Understanding the binding mechanism of succinic acid against phospholipase A_2 from bee venom

H. V. Kutumbarao Nidamarthi; Manisha Choudhury; Devadasan Velmurugan

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Understanding the binding mechanism of succinic acid against phospholipase A_2 from bee venom

机译：了解蜜蜂毒液琥珀酸对磷脂酶A_2的结合机制

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Phospholipase A_2 (PLA_2) is responsible for the release of fatty acids from glycer-ophospholipids. 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 ti-tration calorimetry (ITC) studies. The molecular mechanism of the mode of inhibition was studied using molecular docking and simulation studies.

机译：磷脂酶A_2（PLA_2）负责从甘油磷脂中释放脂肪酸。PLA_2通常存在于哺乳动物组织中。它还存在于昆虫、蜘蛛纲动物和蛇等不同动物的毒液中。花生四烯酸的大量释放会导致炎症和疼痛。鉴定能够抑制PLA_2活性的化合物具有重大的科学和医学意义，因为这些化合物可以作为蛇咬和蜂蜇的解毒剂。在已被测试为抑制PLA_2的不同化合物中，一种次级代谢物琥珀酸被鉴定为抑制PLA_2活性。使用体外PLA2抑制试验和等温滴定量热法（ITC）研究分析抑制作用。通过分子对接和模拟研究，研究了抑制模式的分子机制。

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来源
《Journal of biochemical and molecular toxicology》 |2021年第4期|共1页
作者
H. V. Kutumbarao Nidamarthi; Manisha Choudhury; Devadasan Velmurugan;
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作者单位

Centre of Advanced Study in Crystallography and Biophysics University of Madras Chennai Tamil;

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原文格式 PDF
正文语种 eng
中图分类生物化学;
关键词
bee venom PLA_2; isothermal titration calorimetry (ITC); molecular dynamics simulation; phospholipase A_2 (PLA_2); PLA_2 assay;

机译：蜜蜂毒液PLA_2;等温滴定量热法（ITC）;分子动力学模拟;磷脂酶A_2（PLA_2）;PLA_2测定;

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2. Bee venom phospholipase A2 ameliorates amyloidogenesis and neuroinflammation through inhibition of signal transducer and activator of transcription-3 pathway in Tg2576 mice [J] . Hyeon Joo Ham, Sang-Bae Han, Jaesuk Yun, 转化神经变性病(英文) . 2019,第001期
3. Expression of a bee venom phospholipase A2 from Apis cerana cerana in the baculovirus-insect cell [J] . Li-rong SHEN, Mei-hui DING, Li-wen ZHANG, 浙江大学学报：B卷英文版 . 2010,第005期
4. EXPRESSION OF A BEE-VENOM PHOSPHOLIPASE A2 FROM APIS CERANA CERANA IN E,.qCHERICHIA COLI [J] . Li-rongShen, Jia-anCheng, Chuan-xiZhang 中国昆虫科学：英文版 . 2004,第001期
5. The Molecular Mechanism of Bee Venom Phospholipase A_2 Inactivation by Bolinaquinone [J] . Maria Chiara Monti, Agostino Casapullo, Cosima Santomauro, Chembiochem: A European journal of chemical biology . 2006,第6期

机译：Bolinaquinone灭活蜂毒磷脂酶A_2的分子机制
6. Preliminary Development of DNA Aptamers to Inhibit Phospholipase A_2 Activity of Bee and Cobra Venoms [J] . John G. Bruno, Taylor Phillips, Tiffany Montez Journal of Bionanoscience . 2015,第4期

机译：抑制蜂和眼镜蛇毒液磷脂酶A_2活性的DNA适配子的初步开发。
7. Surface dilution kinetics using substrate analog enantiomers as diluents: Enzymatic lipolysis by bee venom phospholipase A_2 [J] . Singh J., Ranganathan R., Hajdu J. Analytical Biochemistry: An International Journal of Analytical and Preparative Methods . 2010,第2期

机译：使用底物类似物对映体作为稀释剂的表面稀释动力学：蜂毒磷脂酶A_2的酶促脂解
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机译：蜂毒液透明质酸酶碱辅助催化机制的结构证据，蜂毒液的主要过敏原
9. Toward understanding the interfacial activation and binding of phosphatidylinositol-specific phospholipase C (PI-PLC): The effect of organic solvents and non-substrate interfaces. [D] . Wehbi, Hania. 2002

机译：理解磷脂酰肌醇特异性磷脂酶C（PI-PLC）的界面活化和结合：有机溶剂和非底物界面的影响。
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机译：来自对蜂毒磷脂酶A2特异的人T细胞杂交瘤的抗原结合糖基化抑制因子。
11. Localization of Structural Elements of Bee Venom Phospholipase A2 Involved in N-type Receptor Binding and Neurotoxicity* [O] . Michel Lazdunski, Michael H. Gelbi 2015

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12. Pathologic Changes Induced by Phospholipase A2 Isolated from the Venom of Collett's Snake, Pseudechis colletti: A Light and Electron Microscopic Study. (Reannouncement with New Availability Information). [R] . Weinstein, S. A., Bell, R. C., Brown, C. R., 1992

机译：从Collett蛇，pseudechis colletti毒液中分离的磷脂酶a2诱导的病理学变化：光和电子显微镜研究。（重新公布新的可用性信息）。

Understanding the binding mechanism of succinic acid against phospholipase A_2 from bee venom

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