Avaliação de derivados aminoguanidinas hidrazonas com potencial atividade antimicrobiana e migração celular in vitro

Abstract

Aminoguanidines have been of interest in the last 50 years because of their biological and chemical properties. Derivatives of the aminoguanidines hydrazones represent a class of compounds which contain an amidine group (guanyl), attached to a hydrazone moiety. Moreover, present biological activities such as anti-diabetic, antimalarial, antileishmanial, antifungal, antibacterial and anti-HIV. Thus, the aim of this study is to evaluate the derivatives aminoguanidine hydrazones with potential antimicrobial activity and cell migration in vitro. It is an in vitro experimental research with quantitative and qualitative approach. Eighteen hydrazone aminoguanidine derivatives were tested and evaluated for antimicrobial activity against Gram positive and Gram negative bacteria. Cell viability was evaluated by Methyltetrazolium colorimetric method with cell lines of 3T3 fibroblasts at concentrations of 10 and 100 μM and test in vitro cell migration by the scratch assay technique used concentration of 10 μM. The antimicrobial activity of LQM 131 showed a MIC of 12,5 μg/mL for Shigella flexneri, and for LQM 199 the inhibition was at concentrations of 5 to 12,5 μg/mL against strains Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa, Enterobacter cloacae and Shigella flexneri. In relation to cell viability assay, it was observed that in the 10 μM concentration all the substances showed viability higher than 80%, however, in the highest concentration of 100 μM only four substances (LQM 96, 97, 101 and 131) remained viable with a percentage above 80%, the others presented relevant toxicity to the fibroblast lineages. In the evaluation of cellular migration, it was observed that LQM substances 101, 131, 134 and 195 presented a similar form when compared to positive control (55.17%), with percentages of migration of 55,01%, 56,98%, 58,13% and 57,95%, respectively, and LQM 132 showed decreased fibroblast migration with a percentage of 23,31%. However, it was concluded that the aminoguanidines hydrazones showed antimicrobial activity against the tested strains, being LQM substances 106, 131, 198 and 199 with inhibition against the six bacteria tested. The substances maintained cell viability greater than 80% at the 10 μM concentration and at the concentration of 100 μM only four molecules maintained viability greater than 80%. No cellular migration of 3T3 fibroblasts was observed when treated with the aminoguanidines hydrazones.