The Medical Center of General Practice, Sichuan Academy of Medical Science and Sichuan Provincial People's Hospital, Chengdu 610041, Sichuan Province, China.
The Medical Center of General Practice, Sichuan Academy of Medical Science and Sichuan Provincial People's Hospital, Chengdu 610041, Sichuan Province, China.
J Integr Med. 2022 Nov;20(6):488-496. doi: 10.1016/j.joim.2022.08.001. Epub 2022 Aug 9.
At present, a variety of vaccines have been approved, and existing antiviral drugs are being tested to find an effective treatment for coronavirus disease 2019 (COVID-19). However, no standardized treatment has yet been approved by the World Health Organization. The virally encoded chymotrypsin-like protease (3CL) from severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), which facilitates the replication of SARS-CoV in the host cells, is one potential pharmacological target for the development of anti-SARS drugs. Online search engines, such as Web of Science, Google Scholar, Scopus and PubMed, were used to retrieve data on the traditional uses of medicinal plants and their inhibitory effects against the SARS-CoV 3CL. Various pure compounds, including polyphenols, terpenoids, chalcones, alkaloids, biflavonoids, flavanones, anthraquinones and glycosides, have shown potent inhibition of SARS-CoV-2 3CL activity with 50% inhibitory concentration (IC) values ranging from 2-44 µg/mL. Interestingly, most of these active compounds, including xanthoangelol E (isolated from Angelica keiskei), dieckol 1 (isolated from Ecklonia cava), amentoflavone (isolated from Torreya nucifera), celastrol, pristimerin, tingenone and iguesterin (isolated from Tripterygium regelii), tannic acid (isolated from Camellia sinensis), and theaflavin-3,3'-digallate, 3-isotheaflav1in-3 gallate and dihydrotanshinone I (isolated from Salvia miltiorrhiza), had IC values of less than 15 µg/mL. Kinetic mechanistic studies of several active compounds revealed that their mode of inhibition was dose-dependent and competitive, with K values ranging from 2.4-43.8 μmol/L. Given the significance of plant-based compounds and the many promising results obtained, there is still need to explore the phytochemical and mechanistic potentials of plants and their products. These medicinal plants could serve as an effective inexpensive nutraceutical for the general public to help manage COVID-19.
目前,已经有多种疫苗获得批准,现有的抗病毒药物也在进行测试,以期找到针对 2019 年冠状病毒病(COVID-19)的有效治疗方法。然而,世界卫生组织尚未批准任何标准化的治疗方法。严重急性呼吸综合征冠状病毒 2(SARS-CoV-2)编码的病毒蛋白酶 3CL 在宿主细胞中促进 SARS-CoV 的复制,是开发抗 SARS 药物的潜在药理学靶点之一。在线搜索引擎,如 Web of Science、Google Scholar、Scopus 和 PubMed,被用于检索药用植物的传统用途及其对 SARS-CoV 3CL 的抑制作用的数据。各种纯化合物,包括多酚、萜类、查耳酮、生物碱、双黄酮、黄烷酮、蒽醌和糖苷,都显示出对 SARS-CoV-2 3CL 活性的强大抑制作用,其 50%抑制浓度(IC)值范围为 2-44μg/ml。有趣的是,这些具有活性的化合物中的大多数,包括从当归中分离得到的当归醇 E、从裙带菜中分离得到的二咖啡酰奎宁酸 1、从榧树中分离得到的金松双黄酮、从雷公藤中分离得到的雷公藤红素、从卫矛中分离得到的当药黄素、从丹参中分离得到的鞣酸、以及从茶中分离得到的茶黄素-3,3'-二没食子酸酯、3-异茶黄素-1,3-没食子酸酯和二氢丹参酮 I,其 IC 值均小于 15μg/ml。对几种活性化合物的动力学机制研究表明,它们的抑制模式是剂量依赖性和竞争性的,K 值范围为 2.4-43.8μmol/L。鉴于植物化合物的重要性以及获得的许多有希望的结果,仍需要探索植物及其产物的植物化学和机制潜力。这些药用植物可以作为一种有效的、廉价的营养保健品,供公众使用,以帮助管理 COVID-19。