In Vitro and In Vivo Anti-Osteoarthritis Effects of 2,3,5,4'-Tetrahydroxystilbene-2-O-β-d-Glucoside from Polygonum Multiflorum

Molecules. 2018 Mar 3;23(3):571. doi: 10.3390/molecules23030571.

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

  • Animals
  • Anti-Inflammatory Agents / isolation & purification
  • Anti-Inflammatory Agents / pharmacology*
  • Chondrocytes / drug effects
  • Chondrocytes / immunology
  • Chondrocytes / pathology
  • Cyclooxygenase 2 / genetics
  • Cyclooxygenase 2 / metabolism
  • Cyclooxygenase 2 Inhibitors / isolation & purification
  • Cyclooxygenase 2 Inhibitors / pharmacology*
  • Dinoprostone / antagonists & inhibitors
  • Dinoprostone / biosynthesis
  • Edema / chemically induced
  • Edema / drug therapy*
  • Edema / enzymology
  • Edema / pathology
  • Gene Expression Regulation / drug effects
  • Glucosides / isolation & purification
  • Glucosides / pharmacology*
  • Hindlimb
  • Iodoacetic Acid
  • Lipopolysaccharides / pharmacology
  • Male
  • Matrix Metalloproteinase 13 / genetics
  • Matrix Metalloproteinase 13 / metabolism
  • Mice
  • Nitric Oxide / antagonists & inhibitors
  • Nitric Oxide / biosynthesis
  • Nitric Oxide Synthase Type II / antagonists & inhibitors
  • Nitric Oxide Synthase Type II / genetics
  • Nitric Oxide Synthase Type II / metabolism
  • Osteoarthritis / chemically induced
  • Osteoarthritis / drug therapy*
  • Osteoarthritis / enzymology
  • Osteoarthritis / pathology
  • Polygonum / chemistry*
  • Primary Cell Culture
  • RAW 264.7 Cells
  • Rats
  • Stilbenes / isolation & purification
  • Stilbenes / pharmacology*

Substances

  • Anti-Inflammatory Agents
  • Cyclooxygenase 2 Inhibitors
  • Glucosides
  • Lipopolysaccharides
  • Stilbenes
  • 2,3,5,4'-tetrahydroxystilbene 2-O-glucopyranoside
  • Nitric Oxide
  • Nitric Oxide Synthase Type II
  • Nos2 protein, mouse
  • Cyclooxygenase 2
  • Matrix Metalloproteinase 13
  • Mmp13 protein, mouse
  • Dinoprostone
  • Iodoacetic Acid