发现半胱氨酸及其衍生物作为新型抗病毒和抗真菌药物。
Discovery of Cysteine and Its Derivatives as Novel Antiviral and Antifungal Agents.
机构信息
School of Chemical Engineering and Technology, Hebei University of Technology, Tianjin 300130, China.
Tianjin Key Laboratory of Structure and Performance for Functional Molecules, College of Chemistry, Tianjin Normal University, Tianjin 300387, China.
出版信息
Molecules. 2021 Jan 13;26(2):383. doi: 10.3390/molecules26020383.
Based on the structure of the natural product cysteine, a series of thiazolidine-4-carboxylic acids were designed and synthesized. All target compounds bearing thiazolidine-4-carboxylic acid were characterized by H-NMR, C-NMR, and HRMS techniques. The antiviral and antifungal activities of cysteine and its derivatives were evaluated in vitro and in vivo. The results of anti-TMV activity revealed that all compounds exhibited moderate to excellent activities against tobacco mosaic virus (TMV) at the concentration of 500 μg/mL. The compounds cysteine (), -, , , , , , and displayed higher anti-TMV activities than the commercial plant virucide ribavirin (inhibitory rate: 40, 40, and 38% at 500 μg/mL for inactivation, curative, and protection activity in vivo, respectively), especially compound (inhibitory rate: 51%, 47%, and 49% at 500 μg/mL for inactivation, curative, and protection activity in vivo, respectively) with excellent antiviral activity emerged as a new antiviral candidate. Antiviral mechanism research by TEM exhibited that compound could inhibit virus assembly by aggregated the 20S protein disk. Molecular docking results revealed that compound with higher antiviral activities than that of compound did show stronger interaction with TMV CP. Further fungicidal activity tests against 14 kinds of phytopathogenic fungi revealed that these cysteine derivatives displayed broad-spectrum fungicidal activities. Compound exhibited higher antifungal activities against and than commercial fungicides carbendazim and chlorothalonil, which emerged as a new candidate for fungicidal research.
基于天然产物半胱氨酸的结构，设计并合成了一系列噻唑烷-4-羧酸类化合物。所有含有噻唑烷-4-羧酸的目标化合物均通过 H-NMR、C-NMR 和 HRMS 技术进行了表征。在体外和体内评估了半胱氨酸及其衍生物的抗病毒和抗真菌活性。抗 TMV 活性结果表明，所有化合物在 500μg/mL 浓度下对烟草花叶病毒（TMV）均表现出中等至优异的活性。化合物半胱氨酸（）、-、-、-、-、-、-和 显示出比商业植物病毒抑制剂利巴韦林（在 500μg/mL 时体内失活、治疗和保护活性的抑制率分别为 40、40 和 38%）更高的抗 TMV 活性，特别是化合物 （在 500μg/mL 时体内失活、治疗和保护活性的抑制率分别为 51%、47%和 49%）表现出优异的抗病毒活性，成为一种新的抗病毒候选药物。TEM 抗病毒机制研究表明，化合物 可以通过聚集 20S 蛋白盘来抑制病毒组装。分子对接结果表明，具有更高抗病毒活性的化合物 与 TMV CP 的相互作用强于化合物 。进一步对 14 种植物病原菌的杀菌活性测试表明，这些半胱氨酸衍生物表现出广谱杀菌活性。化合物 对 和 的抑菌活性高于商业杀菌剂多菌灵和百菌清，是杀菌剂研究的新候选药物。
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