Molecules 2014, 19(11), 18911-18922; https://doi.org/10.3390/molecules191118911
Preparation of Rotenone Derivatives and in Vitro Analysis of Their Antimalarial, Antileishmanial and Selective Cytotoxic Activities
1
PECET, Instituto de Investigaciones Médicas, Facultad de Medicina, Universidad de Antioquia, Calle 70 #52-21, Medellín 050010, Colombia
2
Grupo Química Orgánica de Productos Naturales, Instituto de Química, Facultad de Ciencias Exactas y Naturales, Universidad de Antioquia, Calle 70 #52-21, Medellín 050010, Colombia
3
Center for Development of Products against Tropical Diseases-CIDEPRO, Medellín 050010, Colombia
*
Author to whom correspondence should be addressed.
Received: 26 August 2014 / Revised: 12 November 2014 / Accepted: 13 November 2014 / Published: 18 November 2014
(This article belongs to the Collection Natural Products as Leads or Drugs against Neglected Tropical Diseases)
Abstract
Six derivatives of the known biopesticide rotenone were prepared by several chemical transformations. Rotenone and its derivatives showed differential in vitro antiparasitic activity and selective cytotoxicity. In general, compounds were more active against Plasmodium falciparum than Leishmania panamensis. Rotenone had an EC50 of 19.0 µM against P. falciparum, and 127.2 µM against L. panamensis. Although chemical transformation does not improve its biological profile against P. falciparum, three of its derivatives showed a significant level of action within an adequate range of activity with EC50 values < 50.0 µM. This antiplasmodial activity was not due to red blood cell hemolysis, since LC50 was >>400 µM. On the other hand, all derivatives displayed a non-specific cytotoxicity on several cell lines and primary human cell cultures. View Full-Text
Figure 1
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Upegui, Y.; Gil, J.F.; Quiñones, W.; Torres, F.; Escobar, G.; Robledo, S.M.; Echeverri, F. Preparation of Rotenone Derivatives and in Vitro Analysis of Their Antimalarial, Antileishmanial and Selective Cytotoxic Activities. Molecules 2014, 19, 18911-18922.
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