Erythrina lysistemon is an African medicinal plant used as a palliative for problems in women. The crude extract of this plant was shown to exhibit estrogenic effects on the female rat reproductive tract and on cell cuture. Using classic chromatographic methods, two compounds have been isolated as major constituents of this extract: alpinumisoflavone (1) and abyssinone V-4'-methyl ether (2). To determine whether both compounds are actives principles accounting for E. lysistemon effects, we applied the classic 3-day uterotrophic assay. We also carried out a ligand binding assay to determine whether the observed effects are estrogen receptor (ER) mediated. This study showed that whereas compound 1 displayed a fourfold preference for ERα, compound 2 bound ERα and ERβ with a same affinity. The in vivo study showed that compound 1 increased the uterine wet weight by 182.23% (p < 0.01) and 71.79% (p < 0.05) at doses of 0.1 and 1 mg/kg BW/day respectively. The uterine epithelium thickened dose-dependently. Vaginal epithelial height also increased by 369.97 and 226.76% respectively (p < 0.01). Compound 2 acted only on the vagina and increased vaginal epithelial height by 244.56% (p < 0.01) at 1 mg/kg BW/day. These results suggest that compounds 1 and 2 are endowed with estrogenic properties accounting, at least in part, for E. lysistemon effects.

These compounds appear to be promising to overcome breast cancer treatment failure. However, despite the interesting activities, additional preclinical investigations are needed in further breast cancer cell/tumor models in vitro and in vivo.

In developing countries, around 80% of the population still resorts on traditional medicine for their primary health care. Erythrina poeppigiana (Walp.) O.F. Cook, one of these medicinal plants, was found to be particularly rich in isoflavonoids which exhibited, individually, significant estrogenic activity in vitro. The possible combined effects of these bioactive isoflavones, as they are naturally found in the crude extracts of E. poeppigiana, prompted us to assess their in vivo estrogenicity. We first tested the ability of the extracts to transactivate estrogen receptor alpha (ERα) in vitro using U2OS human osteosarcoma cells. We next investigated their effects in vivo in an uterotrophic assay, using ovariectomized rats treated with the extracts at the doses of 50, 100, 200, and 400 mg/kg BW/d orally for 3 days. Finally, we assessed their ability to relieve hot flushes, using data loggers. At the end of treatments, animals were sacrificed, and organs (mammary glands, vagina, and uteri) were collected for histo-morphometric analyses. The methanol extract significantly and dose-dependently transactivated ERα at all tested doses. All extracts induced significant increases of vaginal and uterine epithelial heights. Only the dichloromethane extract could significantly relieve hot flushes as estradiol. These results indicate that E. poeppigiana extracts have estrogen-like effects in vivo, suggesting that its active principles act in synergy when they are taken in combination in the crude extract. These findings, therefore, support the traditional use of E. poeppigiana to alleviate some menopausal problems; our previous phytochemical investigations contribute to the standardization of this phytomedicine.

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