当前位置：
X-MOL 学术
›
Pestic. Biochem. Phys.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Design, synthesis and anti-TMV activity of novel α-aminophosphonate derivatives containing a chalcone moiety that induce resistance against plant disease and target the TMV coat protein
Pesticide Biochemistry and Physiology ( IF 4.2 ) Pub Date : 2021-02-01 , DOI: 10.1016/j.pestbp.2020.104749 Xiang Zhou 1 , Yiqiang Ye 1 , Shasha Liu 2 , Wubin Shao 1 , Liwei Liu 1 , Song Yang 1 , Zhibing Wu 1
Pesticide Biochemistry and Physiology ( IF 4.2 ) Pub Date : 2021-02-01 , DOI: 10.1016/j.pestbp.2020.104749 Xiang Zhou 1 , Yiqiang Ye 1 , Shasha Liu 2 , Wubin Shao 1 , Liwei Liu 1 , Song Yang 1 , Zhibing Wu 1
Affiliation
|
Abstract Plant viral diseases, known as “plant cancer”, with high contagiosity can substantially reduce crop quality and yield. To identify potential anti-tobacco mosaic virus (TMV) agents with different mechanisms, a series of novel α-aminophosphonate derivatives containing a chalcone moiety were designed and synthesized. Bioassay results revealed that some target compounds exhibited improved curative activity against TMV in vivo, and the EC50 value of compound B3 was 356.7 mg L−1. The activities of the defensive enzymes POD and CAT from tobacco leaves treated with B3 and B17 showed that these target compounds could improve the photosynthetic ability of the leaves and activate plant host resistance against TMV infection. The binding constant between B3 and TMV Coat Protein (CP) (2.51 × 108 M−1), calculated by the fluorescence titration experiment and docking results, revealed that B3 has a strong interaction with TMV CP. Further docking analysis revealed that B3 was embedded between two layers of the TMV CP, which was consistent with the 2:1 binding mode of TMV CP and B3 determined by the binding affinity experiment. The TEM morphological study of TMV treated with B3 and B17 indicated that this series of target compounds may trigger the disassembly of TMV by interacting directly with TMV CP. This study provides new insight for the discovery of antiviral compounds with two different mechanisms of action.
中文翻译：
含有查耳酮部分的新型 α-氨基膦酸酯衍生物的设计、合成和抗 TMV 活性，可诱导植物病害抗性并靶向 TMV 外壳蛋白
摘要 植物病毒病，又称“植物癌”，具有高度传染性，可大幅降低作物品质和产量。为了鉴定具有不同机制的潜在抗烟草花叶病毒（TMV）药物，设计并合成了一系列含有查耳酮部分的新型α-氨基膦酸酯衍生物。生物测定结果显示，部分目标化合物对TMV体内活性有所提高，化合物B3的EC50值为356.7 mg L−1。用 B3 和 B17 处理的烟叶中防御酶 POD 和 CAT 的活性表明，这些目标化合物可以提高叶片的光合能力，并激活植物宿主对 TMV 感染的抵抗力。通过荧光滴定实验和对接结果计算出B3与TMV外壳蛋白（CP）之间的结合常数（2.51×108 M−1），表明B3与TMV CP具有很强的相互作用。进一步对接分析发现B3嵌入TMV CP的两层之间，这与结合亲和力实验确定的TMV CP与B3的2:1结合模式一致。 B3和B17处理TMV的TEM形态研究表明，该系列目标化合物可能通过与TMV CP直接相互作用而引发TMV的分解。这项研究为发现具有两种不同作用机制的抗病毒化合物提供了新的见解。
更新日期：2021-02-01
中文翻译：
含有查耳酮部分的新型 α-氨基膦酸酯衍生物的设计、合成和抗 TMV 活性，可诱导植物病害抗性并靶向 TMV 外壳蛋白
摘要 植物病毒病，又称“植物癌”，具有高度传染性，可大幅降低作物品质和产量。为了鉴定具有不同机制的潜在抗烟草花叶病毒（TMV）药物，设计并合成了一系列含有查耳酮部分的新型α-氨基膦酸酯衍生物。生物测定结果显示，部分目标化合物对TMV体内活性有所提高，化合物B3的EC50值为356.7 mg L−1。用 B3 和 B17 处理的烟叶中防御酶 POD 和 CAT 的活性表明，这些目标化合物可以提高叶片的光合能力，并激活植物宿主对 TMV 感染的抵抗力。通过荧光滴定实验和对接结果计算出B3与TMV外壳蛋白（CP）之间的结合常数（2.51×108 M−1），表明B3与TMV CP具有很强的相互作用。进一步对接分析发现B3嵌入TMV CP的两层之间，这与结合亲和力实验确定的TMV CP与B3的2:1结合模式一致。 B3和B17处理TMV的TEM形态研究表明，该系列目标化合物可能通过与TMV CP直接相互作用而引发TMV的分解。这项研究为发现具有两种不同作用机制的抗病毒化合物提供了新的见解。
京公网安备 11010802027423号