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血管紧张素转换酶抑制活性测定综述:草药植物药物发现中的快速方法

Review of Angiotensin-converting Enzyme Inhibitory Assay: Rapid Method in Drug Discovery of Herbal Plants.

作者信息

Ahmad Islamudin, Yanuar Arry, Mulia Kamarza, Mun'im Abdul

机构信息

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Mulawarman University, Samarinda, East Kalimantan 75116, Depok, West Java 16424, Indonesia.

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java 16424, Indonesia.

出版信息

Pharmacogn Rev. 2017 Jan-Jun;11(21):1-7. doi: 10.4103/phrev.phrev_45_16.

Abstract

The renin-angiotensin-aldosterone system is a signaling pathway which responsible in the blood pressure regulation. Angiotensin-converting enzyme (ACE) is one of the key elements responsible for the hypertensive mechanism. It converts angiotensin-I to angiotensin-II. The discovery history of the ACE inhibitory activity assay method has been through a long stage for decades and development continues until today. The ACE inhibitory activity has become an effective screening method in the search for new antihypertensive agents from herbal plants. Some of assay methods were used to examine the activity of ACE inhibitors based on the substrate usage, such as; Cushman and Cheung Method using a substrate hippuryl-histidyl-leucine (HHL), Holmquist method using a substrate furanacryloyl-tripeptide, Elbl and Wagner method using a substrate benzoil-[l-14C] glicyl-L-histidine-L-leucine, Carmel and Yaron method using a substrate o-aminobenzoylglycyl-p-nitrophenylalanilproline, and Lam method using 3-hydroxybutyrylglycyl-glycyl-glycine as substrate. Several different methods to measure the results of enzymatic reactions or separating substrate with products, including spectrophotometric, fluorometric, high-performance liquid chromatography, electrophoresis, and radiochemistry. Application of the test method for screening the ACE inhibitors activity and investigation of active compounds from natural products can be done easily with this method, it is very helpful in research because the results obtained are simple, accurate, and rapid.

摘要

肾素-血管紧张素-醛固酮系统是一种负责调节血压的信号通路。血管紧张素转换酶(ACE)是高血压机制的关键要素之一。它将血管紧张素I转化为血管紧张素II。ACE抑制活性测定方法的发现历史经历了数十年的漫长阶段,并且发展一直持续到今天。ACE抑制活性已成为从草药植物中寻找新型抗高血压药物的一种有效筛选方法。一些测定方法基于底物的使用来检测ACE抑制剂的活性,例如:使用底物马尿酰-组氨酰-亮氨酸(HHL)的库什曼和张方法、使用底物呋喃丙烯酰三肽的霍尔姆奎斯特方法、使用底物苯甲酰-[l-14C]甘氨酰-L-组氨酸-L-亮氨酸的埃尔布尔和瓦格纳方法、使用底物邻氨基苯甲酰甘氨酰-对硝基苯丙氨酰脯氨酸的卡梅尔和亚龙方法以及使用3-羟基丁酰甘氨酰-甘氨酰-甘氨酸作为底物的林方法。有几种不同的方法来测量酶促反应的结果或分离底物与产物,包括分光光度法、荧光法、高效液相色谱法、电泳法和放射化学法。使用这种方法可以轻松地进行筛选ACE抑制剂活性的测试方法以及研究天然产物中的活性化合物,它在研究中非常有帮助,因为获得的结果简单、准确且快速。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2e73/5414448/4146d8ad748d/PRev-11-1-g001.jpg

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