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首页> 外文期刊>International Journal of Biological Macromolecules: Structure, Function and Interactions >GdTI, the first thermostable trypsin inhibitor from Geoffroea decorticans seeds. A novel natural drug with potential application in biomedicine
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GdTI, the first thermostable trypsin inhibitor from Geoffroea decorticans seeds. A novel natural drug with potential application in biomedicine

机译：GDTI是来自Geoffroea二晶体种子的第一个热稳定胰蛋白酶抑制剂。 一种新的天然药物，具有生物医学的潜在应用

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摘要

A novel thermostable trypsin inhibitor was obtained from Geoffroea decorticans seeds. G. decorticans trypsin inhibitor (GdTI) is a protein with molecular mass of 6743.7 Da, with a potent inhibitory activity (Ki of 2.1 nM) even at high temperatures and extreme pHs (100% after 5 hat 100 degrees C and 80% after 60 min at pH 2-12) constituting one of the most powerful serine protease inhibitors isolated from a plant source. GdTI displays anticoagulant activity against both extrinsic and intrinsic coagulation pathways, representing the first report of a plant serine protease inhibitor with anticoagulant activity against the extrinsic pathway. Finally, GdTI showed inhibitory activity against alpha-glucosidase (IC50 of 0.18 mu M) evidencing the hypoglycemic effect of this inhibitor. Our results evidence the discovery of a natural molecule with unique features: i) GdTI is one of the most potent serine protease inhibitors founded to date, ii) with the most powerful thermostability reported in literature, iii) with anticoagulant effect against both coagulation pathways and hypoglycemic activity. This report suggest that GdTI could be exploited as a natural and hyperstable antidiabetic drug, in behalf of its antithrombotic and hypoglycemic activities, encouraging future studies with high impact on biomedical research and potential pharmaceutical applications. (C) 2020 Elsevier B.V. All rights reserved.
机译：热稳定的胰蛋白酶抑制剂是从Geoffroea获得一种新颖的decorticans种子。 G. decorticans胰蛋白酶抑制剂（GDTI）与6743.7道尔顿分子量的蛋白质，具有有效的抑制活性（2.1纳米的KI）即使在高温下和极端pH（100％后的5帽子100℃和60后80％分钟在pH 2-12）从植物来源分离的最强大的丝氨酸蛋白酶抑制剂的构成一个。 GDTI显示抗凝血活性对抗外在和内在的凝血途径，较靠外源性途径的抗凝血活性的植物的丝氨酸蛋白酶抑制剂的第一份报告。最后，GDTI显示抑制活性抗α-葡糖苷酶，证明此抑制剂的降血糖作用（0.18微米IC50）。我们的研究结果证明具有独特的功能自然分子的发现：1）GDTI是成立迄今最有力的丝氨酸蛋白酶抑制剂之一，ii）与最强大的热稳定性文献报道，iii）与对两种凝血途径的抗凝血作用和降血糖活性。这份报告表明，GDTI可能被利用作为一种自然和超稳定抗糖尿病药，代其抗血栓和降血糖作用，鼓励未来在生物医学研究和潜在的药用应用的高影响的研究。 （c）2020 Elsevier B.v.保留所有权利。

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