Abstract
Entamoeba histolytica is a unicellular eukaryote that is the causative agent for amebiasis in humans. There are ~100,000 fatalities annually, distributed mostly in developing countries. Cyst‐contaminated food and water disproportionately present in conflict zones. Additionally, lack of resources, clean water, sanitation, and limited access to education and health contribute to the rate of disease worldwide. The current treatment is metronidazole which is effective but has toxic and neurological side effects. The bifunctional alcohol‐aldehyde dehydrogenase (EhADH2) has been suggested as a target for anti‐amebic inhibitors, because it is essential for E. histolytica trophozoite growth. Entamoeba spp use EhADH2 to convert (anaerobically) acetyl‐CoA to acetaldehyde and acetaldehyde to ethanol. Substrate and cofactor (NADH, Fe) cofactor binding sites could be targeted for inhibition. Cyclic carbinol molecules such as cyclobutyl and cyclopropyl inhibit E. histolytica growth by affecting EhADH2 activities. Pyrazoline molecules have also showed inhibitory effects on E. histolytica growth. Three series of pyrazoline inhibitors previously synthesized and preliminarily selected by trophozoite growth inhibition will be tested for their ability to inhibit EhADH2 bifunctional activities. Establishing the mechanism of action for anti‐amebic inhibitors through restriction of EhADH2 activity may provide an alternative treatment to current toxic drugs such as metronidazole.This abstract is from the Experimental Biology 2019 Meeting. There is no full text article associated with this abstract published in The FASEB Journal.
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