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Use of molo glycoside in alpha-glucosaccharase inhibitor

A glucosidase and moroside technology, which is applied in the field of α-glucosidase inhibitor and moroside preparation, can solve the problem of not finding α-glucosidase inhibitory effect, not suitable for mass preparation and industrial production, and moroside. The unstable nature of glycosides and other problems can achieve the effect of controlling postprandial blood sugar, low cost and good glucose tolerance.

Inactive Publication Date: 2006-10-04
江苏吴中苏药医药开发有限责任公司
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  • Claims
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AI Technical Summary

Problems solved by technology

In 2004, Gao Xiaoping found that the extract of Cornus officinalis Sieb.et Zucc. had good α-glucosidase inhibitory effect (patent application number 03135217.0), but still did not explain which ingredients work
However, due to the instability of moroside, it is difficult to separate and the yield is low
The preparation method of morroniside invented by Xiao Wei et al. (patent application number 200410014771.2) uses reversed-phase silica gel, and the separation cost is high, so it is not suitable for mass preparation and industrial production
Moreover, due to the strong hygroscopicity of morroside, it is easy to form a syrupy substance with high viscosity, and it is difficult to obtain crystals, which makes its application difficult.
Morroside is considered to have the effect of nourishing bitterness and invigorating the stomach and the effect of preventing and treating diabetic vascular disease (patent application number 200410014771.2), and no reports of its α-glucosidase inhibitory effect have been found

Method used

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  • Use of molo glycoside in alpha-glucosaccharase inhibitor
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  • Use of molo glycoside in alpha-glucosaccharase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0026] Experimental Example 1 Inhibition of morroside on α-glucosidase

[0027] Purpose of the experiment: To observe the inhibitory effect of morroside on α-glucosidase in vitro by taking alglucoside as a positive control, and to provide in vitro test basis for the study of its mechanism of reducing postprandial blood sugar and improving glucose tolerance.

[0028] Experimental method: Morroside (self-made, content 97.6%) was prepared into 20, 8, 3.2, 1.28, 0.512, 0.2048, 0.08192, 0.032768, 0.013107, 0.005243 μg / μl test solutions with 0.1M phosphate buffer. Mix 40 μl of the test solution with 10 μl α-glucosidase (sigma, batch number WA15194), incubate at 37°C for 10 minutes, add 50 μl of 2.0 mmol / L maltose, continue to incubate at 37°C for 10 minutes, and terminate the reaction in a boiling water bath. The OD value was measured at 490nm by an oxidase microplate reader (BIO-RAD).

[0029] Positive control: Baitangping (Beijing Bayer Medicine and Health Care Co., Ltd., batch n...

experiment example 2

[0033] Experimental example 2 Research on the inhibition type of α-glucosidase by moroside

[0034] Purpose of the experiment: To study the type of inhibition of morroside on α-glucosidase in vitro, and to provide in vitro test basis for the study of its mechanism of lowering postprandial blood sugar and improving glucose tolerance.

[0035] Experimental method: Morroside (self-made, content 97.6%) was prepared into 20, 8 μg / μl test solution with 0.1M phosphate buffer. Under the condition of certain inhibitor concentration, the substrates were added respectively (the concentration is 0.25, 0.5, 1, 2, 3, 4, 5 mmol / l), and the enzyme activity was measured. By changing the inhibitor concentration, the enzyme activity under a series of different substrate concentrations can be obtained. The type of inhibition was determined by Lineweaver-Burk plot.

[0036] Experimental results: Lineweaver-Burk mapping ( figure 1 ) results showed that the inhibition type of α-glucosidase by mor...

experiment example 3

[0037] Experimental Example 3 Effect of Morroside on Blood Glucose, Glycated Serum Protein and Hepatic Glycogen in Streptozotocin Model Rats.

[0038]The purpose of the experiment: to observe the effect of oral administration of Cornus officinalis extract containing 30% morroside on the blood sugar, glycosylated serum protein and liver glycogen levels of streptozotocin model rats, using glucocorticoid as a positive control, for Clinical medication provides the basis for animal experiments.

[0039] Experimental method: Rats were fasted for 24 hours, each ip streptozotocin 70mg / kg, 0.5ml / 100g body weight. After 3 days of normal feeding, fasting for 12 hours, measure fasting serum glucose (FSG), the method is the same as before, FSG greater than 16.7mmol / L is a hyperglycemic rat. According to the blood sugar level, the hyperglycemic rats were divided into 5 groups, 10 in each group, respectively: model control group, positive drug group, test drug high, middle and low dose grou...

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Abstract

The invention provides a novel Moluo glycoside with natural source as an alpha-glucosidase depressant, and discloses a process for preparing the Moluo glycoside from natural plants such as Patrinia villosa Juss. and cornus officinalis. The invention also discloses the use of Muluo in treating diabetes.

Description

technical field [0001] The invention relates to an α-glucosidase inhibitor containing moroside as an active ingredient that can be used in medicines or health care products, and also relates to a method for preparing moroside from natural plants (such as patens and cornus officinalis), belonging to the field of traditional Chinese medicine. Background technique [0002] α-glucosidase is an enzyme that plays a key role in the metabolic process of the body. It is widely distributed in organisms and participates in many biological processes, such as digestion, biosynthesis of glycoproteins, synthesis and decomposition of polysaccharides and carbohydrate complexes Metabolism, etc., are closely related to many diseases caused by metabolic disorders, such as diabetes, cancer, viral infection and hereditary lysosomal storage diseases. α-glucosidase inhibitors can prevent and treat postprandial hyperglycemia and relieve hyperinsulinemia, and at the same time can improve glucose tole...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P3/04A61P3/10C07H1/08C07H17/04
Inventor 印敏楼凤昌曹庆先韩璟超季晖
Owner 江苏吴中苏药医药开发有限责任公司
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