托普森汀生物碱及其衍生物作为新型抗病毒和抗植物病原真菌剂的发现。
Discovery of Topsentin Alkaloids and Their Derivatives as Novel Antiviral and Anti-phytopathogenic Fungus Agents.
作者信息
Ji Xiaofei, Wang Ziwen, Dong Ji, Liu Yuxiu, Lu Aidang, Wang Qingmin
机构信息
Tianjin Key Laboratory of Structure and Performance for Functional Molecules, Key Laboratory of Inorganic-Organic Hybrid Functional Materials Chemistry (Tianjin Normal University), Ministry of Education, College of Chemistry, Tianjin Normal University , Tianjin 300387, China.
State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Nankai University , Tianjin 300071, China.
出版信息
J Agric Food Chem. 2016 Dec 7;64(48):9143-9151. doi: 10.1021/acs.jafc.6b04020. Epub 2016 Nov 22.
Topsentin alkaloids and their derivatives were designed, synthesized, and characterized on the basis of NMR and mass spectroscopy. The antiviral activities against tobacco mosaic virus (TMV) and anti-phytopathogenic fungus activities of these alkaloids were evaluated for the first time. Alkaloids 1c, 1e, 2b, and 2d displayed significantly higher antiviral activities against TMV than Ribavirin, emerging as new lead compounds for anti-TMV research. Further fungicidal activity tests against 14 kinds of phytopathogenic fungi revealed that these alkaloids displayed broad-spectrum fungicidal activities. Topsentin derivative 2d with 4-5 mg/kg EC values against Sclerotinia sclerotiorum (Lib.), Rhizoctonia solani (Kuhn), and Botrytis cinerea (Pers.) emerged as a new lead compound for fungicidal research. Current studies provide support for the application of topsentin alkaloids as novel agrochemicals.
基于核磁共振（NMR）和质谱对托普辛生物碱及其衍生物进行了设计、合成与表征。首次评估了这些生物碱对烟草花叶病毒（TMV）的抗病毒活性以及抗植物病原真菌活性。生物碱1c、1e、2b和2d对TMV的抗病毒活性显著高于利巴韦林，成为抗TMV研究的新先导化合物。对14种植物病原真菌的进一步杀菌活性测试表明，这些生物碱具有广谱杀菌活性。托普辛衍生物2d对核盘菌（Lib.）、立枯丝核菌（Kuhn）和灰葡萄孢（Pers.）的有效浓度（EC）值为4 - 5 mg/kg，成为杀菌研究的新先导化合物。目前的研究为托普辛生物碱作为新型农用化学品的应用提供了支持。
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