Triterpenes from the Fungus Poria cocos and Their Inhibitory Activity on Nitric Oxide Production in Mouse Macrophages via Blockade of Activating Protein-1 Pathway

被引:57
作者
Cai, Tian-Ge [2 ]
Cai, Yu [1 ]
机构
[1] Jinan Univ, Sch Pharm, Guangzhou 510632, Guangdong, Peoples R China
[2] Liaoning Univ, Sch Life Sci, Shenyang 110036, Peoples R China
关键词
Poria cocos; Tumulosic acid; Pachymic acid; Structure?activity relationship (SAR); Inhibitors;
D O I
10.1002/cbdv.201100013
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Two new triterpenes, 29-hydroxydehydrotumulosic acid (1) and 29-hydroxydehydropachymic acid (2), together with six known compounds, dehydropachymic acid (3), dehydrotumulosic acid (4), 29-hydroxypolyporenic acid C (5), polyporenic acid C (6), tumulosic acid (7), and pachymic acid (8), were isolated from the dried sclerotia of Poria cocos. In the in vitro bioassays, these isolated compounds reduced, in a dose-dependent manner, nitric oxide (NO) production from lipopolysaccharide (LPS)-induced RAW 264.7 cells, with compounds 5 and 6, the IC50 values of which were 16.8 +/- 2.7 and 18.2 +/- 3.3 mu M, respectively, exhibiting the greatest inhibition activity. Further Western blot analysis conducted on cells pre-treated with compounds 5 and 6, and luciferase assays on activator protein 1-dependent gene expression revealed that the inhibited NO release was attributed to the reduced expression of iNOs (=inducible NO synthase) enzymes, which might be regulated via the blockade of activator protein-1 signaling pathway.
引用
收藏
页码:2135 / 2143
页数:9
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