Abstract
The methanolic extract of Flemingia macrophylla roots exhibited significant estrogenic activity in the transgenic plant assay system which was comparable to the activity of soybean extract. Utilizing estrogenic activity-guided fractionation, one new compound, fleminigin, together with 23 known compounds were isolated from F. macrophylla roots’ methanolic extract. The structure of the new compound was identified based on intensive spectroscopic analysis and the full spectral data for one of the isolated compounds, flemichin E, was introduced for the first time in the current investigation. The estrogenic and anti-estrogenic activities of the isolated compounds were evaluated revealing that the isolated isoflavonoids may act as partial estrogen agonists, as well as antagonists. Additionally, the anti-inflammatory and the cytotoxic activities of the isolated compounds were studied. These results suggested the potential applications of F. macrophylla extract and its isolated compounds as selective estrogen receptor modulators (SERMs).
Highlights
Plants with estrogenic properties have been widely used as dietary supplements for postmenopausal women in the last few decades [1]
The results showed that compounds 4, 6, 7, and the reference drug, genistein (5), exhibited a significant estrogenic activity (MAC < 5 μM) in the transgenic plant assay system (Table 3)
Compounds 6 and 7 were able to compete in the inhibition of elastase release (IC50 4.32 and 4.33 μg/mL) to the same level demonstrated by the positive control, genistein (5) (IC50 4.25 μg/mL)
Summary
Plants with estrogenic properties have been widely used as dietary supplements for postmenopausal women in the last few decades [1]. Identification of phytoestrogenic natural sources from thousands of terrestrial plants is a challenging task, which represents the bottle neck in developing new dietary supplements and pharmaceutical lead drugs This stern challenge was tackled by several research groups in the past few decades developing in vitro techniques for their detection. In our ongoing research to discover new sources of phytoestrogens, 22 herbal (folk) medicines used in the treatment of fractures, osteoporosis, and related bone diseases were selected for evaluating their estrogenic activity. Recent reports have suggested a close relationship between F. macrophylla estrogen-like activity and its neuroprotective [10] and anti-osteoporotic activities [12] Despite these findings, the effect of F. macrophylla extracts and its purified compounds on estrogen receptors has never been investigated. The anti–inflammatory and cytotoxic activities of the isolated compounds were evaluated
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