Wang Ziwen, Feng Anzheng, Cui Mingbo, Liu Yuxiu, Wang Lizhong, Wang Qingmin
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.
Chem Biol Drug Des. 2014 Nov;84(5):531-42. doi: 10.1111/cbdd.12340. Epub 2014 Jun 3.
A series of 7-methoxycryptopleurine derivatives 2-23 were prepared and evaluated for their antiviral activity against tobacco mosaic virus (TMV) for the first time. The bioassay results showed that most of these compounds exhibited excellent in vivo anti-TMV activity, of which 7-methoxycryptopleurine salt derivatives 16, 19, and 23 displayed significantly higher activity than 7-methoxycryptopleurine (1) and commercial ribavirin and ningnanmycin. Salification, the most commonly employed method for modifying physical-chemical properties, did significantly increase antiviral activity, and different salt forms displayed different antiviral effect. This study provides fundamental support for development and optimization of phenanthroquinolizidine alkaloids as potential inhibitors of plant virus.
首次制备了一系列7-甲氧基隐品碱衍生物2-23，并对其抗烟草花叶病毒（TMV）的活性进行了评估。生物测定结果表明，这些化合物中的大多数表现出优异的体内抗TMV活性，其中7-甲氧基隐品碱盐衍生物16、19和23的活性明显高于7-甲氧基隐品碱（1）以及市售的利巴韦林和宁南霉素。盐化是最常用的改变物理化学性质的方法，它确实显著提高了抗病毒活性，并且不同的盐形式表现出不同的抗病毒效果。本研究为开发和优化菲并喹嗪类生物碱作为植物病毒的潜在抑制剂提供了基础支持。
