He Li-Wei, Liu Hua-Qing, Chen Yu-Qing, Yang Jing-Yan, Wang Tian-Lin, Li Wei
School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, China.
The Second Hospital of Nanjing, 1-1 ZhongFu Road, Nanjing 210003, China.
Molecules. 2014 Dec 12;19(12):20906-12. doi: 10.3390/molecules191220906.
Radix isatidis (Banlangen), a famous traditional Chinese medicine, has been used for thousands of years in China due to its anti-viral activity. Through our research, we inferred that the anti-viral activity of Radix isatidis depended on the water-soluble part. Among the components of this extract, the isoquinoline derivative 1 was isolated for the first time and has shown better anti-viral activity than other constituents. In this study, to solve the problem of sourcing sufficient quantities of compound 1, a total synthesis route is described, and several analogues are also evaluated for their anti-viral activities. Among them, compound 8 shown potent anti-viral activity with an IC50 value of 15.3 µg/mL. The results suggested that isoquinoline derivatives possessed potent anti-viral activity and are worthy further development.
板蓝根是一种著名的传统中药，因其抗病毒活性在中国已使用了数千年。通过我们的研究，我们推断板蓝根的抗病毒活性取决于水溶性部分。在该提取物的成分中，异喹啉衍生物1首次被分离出来，并且已显示出比其他成分更好的抗病毒活性。在本研究中，为了解决获得足够量化合物1的问题，描述了一条全合成路线，并且还评估了几种类似物的抗病毒活性。其中，化合物8显示出强效抗病毒活性，IC50值为15.3μg/mL。结果表明异喹啉衍生物具有强效抗病毒活性，值得进一步开发。
