Rationalization of the traditional use of Antidesma ghaesembilla to treat hormone related disorders

Antidesma ghaesembilla, a tropical Asian plant also known as black currant tree, is widely used as medicine to treat headaches, to stimulate menstrual flow and breast milk production but also as purgative. Antibacterial activity, antioxidant capacity, sedative and anxiolytic potentials of the methanolic extract are already described in literature. Part of the described activities might be attributed to interactions with estrogenic receptors. Thus, the aim of this study was to investigate crude extracts of A. ghaesembilla for estrogenic effects and to identify potential active principle(s).

Experimentally, extracts and single constituents were tested using estrogen receptor subtype specific transactivation assays in human bone-derived U2OS cells. Cytotoxicity was measured by using MTT assay in U2OS cells. Both DCM and MeOH bark extracts exhibited appreciable estrogenic but also subtype specific anti-estrogenic effects. Three compounds, a novel aristolochic acid derivative, 6β-hydroxy-stigmast-4-en-3-one, and asperphenamate were isolated from the DCM extract. Asperphenamate, showed a high, dose-dependent estrogenic activity comparable to the positive control 17β-estradiol. Asperphenamate displays moderate cytotoxic activity against several cancer cell lines but to our knowledge the estrogenic activity is so far unknown. The aristolochic acid derivative showed a weak subtype specific agonistic effect. No estrogenic activity was observed for 6β-hydroxy-stigmast-4-en-3-one. Five single compounds could be isolated from the methanolic extract, but no significant estrogenic effects were detected for those compounds.

This study on estrogenic properties of Antidesma ghaesembilla extracts and their active constituents should contribute to a better, science based understanding of traditionally known medicinal uses of plants.