Screening of the antileishmanial and antiplasmodial potential of synthetic 2-arylquinoline analogs

Abstract

In this study, six analogs of 2-arylquinoline were synthesized and evaluated for their in vitro and in vivo antiplasmodial and leishamanicidal activity. Also, hemolytic activity and drugability were tested in vitro and in silico, respectively. In relationship to leishmanicidal activity, the compounds showed half maximal effective concentration (EC50) values between 3.6µM and 19.3µM. Likewise, treatment using compounds 4a-f caused improvement in most of treated hamsters and cured some of them. Regarding antiplasmodial activity, the compounds showed moderate to high activity, did not show hemolytic activity. Furthermore, 4e and 4f compounds were not able to control P. berghei infection when administered to animal models. Molecular dynamic simulations, molecular docking and ligand binding affinity indicate good bioavailability and absorption characteristics of the studied compounds, which are expected to be active when administered orally. The compounds are absorbable at the hematoencephalic barrier but not in the gastrointestinal tract. ADMET properties suggest that these molecules may be used as a safe treatment for Leishmania.

Actividad antiprotozoaria y antioxidante in vitro de extractos y metabolitos mayoritarios aislados de Pilocarpus alvaradoi (Rutaceae)

“…Con el fin de asegurar una mayor infección de los macrófagos in vitro, la cepa de L. (V) panamensis se mantuvo en hámster (Mesocricetus auratus) infectados experimentalmente. Previamente a la infección in vitro, se hizo un aspirado de la lesión del hámster con solución de fosfatos (PBS) y aguja #26; luego, la muestra aspirada se cultivó en medio NNN e incubados a una temperatura de 27 o C hasta obtener promastigotes (Espinosa et al, 2023).…”