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溴己新及其对脂肪酶的抑制作用 - 动力学和结构研究。

Bromhexine and its inhibitory effect on lipase - kinetics and structural study.

机构信息

Faculty of Life Sciences and Biotechnology, Shahid Beheshti University, Tehran, Iran.

出版信息

Arch Physiol Biochem. 2022 Dec;128(6):1687-1692. doi: 10.1080/13813455.2020.1788606. Epub 2020 Jul 7.

DOI:10.1080/13813455.2020.1788606
PMID:32633559
Abstract

Lipase hydrolyses the ester bonds in triglyceride. It is an important enzyme in medicine and industry. Some pathogen bacteria use this exoenzyme to disrupt the extracellular matrix of host organisms. uses various extracellular enzymes such as lipase to invade its host. In this report, for the first time, bromhexine was introduced as an inhibitor of lipase. Bromhexine is a mucolytic drug which is used in the treatment of respiratory tract disorders. The results showed that bromhexine inhibited the enzyme by competitive inhibition. IC and values of the drug were 0.049 mM and 0.02 mM, respectively. Arrhenius plot showed that the drug reduced the activation energy. The enzyme was purified and SDS-PAGE showed that its molecular weight is 13 kDa. Fluorescence measurement revealed that binding of the drug to lipase could make structural changes in the enzyme. Inhibition of lipase by bromhexine could be applicable in medicine.

摘要

脂肪酶水解甘油三酯中的酯键。它是医学和工业中的一种重要酶。一些病原体细菌利用这种外切酶破坏宿主生物的细胞外基质。利用各种细胞外酶,如脂肪酶,入侵其宿主。在本报告中,溴己新首次被引入作为脂肪酶的抑制剂。溴己新是一种黏液溶解药物,用于治疗呼吸道疾病。结果表明,溴己新通过竞争性抑制来抑制该酶。该药物的 IC 和 值分别为 0.049 mM 和 0.02 mM。Arrhenius 图表明该药物降低了活化能。该酶已被纯化,SDS-PAGE 显示其分子量为 13 kDa。荧光测量表明,药物与脂肪酶的结合可以使酶的结构发生变化。溴己新抑制脂肪酶的作用可能适用于医学领域。

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1
Bromhexine and its inhibitory effect on lipase - kinetics and structural study.溴己新及其对脂肪酶的抑制作用 - 动力学和结构研究。
Arch Physiol Biochem. 2022 Dec;128(6):1687-1692. doi: 10.1080/13813455.2020.1788606. Epub 2020 Jul 7.
2
Discovery of novel inhibitors for lipase enzyme from and studies.从[具体来源]发现新型脂肪酶抑制剂及相关研究。 (注:原文中“from and studies”表述不完整,推测可能是“from [具体来源] and studies” ,这里按推测完整表述翻译处理)
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[Pharmacological effects of brovanexine hydrochloride (BR-222) on the respiratory tract system, particularly on the respiratory tract fluid, mucociliary transport and cough].盐酸溴凡克新(BR - 222)对呼吸道系统的药理作用,特别是对呼吸道黏液、黏液纤毛转运和咳嗽的作用
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Bromhexine elevates REP2 expression to stimulate secretion from human primary conjunctiva fornix epithelial cells.溴己新通过提高 REP2 表达水平刺激人原发性结膜穹窿上皮细胞分泌。
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引用本文的文献

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Combining kinetics and in silico approaches to evaluate bromhexine as an anti-pancreatic lipase agent for obesity management.结合动力学和计算机模拟方法评估溴己新作为一种用于肥胖管理的抗胰脂肪酶药物。
Sci Rep. 2025 May 26;15(1):18420. doi: 10.1038/s41598-025-02625-4.
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Antimicrobial efficiency of bromhexine hydrochloride against endometritis-causing Escherichia coli and Trueperella pyogenes in bovines.盐酸溴己新对奶牛子宫内膜炎大肠杆菌和化脓隐秘杆菌的抗菌效果。
Braz J Microbiol. 2024 Jun;55(2):2013-2024. doi: 10.1007/s42770-024-01320-2. Epub 2024 Apr 19.