Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages.,Bioorganic & Medicinal Chemistry Letters

当前位置： X-MOL 学术 › Bioorg. Med. Chem. Lett. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-01-08 , DOI: 10.1016/j.bmcl.2020.126962
Jun Yeon Park ₁ , Jae Wook Lee ₂ , Chang-Ho Lee ₃ , Hae-Jeung Lee ₄ , Ki Sung Kang ₅

Affiliation

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 μM. E-GS exerted higher efficacy than Z-GS, and its anti-inflammatory effects was mediated through inhibition of iNOS and COX-2 expression.

中文翻译：

顺式古古甾酮的合成及其对脂多糖诱导巨噬细胞中一氧化氮生成的抑制作用。

Guggulsterone是一种天然存在于移栖植物中的生物活性植物固醇。它以各种形式存在，其活性化合物包括异构体顺式古古甾酮（E-GS）和反式古古甾酮（Z-GS）。在这项研究中，这两种异构的孕二烯酮类固醇的抗炎作用针对RAW264.7小鼠巨噬细胞中脂多糖诱导的炎症反应进行了研究。我们的研究结果表明，两种古古甾酮均可以抑制经脂多糖处理的巨噬细胞中NO的产生，IC50值范围为3.0至6.7μM。E-GS具有比Z-GS更高的功效，并且其抗炎作用是通过抑制iNOS和COX-2的表达来介导的。

更新日期：2020-01-09

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11