Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages

被引：4

作者：

Park, Jun Yeon ^{[1
]}

Lee, Jae Wook ^{[2
,3
,4
]}

Lee, Chang-Ho ^{[5
]}

Lee, Hae-Jeung ^{[6
]}

Kang, Ki Sung ^{[7
]}

机构：

[1] Kyonggi Univ, Dept Food Sci & Biotechnol, Suwon 16227, South Korea

[2] Korea Inst Sci & Technol, Nat Prod Res Ctr, Kangnung 25451, South Korea

[3] Korea Inst Sci & Technol, Convergent Res Ctr Dementia, Seoul 02792, South Korea

[4] Korea Univ Sci & Technol, Dept Biol Chem, Daejeon 34113, South Korea

[5] Korea Food Res Inst, Res Grp Funct Food Mat, Wonju 55365, South Korea

[6] Gachon Univ, Dept Food & Nutr, Gyeonggi Do 13120, South Korea

[7] Gachon Univ, Coll Korean Med, Seongnam 13120, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2020年 / 30卷 / 05期

关键词：

Guggulsterone; Inflammation; iNOS; COX-2; RAW264.7; NF-KAPPA-B; X-RECEPTOR; INFLAMMATION; EXTRACT; CELLS; ANTAGONIST; APOPTOSIS; PATHWAYS;

D O I：

10.1016/j.bmcl.2020.126962

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Guggulsterone is a bioactive plant sterol naturally found in migratory plants. It exists in various forms, and its active compounds include the isomers cis-guggulsterone (E-GS) and trans-guggulsterone (Z-GS). In this study, the anti-inflammatory effects of these two isomeric pregnadienedione steroids were investigated against lipopolysaccharide-induced inflammatory reaction in RAW264.7 mouse macrophages. Our results showed that both guggulsterones inhibited the production of NO in macrophages treated with lipopolysaccharide, with IC50 values ranging from 3.0 to 6.7 mu M. E-GS exerted higher efficacy than Z-GS, and its anti-inflammatory effects was mediated through inhibition of iNOS and COX-2 expression.

引用

页数：5

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