Anti-inflammatory activity of oleanolic acid by inhibition of secretory phospholipase A2

Kattepura K. Dharmappa, Raju Venkatesh Kumar, Angaswamy Nataraju, Riyaz Mohamed, Holenarasipura V. Shivaprasad, Bannikuppe S. Vishwanath

Research output: Contribution to journalArticlepeer-review

47 Scopus citations

Abstract

Oleanolic acid, a triterpenoid known for its anti-inflammatory properties, is commonly present in several medicinal plants. The present study evaluated the effect of oleanolic acid on sPLA2, a key enzyme in inflammatory reactions. Oleanolic acid inhibited sPLA2 activities of human synovial fluid (HSF), human pleural fluid (HPF) and Vipera russelli (VRV-PL-V) and Naja naja (NN-PL-I) snake venoms in a concentration-dependent manner. The IC50 values of sPLA2 from these sources ranged from 3.08 to 7.78 μM. Increasing calcium (Ca2+) concentrations from 2.5 to 15 mM and substrate concentration up to 180 nM did not affect the level of inhibition. Oleanolic acid enhanced the relative intrinsic fluorescence intensity of sPLA2 (VRV-PL-V). In the presence of oleanolic acid, an apparent shift in the far UV-CD spectrum of sPLA2 was observed. These studies indicate direct interaction with the enzyme and formation of an sPLA2-oleanolic acid complex. The complex formed resulted in irreversible inhibition of sPLA2. Oleanolic acid inhibited indirect hemolytic activity and mouse pawedema induced by sPLA2. Inhibition of in vitro and in vivo sPLA2 activity by oleanolic acid explains the observed anti-inflammatory properties of several oleanolic acid-containing medicinal plants.

Original languageEnglish (US)
Pages (from-to)211-215
Number of pages5
JournalPlanta Medica
Volume75
Issue number3
DOIs
StatePublished - Feb 2009
Externally publishedYes

Keywords

  • Anti-inflammatory
  • Human pleural fluid
  • Human synovial fluid
  • Oleanolic acid
  • Snake venom PLA
  • sPLA

ASJC Scopus subject areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

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