Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages. Issue 5 (1st March 2020)

• Record Type: Journal Article
• Authors: Park, Jun Yeon; Lee, Jae Wook; Lee, Chang-Ho; Lee, Hae-Jeung; Kang, Ki Sung
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 30:Issue 5(2020)
• Publication Date: 2020-03-01
• Subjects: Guggulsterone -- Inflammation -- iNOS -- COX-2 -- RAW264.7; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2020.126962
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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.