Pseudoguaianolides isolated from Inula britannica var. chinenis as inhibitory constituents against inducible nitric oxide synthase

被引：41

作者：

Lee, HT

Yang, SW

Kim, KH

Seo, EK

Mar, W ^{[1
]}

机构：

[1] Seoul Natl Univ, Coll Pharm, Seoul 110460, South Korea

[2] Seoul Natl Univ, Inst Nat Prod Res, Seoul 110460, South Korea

[3] Ewha Womans Univ, Coll Pharm, Nat Prod Chem Lab, Seoul 120750, South Korea

[4] Kangwon Natl Univ, Coll Pharm, Chunchon 200701, South Korea

来源：

ARCHIVES OF PHARMACAL RESEARCH | 2002年 / 25卷 / 02期

关键词：

Inula britannica var. chinensis; bigelovin; 2,3-dihydroaromaticin; ergolide; iNOS inhibitor;

D O I：

10.1007/BF02976555

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Three pseudogualanolide type sesquiterpenes, bigelovin (1), 2,3-dihydroaromaticin (2), and ergolide (3) were isolated as inhibitory constituents against inducible nitric oxide synthase (NOS) from the flowers of Inula britannica var. chinensis. Bigelovin (1) exhibited a highly potent inhibitory activity on lipopolysaccharide (LPS)-induced iNOS in murine macrophage RAW 264.7 cells with an IC50 value of 0.46 mM, which is about 8 times more potent than the known selective inhibitor of NOS, L-N-6-(1-iminoethyl)lysine (IC50 3.49 muM). 2,3-Dihydroaromaticin (2) and ergolide (3) also exhibited potent inhibitory activities on LPS-induced NOS with IC50 values of 1.05 and 0.69 muM, respectively.

引用

收藏

页码：151 / 153

页数：3

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