2. Academic Validation
  3. Glycyrrhizic acid derivatives as Dengue virus inhibitors

Glycyrrhizic acid derivatives as Dengue virus inhibitors

  • Bioorg Med Chem Lett. 2019 Oct 15;29(20):126645. doi: 10.1016/j.bmcl.2019.126645.
Lidia A Baltina 1,  Yan-Ting Tasi 2,  Su-Hua Huang 3,  Hsueh-Chou Lai 4,  Lia A Baltina 5,  Svetlana F Petrova 5,  Marat S Yunusov 5,  Cheng-Wen Lin 6
Affiliations

Affiliations

  • 1 Ufa Institute of Chemistry, Ufa Federal Research Centre of RAS, 71, Prospect Oktyabrya, Ufa 450054, Russian Federation. Electronic address: baltina@anrb.ru.
  • 2 Department of Medical Laboratory Science and Biotechnology, China Medical University, 91, Hsueh-Shih Rd., Taichung 40402, Taiwan, ROC; Department of Biotechnology, Asia University, 500, Lioufeng Rd., Wufeng, Taichung 41354, Taiwan, ROC.
  • 3 Department of Biotechnology, Asia University, 500, Lioufeng Rd., Wufeng, Taichung 41354, Taiwan, ROC.
  • 4 School of Chinese Medicine, China Medical University, 91, Hsueh-Shih Rd., Taichung 40402, Taiwan, ROC; Division of Hepato-gastroenterology, Department of Internal Medicine, China Medical University Hospital, 2, Yude Rd., Taichung 40447, Taiwan, ROC.
  • 5 Ufa Institute of Chemistry, Ufa Federal Research Centre of RAS, 71, Prospect Oktyabrya, Ufa 450054, Russian Federation.
  • 6 Department of Medical Laboratory Science and Biotechnology, China Medical University, 91, Hsueh-Shih Rd., Taichung 40402, Taiwan, ROC; Department of Biotechnology, Asia University, 500, Lioufeng Rd., Wufeng, Taichung 41354, Taiwan, ROC; Chinese Medicine Research Center, China Medical University, 91, Hsueh-Shih Rd., Taichung 40402, Taiwan, ROC. Electronic address: cwlin@mail.cmu.edu.tw.
PMID: 31519375 DOI: 10.1016/j.bmcl.2019.126645
Abstract

Dengue virus (DENV) is one of the most geographically distributed pathogenic flaviviruses transmitted by mosquitoes Aedes sps. In this study, the structure-antiviral activity relationships of Glycyrrhizic acid (GL) derivatives was evaluated by the inhibitory assays on the cytopathic effect (CPE) and viral infectivity of DENV type 2 (DENV2) in Vero E6 cells. GL (96% purity) had a low cytotoxicity to Vero E6 cells, inhibited DENV2-induced CPE, and reduced the DENV-2 infectivity with the IC50 of 8.1 μM. Conjugation of GL with Amino acids or their methyl esters and the introduction of aromatic acylhydrazide residues into the carbohydrate part strongly influenced on the Antiviral activity. Among compounds tested GL conjugates with isoleucine 13 and 11-aminoundecanoic acid 17 were found as potent anti-DENV2 inhibitors (IC50 1.2-1.3 μM). Therefore, modification of GL is a perspective way in the search of new antivirals against DENV2 Infection.

Keywords

Antiviral activity; Dengue virus; Derivatives; Glycyrrhizic acid.

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