Screening of Sulfonamide-Derivative Compounds and Assessment of Baicalein Anti-Chikungunya Virus Activity

Abstract

Chikungunya is a mosquito-borne virus that can cause primarily acute infections, especially in tropical and subtropical regions. However, some musculoskeletal symptoms can persist even after more than 3 months, characterizing chronic Chikungunya disease (CCD) that develops in around 40% of patients. Currently, all treatment methods are supportive care to treat symptoms, and the complete lack of Chikungunya antivirals poses a major concern. As an attempt to address this gap, this research project explored the potential of antivirals in sulfonamide-derivative compounds and baicalein, both of which have been uncovered in past studies for anti-Dengue activities. High-throughput screening (HTS) was performed on 22 sulfonamide-derivative compounds, however, none of them exhibited cell viability and Chikungunya inhibition at over 90%, failing to pass the screening cut-off altogether. This is potentially due to the differences in protein (nsPs) responsible for viral methyltransferase, which was the predicted target pathway of sulfonamides to Dengue in a previous study. Baicalein on the other hand was analyzed at varying concentrations for cytotoxicity and Chikungunya inhibition. The assays’ results suggested a CC50 of 82.75 μM in Vero cells and an EC50 of 3.18 μM against Chikungunya-infected Vero cells. The mechanism behind baicalein’s anti-Chikungunya activity may target viral attachment, or viral nsP1 methyltransferase activity, as suggested by past research.