Identification of a novel and potent inhibitor of phospholipase A2 in a medicinal plant: crystal structure at 1.93 Å and surface plasmon resonance analysis of phospholipase A2 complexed with berberine

Chandra, D. Naveen ; Prasanth, G. K. ; Singh, Nagendra ; Kumar, Sanjit ; Jithesh, O. ; Sadasivan, C. ; Sharma, Sujatha ; Singh, Tej P. ; Haridas, M. (2011) Identification of a novel and potent inhibitor of phospholipase A2 in a medicinal plant: crystal structure at 1.93 Å and surface plasmon resonance analysis of phospholipase A2 complexed with berberine Biochimica et Biophysica Acta (BBA) - Proteins & Proteomics, 1814 (5). pp. 657-663. ISSN 1570-9639

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Official URL: http://linkinghub.elsevier.com/retrieve/pii/S15709...

Related URL: http://dx.doi.org/10.1016/j.bbapap.2011.03.002

Abstract

Crystal of Russell Viper venom phospholipase A2 complexed with an isoquinoline alkaloid, berberine from a herbaceous plant Cardiospermum halicacabum, was prepared and its structure was solved by X-ray crystallography. The crystal diffracted up to 1.93 Å and the structure solution clearly located the position of berberine in the active site of the enzyme. Two hydrogen bonds, one direct and the other water mediated, were formed between berberine and the enzyme. Gly 30 and His 48 made these two hydrogen bonds. Additionally, the hydrophobic surface of berberine made a number of hydrophobic contacts with side chains of neighboring amino acids. Surface Plasmon Resonance studies revealed strong binding affinity between berberine and phospholipase A2. Enzyme inhibition studies proved that berberine is a competitive inhibitor of phospholipase A2. It was inferred that the isoquinoline alkaloid, berberine, is a potent natural inhibitor of phospholipaseA2.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science..
Keywords:Phospholipase A2 Inhibition; Berberine; X-Ray Crystallography; Surface Plasmon Resonance
ID Code:49167
Deposited On:19 Jul 2011 07:15
Last Modified:19 Jul 2011 07:15

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