Hartini Yustina, Saputra Bakti, Wahono Bryan, Auw Zerlinda, Indayani Friska, Adelya Lintang, Namba Gabriel, Hariono Maywan
Faculty of Pharmacy, Sanata Dharma University, Campus III, Paingan, Maguwoharjo, Depok, Sleman 55282, Yogyakarta, Indonesia.
Results Chem. 2021 Jan;3:100087. doi: 10.1016/j.rechem.2020.100087. Epub 2020 Dec 25.
3CL protease is one of the key proteins expressed by SARS-Coronavirus-2 cell, the potential to be targeted in the discovery of antivirus during this COVID-19 pandemic. This protein regulates the proteolysis of viral polypeptide essential in forming RNA virus. 3CL protease (3CLpro) was commonly targeted in the previous SARS-Coronavirus including bat and MERS, hence, by blocking this protein activity, the coronavirus should be eradicated. This study aims to review the potency of biflavonoid as the SARS-Coronavirus-2 3CLpro inhibitor. The review was initiated by describing the chemical structure of biflavonoid and followed by listing its natural source. Instead, the synthetic pathway of biflavonoid was also elaborated. The 3CLpro structure and its function were also illustrated followed by the list of its 3D-crystal structure available in a protein data bank. Lastly, the pharmacophores of biflavonoid have been identified as a protease inhibitor, was also discussed. This review hopefully will help researchers to obtain packed information about biflavonoid which could lead to the study in designing and discovering a novel SARS-Coronavirus-2 drug by targetting the 3CLpro enzyme.
3CL蛋白酶是严重急性呼吸综合征冠状病毒2（SARS-CoV-2）细胞表达的关键蛋白之一，在此次新型冠状病毒肺炎（COVID-19）大流行期间具有作为抗病毒药物靶点的潜力。该蛋白调节形成RNA病毒所必需的病毒多肽的蛋白水解过程。在之前的包括蝙蝠冠状病毒和中东呼吸综合征冠状病毒（MERS）在内的SARS冠状病毒研究中，3CL蛋白酶（3CLpro）通常是靶点，因此，通过阻断该蛋白的活性，冠状病毒应该能够被根除。本研究旨在综述双黄酮作为SARS-CoV-2 3CLpro抑制剂的潜力。综述首先描述了双黄酮的化学结构，接着列出了其天然来源。此外，还阐述了双黄酮的合成途径。同时还展示了3CLpro的结构及其功能，并列出了蛋白质数据库中可获得的其三维晶体结构。最后，还讨论了已被确定为蛋白酶抑制剂的双黄酮药效基团。本综述有望帮助研究人员获取有关双黄酮的全面信息，从而有助于开展针对3CLpro酶设计和发现新型SARS-CoV-2药物的研究。
