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.
Keywords: Anthonotha macrophylla; MCF-7 cell proliferation assay; antiestrogenic effects; estrogen-dependent cancer.