Anti-Trypanosoma cruzi Potential of Vestitol Isolated from Lyophilized Red Propolis-Reference-Cited by-同舟云学术

Anti-Trypanosoma cruzi Potential of Vestitol Isolated from Lyophilized Red Propolis

Published:2023-11-28 Issue:23 Volume:28 Page:7812
ISSN:1420-3049
Container-title:Molecules
language:en
Short-container-title:Molecules

Author:

Sousa Lucas Resende Dutra¹,Amparo Tatiane Roquete¹^ORCID,Souza Gustavo Henrique Bianco de¹^ORCID,Ferraz Aline Tonhela²,Fonseca Kátia da Silva²,Azevedo Amanda Scofield de³,Nascimento Andréa Mendes do³^ORCID,Andrade Ângela Leão³^ORCID,Seibert Janaína Brandão⁴,Valverde Thalita Marcolan⁵,Braga Saulo Fehelberg Pinto⁶^ORCID,Vieira Paula Melo de Abreu²^ORCID,Santos Viviane Martins Rebello dos³^ORCID

Affiliation:

1. Phytotechnology Laboratory, School of Pharmacy, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil

2. Morphopathology Laboratory, Center for Biological Sciences Research, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil

3. Department of Chemistry, Institute of Exact and Biological Sciences, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil

4. Natural Products Laboratory, Department of Chemistry, Federal University of São Carlos, Rod. Washington Luiz, Sao Carlos 13565-905, SP, Brazil

5. Department of Morphology, Institute of Biological Sciences, Federal University of Minas Gerais, Belo Horizonte 31270-901, MG, Brazil

6. Medicinal Chemistry and Bioassays Laboratory, School of Pharmacy, Federal University of Ouro Preto, Campus Morro do Cruzeiro, Ouro Preto 35400-000, MG, Brazil

Abstract

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.

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

Link

https://www.mdpi.com/1420-3049/28/23/7812/pdf

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