Abstract
Polygonum multiflorum Thunb. is a traditional herbal medicine that is rich in polyphenols. The major compound, 2,3,5,4'-tetrahydroxystilbene-2-O-β-d-glucoside (THSG) has many pharmacological activities, such as antioxidative and free radical-scavenging properties, and the abilities to reduce hyperlipidemia, prevent lipid peroxidation, and protect the cardiovascular system. In this study, the anti-osteoarthritis (OA) effects of THSG were explored using in vitro and in vivo models. THSG inhibited nitric oxide (NO) and prostaglandin E₂ (PGE₂) production and inducible NO synthase (iNOS) and cyclooxygenase-2 expressions by lipopolysaccharide-stimulated RAW 264.7 cells. On the other hand, THSG inhibited PGE₂ production and iNOS and matrix metalloproteinase-13 expressions by interleukin-1β-stimulated primary rat chondrocytes. Through a mono-iodoacetate-induced rat OA model assay, THSG reduced paw edema and improved the weight-bearing distribution. Therefore, THSG has anti-inflammatory activity and could be applied as a lead compound for the development as an OA drug.
Keywords:
">d-glucoside; 2,3,5,4′-tetrahydroxystilbene-2-O-β-; Polygonum multiflorum; anti-inflammation; osteoarthritis.
MeSH terms
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Animals
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Anti-Inflammatory Agents / isolation & purification
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Anti-Inflammatory Agents / pharmacology*
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Chondrocytes / drug effects
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Chondrocytes / immunology
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Chondrocytes / pathology
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Cyclooxygenase 2 / genetics
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Cyclooxygenase 2 / metabolism
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Cyclooxygenase 2 Inhibitors / isolation & purification
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Cyclooxygenase 2 Inhibitors / pharmacology*
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Dinoprostone / antagonists & inhibitors
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Dinoprostone / biosynthesis
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Edema / chemically induced
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Edema / drug therapy*
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Edema / enzymology
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Edema / pathology
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Gene Expression Regulation / drug effects
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Glucosides / isolation & purification
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Glucosides / pharmacology*
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Hindlimb
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Iodoacetic Acid
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Lipopolysaccharides / pharmacology
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Male
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Matrix Metalloproteinase 13 / genetics
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Matrix Metalloproteinase 13 / metabolism
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Mice
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Nitric Oxide / antagonists & inhibitors
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Nitric Oxide / biosynthesis
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Nitric Oxide Synthase Type II / antagonists & inhibitors
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Nitric Oxide Synthase Type II / genetics
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Nitric Oxide Synthase Type II / metabolism
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Osteoarthritis / chemically induced
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Osteoarthritis / drug therapy*
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Osteoarthritis / enzymology
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Osteoarthritis / pathology
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Polygonum / chemistry*
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Primary Cell Culture
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RAW 264.7 Cells
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Rats
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Stilbenes / isolation & purification
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Stilbenes / pharmacology*
Substances
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Anti-Inflammatory Agents
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Cyclooxygenase 2 Inhibitors
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Glucosides
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Lipopolysaccharides
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Stilbenes
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2,3,5,4'-tetrahydroxystilbene 2-O-glucopyranoside
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Nitric Oxide
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Nitric Oxide Synthase Type II
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Nos2 protein, mouse
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Cyclooxygenase 2
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Matrix Metalloproteinase 13
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Mmp13 protein, mouse
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Dinoprostone
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Iodoacetic Acid