Journal
EUROPEAN JOURNAL OF PHARMACOLOGY
Volume 884, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.ejphar.2020.173392
Keywords
Leishmaniasis; Solid lipid nanoparticle; 4-Nitrochalcone; Nanoencapsulation
Categories
Funding
- Conselho Nacional de Desenvolvimento Cientifico e Tecnol.ogico (CNPq, Brazil) [482195/2013-4]
- Coordenac~ao de Aperfeicoamento Pessoal de Nivel Superior (CAPES, Brazil)
Ask authors/readers for more resources
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-alpha, 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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available