USE OF A BENZOTHIAZOLE DERIVATIVE COMPOUND FOR THE INHIBITION OF ENTAMOEBA HISTOLYTICA AND ANTIOXIDANT ENZYMES ASSOCIATED WITH THE PARASITE CAUSING AMEBIASIS.

Abstract

The present invention relates to the use of a benzothiazole derivative as an amebicide against Entamoeba histolytica. In Mexico, amebiasis is a public health problem affecting a large part of the country, especially the most socioeconomically disadvantaged population, since the most commonly used treatment of choice against amebiasis, metronidazole (MTZ), a tissue nitroimidazole, despite its effectiveness, produces serious adverse effects. Furthermore, resistance of Entamoeba histolytica trophozoites to this drug has been described. Therefore, it is important to provide new, safe pharmacological alternatives for the treatment of this amoeba. The present invention demonstrates, for the first time, the in vitro anti-amebic activity of a benzothiazole derivative.The results of the trophozoites treated with the benzothiazole derivative at 5 h showed: I) an 82% decrease in amoebic viability; II) the inhibitory concentration 50 (IC50) is 3.2 times more potent than that of the reference drug (MTZ); III) cytotoxicity assays on VERO cells showed that the benzothiazole derivative is not cytotoxic to cells; IV) a significant decrease in the relative gene expression of antioxidant amoebic enzymes, including thioredoxin (Trx), thioredoxin reductase (TrxR), ruberythrin (Rr), and peroxiredoxin (Prx).The present invention protects an alternative preventive and therapeutic treatment against amoebas that cause pathologies associated with amoeba infection. Additionally, it serves as a blocker of antioxidant enzymes of the amoebas, allowing its use in the academic field, other research, and for drug development, as well as potential application strategies in other fields (food, agriculture) where E. histolytica infection represents relevant risks.