Bioactivity-guided Isolation of Antiosteoporotic Compounds from Ligustrum lucidum
Bioactivity-guided Isolation of Antiosteoporotic Compounds from Ligustrum lucidum
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生物活性引导下从女贞子中分离抗骨质疏松化合物
DOI：
10.1002/ptr.4820
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发表时间：
2013-07-01
影响因子：
7.2
通讯作者：
Wang, Fei
中科院分区：
文献类型：
--
作者：
Chen, Qianfeng;Yang, Lijuan;Wang, Fei
女贞子（FLL）的果实在我国长期用于治疗骨质疏松症，但对FLL中的抗骨质疏松化合物的了解仍然很少。本研究利用成骨样细胞UMR-106，以碱性磷酸酶（ALP）活性为导向，从FLL中分离成骨成分。分离鉴定了8个化合物，分别为酪醇（1）、酪氨酰乙酸酯（2）、羟基酪醇（3）、红景天苷（4）、油苷二甲酯（5）、油苷-7-乙基-11-甲酯（6）、nuzhenide（7）和G13（8）。进一步的研究表明，化合物3、4、7和8在UMR-106细胞中增加ALP活性。化合物5、6和7促进UMR-106细胞的增殖。FLL的水提取物激活ER/-介导的基因转录，而分离的化合物无活性。所有八种分离的化合物也表现出抗氧化活性，其中化合物1、2和3最有效。这些结果表明，FLL的抗肿瘤作用来自不同的化合物，以及不同的机制，如ER依赖性或非依赖性途径和抗氧化作用。红景天苷（4）和nuzhenide（7）作为预防和治疗骨质疏松症的新药物工具值得进一步研究。版权所有（c）2012约翰威利父子有限公司
The fruits of Ligustrum lucidum (FLL) has long been used for the treatment of osteoporosis in China, but the antiosteoporotic compounds in FLL are still poorly understood. In this study, the alkaline phosphatase (ALP) activity-guided isolation of osteogenic components from FLL was carried out by using osteoblast-like UMR-106 cells. Eight compounds, namely tyrosol (1), tyrosyl acetate (2), hydroxytyrosol (3), salidroside (4), oleoside dimethyl ester (5), oleoside-7-ethyl-11-methyl ester (6), nuzhenide (7), and G13 (8), were isolated and identified. Further study showed that compounds 3, 4, 7, and 8 increased ALP activity in UMR-106 cells. Compounds 5, 6, and 7 promoted the proliferation of UMR-106 cells. The aqueous extract of FLL-activated ER/-mediated gene transcription, whereas the isolated compounds were inactive. All eight isolated compounds also exhibited antioxidative activity, with compounds 1, 2, and 3 being the most potent. These results indicate that the antiosteoporotic effect of FLL is derived from different compounds together with different mechanisms such as ER-dependent or independent pathways and antioxidative effects. Salidroside (4) and nuzhenide (7) warrant further investigation as new pharmaceutical tools for the prevention and treatment of osteoporosis. Copyright (c) 2012 John Wiley & Sons, Ltd.