{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,4]],"date-time":"2026-08-04T01:23:15Z","timestamp":1785806595910,"version":"3.56.0"},"reference-count":28,"publisher":"Wiley","issue":"4","license":[{"start":{"date-parts":[[2019,1,29]],"date-time":"2019-01-29T00:00:00Z","timestamp":1548720000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Phytotherapy Research"],"published-print":{"date-parts":[[2019,4]]},"abstract":"<jats:p>The present work deals with the assessment of the in vitro and in vivo estrogenic effects of the triterpenoids (lupenone, lupeol, and stigmastenone) isolated from <jats:italic>Millettia macrophylla<\/jats:italic> extract. The in vitro estrogenicity was performed by a reporter gene assay and estrogen receptor\u2010\u03b1 (ER\u03b1) target gene expression, whereas the in vivo estrogenicity was evaluated by a 3\u2010day uterotrophic assay in ovariectomized rats. As results, lupenone and lupeol did not transactivate ER\u03b1 as well as ER\u03b2 of human embryonic kidney 293T (HEK293T) cells. However, lupeol seems to be antagonistic to estrogen (E2) only in HEK293T\u2010ER\u03b1 (10<jats:sup>\u22129<\/jats:sup> and 10<jats:sup>\u22128<\/jats:sup>\u00a0\u03bcM). Furthermore, lupeol slightly upregulated GREB1 gene expression at the concentration of 1\u00a0\u03bcM, suggesting a weak activation of endogenous ER\u03b1. In vivo, only lupeol at a dose of 1\u00a0mg\/kg significantly increased the uterine wet weight (<jats:italic>p<\/jats:italic>\u00a0&lt;\u00a00.05), uterine (<jats:italic>p<\/jats:italic>\u00a0&lt;\u00a00.05), and vaginal (<jats:italic>p<\/jats:italic>\u00a0&lt;\u00a00.01) epithelial heights. The concomitant administration of lupeol (1\u00a0mg\/kg) with a pure antiestrogen fulvestrant abrogated its effects only in the vagina, whereas in combination with E2, lupeol exhibited a significant antiestrogen\u2010like effect in uterine wet weight and synergistic effects on endometrium. Lupeol has estrogenic effects that is partly through ERs transcriptional activity and does involve alternative mechanisms that are still to be uncovered.<\/jats:p>","DOI":"10.1002\/ptr.6288","type":"journal-article","created":{"date-parts":[[2019,1,29]],"date-time":"2019-01-29T17:53:02Z","timestamp":1548784382000},"page":"949-957","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":10,"title":["Lupeol, the major compound of the dichloromethane extract of <scp><i>Millettia macrophylla<\/i><\/scp> Benth (Fabaceae), displays estrogenic effects in ovariectomized rats"],"prefix":"10.1002","volume":"33","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-4854-8783","authenticated-orcid":false,"given":"St\u00e9phane","family":"Zingue","sequence":"first","affiliation":[{"name":"Department of Life and Earth Sciences Higher Teachers' Training College, University of Maroua  Maroua Cameroon"},{"name":"Department of Animal Biology and Physiology, Faculty of Sciences University of Yaound\u00e9 I  Yaound\u00e9 Cameroon"},{"name":"Department of Applied Chemistry, Faculty of Sciences University of Johannesburg  Doornfontein South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dieudonn\u00e9e Mireille","family":"Ntsa","sequence":"additional","affiliation":[{"name":"Department of Animal Biology and Physiology, Faculty of Sciences University of Yaound\u00e9 I  Yaound\u00e9 Cameroon"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chantal Beatrice","family":"Magne Nde","sequence":"additional","affiliation":[{"name":"Centre of Endocrinology and Metabolism Hudson Institute of Medical Research, Monash University  Clayton Victoria Australia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Thomas","family":"Michel","sequence":"additional","affiliation":[{"name":"Universit\u00e9 C\u00f4te d'Azur, CNRS Institut de Chimie de Nice UMR 7272  06108 Nice France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Derek Tantoh","family":"Ndinteh","sequence":"additional","affiliation":[{"name":"Department of Applied Chemistry, Faculty of Sciences University of Johannesburg  Doornfontein South Africa"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Colin","family":"Clyne","sequence":"additional","affiliation":[{"name":"Centre of Endocrinology and Metabolism Hudson Institute of Medical Research, Monash University  Clayton Victoria Australia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1358-8221","authenticated-orcid":false,"given":"Dieudonn\u00e9","family":"Njamen","sequence":"additional","affiliation":[{"name":"Department of Animal Biology and Physiology, Faculty of Sciences University of Yaound\u00e9 I  Yaound\u00e9 Cameroon"},{"name":"Department of Applied Chemistry, Faculty of Sciences University of Johannesburg  Doornfontein South 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