Dimeric Flavonoids from Arrabidaea brachypoda and Assessment of Their Anti-Trypanosoma cruzi Activity

Autor(es)

da Rocha, Claudia Quintino ^[1] ; Queiroz, Emerson Ferreira ^[2] ; Meira, Cassio Santana ^[3] ; Magalhaes Moreira, Diogo Rodrigo ^[3] ; Pereira Soares, Milena Botelho ^[3] ; Marcourt, Laurence ^[2] ; Vilegas, Wagner ^[1] ; Wolfender, Jean-Luc ^[2]

Afiliação do(s) autor(es)

^[1] Univ Estadual Paulista, UNESP, Lab Biodiversidade & Sustentabilidade, BR-11330900 Sao Vicente - Brazil

^[2] Univ Lausanne, Univ Geneva, Sch Pharmaceut Sci Phytochem & Bioact Nat Prod, CH-1211 Geneva 4 - Switzerland

^[3] Fundacao Oswaldo Cruz Fiocruz, Ctr Pesquisas Goncalo Moniz, BR-40296710 Salvador, BA - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Journal of Natural Products; v. 77, n. 6, p. 1345-1350, JUN 2014.
• Citações Web of Science: 17

Resumo

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. (AU)

• Processo FAPESP: 09/17877-7 - Fitoterápicos padronizados para o tratamento de doenças crônicas: Arrabidaea spp
• Beneficiário: Cláudia Quintino da Rocha
• Linha de fomento: Bolsas no Brasil - Doutorado
• Processo FAPESP: 09/52237-9 - Fitoterápicos padronizados como alvo para o tratamento de doenças crônicas
• Beneficiário: Wagner Vilegas
• Linha de fomento: Auxílio à Pesquisa - Programa BIOTA - Temático