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Title: Dimeric flavonoids from Arrabidaea brachypoda and assessment of their anti-Trypanosoma cruzi activity.
Authors: Rocha, Cláudia Quintino da
Queiroz, Emerson Ferreira
Meira, Cássio Santana
Moreira, Diogo Rodrigo Magalhães
Soares, Milena Botelho Pereira
Marcourt, Laurence
Vilegas, Wagner
Wolfender, Jean-Luc
Affilliation: Universidade Estadual Paulista. Laboratório de Biodiversidade e Sustentabilidade. UNESP  Coastal Campus, Parque Bitaru
Abstract: The nonpolar fraction of an aqueous ethanol extract of the roots of Arrabidaea brachypoda, a Brazilian medicinal plant, demonstrated significant in vitro activity against Trypanosoma cruzi, the parasite responsible for Chagas disease. Targeted isolation of the active constituents led to the isolation of three new dimeric flavonoids (1-3), and their structures were elucidated using UV, NMR, and HRMS analysis, as well as by chemical derivatization. The anti-T. cruzi activity and cytotoxicity toward mammalian cells were determined for these substances. Compound 1 exhibited no activity toward T. cruzi, while flavonoids 2 and 3 exhibited selective activity against these trypomastigotes. Compounds 2 and 3 inhibited the parasite invasion process and its intracellular development in host cells with similar potencies to benznidazole. In addition, compound 2 reduced the blood parasitemia of T. cruzi-infected mice. This study has revealed that these two dimeric flavonoids represent potential anti-T. cruzi lead compounds for further drug development.
DeCS: Bignoniaceae/química
Flavonoides/isolamento & purificação
Tripanossomicidas/isolamento & purificação
Trypanosoma cruzi/efeitos de drogas
Cercopithecus aethiops
Macrófagos Peritoneais/efeitos de drogas
Estrutura Molecular
Testes de Sensibilidade Parasitária
Celulas vero
Issue Date: 2014
Publisher: ACS Publications
Citation: ROCHA, C. et al. Dimeric flavonoids from Arrabidaea brachypoda and assessment of their anti-Trypanosoma cruzi activity. Journal of Natural Products, v. 77, n. 66, p. 1345-1350, 2014.
DOI: 10.1021/np401060j
ISSN: 1520-6025
Copyright: open access
Appears in Collections:BA - IGM - Artigos de Periódicos

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