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没食子酸苯乙酯对体外和体内班氏丝虫的抗丝虫活性。

Antifilarial activity of caffeic acid phenethyl ester on Brugia pahangi in vitro and in vivo.

机构信息

a Faculty of Medicine, Department of Parasitology , University of Malaya , Kuala Lumpur , Malaysia.

c Faculty of Medicine and Health Science, Department of Para Clinic , University of Aden , Aden , Yemen.

出版信息

Pathog Glob Health. 2017 Oct;111(7):388-394. doi: 10.1080/20477724.2017.1380946. Epub 2017 Oct 25.

Abstract

Lymphatic filariasis (LF) is a vector borne disease caused by parasitic worms such as Wuchereria bancrofti, Brugia malayi and B. timori, which are transmitted by mosquitoes. Current therapeutics to treat LF are mainly microfilarcidal, and lack activity against adult worms. This set back, poses a challenge for the control and elimination of filariasis. Thus, in this study the activities of caffeic acid phenethyl ester (CAPE) against the filarial worm B. pahangi and its bacterial endosymbiont, Wolbachia were evaluated. Different concentrations (2, 5, 10, 15, 20 μg/ml) of CAPE were used to assess its effects on motility, viability and microfilarial (mf) production of B. pahangi in vitro. Anti-Wolbachial activity of CAPE was measured in worms by quantification of Wolbachial wsp gene copy number using real-time polymerase chain reaction. Our findings show that CAPE was found to significantly reduce adult worm motility, viability, and mf release both in vitro and in vivo. 20 μg/ml of CAPE halts the release of mf in vitro by day 6 of post treatment. Also, the number of adult worms recovered in vivo were reduced significantly during and after treatment with 50 mg/kg of CAPE relative to control drugs, diethylcarbamazine and doxycycline. Real time PCR based on the Wolbachia ftsZ gene revealed a significant reduction in Wolbachia copy number upon treatment. Anti-Wolbachia and antifilarial properties of CAPE require further investigation as an alternative strategy to treat LF.

摘要

淋巴丝虫病(LF)是一种由寄生虫引起的虫媒病,例如班氏丝虫、马来丝虫和帝汶丝虫,这些寄生虫通过蚊子传播。目前用于治疗 LF 的疗法主要是针对微丝蚴的,缺乏对成虫的活性。这一挫折对丝虫病的控制和消除构成了挑战。因此,在这项研究中,评估了咖啡酸苯乙酯(CAPE)对丝虫 B. pahangi 及其细菌共生体沃尔巴克氏体的活性。使用不同浓度(2、5、10、15、20μg/ml)的 CAPE 来评估其对 B. pahangi 体外运动性、活力和微丝蚴(mf)产生的影响。通过实时聚合酶链反应定量沃尔巴克氏体 wsp 基因拷贝数来测量 CAPE 对沃尔巴克氏体的抗活性。我们的研究结果表明,CAPE 被发现可显著减少成虫的运动性、活力和 mf 的释放,无论是在体外还是体内。20μg/ml 的 CAPE 在处理后第 6 天即可阻止 mf 的释放。此外,与对照药物乙胺嗪和多西环素相比,在治疗期间和治疗后,体内回收的成虫数量明显减少。基于沃尔巴克氏体 ftsZ 基因的实时 PCR 显示,在治疗后沃尔巴克氏体拷贝数显著减少。CAPE 的抗沃尔巴克氏体和抗丝虫特性需要进一步研究,作为治疗 LF 的替代策略。

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