Analgesic and anti-inflammatory activities of the 2,8-dihydroxy-1,6-dimethoxyxanthone from Haploclathra paniculata (Mart) Benth (Guttiferae)

J Med Food. 2014 Jun;17(6):686-93. doi: 10.1089/jmf.2013.0122. Epub 2014 Jan 29.

Abstract

In the present study, the pharmacological effects of 2,8-dihydroxy-1,6-dimethoxyxanthone from the bark of Haploclathra paniculata were investigated in mice using in vivo inflammation and nociception models. Acetic acid-induced writhing, paw licking induced by formalin, hot plate, and carrageenan-induced paw edema tests were used to investigate the anti-inflammatory and antinociceptive activities of the xanthone compound. Xanthone, at both doses, inhibited abdominal writhing and the formalin test. At a dose of 20 mg/kg, the time of reaction to the hot plate increased, and significant effects were observed after 30, 60 and 90 min of treatment. At doses of 10 and 20 mg/kg p.o., the 2,8-dihydroxy-1,6-dimethoxyxanthone significantly reduced paw edema at 3 h after the stimulus. The tests also showed no acute toxicity of the xanthone compound in mice. 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging ability was also studied and confirmed the antioxidant activity of the xanthone. To propose the mechanism of action of anti-inflammatory activity of the xanthone, a molecular docking was performed using the isoenzymes cyclooxygenase 1 and 2 and the results indicate that the molecule is capable of inhibiting both the enzymes. Therefore, it can be concluded that 2,8-dihydroxy-1,6-dimethoxyxanthone from H. paniculata demonstrates analgesic, anti-inflammatory, and antioxidant activities.

Keywords: DPPH; analgesic effect; anti-inflammatory activity; edema; inflammation; oxygenated xanthone.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetic Acid
  • Analgesics / pharmacology
  • Analgesics / therapeutic use*
  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use*
  • Antioxidants / pharmacology
  • Antioxidants / therapeutic use
  • Biphenyl Compounds / metabolism
  • Carrageenan
  • Clusiaceae / chemistry*
  • Cyclooxygenase 2 Inhibitors / pharmacology
  • Cyclooxygenase 2 Inhibitors / therapeutic use
  • Edema / chemically induced
  • Edema / drug therapy
  • Hot Temperature
  • Inflammation / chemically induced
  • Inflammation / drug therapy*
  • Male
  • Pain / chemically induced
  • Pain / drug therapy*
  • Pain Measurement
  • Phytotherapy*
  • Picrates / metabolism
  • Plant Bark
  • Plant Extracts / pharmacology
  • Plant Extracts / therapeutic use
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Rats, Wistar
  • Xanthones / pharmacology
  • Xanthones / therapeutic use*

Substances

  • 2,8-dihydroxy-1,6-dimethoxyxanthone
  • Analgesics
  • Anti-Inflammatory Agents
  • Antioxidants
  • Biphenyl Compounds
  • Cyclooxygenase 2 Inhibitors
  • Picrates
  • Plant Extracts
  • Xanthones
  • Carrageenan
  • 1,1-diphenyl-2-picrylhydrazyl
  • Prostaglandin-Endoperoxide Synthases
  • Acetic Acid