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

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

  • Bioorg Med Chem Lett. 2013 Nov 1;23(21):5904-8. doi: 10.1016/j.bmcl.2013.08.085.
Tian-Xing Shi 1 Shu Wang Ke-Wu Zeng Peng-Fei Tu Yong Jiang
Affiliations

Affiliation

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

Keywords

Absolute configuration; Glycosides; NO inhibition; Polygala tenuifolia.

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