Identification of Potential Antiviral Hops Compounds against Chikungunya Virus

Author(s)

Mandova, Tsvetelina ; Saivish, Marielena Vogel ; La Serra, Leonardo ; Nogueira, Mauricio Lacerda ; Da Costa, Fernando Batista

• Document type: Journal article
• Source: INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES; v. 24, n. 4, p. 18-pg., 2023-02-01.

Abstract

Chikungunya virus (CHIKV) is an arthropod-borne virus that belongs to the genus Alphavirus (family Togaviridae). CHIKV causes chikungunya fever, which is mostly characterized by fever, arthralgia and, sometimes, a maculopapular rash. The bioactive constituents of hops (Humulus lupulus, Cannabaceae), mainly acylphloroglucinols, known as well as alpha- and beta-acids, exerted distinct activity against CHIKV, without showing cytotoxicity. For fast and efficient isolation and identification of such bioactive constituents, a silica-free countercurrent separation method was applied. The antiviral activity was determined by plaque reduction test and was visually confirmed by a cell-based immunofluorescence assay. All hops compounds demonstrated a promising post-treatment viral inhibition, except the fraction of acylphloroglucinols, in mixture. beta-acids fraction of 125 mu g/mL expressed the strongest virucidal activity (EC50 = 15.21 mu g/mL), in a drug-addition experiment on Vero cells. Hypothesis for mechanism of action were proposed for acylphloroglucinols based on their lipophilicity and chemical structure. Therefore, inhibition of some steps of the protein kinase C (PKC) transduction cascades was also discussed. (AU)

• FAPESP's process: 20/12875-5 - Development of the diagnostic method for Rocio virus and use of new compounds as inhibitors of flavivirus protease-helicase NS2B-NS3
• Grantee: Marielena Vogel Saivish
• Support Opportunities: Scholarships in Brazil - Doctorate