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一种针对亚马逊利什曼原虫的有效二芳基衍生物及其对寄生虫与巨噬细胞相互作用的影响。

An effective diaryl derivative against Leishmania amazonensis and its influence on the parasite X macrophage interaction.

作者信息

Alves Luciana V, Cysne-Finkelstein Léa, Temporal Rosane M, Genestra Marcelo S, Leon Leonor L

机构信息

Department of Immunology, Oswaldo Cruz Institute, FIOCRUZ, Rio de Janeiro, Brazil.

出版信息

J Enzyme Inhib Med Chem. 2004 Oct;19(5):437-9. doi: 10.1080/1475636042000198789.

Abstract

The activity of several diarylheptanoid derivatives (curcuminoids) was previously evaluated against Leishmania amazonensis promastigotes and among them the most active compound was 5-hydroxy-7- (4-hydroxy-3-methoxyphenyl)-1-(4-methoxyphenyl)-1,4,6-heptatrien-3-one. This study was carried out to investigate the influence of this diaryl derivative on the infective promastigotes and Balb/c mice peritoneal macrophage interaction. The potential in vitro toxicity was also evaluated. Promastigotes pretreated for 24 hours with the compound had their infective capacity significantly decreased. When the infection of Balb/c macrophage by L. amazonensis promastigotes was already installed, addition of the drug resulted in a diminishing of the infection rate. It was demonstrated that the compound was not toxic to the host macrophage in a concentration equivalent to the LD50/24h from the previous in vitro experiment.

摘要

先前评估了几种二芳基庚烷类衍生物(姜黄素类化合物)对亚马逊利什曼原虫前鞭毛体的活性,其中最具活性的化合物是5-羟基-7-(4-羟基-3-甲氧基苯基)-1-(4-甲氧基苯基)-1,4,6-庚三烯-3-酮。本研究旨在探讨这种二芳基衍生物对感染性前鞭毛体与Balb/c小鼠腹腔巨噬细胞相互作用的影响。还评估了其潜在的体外毒性。用该化合物预处理24小时的前鞭毛体其感染能力显著降低。当亚马逊利什曼原虫前鞭毛体对Balb/c巨噬细胞的感染已经发生时,加入该药物导致感染率降低。结果表明,在相当于先前体外实验中LD50/24h的浓度下,该化合物对宿主巨噬细胞无毒。

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