Carbon Nanotubes Inhibit the Pepsin Activity at High Ionic Strength

Q4 Pharmacology, Toxicology and Pharmaceutics Current Enzyme Inhibition Pub Date : 2020-11-04 DOI:10.2174/1573408016999200603170618
K. M. Jasem, H. Al-Hakeim, Jawad Kadhem Al-Shams
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引用次数: 1

Abstract

Gastroesophageal reflux disease (GERD) is a common chronic gastrointestinal disorder in adults that occurs as the stomach contents reflux and come up into the esophagus due to a dysfunction in the lower oesophageal sphincter. One approach commonly used to treat GERD is inhibition of the activity of pepsin enzyme. Carbon nanotubes (CNTs) are nanoparticles of carbon atoms that possess numerous interesting physical and chemical properties. CTNs functionalization expands the range of their properties to make them soluble in biological fluids and to confer the property of carrying drug or biological macromolecules which increase the scope of their applications in biomedical science. This study aims to utilize CNTs as a pepsin inhibitor and as a new medication for the treatment of GERD. The pepsin activity before and after the addition of an exact amount of the CNTs to the reaction mixture was measured colorimetrically. The results showed that both Vmax and Km changed after the addition of CNTs to the pepsin solution indicating a mixed inhibition of pepsin activity. This finding pointed to the ability of CNTs to bind with the pepsin molecule and pepsin-protein complex, therefore inhibiting the enzyme activity. The findings also demonstrated a complete inhibition of pepsin activity by CNTs when increasing the ionic strength of the reaction mixture. It can be inferred that using CNTs at a high concentration of NaCl at 37°C is the optimal condition for pepsin inhibition.
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碳纳米管在高离子强度下抑制胃蛋白酶活性
胃食管反流病(GERD)是一种常见的成人慢性胃肠道疾病,发生于胃内容物反流,并由于食管下括约肌功能障碍而进入食道。一种常用的治疗GERD的方法是抑制胃蛋白酶的活性。碳纳米管是碳原子的纳米颗粒,具有许多有趣的物理和化学性质。CTNs功能化扩大了其性质的范围,使其可溶于生物流体,并赋予其携带药物或生物大分子的性质,这增加了其在生物医学科学中的应用范围。本研究旨在利用CNTs作为胃蛋白酶抑制剂和治疗胃食管反流病的新药。在向反应混合物中加入精确量的CNT之前和之后的胃蛋白酶活性用色度法测量。结果表明,在胃蛋白酶溶液中加入CNTs后,Vmax和Km都发生了变化,表明胃蛋白酶活性受到混合抑制。这一发现表明CNTs能够和胃蛋白酶分子和胃蛋白酶蛋白复合物结合,从而抑制酶的活性。研究结果还表明,当增加反应混合物的离子强度时,CNT完全抑制胃蛋白酶活性。可以推断,在37°C的高浓度NaCl下使用CNTs是抑制胃蛋白酶的最佳条件。
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来源期刊
Current Enzyme Inhibition
Current Enzyme Inhibition Pharmacology, Toxicology and Pharmaceutics-Drug Discovery
CiteScore
1.30
自引率
0.00%
发文量
30
期刊介绍: Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.
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