Preliminary Evaluation of antiherpes activity of caffeic acid derivatives

RIGOTTO, C.; MAROSTICA, L. L.; MARTINEZ, M.D.; REGINATTO F. H.; DURAN, F. J.; SIMOES C. M. O.

Foz de Iguazú

Congreso; XXIII Congreso Brasileiro de Virología -VII Encontro de Virología do Mercosul; 2012

Sociedade Brasilera de Virologia

Among the several biological responses elicited by caffeic acid derivatives, the inhibition of human immunodeficiency virus type 1 (HIV-1) appeared recently as the most promising pharmacological activity. Herpes Simplex Virus (HSV) are responsible for infections of oral, ocular and genital regions, and efforts have been made to find new drugs for their treatment, mainly due to their resistance to the most common available treatment (e.g. acyclovir valacyclovir, fancyclovir and pencyclovir). Synthetic analogues derived from natural products are an interesting source of bioactive molecules with promising pharmacological activities, including antiviral activity, which justifies the research in this area. In this study, we evaluated the antiherpes activity of twenty four synthetic caffeic acid derivatives. Cytotoxicity was evaluated on Vero cells by using MTT assay, and antiviral activity was tested against HSV-1 (KOS strain) by viral plaque number reduction assay. Results were expressed as 50% cytotoxic concentrations (CC50) and 50% viral replication inhibitory concentrations (IC50), respectively, in order to calculate the selectivity index (SI=CC50/IC50) of each tested sample. Among the tested compounds, seven inhibited HSV-1 replication showing SI values between 2.1 and 12.76. Further studies are required to elucidate the mechanism of antiherpes action of the most active derivatives as well as to perform chemical modifications in order to enhance their antiviral activity.