Centre of Advanced Study in Crystallography and Biophysics, University of Madras, Chennai, Tamil Nadu, India.
Department of Biosciences and Bioengineering, IIT Bombay, Powai, Mumbai, Maharashtra, India.
J Biochem Mol Toxicol. 2021 Apr;35(4):e22715. doi: 10.1002/jbt.22715. Epub 2021 Feb 13.
Phospholipase A (PLA ) is responsible for the release of fatty acids from glycerophospholipids. PLA 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 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 , a secondary metabolite succinic acid is identified to inhibit PLA activity. The inhibition was analyzed using an in vitro PLA inhibition assay and isothermal titration calorimetry (ITC) studies. The molecular mechanism of the mode of inhibition was studied using molecular docking and simulation studies.
磷脂酶 A（PLA）负责从甘油磷脂释放脂肪酸。PLA 在哺乳动物组织中普遍存在。它也存在于不同动物的毒液中，包括昆虫、蛛形纲动物和蛇。大量释放花生四烯酸会导致炎症和疼痛。鉴定能够抑制 PLA 活性的化合物具有重要的科学和医学意义，因为这些化合物可以作为蛇咬伤和蜂蜇的解毒剂。在已经测试过的抑制 PLA 的不同化合物中，鉴定出一种次级代谢产物琥珀酸能够抑制 PLA 的活性。使用体外 PLA 抑制测定法和等温热滴定法（ITC）研究来分析抑制作用。通过分子对接和模拟研究研究了抑制模式的分子机制。
