4.6 Article

Total Synthesis and Anti-Viral Activities of an Extract of Radix isatidis

Journal

MOLECULES
Volume 19, Issue 12, Pages 20906-20912

Publisher

MDPI
DOI: 10.3390/molecules191220906

Keywords

Radix isatidis; isoquinoline derivative; anti-viral activity

Funding

  1. National Natural Science Foundation of China [81473316]
  2. Priority Academic Program Development of Jiangsu Higher Education Institutions

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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 mu g/mL. The results suggested that isoquinoline derivatives possessed potent anti-viral activity and are worthy further development.

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