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Inhibition of α-Amylases by Condensed and Hydrolysable Tannins: Focus on Kinetics and Hypoglycemic Actions

机译:缩合和可水解鞣质对α-淀粉酶的抑制作用:集中在动力学和降血糖作用上

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摘要

The aim of the present study was to compare the in vitro inhibitory effects on the salivary and pancreatic α-amylases and the in vivo hypoglycemic actions of the hydrolysable tannin from Chinese natural gall and the condensed tannin from Acacia mearnsii. The human salivary α-amylase was more strongly inhibited by the hydrolysable than by the condensed tannin, with the concentrations for 50% inhibition (IC50) being 47.0 and 285.4 μM, respectively. The inhibitory capacities of both tannins on the pancreatic α-amylase were also different, with IC50 values being 141.1 μM for the hydrolysable tannin and 248.1 μM for the condensed tannin. The kinetics of the inhibition presented complex patterns in that for both inhibitors more than one molecule can bind simultaneously to either the free enzyme of the substrate-complexed enzyme (parabolic mixed inhibition). Both tannins were able to inhibit the intestinal starch absorption. Inhibition by the hydrolysable tannin was concentration-dependent, with 53% inhibition at the dose of 58.8 μmol/kg and 88% inhibition at the dose of 294 μmol/kg. For the condensed tannin, inhibition was not substantially different for doses between 124.4 μmol/kg (49%) and 620 μmol/kg (57%). It can be concluded that both tannins, but especially the hydrolysable one, could be useful in controlling the postprandial glycemic levels in diabetes.
机译:本研究的目的是比较体外抑制唾液和胰腺α-淀粉酶的作用以及中药天然胆汁可水解单宁和金合欢浓缩单宁在体内的降血糖作用。人唾液α-淀粉酶受水解性的抑制作用强于缩合单宁,抑制50%(IC50)的浓度分别为47.0和285.4μM。两种单宁对胰腺α-淀粉酶的抑制能力也有所不同,可水解单宁的IC50值为141.1μm,缩合单宁的IC50值为248.1μm。抑制的动力学表现出复杂的模式,因为对于两种抑制剂,一个以上的分子可以同时与底物复合酶的任一游离酶结合(抛物线混合抑制)。两种单宁都能抑制肠淀粉的吸收。可水解单宁的抑制作用是浓度依赖性的,在58.8μmol/ kg的剂量下抑制率为53%,在294μμmol/ kg的剂量下抑制率为88%。对于缩合单宁,对于124.4μmol/ kg(49%)和620μμmol/ kg(57%)之间的剂量,抑制作用没有实质性差异。可以得出结论,两种单宁,特别是可水解单宁,可用于控制糖尿病的餐后血糖水平。

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