Estrogenic effects of Ficus umbellata Vahl. (Moraceae) extracts and their ability to alleviate some menopausal symptoms induced by ovariectomy in Wistar rats

• Published in: Journal of ethnopharmacology 2016-02, Vol.179, p.332-344
• Main Authors: Zingue, Stéphane, Michel, Thomas, Tchatchou, Jules, Chantal Beatrice Magne, Nde, Winter, Evelyn, Monchot, André, Awounfack, Charline Florence, Djiogue, Sefirin, Clyne, Colin, Fernandez, Xavier, Creczynski-Pasa, Tânia Beatriz, Njamen, Dieudonné
• Format: Article
• Language: English
• Subjects: Animals; Cell Survival - drug effects; Cells, Cultured; Chemical Sciences; Coumarins; Epithelium - drug effects; Estrogens - adverse effects; Estrogens - pharmacology; Estrogens - therapeutic use; Female; Ficus - chemistry; Ficus umbellata; Hot Flashes - drug therapy; Hot flushes; Humans; Mammary Glands, Human - drug effects; Menopause - drug effects; Organ Size - drug effects; Ovariectomy - adverse effects; Phytoestrogens; Plant Extracts - adverse effects; Plant Extracts - chemistry; Plant Extracts - pharmacology; Plant Extracts - therapeutic use; Proteins - metabolism; Rats; Rats, Wistar; Receptors, Estrogen - metabolism; Umbelliferones - pharmacology; Uterotrophic effects; Uterus - drug effects; Uterus - metabolism; Vagina - drug effects
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2016.01.004

Ficus umbellata Vahl. (Moraceae) is a medicinal plant used in Cameroon to treat amenorrhea as well as other physiological disorders related to menopause. In order to justify scientifically its traditional use, the estrogen-like properties of the aqueous (AE) and methanol (MeOH) extracts of F. umbellata were investigated. In vitro, the ability of different extracts of F. umbellata to activate estrogen receptors α (ERα) and β (ERβ) in cell-based reporter gene assays using human embryonic kidney (HEK293T) cells transfected with ERs was tested. In vivo, a 3-day uterotrophic assay and the capacity of the extracts to alleviate hot flushes in ovariectomized adult rats were tested. Using a bioassay-guided fractionation the major compound of F. umbellata was isolated and tested in vitro on HEK293T-ERα and ERβ cells. AE and MeOH extracts significantly altered ERα as well as ERβ activities. In vivo, both extracts significantly increase the uterine and vaginal epithelium thickness, and uterine total protein levels in a dose dependent manner. Interestingly, both extracts of F. umbellata at the dose of 100 mg/kg BW significantly decreased the total number, average duration as well as frequency of hot flushes in experimental rats compared to age-matched OVX controls. Finally, 7-methylumbelliferone, a coumarin was characterized as the major compound of F. umbellata; however this compound did not transactivate ERα as well ERβ in vitro. These aforementioned results suggest that F. umbellata extracts as used by the traditional practitioner have estrogen-like effects and may alleviate some menopausal problems such as vaginal dryness and hot flushes. Ficus umbellata extracts exhibited in vitro and in vivo estrogen-like effects. These extracts may contain promising phytoestrogens. [Display omitted]