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Inhibitory effects of 2,3,5,4'-tetrahydroxystilbene-2-O--d-glucoside on experimental inflammation and cyclooxygenase 2 activity

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The inhibitory effects of 2,3,5,4'-tetrahydroxystilbene-2-O--d-glucoside (THSG), extracted from the roots of Polygonum multiflorum Thunb, on inflammatory activity in animal models and cyclooxygenase-2 (COX-2) activity in lipopolysaccharide (LPS)-induced mouse RAW264.7 macrophage cells were investigated. The carrageenin (CGN)-induced rat paw oedema model and dimethylbenzene-induced mouse ear oedema model were prepared; MTT assay, semi-quantitative RT-PCR, Western blot and ELISA were adopted. THSG 2.3, 4.6 and 9.2 mg kg- 1 by oral administration inhibited mouse ear oedema and the percentage of inhibition of THSG 9.2 mg kg- 1 is 87%. THSG 3.2, 6.4 and 12.8 mg kg- 1 by oral administration dose-dependently inhibited rat paw oedema and the percentage of inhibition of THSG 12.8 mg kg- 1 is 56% at 6 h. Indomethacin 13 and 9 mg kg- 1 showed 90% and 57% inhibition in the same animal models, respectively. LPS 1 g ml- 1 significantly up-regulated prostaglandin E2 (PGE2) production (inducing COX-2 activity) by 35% (exogenous arachidonic acid, AA), which was dose-dependently decreased by THSG 1, 10, and 100 mol L- 1 and the percentage of inhibition of THSG 10 mol L- 1 was 40%. NS-398 10 mol L- 1 decreased PGE2 production by 42%. THSG 1, 10, 100 mol L- 1 was shown to markedly inhibit the LPS-induced COX-2 protein and mRNA expression in RAW264.7 cells (P < 0.05) but had no effect on COX-1 protein and mRNA (P>0.05). In summary, the data showed that THSG possessed an anti-inflammatory effect, which was perhaps related to the inhibition of COX-2 enzyme activity and expression in RAW264.7 macrophage cells.
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Keywords: 2,3,5,4'-Tetrahydroxystilbene-2-O--d-glucoside; Cyclooxygenase-2; Inflammation; Lipopolysaccharide; Polygonum multiflorum Thunb; Prostaglandin E2

Document Type: Research Article

Affiliations: Department of Pharmacology, Tongji Medical College of Huazhong University of Science and Technology, Wuhan, China

Publication date: January 1, 2007

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