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Synthesis and Inhibitory Effect of Cis-Guggulsterone on Lipopolysaccharide-Induced Production of Nitric Oxide in Macrophages

Jun Yeon Park, Jae Wook Lee, Chang-Ho Lee, Hae-Jeung Lee, Ki Sung Kang

Bioorg Med Chem Lett. 2020 Mar 1;30(5):126962.

PMID: 31980338

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP39025235-A Guggulsterone Z Guggulsterone Z 39025-23-5 Price
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