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筛选临床前和临床研究中的天然和衍生生物活性化合物:抗击冠状病毒大流行的前沿之一。

Screening for natural and derived bio-active compounds in preclinical and clinical studies: One of the frontlines of fighting the coronaviruses pandemic.

机构信息

Department of Molecular Biosciences, The Wenner-Gren Institute, Stockholm University, S-106 91, Stockholm, Sweden.

Department of Chemistry, Faculty of Science, Menoufia University, 32512 Shebin El-Kom, Egypt; School of Food and Biological Engineering, Jiangsu University, Zhenjiang 212013, China.

出版信息

Phytomedicine. 2021 May;85:153311. doi: 10.1016/j.phymed.2020.153311. Epub 2020 Aug 29.

Abstract

BACKGROUND

Starting December 2019, mankind faced an unprecedented enemy, the COVID-19 virus. The world convened in international efforts, experiences and technologies in order to fight the emerging pandemic. Isolation, hygiene measure, diagnosis, and treatment are the most efficient ways of prevention and intervention nowadays. The health organizations and global care systems screened the available resources and offered recommendations of approved and proposed medications. However, the search for a specific selective therapy or vaccine against COVID-19 remains a challenge.

METHODS

A literature search was performed for the screening of natural and derived bio-active compounds which showed potent antiviral activity against coronaviruses using published articles, patents, clinical trials website (https://clinicaltrials.gov/) and web databases (PubMed, SCI Finder, Science Direct, and Google Scholar).

RESULTS

Through the screening for natural products with antiviral activities against different types of the human coronavirus, extracts of Lycoris radiata (L'Hér.), Gentiana scabra Bunge, Dioscorea batatas Decne., Cassia tora L., Taxillus chinensis (DC.), Cibotium barometz L. and Echinacea purpurea L. showed a promising effect against SARS-CoV. Out of the listed compound Lycorine, emetine dihydrochloride hydrate, pristimerin, harmine, conessine, berbamine, 4`-hydroxychalcone, papaverine, mycophenolic acid, mycophenolate mofetil, monensin sodium, cycloheximide, oligomycin and valinomycin show potent activity against human coronaviruses. Additionally, it is worth noting that some compounds have already moved into clinical trials for their activity against COVID-19 including fingolimod, methylprednisolone, chloroquine, tetrandrine and tocilizumab.

CONCLUSION

Natural compounds and their derivatives could be used for developing potent therapeutics with significant activity against SARS-COV-2, providing a promising frontline in the fighting against COVID-19.

摘要

背景

自 2019 年 12 月以来,人类面临着前所未有的敌人,即 COVID-19 病毒。为了应对这一新兴的大流行,全世界都在共同努力,分享经验和技术。目前,隔离、卫生措施、诊断和治疗是预防和干预的最有效方法。卫生组织和全球护理系统筛选了现有资源,并提出了已批准和建议使用的药物的建议。然而,寻找针对 COVID-19 的特定选择性治疗方法或疫苗仍然是一个挑战。

方法

通过对已发表的文章、专利、临床试验网站(https://clinicaltrials.gov/)和网络数据库(PubMed、SCI Finder、Science Direct 和 Google Scholar)进行文献检索,筛选出对冠状病毒具有潜在抗病毒活性的天然和衍生生物活性化合物。

结果

通过筛选对不同类型人冠状病毒具有抗病毒活性的天然产物,发现石蒜(L'Hér.)、龙胆(Gentiana scabra Bunge)、山药(Dioscorea batatas Decne.)、槐树(Cassia tora L.)、中国旌节花(Taxillus chinensis (DC.))、紫萁贯众(Cibotium barometz L.)和紫锥菊(Echinacea purpurea L.)的提取物对 SARS-CoV 具有良好的效果。在所列出的化合物中,石蒜碱、盐酸依米丁水合物、薯蓣皂素、哈尔明碱、康纳辛、小檗胺、4`-羟基查耳酮、罂粟碱、霉酚酸、霉酚酸酯、莫能菌素钠、环己酰亚胺、寡霉素和缬氨霉素对人冠状病毒具有很强的活性。此外,值得注意的是,一些化合物已经进入针对 COVID-19 的临床试验,包括芬戈莫德、甲泼尼龙、氯喹、汉防己甲素和托珠单抗。

结论

天然化合物及其衍生物可用于开发针对 SARS-COV-2 的有效治疗方法,为抗击 COVID-19 提供了一个有前景的一线治疗手段。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/65d4/7455571/8f55ed195e7a/fx1_lrg.jpg

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