Inhibition of pepsin activity by alginates in vitro and the effect of epimerization
Inhibition of pepsin activity by alginates in vitro and the effect of epimerization
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DOI：
10.1016/j.ijpharm.2005.07.017
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发表时间：
2005-11-04
影响因子：
5.8
通讯作者：
Dettmar, PW
中科院分区：
文献类型：
--
作者：
Strugala, V;Kennington, EJ;Dettmar, PW
藻酸盐是广泛用于食品、纺织和制药工业的多功能生物聚合物。其中一个主要用途是在治疗反流病，在这里，我们调查是否藻酸盐可以影响胃蛋白酶的活动，在反流病的主要侵略者。可以使用差向异构酶技术改变藻酸盐的初级糖醛酸结构，并且我们测试定制的藻酸盐以鉴定用于胃蛋白酶抑制的最佳结构。在藻酸盐存在下的胃蛋白酶的活性进行了研究，使用体外N-末端测定和酶动力学，使用显色肽。所描述的数据清楚地表明，藻酸盐能够在体外以非竞争性方式浓度依赖性地降低胃蛋白酶的活性。这是不同的藻酸盐之间的广泛的结构和大小与交替序列的甘露糖醛酸和古洛糖醛酸的正相关性。我们推测，藻酸盐可能有一个更广泛的作用，在治疗反流性疾病，通过抑制胃蛋白酶，一个破坏性的成分反流。(c)2005年爱思唯尔B。V.保留所有权利。
Alginates are versatile biopolymers used extensively in the food, textile and pharmaceutical industries. One of the major uses is in the treatment of reflux disease and here we investigate whether alginates can influence pepsin activity, a major aggressor in reflux disease. The primary uronic acid structure of alginates can be altered using epimerase technology and we test tailor-made alginates to identify the optimal structure for pepsin inhibition. Pepsin activity in the presence of alginates was studied using an in vitro N-terminal assay and enzyme kinetics using a chromagenic peptide. The data described showed clearly that alginates were capable of concentration dependently reducing the activity of pepsin in a non-competitive manner, in vitro. This was variable between different alginates of wide ranging structure and size with positive correlation with alternating sequences of mannuronic and guluronic acid. We hypothesize that alginates may have a more extensive role in the treatment of reflux disease by inhibiting pepsin, a damaging component of the refluxate. (c) 2005 Elsevier B. V. All rights reserved.