Anti-<i>Trypanosoma cruzi</i> Potential of Vestitol Isolated from Lyophilized Red Propolis
Lucas Resende Dutra Sousa,
Tatiane Roquete Amparo,
Gustavo Henrique Bianco de Souza,
Aline Tonhela Ferraz,
Kátia da Silva Fonseca,
Amanda Scofield de Azevedo,
Andréa Mendes do Nascimento,
Ângela Leão Andrade,
Janaína Brandão Seibert,
Thalita Marcolan Valverde,
Saulo Fehelberg Pinto Braga,
Paula Melo de Abreu Vieira,
Viviane Martins Rebello dos Santos
Affiliations
Lucas Resende Dutra Sousa
Phytotechnology Laboratory, School of Pharmacy, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Tatiane Roquete Amparo
Phytotechnology Laboratory, School of Pharmacy, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Gustavo Henrique Bianco de Souza
Phytotechnology Laboratory, School of Pharmacy, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Aline Tonhela Ferraz
Morphopathology Laboratory, Center for Biological Sciences Research, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Kátia da Silva Fonseca
Morphopathology Laboratory, Center for Biological Sciences Research, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Amanda Scofield de Azevedo
Department of Chemistry, Institute of Exact and Biological Sciences, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Andréa Mendes do Nascimento
Department of Chemistry, Institute of Exact and Biological Sciences, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Ângela Leão Andrade
Department of Chemistry, Institute of Exact and Biological Sciences, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Janaína Brandão Seibert
Natural Products Laboratory, Department of Chemistry, Federal University of São Carlos, Rod. Washington Luiz, Sao Carlos 13565-905, SP, Brazil
Thalita Marcolan Valverde
Department of Morphology, Institute of Biological Sciences, Federal University of Minas Gerais, Belo Horizonte 31270-901, MG, Brazil
Saulo Fehelberg Pinto Braga
Medicinal Chemistry and Bioassays Laboratory, School of Pharmacy, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Paula Melo de Abreu Vieira
Morphopathology Laboratory, Center for Biological Sciences Research, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Viviane Martins Rebello dos Santos
Department of Chemistry, Institute of Exact and Biological Sciences, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil
Chagas disease (CD) is a worldwide public health problem, and the drugs available for its treatment have severe limitations. Red propolis is a natural extract known for its high content of phenolic compounds and for having activity against T. cruzi. The aim of this study was to investigate the trypanocidal potential of red propolis to isolate, identify, and indicate the mode of action of the bioactive compounds. The results revealed that the total phenolic content was 15.4 mg GAE/g, and flavonoids were 7.2 mg QE/g. The extract was fractionated through liquid–liquid partitioning, and the trypanocidal potential of the samples was evaluated using the epimastigote forms of the Y strain of T. cruzi. In this process, one compound was characterized by MS, 1H, and 13C NMR and identified as vestitol. Cytotoxicity was evaluated employing MRC-5 fibroblasts and H9C2 cardiomyocytes, showing cytotoxic concentrations above 15.62 μg/mL and 31.25 μg/mL, respectively. In silico analyses were applied, and the data suggested that the substance had a membrane-permeation-enhancing effect, which was confirmed through an in vitro assay. Finally, a molecular docking analysis revealed a higher affinity of vestitol with farnesyl diphosphate synthase (FPPS). The identified isoflavan appears to be a promising lead compound for further development to treat Chagas disease.
