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

被引：55

作者：

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
]}

机构：

[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

来源：

JOURNAL OF NATURAL PRODUCTS | 2014年 / 77卷 / 06期

基金：

巴西圣保罗研究基金会;

关键词：

PROTOZOAN NEGLECTED DISEASES; CHAGAS-DISEASE; SECONDARY METABOLITES; IN-VITRO; PLANTS; BIGNONIACEAE; CONSTITUENTS; DERIVATIVES; DRUGS; LEADS;

D O I：

10.1021/np401060j

中图分类号：

Q94 [植物学];

学科分类号：

071001 ;

摘要：

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.

引用

页码：1345 / 1350

页数：6

共 18 条

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