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委内瑞拉药用植物的抗分枝杆菌及PknB抑制活性

Antimycobacterial and PknB Inhibitory Activities of Venezuelan Medicinal Plants.

作者信息

Aranaga C A, Fraile S, Torres A, Falco A, Michelangeli F, Takiff H

机构信息

Grupo de Investigación en Química y Biotecnología, Facultad de Ciencias Básicas, Universidad Santiago de Cali, Cali, Colombia.

Laboratorio de Genética Molecular, Instituto Venezolano de Investigaciones Científicas, Caracas, Venezuela.

出版信息

Int J Microbiol. 2020 Aug 1;2020:8823764. doi: 10.1155/2020/8823764. eCollection 2020.

Abstract

Global control and elimination of tuberculosis are hindered by the high prevalence of drug-resistant strains, making the development of new drugs to fight tuberculosis a public health priority. In this study, we evaluated 118 extracts from 58 Venezuelan plant species for their ability to inhibit the growth of mc6020, using the agar dilution method. Additionally, we determined the ability of these extracts to inhibit the activity of PknB protein, an essential serine/threonine kinase, using a high-throughput luminescent assay. Of the 118 extracts tested, 14 inhibited bacterial growth with a minimum inhibitory concentration ≤500 g/ml, and 36 inhibited the kinase activity with a half-maximal inhibitory concentration <200 g/ml. Five extracts inhibited growth and inhibited the activity of the kinase protein, suggesting that this could be the basis of their growth inhibition.

摘要

耐药菌株的高流行率阻碍了全球结核病的控制和消除,这使得开发抗结核新药成为公共卫生的优先事项。在本研究中,我们使用琼脂稀释法评估了来自58种委内瑞拉植物物种的118种提取物抑制mc6020生长的能力。此外,我们使用高通量发光测定法确定了这些提取物抑制必需的丝氨酸/苏氨酸激酶PknB蛋白活性的能力。在测试的118种提取物中,14种以最小抑菌浓度≤500μg/ml抑制细菌生长,36种以半数最大抑制浓度<200μg/ml抑制激酶活性。五种提取物抑制生长并抑制激酶蛋白的活性,这表明这可能是它们抑制生长的基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/39b8/7416274/7de81ba0eac4/ijmicro2020-8823764.001.jpg

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