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二芳基乙烯显示出体外抗结核活性，并且是靶向结核分枝杆菌HU蛋白的有效命中物。

Diarylethenes Display In Vitro Anti-TB Activity and Are Efficient Hits Targeting the Mycobacterium tuberculosis HU Protein.

作者信息

Suarez María Angélica, Valencia Jhesua, Cadena Christian Camilo, Maiti Raktim, Datta Chandreyee, Puerto Gloria, Isaza José Hipólito, San Juan Homero, Nagaraja Valakunja, Guzman Juan David

机构信息

Departamento de Química y Biología, División de Ciencias Básicas, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia.

Departamento de Medicina, División de Ciencias de la Salud, Universidad del Norte, Km 5 vía Puerto Colombia, Barranquilla 081007, Colombia.

出版信息

Molecules. 2017 Jul 25;22(8):1245. doi: 10.3390/molecules22081245.

DOI:10.3390/molecules22081245
PMID:28757569
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6151991/
Abstract

Tuberculosis continues to be a great source of concern in global health because of the large reservoir of humans infected with the bacilli and the appearance of clinical isolates resistant to a wide array of anti-tuberculosis drugs. New drugs with novel mechanisms of action on new targets are urgently required to reduce global tuberculosis burden. nucleoid associated protein (NAP) HU has been shown to be druggable and essential for the organism's survival. In this study, four diarylethenes were synthesized using a one-pot decarboxylated Heck-coupling of coumaric acids with iodoanisoles. The prepared compounds - were tested for their in vitro growth inhibition of H37Rv using the spot culture growth inhibition assay, displaying minimum inhibitory concentrations between 9 and 22 µM. Their cytotoxicity against BHK-21 cell line showed half inhibition at concentrations between 98 and 729 µM. The most selective hit (SI = 81), demonstrated inhibition of HU protein involved in maintaining bacterial genome architecture.

摘要

由于感染结核杆菌的人群基数庞大，且出现了对多种抗结核药物耐药的临床分离株，结核病仍然是全球卫生领域极为关注的问题。迫切需要研发针对新靶点、具有新作用机制的新型药物，以减轻全球结核病负担。已证明类核相关蛋白（NAP）HU是可成药的，且对该生物体的存活至关重要。在本研究中，通过香豆酸与碘代苯甲醚的一锅法脱羧Heck偶联反应合成了四种二芳基乙烯。使用斑点培养生长抑制试验测试了所制备化合物对H37Rv的体外生长抑制作用，其最低抑菌浓度在9至22 μM之间。它们对BHK - 21细胞系的细胞毒性在浓度为98至729 μM时表现出半数抑制。最具选择性的命中物（SI = 81）显示出对参与维持细菌基因组结构的HU蛋白具有抑制作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0ed7/6151991/5ccee6371660/molecules-22-01245-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0ed7/6151991/4f45524dfe39/molecules-22-01245-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0ed7/6151991/84112fcc2ea4/molecules-22-01245-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0ed7/6151991/5ccee6371660/molecules-22-01245-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0ed7/6151991/4f45524dfe39/molecules-22-01245-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0ed7/6151991/84112fcc2ea4/molecules-22-01245-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0ed7/6151991/5ccee6371660/molecules-22-01245-g002.jpg

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