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Application of hesperetin to preparation of medicines for preventing and treating diabetes

A technology of hesperetin and diabetes, which is applied in the new application field of hesperetin or hesperidin, and can solve the problems such as exacerbation of type II diabetes

Inactive Publication Date: 2017-07-07
UNKNOWN +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, for patients with type II diabetes, when the activity of α-glucosidase is high, the ability to hydrolyze glycogen is strong, which increases the level of glucose in plasma, thereby aggravating type II diabetes, and even causing clinically severe as a result of

Method used

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  • Application of hesperetin to preparation of medicines for preventing and treating diabetes
  • Application of hesperetin to preparation of medicines for preventing and treating diabetes
  • Application of hesperetin to preparation of medicines for preventing and treating diabetes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1: Inhibitory effect of hesperetin on α-glucosidase

[0068] The following experiments were carried out under the conditions of the substrate system containing hesperetin and without hesperetin.

[0069] 1. The substrate system contains hesperetin

[0070] 1. Experimental method

[0071] (1) The α-glucosidase solution is mixed with different concentrations of hesperetin solutions at a volume ratio of 20:1, and the concentration of hesperetin after mixing is 0mM, 0.1mM, 0.2mM, 0.3mM, 0.4mM, 0.5mM, 0.8mM, 1.0mM, 1.5mM, 2.0mM, 2.5mM, in a water bath at 25°C for 10min, and 11 parts of the mixture were obtained.

[0072] (2) 10 μL of each part of the above mixture was added to 1 ml of the substrate system, wherein the substrate system was prepared from pNPG solution and corresponding concentration of hesperetin solution at a volume ratio of 95:5. The purpose of adding hesperetin here is to ensure that after adding to the substrate system, the concentration of he...

Embodiment 2

[0087] Example 2: Verification experiment of inhibition reversibility

[0088] In order to detect and verify the reversibility of hesperetin as an α-glucosidase inhibitor, to further prove the experimental results of Example 1, the relationship between the enzyme residual activity and the enzyme concentration was made under the condition of changing the concentration of hesperetin.

[0089] 1. Experimental method

[0090] (1) The α-glucosidase solution was mixed with different concentrations of hesperetin solutions (hesperetin concentrations: 0mM, 0.2mM, 0.5mM, 1.0mM and 2.0mM) at a volume ratio of 20:1, at 25°C In a water bath for 10 min, 5 parts of the mixture were obtained.

[0091] (2) 10 μL of the above mixture was added to 1 ml of the substrate system, wherein the substrate system was prepared from pNPG solution and hesperetin solution of corresponding concentration at a volume ratio of 95:5. The initial reaction concentration of the substrate pNPG is 2.0 mM, and [E]...

Embodiment 3

[0098] Example 3: Time course kinetics of the inhibitory effect of hesperetin on α-glucosidase

[0099] 1. Experimental method

[0100] (1) The α-glucosidase solution is mixed with different concentrations of hesperetin solutions (0mM, 1mM, 4mM, 6mM, 10mM, 16mM) at a volume ratio of 20:1 to obtain 6 parts of the mixture, which are placed in a water bath at 25°C , specified time intervals: 1, 2, 3, 4, 5, 10, 15, 20, 25, 30min, respectively take 10μL of the above mixture and add it to the substrate system (1ml) corresponding to the concentration of hesperetin, The substrate system is obtained by preparing pNPG solution and hesperetin solution of corresponding concentration at a volume ratio of 95:5. The initial reaction concentration of the substrate pNPG was 2.0 mM, and that of α-glucosidase was 0.1 μM.

[0101] (2) Measure the activity change of α-glucosidase with an ultraviolet spectrophotometer under the condition of emission wavelength 400nm / min, and the measurement tem...

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PUM

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Abstract

The invention belongs to the field of biological medicines, relates to hesperetin or novel application of hesperetin and particularly relates to hesperetin or pharmaceutically acceptable salts thereof or application of hesperetin or pharmaceutically acceptable salts to preparation of any one of the following medicines: (1) alpha-glucosidase inhibitors; (2) medicines for treating and / or preventing diabetes; and (3) medicines for treating and / or preventing tumor. The hesperetin is capable of effectively inhibiting alpha-glucosidase and has potential for preparing medicines for preventing and treating diabetes, especially type II diabetes.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a new application of hesperetin or hesperidin. Background technique [0002] Hesperetin (3',5,7-trihydroxy-4-methoxyflavanone, 3',5,7-trihydroxy-4'-methoxyflavanone) is commonly found in citrus fruits. Epidemiological studies have shown that increasing daily intake of hesperetin can reduce human mortality from cardiovascular disease, lung cancer and asthma. Studies have also shown that hesperetin can effectively treat many diseases, and it can produce a wide range of biological effects, including vasodilation, antioxidant effects, neuroprotection, anti-inflammatory effects, antiviral effects and cholesterol-lowering effects (Wang H, Wang H, Zhang H, et al. Inhibitory effects of hesperetin on Nav1.5 channels stably expressed in HEK 293 cells and on the voltage-gated cardiac sodium current in human atrial myocytes[J]. Acta Pharmacologica Sinica, 2016, 789: 98-108. ). The structural formu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P3/10A61K31/7036A61K31/133A61K31/445A61K31/155A61K45/06
CPCA61K31/352A61K31/133A61K31/155A61K31/445A61K31/7036A61K45/06A61K2300/00
Inventor 龚秦修远朴龙斗
Owner UNKNOWN
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