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商业制剂依米丁的各个成分并不比混合物具有更强的杀锥虫活性,也不能绕过依米丁耐药性。

The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance.

机构信息

Institute of Infection, Immunity and Inflammation, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, United Kingdom; Medical Biochemistry Department, Faculty of Basic Medical Sciences, College of Medicine, University of Nigeria, Enugu Campus, Enugu, Nigeria.

Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UK; Department of Chemistry, College of Science, University of Agriculture, Makurdi, Nigeria.

出版信息

Int J Parasitol Drugs Drug Resist. 2019 Apr;9:54-58. doi: 10.1016/j.ijpddr.2019.01.003. Epub 2019 Jan 21.

Abstract

The four components present in the trypanocidal treatment Samorin, the commercially available formulation of isometamidium, were separated and purified by column chromatography. These compounds as well as the Samorin mixture and the other phenanthridine trypanocide, homidium, were tested on Trypanosoma congolense and wild type, diamidine- and isometamidium-resistant Trypanosoma brucei brucei strains using an Alamar blue drug sensitivity assay. EC values obtained suggest that M&B4180A (2) was the most active of the components, followed by M&B38897 (1) in all the strains tested, whereas M&B4596 (4) was inactive. Samorin was found to be significantly more active than any of the individual components alone, against T. congolense and all three T. b, brucei strains. Samorin and all its active constituents displayed reduced activity against the previously characterised isometamidium-resistant strain ISMR1.

摘要

经柱层析分离和纯化,从噻苯咪唑治疗药物萨莫林(市售的异咪定制剂)中分离出四种成分。采用阿马蓝药物敏感性检测法,用这些化合物以及萨莫林混合物和另一种菲啶类杀锥虫药物羟咪定,对刚果锥虫和野生型、二脒定和异咪定耐药的布氏锥虫布鲁斯株进行了测试。得到的 EC 值表明,在所测试的所有菌株中,M&B4180A(2)是活性最强的成分,其次是 M&B38897(1),而 M&B4596(4)则没有活性。与单独使用任何一种成分相比,萨莫林对刚果锥虫和三种布氏锥虫布鲁斯株均显示出更高的活性。萨莫林及其所有活性成分对先前表征的异咪定耐药株 ISMR1 的活性均降低。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8374/6356087/f8336b96b7c3/fx1.jpg

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