Trypanosoma cruzi:: Activities of lapachol and α- and β-lapachone derivatives against epimastigote and trypomastigote forms

被引：119
|
作者：
Salas, Cristian [1 ]
Tapia, Ricardo A. [1 ]
Ciudad, Karina [1 ]
Armstrong, Veronica [1 ]
Orellana, Myriam [2 ]
Kemmerling, Ulrike [2 ]
Ferreira, Jorge [2 ]
Maya, Juan Diego [2 ]
Morello, Antonio [2 ]
机构：
[1] Pontificia Univ Catolica Chile, Fac Quim, Dept Quim Organ, Santiago 6094411, Chile
[2] Univ Chile, Fac Med, Dept Farmacol Mol & Clin, Santiago 7, Chile
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 02期
关键词：
D O I：
10.1016/j.bmc.2007.10.038
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Derivatives of natural quinones with biological activities, such as lapachol, alpha- and beta-lapachones, have been synthesized and their trypanocidal activity evaluated in vitro in Trypanosoma cruzi cells. All tested compounds inhibited epimastigote growth and trypomastigote viability. Several compounds showed similar or higher activity as compared with current trypanocidal drugs, nifurtimox and benznidazole. The results presented here show that the anti-T Cruzi activity of the alpha-lapachone derivatives can be increased by the replacement of the benzene ring by a pyridine moiety. Free radical production and consequently oxidative stress through redox cycling or production of electrophilic metabolites are the potential biological mechanism of action for these synthetic quinones. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：668 / 674
页数：7
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