阅读说明：本技术 洋艾内酯A、B用作α-葡萄糖苷酶抑制剂进而用于制备降血糖药物的医药用途 (Pharmaceutical application of elaeagnus pungens A, B used as α -glucosidase inhibitor and further used for preparing hypoglycemic drugs ) 是由 朱阳晨 赵玲 于 2019-11-22 设计创作，主要内容包括：本发明公开了洋艾内酯A、B用作α-葡萄糖苷酶抑制剂进而用于制备降血糖药物的医药用途。本发明实施例研究结果表明,洋艾内酯A、洋艾内酯B对α-葡萄糖苷酶均具有显著的抑制作用,二者的抑制强度均优于阳性药阿卡波糖,二者可以用于制备降血糖药物。进一步地,与洋艾内酯A相比,洋艾内酯B对α-葡萄糖苷酶的抑制强度显著更高,是洋艾内酯A抑制强度的15倍以上,是一种更具有前景的降血糖药物。(The research result of the embodiment of the invention shows that the absinthin A, B has obvious inhibition effect on α -glucosidase, the inhibition intensity of both absinthin A and absinthin B is superior to that of positive drug acarbose, and the absinthin B can be used for preparing the hypoglycemic drug.)

1. A medicinal use of elaeostearolide A or elaeostearolide B as α -glucosidase inhibitor is provided.

2. The application of elaeagnus pungens lactone A or elaeagnus pungens lactone B in preparing α -glucosidase inhibitor medicine is provided.

3. The medical application of the absinthin A or B in preparing hypoglycemic drugs.

4. The pharmaceutical use according to claim 3, wherein the medicament is a pharmaceutical preparation, and the active ingredient of elaeagnus pungens A or B is prepared into a pharmaceutical preparation in a conventional dosage form by using conventional pharmaceutical excipients.

Technical Field

The invention belongs to the field of medicines, and particularly relates to a medical application of elaeagnus pungens A, B used as a α -glucosidase inhibitor and further used for preparing a hypoglycemic drug.

Background

Absintholide A and absintholide B are a pair of isomers which differ only in one linkage of-OH and-CH₃The chirality of the carbon atoms of (a), the chemical structure of absinthin A, B is as follows:

starch in food is digested into oligosaccharide containing a small number of glucose molecules, disaccharide and trisaccharide by salivary enzyme in oral cavity, gastric acid and pancreatic amylase in digestive tract, and membrane-bound enzyme, maltotriose and disaccharide water existing via brush border membrane of small intestine villus epithelial cellLyase (α -glucosidase, sucrase, maltase) and the like to decompose into monosaccharides, and Na such as glucose, lactose, maltose and the like directly existing through brush border membrane⁺Dependence mechanism (Na)⁺The α -glucosidase inhibitor can be combined with the central active site of α -glucosidase in the small intestine to inhibit the exertion of enzyme activity, block the hydrolysis of disaccharide into monosaccharide, and prolong the absorption time, thereby being beneficial to reducing postprandial hyperglycemia.

That is, α -glucosidase inhibitor can competitively inhibit glucoside hydrolase, further inhibit decomposition of polysaccharide and sucrose, inhibit absorption of carbohydrate in upper part of small intestine, slow increase of postprandial blood sugar, prevent cardiovascular diseases caused by blood sugar fluctuation, etc. α -glucosidase inhibitor is an active ingredient of a suitable auxiliary blood sugar lowering drug.

At present, there is no report that the absinthin A, B is used as a α -glucosidase inhibitor and is further used for preparing hypoglycemic drugs.

Disclosure of Invention

The invention aims to provide a new application of elaeagnus pungens A, B, and particularly provides a medical application of elaeagnus pungens A, B used as a α -glucosidase inhibitor and further used for preparing a hypoglycemic drug.

The technical scheme of the invention is as follows:

a medicinal use of elaeostearolide A or elaeostearolide B as α -glucosidase inhibitor is provided.

The application of elaeagnus pungens lactone A or elaeagnus pungens lactone B in preparing α -glucosidase inhibitor medicine is provided.

The medical application of the absinthin A or B in preparing hypoglycemic drugs.

Further, the medicine is a medicinal preparation, and the active ingredient of the elaeagnus pungens lactone A or the elaeagnus pungens lactone B is prepared into a medicinal preparation with a conventional dosage form by using conventional medicinal auxiliary materials.

The beneficial technical effects are as follows:

the invention discovers that the absinthin A and the absinthin B both have obvious inhibition effect on α -glucosidase, the inhibition intensity of both is superior to that of the positive drug acarbose, and both can be used for preparing hypoglycemic drugs.

Drawings

FIG. 1 is a comparison of IC50 values of absinthin A, absinthin B and positive drug against α -glucosidase inhibition.

Detailed Description

The following examples are intended to illustrate the essence of the present invention, but should not be construed as limiting the scope of the present invention.