Anthonotha macrophylla P. Beauv (Caesalpiniaceae) aqueous extract exhibits antiestrogenic effects in vitro and in vivo.

Background Phytoestrogens are natural compounds known as natural selective estrogen receptor modulators used as alternatives against estrogen-dependent cancers. This study aims to evaluate the antiestrogenic effects of Anthonotha macrophylla, a plant used to treat cancer in Cameroon. Methods The estrogenic/antiestrogenic activities of A. macrophylla aqueous extract were evaluated in vitro using MCF-7 cell proliferation assay. Moreover, a classical uterotrophic test was carried out to evaluate the antiestrogenic effects of A. macrophylla in rats. Changes in the uterus, vagina, and mammary glands were used as endpoints of estrogenicity. Results Anthonotha macrophylla induced antiestrogenic effects in vitro at all the tested concentrations by inhibiting estradiol-induced MCF-7 cell proliferation (p < 0.001). In vivo, a coadministration of estradiol with A. macrophylla extract led to the decrease of uterine [150 (p < 0.05) and 300 (p < 0.01) mg/kg body weight (BW)] and vaginal [75 (p < 0.01) and 300 (p < 0.05) mg/kg BW] epithelial thickness. In addition, a reduction in the mammary gland acini lumen's diameter was also observed at 75 and 150 mg/kg. Gas chromatography-time-of-flight-mass spectrometry analysis showed that phenolic acid derivatives are present in A. macrophylla extract, which are well known to be endowed with estrogenic/antiestrogenic properties. The LD50 of A. macrophylla was estimated to be less than 2000 mg/kg. Conclusions Anthonotha macrophylla aqueous extract has antiestrogenic properties. This could promote more studies to explore its ability to prevent estrogen-dependent cancers.

Abyssinone V-4' Methyl Ether Isolated from Erythrina droogmansiana (Leguminosae) Inhibits Cell Growth and Mammary Glands Hyperplasia Induced in Swiss Mice by the 7,12-Dimethylbenz(a)anthracene.

There is a long standing interest in the identification of medicinal plants and derived natural products for developing cancer therapeutics. The present study was designed to evaluate the in vitro and in vivo antiproliferative effects of Abyssinone V-4' methyl ether (AVME) on breast tissue of mice. The cytotoxicity of AVME was evaluated using MTT assay in four cancer cell lines (DU145, PC3, HepG2, and MCF-7). Further, a protective effect of AVME was evaluated on 7,12-dimethylbenz(a)anthracene- (DMBA-) induced breast tumor in Swiss mice. Incidence, burden, volume, and histological analysis of mammary tumors were measured. As a result, AVME inhibits DU145, PC3, HepG2, and MCF-7 cells growth. In vivo, no tumor was detected in mice from the normal group as compared to those of DMBA group. Moreover, AVME inhibits the DMBA-induced mammary glands hyperplasia in mice at the dose of 10 mg/kg, evidenced by a decrease of tumor incidence, tumor weight, and volume as well as a protective effect against the lobular alveolar hyperplasia. Taken all together, these results suggest that Abyssinone V-4' methyl ether is endowed with antitumor properties and could be a source of traditional medicine which deserves to be more elucidated and explored in the foreseeable future.

Erythrina lysistemon-derived flavonoids account only in part for the plant's specific effects on rat uterus and vagina.

BACKGROUND: The stem bark ethyl acetate extract of Erythrina lysistemon was found to induce vaginal proliferation in ovariectomized rats orally treated. Alpinumisoflavone (AIF) and abyssinone V-4'-methyl-ether (AME), isolated as its major constituents, were reported to separately provoke uterine growth and/or vaginal proliferation. The present study aimed at evaluating the effects of the mixture of AIF and AME (51 mg/kg [AIF]+153 mg/kg [AME]) following their relative abundance in the extract, in order to compare these effects to those of E. lysistemon. METHODS: The study was performed in ovariectomized rats treated intraperitoneally for 3 days. Estradiol valerate (E2 V) and AME were used for positive controls. Morphological and histological changes of animals' uterus and vagina were used as the hallmark of estrogenicity. RESULTS: E. lysistemon extract induced estrogen-like effects only on the uterus and significantly increased uterine wet weight (p<0.01) and uterine epithelial height (p<0.01). These results suggest a tissue-selective action of E. lysistemon extract depending on the route of administration. The mixture of AIF and AME induced E. lysistemon-like effects only at a dose of 1 mg/kg BW/d (0.25 mg/kg+0.75 mg/kg), although these effects were lower in magnitude (p<0.05) compared to those induced by E. lysistemon extract. CONCLUSIONS: Effects induced by the mixture of AIF and AME are analogous to those of E. lysistemon, but the low magnitude of these effects suggests that there are minor metabolites that interact with AIF and AME to provoke the specific effects of E. lysistemon.