利用分子对接研究、ADME和毒性分析鉴定基于蓝藻的抗SARS-CoV-2药物靶点ACE2天然抑制剂

IF 1.5 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY Indian Journal of Clinical Biochemistry Pub Date : 2023-07-01 Epub Date: 2022-07-05 DOI:10.1007/s12291-022-01056-6
Niharika Sahu, Sonal Mishra, Minu Kesheri, Swarna Kanchan, Rajeshwar P Sinha
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引用次数: 9

摘要

2019-2020年,新型“严重急性呼吸综合征冠状病毒-2(SARS-CoV-2)”成为人类面临的最大挑战,导致“冠状病毒疾病19(新冠肺炎)”。世界各地的科学家一直在不断努力开发严重急性呼吸系统综合征冠状病毒2型的潜在抑制剂。我们进行了计算研究,帮助我们确定蓝藻光保护化合物是对抗严重急性呼吸系统综合征冠状病毒2型药物靶向人类血管紧张素转换酶(ACE2)的潜在抑制剂,该酶在病毒附着和进入细胞中起着至关重要的作用。阻断ACE2的受体结合结构域可以阻止病毒进入隔室。使用AutoDock工具在光保护化合物分枝杆菌素样氨基酸、scytonemins和ACE2蛋白之间进行了分子对接研究。在16种分子对接代谢产物中,选择了7种具有结合能的化合物
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Identification of Cyanobacteria-Based Natural Inhibitors Against SARS-CoV-2 Druggable Target ACE2 Using Molecular Docking Study, ADME and Toxicity Analysis.

In 2019-2020, the novel "severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2)" had emerged as the biggest challenge for humanity, causing "coronavirus disease 19 (COVID-19)". Scientists around the world have been putting continuous efforts to unfold potential inhibitors of SARS-CoV-2. We have performed computational studies that help us to identify cyanobacterial photoprotective compounds as potential inhibitors against SARS-CoV-2 druggable target human angiotensin-converting enzyme (ACE2), which plays a vital role in the attachment and entry of the virus into the cell. Blocking the receptor-binding domain of ACE2 can prevent the access of the virus into the compartment. A molecular docking study was performed between photoprotective compounds mycosporine-like amino acids, scytonemins and ACE2 protein using AutoDock tools. Among sixteen molecularly docked metabolites, seven compounds were selected with binding energy < 6.8 kcal/mol. Afterwards, drug-likeness and toxicity of the top candidate were predicted using Swiss ADME and Pro Tox-II online servers. All top hits show desirable drug-likeness properties, but toxicity pattern analysis discloses the toxic effect of scytonemin and its derivatives, resulting in the elimination from the screening pipeline. Further molecular interaction study of the rest two ligands, mycosporine-glycine-valine and shinorine with ACE2 was performed using PyMol, Biovia Discovery studio and LigPlot+. Lastly biological activity of both the ligands was predicted by using the PASS online server. Combining the docking score and other studied properties, we believe that mycosporine-glycine-valine and shinorine have potential to be potent inhibitors of ACE2 and can be explored further to use against COVID-19.

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来源期刊
Indian Journal of Clinical Biochemistry
Indian Journal of Clinical Biochemistry BIOCHEMISTRY & MOLECULAR BIOLOGY-
CiteScore
4.50
自引率
4.80%
发文量
74
期刊介绍: The primary mission of the journal is to promote improvement in the health and well-being of community through the development and practice of clinical biochemistry and dissemination of knowledge and recent advances in this discipline among professionals, diagnostics industry, government and non-government organizations. Indian Journal of Clinical Biochemistry (IJCB) publishes peer reviewed articles that contribute to the existing knowledge in all fields of Clinical biochemistry, either experimental or theoretical, particularly deal with the applications of biochemistry, molecular biology, genetics, biotechnology, and immunology to the diagnosis, treatment, monitoring and prevention of human diseases. The articles published also include those covering the analytical and molecular diagnostic techniques, instrumentation, data processing, quality assurance and accreditation aspects of the clinical investigations in which chemistry has played a major role, or laboratory animal studies with biochemical and clinical relevance.
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