Abstract
Broussonetia papyrifera leaves (BPL) as a traditional Chinese medicine are also used in livestock feed for stimulating reproduction, adipose tissue and muscle development; however, the mechanism of their action is still unknown. Through estrogen biosynthesis-guided fractionation in human ovarian granulosa-like KGN cells, five new phenolic glycosides, broussoside A–E(1–5), along with fifteen known dietary phenolic compounds, were isolated from the n-butanol extract of BPL, and their structures were elucidated on the basis of NMR spectra analysis and chemical evidence. New compounds 3, 4, 5 and the known compounds 9 and 10 were found to potently inhibit estrogen biosynthesis in KGN cells. In addition, compounds 9, 17, 18, and 20 showed strong antioxidant activity against ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) and DPPH (1, 1′-diphenyl -2-picryl-hydrazyl radical) assays. These findings suggest that BPL may improve meat quality through the regulation of estrogen biosynthesis. Furthermore, they may be useful for the discovery of potential aromatase modulators from natural products. Finally, they could be considered as a new source for natural antioxidants.
Highlights
Estrogen plays a vital role in the regulation of many biological processes, which is synthesized by aromatase in the body, the only enzyme in vertebrate that can catalyze the formation of estrogens by using androgens as substrates [1]
Letrozole is a potent non-steroidal aromatase inhibitor registered for clinical use, and we used it here as a positive control for an estrogen biosynthesis antagonist [23]
To investigate the effect of Broussonetia papyrifera leaves (BPL) on oxidation, we evaluated the antioxidant activity of the BPL extracts
Summary
Estrogen plays a vital role in the regulation of many biological processes, which is synthesized by aromatase in the body, the only enzyme in vertebrate that can catalyze the formation of estrogens by using androgens as substrates [1]. Synthetic aromatase inhibitors have been developed for the treatment of breast cancer; their clinical uses are severely limited by their side effects such as increased risk for osteoporosis and cardiovascular disease [2]. Natural products are considered a good source of aromatase inhibitors; only about 300 natural products have been evaluated for their effects on aromatase [3]. Hormones such as estrogen are widely used to stimulate these processes, but they often lead to food safety issues caused by the residual hormones [5]. Finding new natural aromatase modulators and feeding sources is a new option for estrogen-related diseases and livestock culturing
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