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Título: Valorizing constituents of cashew nut shell liquid toward the sustainable development of new drugs against chagas disease
Autor(es): Lemes, Laís Flávia Nunes
Magoulas, George E.
Oliveira, Andressa Souza de
Barrias, Emile
Nascente, Luciana de Camargo
Granado, Renato
Silva, Sara Teixeira de Macedo
Assimomytis, Nikos
Souza, Wanderley de
Bolognesi, Maria Laura
Romeiro, Luiz Antonio Soares
Calogeropoulou, Theodora
ORCID: https://orcid.org/0000-0002-1289-5361
https://orcid.org/0000-0001-5679-0820
https://orcid.org/0000-0002-3369-5393
Afiliação do autor: University of Brasília, Faculty of Medicine, Tropical Medicine Center
National Hellenic Research Foundation, Institute of Chemical Biology
University of Brasília, Faculty of Health Sciences, Department of Pharmacy
Universidade Federal do Rio de Janeiro, Instituto de Biofísica Carlos Chagas Filho
University of Brasília, Faculty of Health Sciences, Department of Pharmacy
National Institute of Metrology, Quality and Technology - Inmetro, Laboratory of Metrology Applied to Life Sciences
Universidade Federal do Rio de Janeiro, Centro Nacional de Biologia Estrutural e Bioimagem, Centro de Ciências da Saúde (CCS)
National Hellenic Research Foundation, Institute of Chemical Biology
Universidade Federal do Rio de Janeiro, Instituto de Biofísica Carlos Chagas Filho
Alma Mater Studiorum - University of Bologna, Department of Pharmacy and Biotechnology
University of Brasília, Faculty of Medicine, Tropical Medicine Center
University of Brasília, Faculty of Health Sciences, Department of Pharmacy
National Hellenic Research Foundation, Institute of Chemical Biology
Assunto: Castanha de caju
Atividade antiparasitária
Trypanosoma cruzi
Data de publicação: 12-Jun-2023
Editora: American Chemical Society
Referência: LEMES, Laís Flávia Nunes et al. Valorizing constituents of cashew nut shell liquid toward the sustainable development of new drugs against chagas disease. ACS Infectious Diseases, [S. l.], v. 9, n. 7, 1334-1345, 2023. DOI: https://doi.org/10.1021/acsinfecdis.3c00076.
Abstract: Six new ether phospholipid analogues encompassing constituents from cashew nut shell liquid as the lipid portion were synthesized in an effort to valorize byproducts of the cashew industry toward the generation of potent compounds against Chagas disease. Anacardic acids, cardanols, and cardols were used as the lipid portions and choline as the polar headgroup. The compounds were evaluated for their in vitro antiparasitic activity against different developmental stages of Trypanosoma cruzi. Compounds 16 and 17 were found to be the most potent against T. cruzi epimastigotes, trypomastigotes, and intracellular amastigotes exhibiting selectivity indices against the latter 32-fold and 7-fold higher than current drug benznidazole, respectively. Hence, four out of six analogues can be considered as hit-compounds toward the sustainable development of new treatments for Chagas disease, based on inexpensive agro-waste material.
Unidade Acadêmica: Faculdade de Medicina (FM)
Faculdade de Ciências da Saúde (FS)
Departamento de Farmácia (FS FAR)
DOI: https://doi.org/10.1021/acsinfecdis.3c00076
Versão da editora: https://pubs.acs.org/doi/10.1021/acsinfecdis.3c00076?ref=PDF
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