Affordable Access

deepdyve-link
Publisher Website

Nanoemulsions of sulfonamide carbonic anhydrase inhibitors strongly inhibit the growth of Trypanosoma cruzi.

Authors
  • Vermelho, Alane Beatriz1
  • da Silva Cardoso, Verônica1
  • Ricci Junior, Eduardo2
  • Dos Santos, Elisabete Pereira2
  • Supuran, Claudiu T1, 3
  • 1 a Bioinovar-Biotecnologia: Unidade de Biocatálise, Bioprodutos e Bioenergia (BIOINOVAR) , Instituto de Microbiologia Paulo de Góes, Universidade Federal do Rio de Janeiro , Rio de Janeiro , RJ , Brazil. , (Brazil)
  • 2 b Laboratório de Desenvolvimento Galênico (LADEG), Departamento de Medicamentos , Universidade Federal do Rio de Janeiro , Rio de Janeiro , RJ , Brazil. , (Brazil)
  • 3 c NEUROFARBA Dept., Sezione di Scienze Farmaceutiche , Università degli Studi di Firenze , Florence , Italy. , (Italy)
Type
Published Article
Journal
Journal of Enzyme Inhibition and Medicinal Chemistry
Publisher
Informa UK (Taylor & Francis)
Publication Date
Dec 01, 2018
Volume
33
Issue
1
Pages
139–146
Identifiers
DOI: 10.1080/14756366.2017.1405264
PMID: 29192555
Source
Medline
Keywords
License
Unknown

Abstract

Sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitors targeting the α-class enzyme from the protozoan pathogen Trypanosoma cruzi, responsible of Chagas disease, were recently reported. Although many such derivatives showed low nanomolar activity in vitro, they were inefficient anti-T. cruzi agents in vivo. Here, we show that by formulating such sulfonamides as nanoemulsions in clove (Eugenia caryophyllus) oil, highly efficient anti-protozoan effects are observed against two different strains of T. cruzi. These effects are probably due to an enhanced permeation of the enzyme inhibitor through the nanoemulsion formulation, interfering in this way with the life cycle of the pathogen either by inhibiting pH regulation or carboxylating reactions in which bicarbonate/CO2 are involved. This type of formulation of sulfonamides with T. cruzi CA inhibitory effects may lead to novel therapeutic approaches against this orphan disease.

Report this publication

Statistics

Seen <100 times