Dimeric Flavonoids from Arrabidaea brachypoda and Assessment of Their Anti-Trypanosoma cruzi Activity
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- 作者：Cl谩udia Quintino da Rocha ; Emerson Ferreira Queiroz ; C谩ssio Santana Meira ; Diogo Rodrigo Magalh茫es Moreira ; Milena Botelho Pereira Soares ; Laurence Marcourt ; Wagner Vilegas ; Jean-Luc Wolfender
- 刊名：Journal of Natural Products
- 出版年：2014
- 出版时间：June 27, 2014
- 年：2014
- 卷：77
- 期：6
- 页码：1345-1350
- 全文大小：273K
- ISSN：1520-6025
文摘
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鈥?b>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.