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Planta Med 2009; 75(3): 211-215
DOI: 10.1055/s-0028-1088374
Pharmacology
Original Paper
© Georg Thieme Verlag KG Stuttgart · New York

Anti-Inflammatory Activity of Oleanolic Acid by Inhibition of Secretory Phospholipase A2

Kattepura K. Dharmappa1 , Raju Venkatesh Kumar1 , Angaswamy Nataraju1 , 2 , Riyaz Mohamed1 , Holenarasipura V. Shivaprasad1 , Bannikuppe S. Vishwanath1
  • 1Department of Studies in Biochemistry, University of Mysore, Mysore, India
  • 2Department of Surgery, Washington University School of Medicine, St. Louis, Missouri, USA
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Publikationsverlauf

Received: April 16, 2008 Revised: October 16, 2008

Accepted: October 23, 2008

Publikationsdatum:
11. Dezember 2008 (online)

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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 paw edema 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.

Abbreviations

COX.1/2:cyclooxygenase-1/2

HPF:human pleural fluid

HSF:human synovial fluid

LOX:lipoxygenase

NN-PL-I:Naja naja phospholipase-I

PAF:platelet activation factor

p-BPB:para-bromophenacyl bromide

sPLA2:secretory phospholipase A2

UV-CD:ultraviolet circular dichroism

VRV-PL-V:Vipera russelli venom phospholipase-V

Key words

oleanolic acid - human synovial fluid - human pleural fluid - anti-inflammatory - sPLA2 - snake venom PLA2

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Prof. B. S. Vishwanath

Department of Studies in Biochemistry

University of Mysore

Manasagangotri

Mysore 570 006

India

Telefon: +91-821-241-9621

eMail: vishmy@yahoo.co.uk