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Glycoside-hydrolase enzyme inhibitors

机译:糖苷水解酶抑制剂

摘要

This invention relates to inhibitors for glycosidehydrolases derived from bacteria of the order Actinomycetales, means for their production comprising cultivation of a microorganism of the order Actinomycetales in appropriate nutrient solutions under conditions most favorable to growth and production of the enzyme inhibitor and recovering, as a new product, glycoside-hydrolase enzyme inhibitors, from the culture as well as the use of said enzyme inhibitors in pharmaceutically acceptable therapeutic compositions in the treatment of conditions indicating obesity, diabetes, pre-diabetes, gastritis, gastric ulcer, hyperlipidemia (arteriosclerosis) and the like. The invention also contemplates the provision of methods of inhibiting the reaction of carbohydrates and glycoside-hydrolase enzymes and particularly carbohydrate-splitting glycoside-hydrolase enzymes of the digestive tract by means of conducting said reaction of said carbohydrates and glycoside- hydrolase enzymes in the presence of a glycoside-hydrolase enzyme inhibitor for said glycoside-hydrolase enzyme derived from a strain of microorganism of the order Actinomycetales. The invention further contemplates the provision of methods for the treatment of indications of the group consisting of obesity, adipose, hyperlipidemia (arteriosclerosis), diabetes, pre-diabetes, gastritis, gastric ulcer, duodenal ulcer, and caries induced by the action of glycoside-hydrolase enzymes and carbohydrates, the improvement which comprises employing an enzyme inhibitor for glycoside-hydrolase enzymes produced by a strain of microorganism of the order Actinomycetales.
机译:本发明涉及放线菌属细菌衍生的糖苷水解酶的抑制剂,其生产方法包括在合适的营养液中在最有利于酶抑制剂生长和生产并作为新的回收条件下培养放线菌微生物。产物,糖苷水解酶抑制剂,来自培养物,以及所述酶抑制剂在药学上可接受的治疗性组合物中的用途,用于治疗指示肥胖,糖尿病,糖尿病前期,胃炎,胃溃疡,高脂血症(动脉硬化)和喜欢。本发明还考虑了通过在有糖的存在下进行所述碳水化合物和糖苷水解酶的反应来抑制碳水化合物和糖苷水解酶特别是消化道的碳水化合物分解糖苷水解酶反应的方法。一种用于所述糖苷水解酶的糖苷水解酶抑制剂,其衍生自放线菌属的微生物菌株。本发明进一步预期提供用于治疗由糖苷-作用引起的肥胖症,脂肪,高脂血症(动脉硬化),糖尿病,糖尿病前期,胃炎,胃溃疡,十二指肠溃疡和龋齿的适应症的方法。水解酶和碳水化合物,该改进包括对由放线菌属的微生物菌株产生的糖苷水解酶使用酶抑制剂。

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