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从远志地上部分分离得到的抑制成分对 LPS 诱导的 BV2 小胶质细胞中 NO 产生的抑制作用。

Inhibitory constituents from the aerial parts of Polygala tenuifolia on LPS-induced NO production in BV2 microglia cells.

机构信息

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, People's Republic of China.

出版信息

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5904-8. doi: 10.1016/j.bmcl.2013.08.085. Epub 2013 Aug 30.

Abstract

Five new phenolic glycosides, tenuisides A-E (1-5), and a new megastigmane glycoside, tenuiside F (6), along with seventeen known compounds (7-23) were isolated from the aerial parts of Polygala tenuifolia Willd. Their structures were established by detailed analysis of NMR and HRESIMS spectroscopic data, and the absolute configurations of compounds 5 and 6 were determined by CD spectra and in-NMR-tube Mosher's method. The inhibitory effects of these compounds were evaluated on NO production in LPS-activated BV-2 microglia cells. Compound 17 showed the strongest activity, with an IC50 value of 7.4μM, while compounds 1, 8, 14, and 18 showed the moderate activities, with IC50 values of 16.2-38.5μM. And their primary structure-activity relationships (SARs) of NO inhibitory effects were also briefly discussed.

摘要

从远志属植物远志的地上部分分离得到五个新的酚糖苷化合物,即纤细糖苷 A-E(1-5)和一个新的巨型香叶烷糖苷,即纤细糖苷 F(6),以及十七个已知化合物(7-23)。通过 NMR 和 HRESIMS 光谱数据的详细分析确定了它们的结构,并且通过 CD 光谱和在-NMR 管中 Mosher 的方法确定了化合物 5 和 6 的绝对构型。评估了这些化合物对 LPS 激活的 BV-2 小胶质细胞中 NO 产生的抑制作用。化合物 17 表现出最强的活性,IC50 值为 7.4μM,而化合物 1、8、14 和 18 表现出中等活性,IC50 值为 16.2-38.5μM。并且还简要讨论了它们对 NO 抑制作用的构效关系(SAR)。

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