Nancy ; Constantinou, Andreas I ; Pezzuto, John M ; Fong, Harry H. S ; Farnsworth, Norman R ; Bolton, Judy L</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-a445t-fa0a8e3ec7444d1067be203b8a9da9716d10cbf71704b74c29d7a8980eaa70f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2001</creationdate><topic>Binding, Competitive</topic><topic>Biological and medical sciences</topic><topic>Cells, Cultured</topic><topic>Dietary Supplements</topic><topic>Estrogens - physiology</topic><topic>Estrogens, Non-Steroidal - pharmacology</topic><topic>General pharmacology</topic><topic>Humans</topic><topic>Isoflavones</topic><topic>Medical sciences</topic><topic>Menopause - drug effects</topic><topic>Pharmacognosy. Homeopathy. Health food</topic><topic>Pharmacology. Drug treatments</topic><topic>Phytoestrogens</topic><topic>Plant Extracts - chemistry</topic><topic>Plant Preparations</topic><topic>Receptors, Estrogen - metabolism</topic><topic>Receptors, Progesterone - metabolism</topic><topic>Up-Regulation</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Liu, Jianghua</creatorcontrib><creatorcontrib>Burdette, Joanna E</creatorcontrib><creatorcontrib>Xu, Haiyan</creatorcontrib><creatorcontrib>Gu, Chungang</creatorcontrib><creatorcontrib>van Breemen, Richard B</creatorcontrib><creatorcontrib>Bhat, Krishna P. L</creatorcontrib><creatorcontrib>Booth, Nancy</creatorcontrib><creatorcontrib>Constantinou, Andreas I</creatorcontrib><creatorcontrib>Pezzuto, John M</creatorcontrib><creatorcontrib>Fong, Harry H. S</creatorcontrib><creatorcontrib>Farnsworth, Norman R</creatorcontrib><creatorcontrib>Bolton, Judy L</creatorcontrib><collection>Istex</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><jtitle>Journal of agricultural and food chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Liu, Jianghua</au><au>Burdette, Joanna E</au><au>Xu, Haiyan</au><au>Gu, Chungang</au><au>van Breemen, Richard B</au><au>Bhat, Krishna P. L</au><au>Booth, Nancy</au><au>Constantinou, Andreas I</au><au>Pezzuto, John M</au><au>Fong, Harry H. S</au><au>Farnsworth, Norman R</au><au>Bolton, Judy L</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Evaluation of Estrogenic Activity of Plant Extracts for the Potential Treatment of Menopausal Symptoms</atitle><jtitle>Journal of agricultural and food chemistry</jtitle><addtitle>J. Agric. Food Chem</addtitle><date>2001-05-01</date><risdate>2001</risdate><volume>49</volume><issue>5</issue><spage>2472</spage><epage>2479</epage><pages>2472-2479</pages><issn>0021-8561</issn><eissn>1520-5118</eissn><coden>JAFCAU</coden><abstract>Eight botanical preparations that are commonly used for the treatment of menopausal symptoms were tested for estrogenic activity. Methanol extracts of red clover (Trifolium pratense L.), chasteberry (Vitex agnus-castus L.), and hops (Humulus lupulus L.) showed significant competitive binding to estrogen receptors α (ERα) and β (ERβ). With cultured Ishikawa (endometrial) cells, red clover and hops exhibited estrogenic activity as indicated by induction of alkaline phosphatase (AP) activity and up-regulation of progesterone receptor (PR) mRNA. Chasteberry also stimulated PR expression, but no induction of AP activity was observed. In S30 breast cancer cells, pS2 (presenelin-2), another estrogen-inducible gene, was up-regulated in the presence of red clover, hops, and chasteberry. Interestingly, extracts of Asian ginseng (Panax ginseng C.A. Meyer) and North American ginseng (Panax quinquefolius L.) induced pS2 mRNA expression in S30 cells, but no significant ER binding affinity, AP induction, or PR expression was noted in Ishikawa cells. Dong quai [Angelica sinensis (Oliv.) Diels] and licorice (Glycyrrhiza glabra L.) showed only weak ER binding and PR and pS2 mRNA induction. Black cohosh [Cimicifuga racemosa (L.) Nutt.] showed no activity in any of the above in vitro assays. Bioassay-guided isolation utilizing ER competitive binding as a monitor and screening using ultrafiltration LC-MS revealed that genistein was the most active component of red clover. Consistent with this observation, genistein was found to be the most effective of four red clover isoflavones tested in the above in vitro assays. Therefore, estrogenic components of plant extracts can be identified using assays for estrogenic activity along with screening and identification of the active components using ultrafiltration LC-MS. These data suggest a potential use for some dietary supplements, ingested by human beings, in the treatment of menopausal symptoms. Keywords: Estrogen receptor; alkaline phosphatase; progesterone receptor; pS2; dietary supplement; phytoestrogens; isoflavones</abstract><cop>Washington, DC</cop><pub>American Chemical Society</pub><pmid>11368622</pmid><doi>10.1021/jf0014157</doi><tpages>8</tpages></addata></record> |
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| subjects | Binding, Competitive Biological and medical sciences Cells, Cultured Dietary Supplements Estrogens - physiology Estrogens, Non-Steroidal - pharmacology General pharmacology Humans Isoflavones Medical sciences Menopause - drug effects Pharmacognosy. Homeopathy. Health food Pharmacology. Drug treatments Phytoestrogens Plant Extracts - chemistry Plant Preparations Receptors, Estrogen - metabolism Receptors, Progesterone - metabolism Up-Regulation |
| title | Evaluation of Estrogenic Activity of Plant Extracts for the Potential Treatment of Menopausal Symptoms |
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