Silva J S, Ferrioli-Filho F, Kanesiro M M, Ferreira V F, Santos S C, Pinto C N, Fonseca J L, Mizrahy H E, Gilbert B, Pinto M C
Departamento de Imunologia, Faculdade Medicina, USP, Ribeirão Preto, Brasil.
Mem Inst Oswaldo Cruz. 1992 Jul-Sep;87(3):345-51. doi: 10.1590/s0074-02761992000300003.
Accidental transmission of Chagas' disease to man by blood transfusion is a serious problem in Latin-America. This paper describes the testing of several synthetic, semi-synthetic, and natural compounds for their activity against blood trypomastigotes in vitro at 4 degrees C. The compounds embody several types of chemical structures: benzoquinone, naphthoquinone, anthracenequinone, phenanthrenequinone, imidazole, piperazine, quinoline, xanthene, and simple benzenic and naphthalenic derivatives. Some of them are for the first time tested against Trypanosoma cruzi. The toxic effect of these compounds on this parasite was done by two quite distinct sets of experiments. In one set, the compounds were added to infected blood as ethanolic solution. In this situation the most active one was a furan-1,2-naphthoquinone, in the same range as gentian violet, a new fact to be considered in the assessment of structure-activity relationships in this class of compounds. In other set, we tentatively evaluated the biological activity of water insoluble compounds by adding them in a pure form without solvent into infected blood. In this way some appear to be very active and it was postulated that the effectiveness of such compounds must result from interactions between them and specific blood components.
在拉丁美洲,因输血导致恰加斯病意外传播给人类是一个严重问题。本文描述了对几种合成、半合成和天然化合物在4摄氏度下体外抗血液锥鞭毛虫活性的测试。这些化合物包含几种化学结构类型:苯醌、萘醌、蒽醌、菲醌、咪唑、哌嗪、喹啉、呫吨以及简单的苯和萘衍生物。其中一些化合物首次针对克氏锥虫进行测试。通过两组截然不同的实验研究了这些化合物对该寄生虫的毒性作用。在一组实验中,将化合物以乙醇溶液形式添加到感染血液中。在这种情况下,最具活性的是一种呋喃 - 1,2 - 萘醌,其活性与龙胆紫相当,这是在评估此类化合物构效关系时需要考虑的一个新事实。在另一组实验中,我们通过将不溶于水的化合物以纯形式无溶剂添加到感染血液中,初步评估了它们的生物活性。结果发现有些化合物似乎非常活跃,并推测此类化合物的有效性必定源于它们与特定血液成分之间的相互作用。