State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, People's Republic of China.
Bioorg Med Chem Lett. 2013 Nov 1;23(21):5904-8. doi: 10.1016/j.bmcl.2013.08.085. Epub 2013 Aug 30.
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.
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)。