Isolation and characterization of new phenolic compounds with estrogen biosynthesis-inhibiting and antioxidation activities from Broussonetia papyrifera leaves.

Isolation and characterization of new phenolic compounds with estrogen biosynthesis-inhibiting and antioxidation activities from Broussonetia papyrifera leaves.
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DOI:
10.1371/journal.pone.0094198
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发表时间:
2014
期刊:
影响因子:
3.7
通讯作者:
Wang M
Wang M
中科院分区:
综合性期刊3区
文献类型:
--
作者:
Yang C;Li F;Du B;Chen B;Wang F;Wang M

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纸莎草叶(BPL)作为一种传统中药,也被用于牲畜饲料中,以刺激繁殖、脂肪组织和肌肉发育;然而,其作用机制尚不清楚。通过雌激素生物合成引导分离人卵巢颗粒样KGN细胞,从BPL正丁醇提取物中分离到5个新的酚类苷,brooussoside A-E(1-5),以及15个已知的膳食酚类化合物,并根据NMR谱分析和化学证据对其结构进行了鉴定。发现新化合物3、4、5和已知化合物9、10能有效抑制KGN细胞雌激素的生物合成。此外,化合物9、17、18和20对ABTS(2,2′-氮基-双(3-乙基苯并噻唑-6-磺酸)二铵盐)和DPPH(1,1′-二苯基-2-吡啶-肼基自由基)具有较强的抗氧化活性。这些结果表明,BPL可能通过调节雌激素的生物合成来改善肉质。此外,它们可能有助于从天然产物中发现潜在的芳香化酶调节剂。最后,它们可以被认为是天然抗氧化剂的新来源。
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.
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