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Cordycepin (3'-deoxyadenosine) and pentostatin (deoxycoformycin) against Trypanosoma cruzi

机译:冬虫夏蛋白(3'-脱氧腺苷)和五酮蛋白(脱氧基霉素)对抗锥虫瘤Cruzi

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摘要

The aim of this study was to evaluate in vitro the efficacy of cordycepin and pentostatin (alone or combined) against Trypanosoma cruzi, as well as the therapeutic efficiency of protocols of cordycepin and pentostatin combinations in mice experimentally infected with T.cruzi. In vitro, the cordycepin (3'-deoxyadenosine) and pentostatin (deoxycoformycin) exerted potent trypanocidal effect against T. cruzi (Colombian strain), similarly to benznidazole, which is the reference drug. For epimastigotes, the lethal dose of cordycepin capable of killing 50% (LD50) and 20% (LD20) of the parasites was 0.072 and 0.031 mg/mL, respectively and for trypomastigotes was 0.047 and 0.015 mg/mL, respectively. The combined use of cordycepin and pentostatin resulted in a LD50 and LD20 for epimastigotes of 0.068 and 0.027 mg/mL, respectively, as well as 0.056 and 0.018 mg/mL for trypomastigotes, respectively. In vivo, the combined use of cordycepin and pentostatin did not show the expected curative effect, however it was able to control the parasitema in the peak period. In summary, the combination of cordycepin and pentostatin showed no curative effect in mice infected by T. cruzi, despite the in vitro reduction of epimastigotes and trypomastigotes.
机译:本研究的目的是评估冬虫夏素和五酮蛋白(单独或组合)对睾丸瘤Cruzi的疗效,以及在实验感染的小鼠中冬虫夏宾和五阳蛋白组合的疗效效果。体外,冬虫夏蛋白(3'-脱氧糖苷)和五酮蛋白(脱氧基霉素)对T.Cruzi(哥伦比亚菌株)施加有效的胰蛋白酶作用,类似于苯并咪唑,即作为参考药物。对于Epimastigotes,能够杀死50%(LD50)和20%(LD20)寄生虫的肠道剂量分别为0.072和0.031mg / ml,分别为胰蛋白酶,分别为0.047和0.015mg / ml。冬虫夏蛋白和五酮蛋白的结合使用,分别为0.068和0.027mg / ml的偏移引起的LD50和LD20,分别为0.056和0.018mg / ml,用于Trypomastigotes。在体内,冬虫夏素和五酮蛋白的结合使用没有显示预期的疗效,但它能够在峰值期内控制寄生虫。总之,冬虫氏素和五酮肽的组合表明,尽管对椎间壳素和肌动蛋白酶的体外还原,但肠道蛋白酶和五酮蛋白的组合表现出T.Cruzi感染的疗效。

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