Evaluation of Cissus Quadrangularis Extracts as an Inhibitor of COX, 5-LOX, and Proinflammatory Mediators

J Ethnopharmacol. 2012 Jun 14;141(3):989-96. doi: 10.1016/j.jep.2012.03.044. Epub 2012 Mar 30.


Ethnopharmacological relevance: Cissus quadrangularis is an ancient medicinal plant. It is an active ingredient of one Ayurvedic formula called "Laksha Gogglu". Its stem is used in food preparation in India. Traditionally it is used to treat various diseases like asthma, indigestion, ear diseases, irregular menstruation, skin diseases, piles, fractured bones, etc.

Aim of the study: This study aimed to evaluate the ability of the plant extracts to inhibit cycloxygenase (COX-1), cycloxygenase (COX-2), and 5-lipoxygenase (5-LOX) enzyme activity. Western blot analysis was also carried out in the quest to determine the effect of active acetone fraction of Cissus quadrangularis (AFCQ) on proinflammatory mediators as acetone extract is found to be the most effective in this study.

Materials and methods: The differential extract of the stem were tested for enzyme inhibition of COX and 5-LOX using spectroscopic and polarigraphic method. Effective acetone extract was partially purified by silica column, one of the active fraction showed dual inhibition against COX and 5-LOX. Western blotting shows downregulation of proinflammatory mediators as well as upregulation of phase-II enzymes.

Results: AFCQ extract showed COX and 5-LOX inhibition with IC(50) values of 7 μg/ml, 0.4 μg/ml, and 20 μg/ml for COX-1, COX-2 and 5-LOX respectively. It also showed anti-inflammatory activity on RAW 264.7 cell line with IC(50) value 65 μg/ml. In addition to this it is showing inhibition of proinflammatory mediators like iNOS and TNFα, along with translocation of Nrf-2 and upregulation of HO-1.

Conclusion: AFCQ is a COX and 5-LOX inhibitor isolated from the stems of Cissus quadrangularis. It is also effectively downregulate the iNOS, TNFα, and upregulation of HO-1.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Arachidonate 5-Lipoxygenase / metabolism
  • Cell Line
  • Cell Proliferation / drug effects
  • Cissus*
  • Cyclooxygenase 1 / metabolism
  • Cyclooxygenase 2 / metabolism
  • Cyclooxygenase Inhibitors / pharmacology*
  • Heme Oxygenase-1 / metabolism
  • Lipoxygenase Inhibitors / pharmacology*
  • Membrane Proteins / metabolism
  • Mice
  • NF-E2-Related Factor 2 / metabolism
  • Plant Extracts / pharmacology*


  • Anti-Inflammatory Agents
  • Cyclooxygenase Inhibitors
  • Lipoxygenase Inhibitors
  • Membrane Proteins
  • NF-E2-Related Factor 2
  • Nfe2l2 protein, mouse
  • Plant Extracts
  • Arachidonate 5-Lipoxygenase
  • Heme Oxygenase-1
  • Hmox1 protein, mouse
  • Cyclooxygenase 1
  • Cyclooxygenase 2