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一种砷化合物(RM 110、美拉胂醇、环美胂醇)对敏感及耐药布氏布氏锥虫和伊氏锥虫的评估。

Evaluation of an arsenical compound (RM 110, mel Cy, Cymelarsan) against susceptible and drug-resistant Trypanosoma brucei brucei and T.b. evansi.

作者信息

Zweygarth E, Kaminsky R

机构信息

Kenya Trypanosomiasis Research Institute, Kikuyu.

出版信息

Trop Med Parasitol. 1990 Jun;41(2):208-12.

PMID:2382101
Abstract

The trypanocidal activity of an arsenical compound (RM 110; mel Cy; Cymelarsan) was tested in susceptible and drug-resistant stocks of T.b. brucei and T.b. evansi in vitro and in vivo. The trypanosome stocks showed different levels of susceptibility in an in vitro test, their IC50 values ranging from 3-26.9 nM. Mel Cy was 2.2-2.7 times more active against T.b. brucei stocks when compared to another arsenical (mel W; Trimelarsan). The logarithmically transformed IC50 values for both drugs obtained with T.b. brucei stocks correlated significantly. Significant correlations were also found between the log IC50 values of each of the two drugs and diminazene aceturate. In mice, the least susceptible stock was cured with a single i.p. dose of mel Cy which was about 16 times higher than that needed to cure a susceptible stock.

摘要

在体外和体内对布氏锥虫和伊氏锥虫的敏感株及耐药株测试了一种砷化合物(RM 110;美拉胂醇;环美胂醇)的杀锥虫活性。锥虫株在体外试验中表现出不同程度的敏感性,其IC50值在3 - 26.9 nM之间。与另一种砷化合物(美拉W;三美胂醇)相比,美拉胂醇对布氏锥虫株的活性高2.2 - 2.7倍。用布氏锥虫株获得的两种药物的对数转换IC50值显著相关。两种药物各自的log IC50值与乙酰氨基阿苯达唑之间也发现了显著相关性。在小鼠中,最不敏感的株系经单次腹腔注射美拉胂醇治愈,该剂量比治愈敏感株系所需剂量高约16倍。

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