In vitro and in vivo trypanocidal activity of the ethyl esters of N-allyl and N-propyl oxamates using different Trypanosoma cruzi strains

被引：8
作者：
Aguirre-Alvarado, Charmina
Zaragoza-Martinez, Fabiola
Rodriguez-Paez, Lorena
Nogueda, Benjamin
Baeza, Isabel
Wong, Carlos
机构：
[1] Inst Politecn Nacl, Dept Bioquim, Escuela Nacl Ciencias Biol, Mexico City 06401, DF, Mexico
[2] Inst Politecn Nacl, Dept Parasitol, Escuela Nacl Ciencias Biol, Mexico City 06401, DF, Mexico
来源：
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2007年 / 22卷 / 02期
关键词：
Trypanosoma cruzi; (alpha-hydroxyacid dehydrogenase-isozyme II inhibition; ethyl N-allyl oxamate; ethyl N-propyl oxamate; (alpha-hydroxyacid dehydrogenase (HADH);
D O I：
10.1080/14756360601051233
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：
The trypanocidal activity of N-allyl (NAOx) and N-propyl (NPOx) oxamates and that of the ethyl esters of N-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested on cultured epimastigotes ( in vitro) and murine trypanosomiasis ( in vivo) using five different T. cruzi strains. NAOx and NPOx did not penetrate intact epimastigotes and therefore we were not able to detect any trypanocidal effect with these oxamates. Whereas the ethyl esters (Et-NAOx and Et-NPOx), acting as prodrugs, exhibited in vitro and in vivo trypanocidal activity on the five tested T. cruzi strains. On the contrary, when Nifurtimox and Benznidazole used as reference drugs were tested, we found that only three of the five tested T. cruzi strains were affected, whereas the other two strains, Miguz and Compostela, were resistant to the in vitro and in vivo trypanocidal activity of these compounds.
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收藏
页码：227 / 233
页数：7
相关论文
共 25 条
[1]   THE CARBOXYLESTERASES OF TRYPANOSOMA-CRUZI EPIMASTIGOTES [J].
ALDUNATE, J ;
REPETTO, Y ;
LETELIER, ME ;
MORELLO, A .
COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY B-BIOCHEMISTRY & MOLECULAR BIOLOGY, 1987, 86 (01) :67-71
[2]   The Trypanosoma cruzi proteome [J].
Atwood, JA ;
Weatherly, DB ;
Minning, TA ;
Bundy, B ;
Cavola, C ;
Opperdoes, FR ;
Orlando, R ;
Tarleton, RL .
SCIENCE, 2005, 309 (5733) :473-476
[3]   Metabolic control analysis of glycolysis in trypanosomes as an approach to improve selectivity and effectiveness of drugs [J].
Bakker, BM ;
Westerhoff, HV ;
Opperdoes, FR ;
Michels, PAM .
MOLECULAR AND BIOCHEMICAL PARASITOLOGY, 2000, 106 (01) :1-10
[4]   Activity of lytic peptides against intracellular Trypanosoma cruzi amastigotes in vitro and parasitemias in mice [J].
Barr, SC ;
Rose, D ;
Jaynes, JM .
JOURNAL OF PARASITOLOGY, 1995, 81 (06) :974-978
[5]  
Brener Z., 1984, Memorias do Instituto Oswaldo Cruz, V79, P149, DOI 10.1590/S0074-02761984000500026
[6]  
BRONFEN E, 1989, MEM I O CRUZ, V84, P234
[7]   Trypanocidal activity of N-isopropyl oxamate on cultured epimastigotes and murine trypanosomiasis using different Trypanosoma cruzi strains [J].
Chena, MA ;
Elizondo, S ;
Rodríguez-Páez, L ;
Nogueda, B ;
Baeza, I ;
Wong, C .
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 2005, 20 (02) :189-197
[8]   Trypanosoma cruzi:: Inhibition of α-hydroxyacid dehydrogenase isozyme II by N-allyl and N-propyl oxamates and their effects on intact epimastigotes [J].
Chena, MA ;
Elizondo-Jiménez, S ;
Rodríguez-Páez, L ;
Nogueda-Torres, B ;
Baeza-Ramírez, I ;
Wong-Ramírez, C .
MEMORIAS DO INSTITUTO OSWALDO CRUZ, 2004, 99 (08) :831-837
[9]  
Chiari E, 1989, Rev Soc Bras Med Trop, V22, P19, DOI 10.1590/S0037-86821989000100004
[10]   PROPERTIES OF ALPHA-HYDROXYACID DEHYDROGENASE ISOZYMES FROM TRYPANOSOMA-CRUZI [J].
CORONEL, C ;
ROVAI, LE ;
DEBURGOS, NMG ;
BURGOS, C ;
BLANCO, A .
MOLECULAR AND BIOCHEMICAL PARASITOLOGY, 1981, 4 (1-2) :29-38
123