Total synthesis and anti-viral activities of an extract of Radix isatidis

• Published in: Molecules (Basel, Switzerland) Vol. 19; no. 12; pp. 20906 - 20912
• Main Authors: He, Li-Wei, Liu, Hua-Qing, Chen, Yu-Qing, Yang, Jing-Yan, Wang, Tian-Lin, Li, Wei
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 12.12.2014; MDPI
• Subjects: Animals; anti-viral activity; Antiviral Agents - chemical synthesis; Antiviral Agents - pharmacology; Cell Survival - drug effects; Cercopithecus aethiops; China; Chinese medicine; Constituents; Derivatives; Drugs, Chinese Herbal - chemistry; Herpesvirus 1, Human - drug effects; Inhibitory Concentration 50; isoquinoline derivative; Isoquinolines - chemical synthesis; Isoquinolines - pharmacology; Radix isatidis; Sourcing; Sulfuric acid; Synthesis; Traditional chinese medicine; Vero Cells; Beijing China; Switzerland; China
• ISSN: 1420-3049; 1420-3049
• 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.