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C. Ciências Biológicas - 10. Microbiologia - 2. Microbiologia Aplicada

ANTIVIRAL AND CYTOTOXICITY EVALUATION OF N-ALQUIL-ESTERS OF GALLIC ACID

Luciane Anita Savi 1
Paulo César Leal  2
Ricardo Nunes 2
Rosendo Yunes  2
Célia Regina Monte Barardi  1
Cláudia Maria Oliveira Simões 3
(1. Departamento de Microbiologia e Parasitologia / UFSC; 2. Departamento de Química / UFSC; 3. Departamento de Ciências Farmacêuticas / UFSC)
INTRODUÇÃO:

The n-alquil-esters of gallic acid (= gallates) have a diverse range of industrial uses as antioxidants in food, cosmetics and pharmaceutical industries. Studies realized with these compounds showed that they possess many potential therapeutic properties including anti-cancer, antiviral and antimicrobial properties, among others. Most interest has been devoted to the high antioxidant activity of gallates which is linked to their antiviral property. In this study, gallic acid, methyl-, ethyl-, propyl-, butyl-, pentyl-, hexyl-, heptyl-, octyl-, decyl-, undecyl-, dodecyl-, tetradecyl-, cetyl- and octadecyl gallates were tested for their cytotoxicity and antiviral activity by MTT colorimetric method.

METODOLOGIA:

The tested virus was Herpes Simplex Virus type 1 (HSV-1, strains KOS and 29-R/acyclovir resistant) and VERO cells were used in these tests. Acyclovir was tested as a reference drug. The in vitro selectivity index (SI=CC50/IC50) for each compound was calculated using the 50% cytotoxic concentration for cell growth (CC50) and the 50% inhibitory concentration of the viral effect (IC50). These therapeutic indices values permitted us to establish some structure-activity relationships as well as to identify important structural features responsible for the biological activity of the tested molecules.

RESULTADOS:

According to our results, all the substances have showed low toxicity to VERO cells and promising antiherpetic activity with SI values varying from 0.89 to 11.48 for KOS strain and 1.33 to 18.34 for 29-R strain.

CONCLUSÕES:

It was observed that the presence of hydroxyl groups in these molecules, which are also responsible for their antioxidant action, and the length of lateral carbonic chain influence their antiherpetic activity. However, additional studies are required to obtain the ideal structure of gallates to stand out this activity.

Instituição de fomento: CNPq/MCT/Brazil.
 
Palavras-chave: n-alquil-esters of gallic acid; HSV-1; MTT assay .
Anais da 58ª Reunião Anual da SBPC - Florianópolis, SC - Julho/2006