Derivados triterpênicos sintéticos anti-Trichomonas vaginalis : uma alternativa promissora

Abstract

Trichomonas vaginalis is an extracellular protozoan parasite that binds to the epithelium of the human urogenital tract during infection named trichomoniasis. In view of increased resistance to drugs belonging to 5-nitroimidazoles class, new treatment alternatives are urgently needed. In this study, eight triterpenes derivatives were synthetized and evaluated for their in vitro anti-T. vaginalis activity. Compounds obtained from ursolic acid presented better activity than those from betulinic acid. UA-OXYMA, derivative of ursolic acid presented minimum inhibitory concentration (MIC) of 25 μM. To evaluate the behavior of this compound regarding the anti-T. vaginalis potential some tests were made. Screening with different T. vaginalis fresh clinical isolates showed that the derivative UA-OXYMA was efficient against all parasites. The growth kinetics curve revealed that the compound inhibited parasites growth after six hours of incubation and it totally abolished the parasites proliferation in 24 hours. Hemolysis tests resulted in low hemolytic activity of compound UA-OXYMA; however another test was conducted to identify whether it was cytotoxic and it proved to be in the concentration of 25 μM. Finally, we demonstrated that the compound acts synergistically with the drug of choice, metronidazole. This report reveals the high potential of the triterpenoid derivative compound UA-OXYMA as trichomonicidal agent.