Potent Inhibitory Activities of the Adenosine Analogue Cordycepin on SARS-CoV-2 Replication.
Potent Inhibitory Activities of the Adenosine Analogue Cordycepin on SARS-CoV-2 Replication.
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DOI：
10.1021/acsomega.1c05998
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发表时间：
2022-01-25
期刊：
影响因子：
4.1
通讯作者：
Rabie AM
中科院分区：
文献类型：
--
作者：
Rabie AM
核苷类似物是药物化学中最成功的生物活性类药物化合物之一，因为它们因其对人类的众多有效生物活性而闻名，特别是作为抗病毒和抗癌药物。 2019 年冠状病毒病 (COVID-19) 仍然无法治愈，其致病病毒严重急性呼吸系统综合症冠状病毒 2 (SARS-CoV-2) 继续在各地造成严重破坏。这种复杂的国际形势敦促所有相关科学家，包括药物化学家和药物发现者，寻找有效的抗COVID-19药物。虫草素（3'-脱氧腺苷）是一种已知的真菌来源的天然腺苷类似物，也可以合成生产。这种具有生物活性的植物化合物具有多种已被证实的强大药理作用，可有效促进 COVID-19 的综合治疗，其中抗病毒活性是最主要的。一些新研究基于计算方法预测了虫草素对主要 SARS-CoV-2 蛋白靶点（例如 SARS-CoV-2 刺突 (S) 蛋白、主要蛋白酶 (Mpro) 和 RNA 依赖性 RNA 聚合酶 (RdRp) 酶）可能的抑制亲和力。有趣的是，目前的研究首次表明，虫草素能够有效抑制SARS-CoV-2新耐药株的增殖，其体外抗SARS-CoV-2 EC50极小，约为2 μM，略高于瑞德西韦及其活性代谢物GS-441524。虫草素分子理想的药效特征使其成为典型的 SARS-CoV-2 复制抑制剂，其灵活的结构为未来大多数类型的衍生化开放。简而言之，目前的研究结果进一步支持并表明了虫草素针对 COVID-19 的重新利用可能性，并极大地鼓励我们充满信心地快速开始其综合治疗 COVID-19 的临床前/临床评估。
Nucleoside analogues are among the most successful bioactive classes of druglike compounds in pharmaceutical chemistry as they are well-known for their numerous effective bioactivities in humans, especially as antiviral and anticancer agents. Coronavirus disease 2019 (COVID-19) is still untreatable, with its causing virus, the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), continuing to wreak havoc on the ground everywhere. This complicated international situation urged all concerned scientists, including medicinal chemists and drug discoverers, to search for a potent anti-COVID-19 drug. Cordycepin (3′-deoxyadenosine) is a known natural adenosine analogue of fungal origin, which could also be synthetically produced. This bioactive phytochemical compound is characterized by several proven strong pharmacological actions that may effectively contribute to the comprehensive treatment of COVID-19, with the antiviral activities being the leading ones. Some new studies predicted the possible inhibitory affinities of cordycepin against the principal SARS-CoV-2 protein targets (e.g., SARS-CoV-2 spike (S) protein, main protease (Mpro) enzyme, and RNA-dependent RNA polymerase (RdRp) enzyme) based on the computational approach. Interestingly, the current research showed, for the first time, that cordycepin is able to potently inhibit the multiplication of the new resistant strains of SARS-CoV-2 with a very minute in vitro anti-SARS-CoV-2 EC50 of about 2 μM, edging over both remdesivir and its active metabolite GS-441524. The ideal pharmacophoric features of the cordycepin molecule render it a typical inhibitor of SARS-CoV-2 replication, with its flexible structure open for most types of derivatization in the future. Briefly, the current findings further support and suggest the repurposing possibility of cordycepin against COVID-19 and greatly encourage us to confidently and rapidly begin its preclinical/clinical evaluations for the comprehensive treatment of COVID-19.
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影响因子：
4.4
作者：
Chien M;Anderson TK;Jockusch S;Tao C;Li X;Kumar S;Russo JJ;Kirchdoerfer RN;Ju J
通讯作者：
Ju J
影响因子：
3.7
作者：
Ip A;Ahn J;Zhou Y;Goy AH;Hansen E;Pecora AL;Sinclaire BA;Bednarz U;Marafelias M;Sawczuk IS;Underwood JP 3rd;Walker DM;Prasad R;Sweeney RL;Ponce MG;La Capra S;Cunningham FJ;Calise AG;Pulver BL;Ruocco D;Mojares GE;Eagan MP;Ziontz KL;Mastrokyriakos P;Goldberg SL
通讯作者：
Goldberg SL
影响因子：
2.9
作者：
MULLER, WEG;WEILER, BE;SCHRODER, HC
通讯作者：
SCHRODER, HC
影响因子：
7.6
作者：
Caly, Leon;Druce, Julian D;Wagstaff, Kylie M
通讯作者：
Wagstaff, Kylie M
DOI：
10.3390/molecules26113118
发表时间：
2021-05-23
期刊：
Molecules (Basel, Switzerland)
影响因子：
--
作者：
Panya A;Songprakhon P;Panwong S;Jantakee K;Kaewkod T;Tragoolpua Y;Sawasdee N;Lee VS;Nimmanpipug P;Yenchitsomanus PT
通讯作者：
Yenchitsomanus PT