Avaliação das atividades de migração celular e antimicrobiana de derivados aminoguanidínicos

Abstract

The high rates of antimicrobial resistance and therapeutic stagnation make it necessary to produce new antibacterials. Aminoguanidine derivatives are therapeutically promising drugs, since they have several reported activities like antimicrobial, antitumor, antinociceptive and antiglycation properties. The following study aims to evaluate antimicrobial and migration activity of fibroblasts of aminoguanidine derivatives. The aminoguanidine derivatives LQM 98, LQM 99, LQM 100, LQM 157, LQM 159, LQM 161 and LQM 162 were given by the Medicinal Chemistry Laboratory of Pharmacy and Nursing School (LQM/ICF/UFAL). The antibacterial activity was evaluated by broth microdilution method at stock concentrations of 40 μg / ml and 400 μg / ml for Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa, Enterobacter cloacae e Shigella flexneri; the cell viability was evaluated by the colorimetric method of methyltetrazolium (MTT) and the in vitro cell migration for fibroblasts by scratch assay. The aminoguanidine derivatives LQM 98, LQM 99, LQM 100 and LQM 162 showed inhibitory activity towards the tested bacteria, but the derivatives LQM 157, LQM 159 and LQM 161 did not show any antimicrobial activity. In relation to the cell viability assay, only the derivative LQM 162 was slightly cytotoxic at 10 μM, but the other derivatives were non-cytotoxic; the treatment at 100 μM with derivatives LQM 99, LQM 100 e LQM 162 induced a decrease in the percentage of viable cell, but the derivatives LQM 157, LQM 159 e LQM 161 were non-cytotoxic. In the in vitro scratch assay, none of aminoguanidine derivatives had significant effects on the cell migration of the fibroblastos. In view of the found results, the aminoguanidine derivatives showed antibacterial activity for Gram positive and Gram negative bacteria, no cytotoxic or slightly cytotoxic effects to fibroblast at 10 μM and lack of wound healing potencial. As perspective, new aminoguanidine derivatives will be planned, aiming to obtain a new class of substances more active for antimicrobial and cell migration purpose.