Loading…
Inhibition of skin 5α-reductase by oral contraceptive progestins in vitro
Androgenic disorders of female skin such as hirsutism, acne and alopecia are etiologically caused by androgen excess. Skin 5α-reductase activity is a major factor influencing the manifestation of endogenous androgen excess in women. Oral contraceptives have proven useful for the treatment of androge...
Saved in:
Published in: | Gynecological endocrinology 2000, Vol.14 (4), p.223-230 |
---|---|
Main Authors: | , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
cited_by | cdi_FETCH-LOGICAL-c431t-7d1ca11dde84b4e667eb47e9c1b653411368412482ee822884ddb4015e9f54f73 |
---|---|
cites | cdi_FETCH-LOGICAL-c431t-7d1ca11dde84b4e667eb47e9c1b653411368412482ee822884ddb4015e9f54f73 |
container_end_page | 230 |
container_issue | 4 |
container_start_page | 223 |
container_title | Gynecological endocrinology |
container_volume | 14 |
creator | Rabe, T. Kowald, A. Ortmann, J. Rehberger-Schneider, S. |
description | Androgenic disorders of female skin such as hirsutism, acne and alopecia are etiologically caused by androgen excess. Skin 5α-reductase activity is a major factor influencing the manifestation of endogenous androgen excess in women. Oral contraceptives have proven useful for the treatment of androgen disorders of the skin. The mechanisms of action by which oral contraceptives correct skin androgen levels may include inhibition of 5α-reductase and androgen receptor activity. We investigated the inhibitory effect of oral contraceptive progestins and ethinyl estradiol on skin 5α-reductase and their influence on androgen receptor activity and affinity, using three different in vitro assay systems. It was shown that norgestimate blocked 5α-reductase activity with an IC50 value of 10 μM, followed by levonorgestrel (IC50 52 μM), dienogest (IC50 55 μM), cyproterone acetate (IC50 87 μM) and gestodene (IC50 98 μM). To determine the full androgenic potential of the progestins, androgen receptor binding affinities and activation potentials were determined. The progestins norgestimate and dienogest in particular combined 5α-reductase inhibition with minimal androgenic potential. These data demonstrate that the progestins norgestimate and dienogest might help in the treatment of clinical hyperandrogeny in women. |
doi_str_mv | 10.3109/09513590009167685 |
format | article |
fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_72407307</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>72407307</sourcerecordid><originalsourceid>FETCH-LOGICAL-c431t-7d1ca11dde84b4e667eb47e9c1b653411368412482ee822884ddb4015e9f54f73</originalsourceid><addsrcrecordid>eNp9kM9O20AQh1cVqEnTPkAvyAfEzbDj_WcLLhWiJQiJC5yt9XrcLDi7YXdNlcfqi_BMdZRUCCHlNIf5vtFvfoR8B3rKgFZntBLAREUprUAqWYpPZApcsZwqKQ_IdLPPN8CEfInxkVJgXBWfyQSAKlFUdEpu5m5hG5usd5nvsvhkXSZe_-YB28EkHTFr1pkPus-Mdylog6tkXzBbBf8bY7IuZqPxYlPwX8lhp_uI33ZzRh5-Xt1fXue3d7_mlz9uc8MZpFy1YDRA22LJG45SKmy4wspAIwXjAEyWHApeFohlUZQlb9uGUxBYdYJ3is3IyfbumOF5GEPUSxsN9r126IdYq4JTxegGhC1ogo8xYFevgl3qsK6B1psC6w8Fjs7R7vjQLLF9M3aNjcDxDtDR6L4L2hkb3zgBsqTViF1sMes6H5b6jw99Wye97n3477B9Mc7f6QvUfVoYHbB-9ENwY797nvgHEp6dNw</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>72407307</pqid></control><display><type>article</type><title>Inhibition of skin 5α-reductase by oral contraceptive progestins in vitro</title><source>Taylor and Francis:Jisc Collections:Taylor and Francis Read and Publish Agreement 2024-2025:Medical Collection (Reading list)</source><creator>Rabe, T. ; Kowald, A. ; Ortmann, J. ; Rehberger-Schneider, S.</creator><creatorcontrib>Rabe, T. ; Kowald, A. ; Ortmann, J. ; Rehberger-Schneider, S.</creatorcontrib><description>Androgenic disorders of female skin such as hirsutism, acne and alopecia are etiologically caused by androgen excess. Skin 5α-reductase activity is a major factor influencing the manifestation of endogenous androgen excess in women. Oral contraceptives have proven useful for the treatment of androgen disorders of the skin. The mechanisms of action by which oral contraceptives correct skin androgen levels may include inhibition of 5α-reductase and androgen receptor activity. We investigated the inhibitory effect of oral contraceptive progestins and ethinyl estradiol on skin 5α-reductase and their influence on androgen receptor activity and affinity, using three different in vitro assay systems. It was shown that norgestimate blocked 5α-reductase activity with an IC50 value of 10 μM, followed by levonorgestrel (IC50 52 μM), dienogest (IC50 55 μM), cyproterone acetate (IC50 87 μM) and gestodene (IC50 98 μM). To determine the full androgenic potential of the progestins, androgen receptor binding affinities and activation potentials were determined. The progestins norgestimate and dienogest in particular combined 5α-reductase inhibition with minimal androgenic potential. These data demonstrate that the progestins norgestimate and dienogest might help in the treatment of clinical hyperandrogeny in women.</description><identifier>ISSN: 0951-3590</identifier><identifier>EISSN: 1473-0766</identifier><identifier>DOI: 10.3109/09513590009167685</identifier><identifier>PMID: 11075290</identifier><language>eng</language><publisher>Carnforth: Informa UK Ltd</publisher><subject>3-Oxo-5-alpha-Steroid 4-Dehydrogenase - drug effects ; 5α-Reductase ; Adolescent ; Adult ; Biological and medical sciences ; Birth control ; Contraceptives, Oral - pharmacology ; Dose-Response Relationship, Drug ; Female ; Gynecology. Andrology. Obstetrics ; Hormonal contraception ; Humans ; Hyperandrogenism - prevention & control ; Medical sciences ; Nandrolone - analogs & derivatives ; Nandrolone - pharmacology ; Norgestrel - analogs & derivatives ; Norgestrel - pharmacology ; Oral Contraceptive ; Progestin ; Progestins - pharmacology ; Receptors, Androgen - drug effects ; Skin - enzymology ; Skin - metabolism</subject><ispartof>Gynecological endocrinology, 2000, Vol.14 (4), p.223-230</ispartof><rights>2000 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 2000</rights><rights>2000 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c431t-7d1ca11dde84b4e667eb47e9c1b653411368412482ee822884ddb4015e9f54f73</citedby><cites>FETCH-LOGICAL-c431t-7d1ca11dde84b4e667eb47e9c1b653411368412482ee822884ddb4015e9f54f73</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,4010,27900,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1516809$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11075290$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Rabe, T.</creatorcontrib><creatorcontrib>Kowald, A.</creatorcontrib><creatorcontrib>Ortmann, J.</creatorcontrib><creatorcontrib>Rehberger-Schneider, S.</creatorcontrib><title>Inhibition of skin 5α-reductase by oral contraceptive progestins in vitro</title><title>Gynecological endocrinology</title><addtitle>Gynecol Endocrinol</addtitle><description>Androgenic disorders of female skin such as hirsutism, acne and alopecia are etiologically caused by androgen excess. Skin 5α-reductase activity is a major factor influencing the manifestation of endogenous androgen excess in women. Oral contraceptives have proven useful for the treatment of androgen disorders of the skin. The mechanisms of action by which oral contraceptives correct skin androgen levels may include inhibition of 5α-reductase and androgen receptor activity. We investigated the inhibitory effect of oral contraceptive progestins and ethinyl estradiol on skin 5α-reductase and their influence on androgen receptor activity and affinity, using three different in vitro assay systems. It was shown that norgestimate blocked 5α-reductase activity with an IC50 value of 10 μM, followed by levonorgestrel (IC50 52 μM), dienogest (IC50 55 μM), cyproterone acetate (IC50 87 μM) and gestodene (IC50 98 μM). To determine the full androgenic potential of the progestins, androgen receptor binding affinities and activation potentials were determined. The progestins norgestimate and dienogest in particular combined 5α-reductase inhibition with minimal androgenic potential. These data demonstrate that the progestins norgestimate and dienogest might help in the treatment of clinical hyperandrogeny in women.</description><subject>3-Oxo-5-alpha-Steroid 4-Dehydrogenase - drug effects</subject><subject>5α-Reductase</subject><subject>Adolescent</subject><subject>Adult</subject><subject>Biological and medical sciences</subject><subject>Birth control</subject><subject>Contraceptives, Oral - pharmacology</subject><subject>Dose-Response Relationship, Drug</subject><subject>Female</subject><subject>Gynecology. Andrology. Obstetrics</subject><subject>Hormonal contraception</subject><subject>Humans</subject><subject>Hyperandrogenism - prevention & control</subject><subject>Medical sciences</subject><subject>Nandrolone - analogs & derivatives</subject><subject>Nandrolone - pharmacology</subject><subject>Norgestrel - analogs & derivatives</subject><subject>Norgestrel - pharmacology</subject><subject>Oral Contraceptive</subject><subject>Progestin</subject><subject>Progestins - pharmacology</subject><subject>Receptors, Androgen - drug effects</subject><subject>Skin - enzymology</subject><subject>Skin - metabolism</subject><issn>0951-3590</issn><issn>1473-0766</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><recordid>eNp9kM9O20AQh1cVqEnTPkAvyAfEzbDj_WcLLhWiJQiJC5yt9XrcLDi7YXdNlcfqi_BMdZRUCCHlNIf5vtFvfoR8B3rKgFZntBLAREUprUAqWYpPZApcsZwqKQ_IdLPPN8CEfInxkVJgXBWfyQSAKlFUdEpu5m5hG5usd5nvsvhkXSZe_-YB28EkHTFr1pkPus-Mdylog6tkXzBbBf8bY7IuZqPxYlPwX8lhp_uI33ZzRh5-Xt1fXue3d7_mlz9uc8MZpFy1YDRA22LJG45SKmy4wspAIwXjAEyWHApeFohlUZQlb9uGUxBYdYJ3is3IyfbumOF5GEPUSxsN9r126IdYq4JTxegGhC1ogo8xYFevgl3qsK6B1psC6w8Fjs7R7vjQLLF9M3aNjcDxDtDR6L4L2hkb3zgBsqTViF1sMes6H5b6jw99Wye97n3477B9Mc7f6QvUfVoYHbB-9ENwY797nvgHEp6dNw</recordid><startdate>2000</startdate><enddate>2000</enddate><creator>Rabe, T.</creator><creator>Kowald, A.</creator><creator>Ortmann, J.</creator><creator>Rehberger-Schneider, S.</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><general>Parthenon</general><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>2000</creationdate><title>Inhibition of skin 5α-reductase by oral contraceptive progestins in vitro</title><author>Rabe, T. ; Kowald, A. ; Ortmann, J. ; Rehberger-Schneider, S.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c431t-7d1ca11dde84b4e667eb47e9c1b653411368412482ee822884ddb4015e9f54f73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>3-Oxo-5-alpha-Steroid 4-Dehydrogenase - drug effects</topic><topic>5α-Reductase</topic><topic>Adolescent</topic><topic>Adult</topic><topic>Biological and medical sciences</topic><topic>Birth control</topic><topic>Contraceptives, Oral - pharmacology</topic><topic>Dose-Response Relationship, Drug</topic><topic>Female</topic><topic>Gynecology. Andrology. Obstetrics</topic><topic>Hormonal contraception</topic><topic>Humans</topic><topic>Hyperandrogenism - prevention & control</topic><topic>Medical sciences</topic><topic>Nandrolone - analogs & derivatives</topic><topic>Nandrolone - pharmacology</topic><topic>Norgestrel - analogs & derivatives</topic><topic>Norgestrel - pharmacology</topic><topic>Oral Contraceptive</topic><topic>Progestin</topic><topic>Progestins - pharmacology</topic><topic>Receptors, Androgen - drug effects</topic><topic>Skin - enzymology</topic><topic>Skin - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Rabe, T.</creatorcontrib><creatorcontrib>Kowald, A.</creatorcontrib><creatorcontrib>Ortmann, J.</creatorcontrib><creatorcontrib>Rehberger-Schneider, S.</creatorcontrib><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>Gynecological endocrinology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Rabe, T.</au><au>Kowald, A.</au><au>Ortmann, J.</au><au>Rehberger-Schneider, S.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Inhibition of skin 5α-reductase by oral contraceptive progestins in vitro</atitle><jtitle>Gynecological endocrinology</jtitle><addtitle>Gynecol Endocrinol</addtitle><date>2000</date><risdate>2000</risdate><volume>14</volume><issue>4</issue><spage>223</spage><epage>230</epage><pages>223-230</pages><issn>0951-3590</issn><eissn>1473-0766</eissn><abstract>Androgenic disorders of female skin such as hirsutism, acne and alopecia are etiologically caused by androgen excess. Skin 5α-reductase activity is a major factor influencing the manifestation of endogenous androgen excess in women. Oral contraceptives have proven useful for the treatment of androgen disorders of the skin. The mechanisms of action by which oral contraceptives correct skin androgen levels may include inhibition of 5α-reductase and androgen receptor activity. We investigated the inhibitory effect of oral contraceptive progestins and ethinyl estradiol on skin 5α-reductase and their influence on androgen receptor activity and affinity, using three different in vitro assay systems. It was shown that norgestimate blocked 5α-reductase activity with an IC50 value of 10 μM, followed by levonorgestrel (IC50 52 μM), dienogest (IC50 55 μM), cyproterone acetate (IC50 87 μM) and gestodene (IC50 98 μM). To determine the full androgenic potential of the progestins, androgen receptor binding affinities and activation potentials were determined. The progestins norgestimate and dienogest in particular combined 5α-reductase inhibition with minimal androgenic potential. These data demonstrate that the progestins norgestimate and dienogest might help in the treatment of clinical hyperandrogeny in women.</abstract><cop>Carnforth</cop><pub>Informa UK Ltd</pub><pmid>11075290</pmid><doi>10.3109/09513590009167685</doi><tpages>8</tpages></addata></record> |
fulltext | fulltext |
identifier | ISSN: 0951-3590 |
ispartof | Gynecological endocrinology, 2000, Vol.14 (4), p.223-230 |
issn | 0951-3590 1473-0766 |
language | eng |
recordid | cdi_proquest_miscellaneous_72407307 |
source | Taylor and Francis:Jisc Collections:Taylor and Francis Read and Publish Agreement 2024-2025:Medical Collection (Reading list) |
subjects | 3-Oxo-5-alpha-Steroid 4-Dehydrogenase - drug effects 5α-Reductase Adolescent Adult Biological and medical sciences Birth control Contraceptives, Oral - pharmacology Dose-Response Relationship, Drug Female Gynecology. Andrology. Obstetrics Hormonal contraception Humans Hyperandrogenism - prevention & control Medical sciences Nandrolone - analogs & derivatives Nandrolone - pharmacology Norgestrel - analogs & derivatives Norgestrel - pharmacology Oral Contraceptive Progestin Progestins - pharmacology Receptors, Androgen - drug effects Skin - enzymology Skin - metabolism |
title | Inhibition of skin 5α-reductase by oral contraceptive progestins in vitro |
url | http://sfxeu10.hosted.exlibrisgroup.com/loughborough?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-30T09%3A09%3A29IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Inhibition%20of%20skin%205%CE%B1-reductase%20by%20oral%20contraceptive%20progestins%20in%20vitro&rft.jtitle=Gynecological%20endocrinology&rft.au=Rabe,%20T.&rft.date=2000&rft.volume=14&rft.issue=4&rft.spage=223&rft.epage=230&rft.pages=223-230&rft.issn=0951-3590&rft.eissn=1473-0766&rft_id=info:doi/10.3109/09513590009167685&rft_dat=%3Cproquest_cross%3E72407307%3C/proquest_cross%3E%3Cgrp_id%3Ecdi_FETCH-LOGICAL-c431t-7d1ca11dde84b4e667eb47e9c1b653411368412482ee822884ddb4015e9f54f73%3C/grp_id%3E%3Coa%3E%3C/oa%3E%3Curl%3E%3C/url%3E&rft_id=info:oai/&rft_pqid=72407307&rft_id=info:pmid/11075290&rfr_iscdi=true |