Xin Hui, Tian Jiao, Deng Tianyu, Zhou Qing, Wang Yuhong, Fu Hong, Pu Haotao, Xue Wei
State Key Laboratory of Green Pesticide, Center for R&D of Fine Chemicals, Guizhou University, Guiyang, 550025, China.
Mol Divers. 2024 Dec 2. doi: 10.1007/s11030-024-11049-7.
A series of chalcone derivatives containing 1,2,4-triazole and pyridine were designed and synthesized, and their antiviral activities against tobacco mosaic virus (TMV) were evaluated. Notably, S7 (EC = 89.7 μg/mL) exhibited excellent curative activity against the TMV, which was superior to that of ningnanmycin (NNM: EC = 201.7 μg/mL). Molecular docking showed that S7 exhibited satisfactory affinities for the TMV coat protein (TMV-CP), with four strong conventional hydrogen bonds with amino acid residues. Further, microscale thermophoresis (MST) showed that S7 (Kd = 0.5340 ± 0.2233 μmol/L) bound more strongly to TMV-CP than NNM (Kd = 5.1186 ± 1.9568 μmol/L). The results of chlorophyll content, malondialdehyde (MDA) content, and biological enzyme activity confirmed that S7 enhanced the disease resistance of tobacco plants by affecting the change of chlorophyll content, interfering with plant lipid peroxidation, and enhancing SOD activity in plants, respectively.
设计并合成了一系列含1,2,4-三唑和吡啶的查尔酮衍生物，并评估了它们对烟草花叶病毒（TMV）的抗病毒活性。值得注意的是，S7（EC = 89.7 μg/mL）对TMV表现出优异的治疗活性，优于宁南霉素（NNM：EC = 201.7 μg/mL）。分子对接表明，S7对TMV外壳蛋白（TMV-CP）表现出令人满意的亲和力，与氨基酸残基形成四个强常规氢键。此外，微量热泳（MST）表明，S7（Kd = 0.5340 ± 0.2233 μmol/L）与TMV-CP的结合比NNM（Kd = 5.1186 ± 1.9568 μmol/L）更强。叶绿素含量、丙二醛（MDA）含量和生物酶活性的结果证实，S7分别通过影响叶绿素含量的变化、干扰植物脂质过氧化和增强植物中的超氧化物歧化酶（SOD）活性来增强烟草植株的抗病性。
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