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WR6026作为预防输血传播的美洲锥虫病的潜在用途。

Potential use of WR6026 as prophylaxis against transfusion-transmitted American trypanosomiasis.

作者信息

Chiari E, Oliveira A B, Prado M A, Alves R J, Galvão L M, Araujo F G

机构信息

Department of Parasitology, Federal University of Minas Gerais, Belo Horizonte, MG, Brazil.

出版信息

Antimicrob Agents Chemother. 1996 Mar;40(3):613-5. doi: 10.1128/AAC.40.3.613.

Abstract

Since transmission of Chagas' disease by the insect vector is under control in Brazil, transmission by blood transfusion is acquiring special relevance in areas where the disease is endemic and also in countries whose populations are free of infection but that are receiving immigrants from areas where the disease is endemic. Gentian violet, a phenylmethane dye, was the first agent used for the chemical prophylaxis of blood destined for transfusion. A concentration of 0.6 mmol of this dye per liter is effective at eliminating trypomastigotes from blood after 24 h of incubation at 4 degrees C. It is the only effective trypanosomicidal agent available. In the search of alternate compounds, we examined a number of synthetic compounds. They were screened for their activities against blood trypomastigotes of the Y, CL, and B229 strains of Trypanosoma cruzi by using two or more dilutions of each compound. We found that compound Q45, a 6-methoxy-8(diethylaminohexylamino)lepidine dihydrochloride, was highly effective at clearing parasites from infected blood. Doses of 65 and 130 micrograms of this compound eliminated trypomastigotes from blood experimentally contaminated with T. cruzi parasites. These results indicate that Q45 is remarkably active against circulating trypomastigotes. Further studies evaluating Q45 as a prophylactic agent for preventing the transmission of T. cruzi by blood transfusion are of interest.

摘要

由于在巴西,恰加斯病通过昆虫媒介的传播已得到控制,在该病的流行地区以及在其本国人口无感染但接收来自流行地区移民的国家,输血传播正变得格外重要。结晶紫,一种苯甲烷染料,是第一种用于对输血用血液进行化学预防的药剂。每升血液中含有0.6毫摩尔这种染料,在4摄氏度下孵育24小时后,可有效清除血液中的锥鞭毛体。它是唯一可用的有效杀锥虫剂。在寻找替代化合物的过程中,我们研究了许多合成化合物。通过使用每种化合物的两种或更多种稀释液,对它们针对克氏锥虫Y、CL和B229菌株血液锥鞭毛体的活性进行了筛选。我们发现化合物Q45,即6-甲氧基-8(二乙氨基己基氨基)勒皮啶二盐酸盐,在清除感染血液中的寄生虫方面非常有效。65微克和130微克剂量的该化合物可从实验感染克氏锥虫寄生虫的血液中清除锥鞭毛体。这些结果表明,Q45对循环锥鞭毛体具有显著活性。进一步评估Q45作为预防输血传播克氏锥虫的预防剂的研究很有意义。

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