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Arch Biochem Biophys ; 498(2): 105-10, 2010 Jun 15.
Article in English | MEDLINE | ID: mdl-20417174

ABSTRACT

In inflammation, nitric oxide (NO) acts as a pro-inflammatory mediator, which is synthesized by inducible nitric oxide synthase (iNOS) in response to pro-inflammatory agents such as lipopolysaccharide (LPS). Quercetin (Qt) has anti-inflammatory properties through its ability to inhibits nitric oxide production and iNOS expression in different cellular types. In the present study, we evaluated the effect of a semi-synthetic acetyl (quercetin-3,5,7,3'-tetraacetyl: TAQt) Qt derivative and two natural sulphated (quercetin-3-acetyl-7,3',4'-trisulphate: ATS and quercetin-3,7,3',4'-tetrasulphate: QTS) Qt derivatives on the LPS-induced NO production and iNOS expression in J774A.1 cells. Our results demonstrate that only TAQt inhibited the NO production by decreasing the iNOS mRNA and protein levels. In addition, we showed that TAQt blocked the LPS-induced nuclear NF-kappaB translocation by inhibiting the IkappaB-alpha degradation. Hence, as TAQt inhibited the LPS-induced iNOS expression and NO production, it could therefore be considered as a potential therapeutic agent for the treatment of inflammatory diseases related with the NO system.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Gene Expression Regulation, Enzymologic/drug effects , Lipopolysaccharides/pharmacology , Nitric Oxide Synthase Type II/biosynthesis , Quercetin/pharmacology , Animals , Antioxidants/pharmacology , Cell Line , I-kappa B Proteins/metabolism , Inflammation/drug therapy , Inflammation/metabolism , Inflammation Mediators/metabolism , Macrophages , Mice , NF-KappaB Inhibitor alpha , NF-kappa B/metabolism , Nitric Oxide/biosynthesis , Quercetin/analogs & derivatives , RNA, Messenger/biosynthesis
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