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金属蛋白酶-A的天然配体——一个多面性的药物靶点。

The Natural Ligand for Metalloproteinase-A Multifaceted Drug Target.

作者信息

Shivashankar Saranya, Sangeetha Marimuthu Kannan

机构信息

School of Life Sciences, B.S.Abdur Rahman Crescent Institute of Science and Technology, Chennai, India.

出版信息

Appl Biochem Biotechnol. 2022 Apr;194(4):1716-1739. doi: 10.1007/s12010-021-03778-4. Epub 2022 Jan 8.

Abstract

Metalloproteinase is one of the key components of Russell viper venom and it is the root cause of edema, blood coagulation, local tissue damage, hemorrhage, and inflammation during snakebite envenoming. Hence, finding a suitable metalloproteinase inhibitor from natural source will be of great biological importance in mitigating pathological effects. In this current study, we employed computational analysis to examine the inhibition of metalloproteinase by phytochemicals present in Andrographis paniculata. Molecular docking studies revealed interaction of A. paniculata phytochemicals with the catalytic M domain's active site amino acid residues, namely ASN203, ARG293, PHE203, LEU206, LYS199, and ALA122, similar to that of the reference compound Batimastat. 14-acetylandrographolide, 14-deoxy-11,12 didehydroandrographolide, Andrograpanin, Isoandrographolide, and 14-deoxy-11-oxoandrographolide displayed high binding energy and inhibition against the metalloproteinase. Molecular dynamic simulation analysis revealed less root mean square fluctuation of amino acid residues of metalloproteinase-14-acetylandrographolide complex than metalloproteinase-Batimastat complex indicating the high stability for metalloproteinase with the phytochemical. In silico analysis of parameters like ADME properties and drug-likeness of the phytochemicals exhibited good pharmacokinetic properties. Ligand-based virtual screening of phytochemicals to identify similarity to FDA-approved drugs and identification of their possible targets were also performed. The outcome of the current study strengthens the significance of these phytochemicals as promising lead candidates for the treatment of snakebite envenomation. Moreover, the study also encourages the in vivo and in vitro evaluation of the phytochemicals to validate the computational findings.

摘要

金属蛋白酶是罗素蝰蛇毒液的关键成分之一,是蛇咬伤中毒时水肿、血液凝固、局部组织损伤、出血和炎症的根本原因。因此,从天然来源中找到合适的金属蛋白酶抑制剂对于减轻病理影响具有重要的生物学意义。在本研究中,我们采用计算分析方法来研究穿心莲中存在的植物化学物质对金属蛋白酶的抑制作用。分子对接研究表明,穿心莲植物化学物质与催化M结构域的活性位点氨基酸残基(即ASN203、ARG293、PHE203、LEU206、LYS199和ALA122)相互作用,类似于参考化合物batimastat。14-乙酰穿心莲内酯、14-脱氧-11,12-二脱氢穿心莲内酯、穿心莲宁、异穿心莲内酯和14-脱氧-11-氧代穿心莲内酯对金属蛋白酶表现出高结合能和抑制作用。分子动力学模拟分析表明,金属蛋白酶-14-乙酰穿心莲内酯复合物的氨基酸残基的均方根波动比金属蛋白酶-batimastat复合物小,表明金属蛋白酶与植物化学物质具有高稳定性。对植物化学物质的ADME性质和类药性等参数进行的计算机分析显示出良好的药代动力学性质。还进行了基于配体的植物化学物质虚拟筛选,以确定与FDA批准药物的相似性并确定其可能的靶点。本研究结果强化了这些植物化学物质作为治疗蛇咬伤中毒有前景的先导候选物的重要性。此外,该研究还鼓励对植物化学物质进行体内和体外评估,以验证计算结果。

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