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4-nitrochalcone exerts leishmanicidal effect on L. amazonensis promastigotes and intracellular amastigotes, and the 4-nitrochalcone encapsulation in beeswax copaiba oil nanoparticles reduces macrophages cytotoxicity.

Authors :
Assolini JP
da Silva TP
da Silva Bortoleti BT
Gonçalves MD
Tomiotto-Pellissier F
Sahd CS
Carloto ACM
Feuser PE
Cordeiro AP
Sayer C
Hermes de Araújo PH
Costa IN
Conchon-Costa I
Miranda-Sapla MM
Pavanelli WR
Source :
European journal of pharmacology [Eur J Pharmacol] 2020 Oct 05; Vol. 884, pp. 173392. Date of Electronic Publication: 2020 Jul 28.
Publication Year :
2020

Abstract

The Leishmaniasis treatment currently available involves some difficulties, such as high toxicity, variable efficacy, high cost, therefore, it is crucial to search for new therapeutic alternatives. Over the past few years, research on new drugs has focused on the use of natural compounds such as chalcones and nanotechnology. In this context, this research aimed at assessing the in vitro leishmanicidal activity of free 4-nitrochalcone (4NC) on promastigotes and encapsulated 4NC on L. amazonensis-infected macrophages, as well as their action mechanisms. Free 4NC was able to reduce the viability of promastigotes, induce reactive oxygen species production, decrease mitochondrial membrane potential, increase plasma membrane permeability, and expose phosphatidylserine, in addition to altering the morphology and lowering parasite cellular volume. Treatment containing encapsulated 4NC in beeswax-copaiba oil nanoparticles (4NC-beeswax-CO Nps) did not alter the viability of macrophages. Furthermore, 4NC-beeswax-CO Nps reduced the percentage of infected macrophages and the number of amastigotes per macrophages, increasing the production of reactive oxygen species, NO, TNF-α, and IL-10. Therefore, free 4NC proved to exert anti-promastigote effect, while 4NC-beeswax-CO Nps showed a leishmanicidal effect on L. amazonensis-infected macrophages by activating the macrophage microbicidal machinery.<br /> (Copyright © 2020 Elsevier B.V. All rights reserved.)

Details

Language :
English
ISSN :
1879-0712
Volume :
884
Database :
MEDLINE
Journal :
European journal of pharmacology
Publication Type :
Academic Journal
Accession number :
32735985
Full Text :
https://doi.org/10.1016/j.ejphar.2020.173392