Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages.
Bioorg Med Chem Lett
; 30(5): 126962, 2020 03 01.
Article
em En
| MEDLINE
| ID: mdl-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.
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Base de dados:
MEDLINE
Assunto principal:
Pregnenodionas
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Inibidores de Ciclo-Oxigenase 2
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Macrófagos
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Anti-Inflamatórios
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Óxido Nítrico
Limite:
Animals
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article