In vivo and in vitro anti-inflammatory activity of neorogioltriol, a new diterpene extracted from the red algae Laurencia glandulifera

Mar Drugs. 2011;9(7):1293-1306. doi: 10.3390/md9071293. Epub 2011 Jul 22.

Abstract

Neorogioltriol is a tricyclic brominated diterpenoid isolated from the organic extract of the red algae Laurencia glandulifera. In the present study, the anti-inflammatory effects of neorogioltriol were evaluated both in vivo using carrageenan-induced paw edema and in vitro on lipopolysaccharide (LPS)-treated Raw264.7 macrophages. The in vivo study demonstrated that the administration of 1 mg/kg of neorogioltriol resulted in the significant reduction of carregeenan-induced rat edema. In vitro, our results show that neorogioltriol treatment decreased the luciferase activity in LPS-stimulated Raw264.7 cells, stably transfected with the NF-κB-dependent luciferase reporter. This effect on NF-κB activation is not mediated through MAPK pathways. The inhibition of NF-κB activity correlates with decreased levels of LPS-induced tumor necrosis factor-alpha (TNFα) present in neorogioltriol treated supernatant cell culture. Further analyses indicated that this product also significantly inhibited the release of nitric oxide and the expression of cyclooxygenase-2 (COX-2) in LPS-stimulated Raw264.7 cells. These latter effects could only be observed for neorogioltriol concentrations below 62.5 μM. To our knowledge, this is the first report describing a molecule derived from Laurencia glandulifera with anti-inflammatory activity both in vivo and in vitro. The effect demonstrated in vitro may be explained by the inhibition of the LPS-induced NF-κB activation and TNFα production. NO release and COX-2 expression may reinforce this effect.

Keywords: COX-2; Laurencia; NF-κB; NO; TNFα; anti-inflammatory; carrageenan; neorogioltriol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / isolation & purification
  • Anti-Inflammatory Agents / metabolism
  • Anti-Inflammatory Agents / pharmacology*
  • Anti-Inflammatory Agents / toxicity
  • Anti-Inflammatory Agents, Non-Steroidal / isolation & purification
  • Anti-Inflammatory Agents, Non-Steroidal / metabolism
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Anti-Inflammatory Agents, Non-Steroidal / toxicity
  • Arthritis / drug therapy
  • Aspirin / pharmacology
  • Cell Survival / drug effects
  • Control Groups
  • Dexamethasone / pharmacology
  • Disease Models, Animal
  • Diterpenes / isolation & purification
  • Diterpenes / metabolism
  • Diterpenes / pharmacology*
  • Diterpenes / toxicity
  • Dose-Response Relationship, Drug
  • Edema / chemically induced
  • Edema / drug therapy*
  • Inflammation Mediators / antagonists & inhibitors
  • Inflammation Mediators / physiology
  • Laurencia / chemistry*
  • Lipopolysaccharides / metabolism
  • Lipopolysaccharides / physiology
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Mice
  • Phytotherapy
  • Plant Extracts / isolation & purification
  • Plant Extracts / metabolism
  • Plant Extracts / pharmacology*
  • Plant Extracts / toxicity
  • Rats
  • Time Factors

Substances

  • Anti-Inflammatory Agents
  • Anti-Inflammatory Agents, Non-Steroidal
  • Diterpenes
  • Inflammation Mediators
  • Lipopolysaccharides
  • Plant Extracts
  • neorogioltriol
  • Dexamethasone
  • Aspirin