4.5 Article

Understanding the binding mechanism of succinic acid against phospholipase A2 from bee venom

Journal

Publisher

WILEY
DOI: 10.1002/jbt.22715

Keywords

bee venom PLA(2); isothermal titration calorimetry (ITC); molecular dynamics simulation; phospholipase A(2) (PLA(2)); PLA(2) assay

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Phospholipase A(2) is an enzyme responsible for releasing fatty acids from glycerophospholipids, commonly found in mammalian tissues and venom from different animals. Compounds that inhibit the activity of PLA(2) are of scientific and medicinal interest as potential antidotes for snake bites and bee stings. Among the tested compounds, succinic acid has been identified to inhibit PLA(2) activity through molecular mechanism studies.
Phospholipase A(2) (PLA(2)) is responsible for the release of fatty acids from glycerophospholipids. PLA(2) is commonly found in mammalian tissues. It is also found in venom from different animals ranging from insects, arachnid, and snakes. The release of arachidonic acid in large amount results in inflammation and pain. Identification of compounds that can inhibit the activity of PLA(2) is of large scientific and medicinal interest as these compounds can act as antidotes toward snake bites and bee stings. Among the different compounds that have been tested for inhibition of PLA(2), a secondary metabolite succinic acid is identified to inhibit PLA(2) activity. The inhibition was analyzed using an in vitro PLA(2) inhibition assay and isothermal titration calorimetry (ITC) studies. The molecular mechanism of the mode of inhibition was studied using molecular docking and simulation studies.

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