title: Total synthesis and anti-viral activities of an extract of Radix isatidis.
abstract: 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.
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, China. he_lw@163.com.
authors.forename: Li-Wei
authors.initials: LW
authors.lastname: He
authors.affiliation: The Second Hospital of Nanjing, 1-1 ZhongFu Road, Nanjing 210003, China. layuer@163.com.
authors.forename: Hua-Qing
authors.initials: HQ
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, China. drcoreychen@gmail.com.
authors.forename: Yu-Qing
authors.initials: YQ
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, China. jingyan_1024@163.com.
authors.forename: Jing-Yan
authors.initials: JY
authors.lastname: Yang
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, China. cpuwtl@gmail.com.
authors.forename: Tian-Lin
authors.initials: TL
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, China. liwaii@126.com.
authors.forename: Wei
authors.initials: W
authors.lastname: Li
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D004365:Drugs, Chinese Herbal / Q000737:chemistry*; D018259:Herpesvirus 1, Human / Q000187:drug effects; D020128:Inhibitory Concentration 50; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D014709:Vero Cells
chemical_list: D000998:Antiviral Agents; D004365:Drugs, Chinese Herbal; D007546:Isoquinolines; C540579:banlangen