Antiviral activity of selected flavonoids against Chikungunya virus

Antiviral Res. 2016 Sep:133:50-61. doi: 10.1016/j.antiviral.2016.07.009. Epub 2016 Jul 25.

Abstract

This study focuses on the antiviral activity of selected flavonoids against the Chikungunya virus (CHIKV), a mosquito-transmitted virus that can cause incapacitating arthritis in infected individuals. Based on the results of screening on Vero cells, the tested compounds were evaluated further with various assays, including cytotoxicity assay, virus yield assay by quantitative reverse transcription polymerase chain reaction (qRT-PCR), virus RNA replication assay with a CHIKV replicon cell line, Western blotting, and quantitative immunofluorescence assay. Baicalein, fisetin, and quercetagetin displayed potent inhibition of CHIKV infection, with 50% inhibitory concentrations [IC50] of 1.891 μg/ml (6.997 μM), 8.444 μg/ml (29.5 μM), and 13.85 μg/ml (43.52 μM), respectively, and with minimal cytotoxicity. The time-of-addition studies and various antiviral assays demonstrated that baicalein and quercetagetin mainly inhibited CHIKV binding to the Vero cells and displayed potent activity against extracellular CHIKV particles. The qRT-PCR, immunofluorescence assay, and Western blot analyses indicated that each of these flavonoids affects CHIKV RNA production and viral protein expression. These data provide the first evidence of the intracellular anti-CHIKV activity of baicalein, fisetin, and quercetagetin.

Keywords: Antiviral effect; Chikungunya virus; Flavonoids; Natural compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Biological Products / pharmacology
  • Cell Line
  • Chikungunya virus / drug effects*
  • Chikungunya virus / genetics
  • Cricetinae
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical
  • Flavonoids / chemistry
  • Flavonoids / pharmacology*
  • Genotype
  • Inhibitory Concentration 50
  • Vero Cells
  • Virus Replication / drug effects

Substances

  • Antiviral Agents
  • Biological Products
  • Flavonoids