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Application of hesperetin in preparation of drug for inhibiting activity of beta secretase

An active drug, orange peel technology, applied in the application, drug combination, organic active ingredients and other directions, can solve the problems of retinopathy, no safe and effective drugs, safety problems, etc., to reduce wrong cutting, enhance learning and memory ability, Improve the effect of Alzheimer's disease

Inactive Publication Date: 2021-02-26
JIANGHAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, currently known several drugs, such as BACE-1 inhibitors, virus-encapsulated BACE1-siRNA, etc., usually have unimaginable side effects, such as severe retinopathy or other safety issues
At present, there is no suitable safe and effective drug at home and abroad
However, there is no research on the target of tangeretin for Alzheimer's disease

Method used

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  • Application of hesperetin in preparation of drug for inhibiting activity of beta secretase
  • Application of hesperetin in preparation of drug for inhibiting activity of beta secretase
  • Application of hesperetin in preparation of drug for inhibiting activity of beta secretase

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 Tangeretin Inhibition of BACE-1 Activity

[0024] This example adopts the method of molecular docking simulation to study and compare the tangeretin molecule (purchased from Chengdu Purifa Technology Development Co., Ltd.) and the known chemically synthesized BACE-1 inhibitor BACE1-IN-1 (purchased from Shanghai Tao Su Biochemical Technology Co., Ltd.) and BACE1 binding ability, the specific operation is as follows:

[0025] The BACE-1 molecule (PDB ID: 2WJO) removed the small molecule (QUD) and all the water molecules bound to it by the PyMOL Molecular Graphics System (2.4.0) software, and evenly distributed the charge and added by Autodock Tools4.2 hydrogen atom. The structural files of both tangeretin and BACE-IN-1 molecules were downloaded from the NCBI database. The software used for molecular docking is Autodock4.2, the docking algorithm is Lamarck genetic algorithm, and the scope of molecular docking is the overall structure of BACE-1.

[0026] The do...

Embodiment 2

[0027] Example 2 Tangeretin improves APP / PS1 mice's learning and memory ability and inhibits BACE-1 activity Experimental model: Alzheimer's disease transgenic mouse model, ie APP / PS1 double transgenic mice.

[0028] Experimental method: choose 12 APP / PS1 mice of the age of two and a half months, and divide them into two groups on average. The administration group (Tangeretin group) orally administrates 100 mg / kg Tangeretin (dissolved in 1% carboxymethylcellulose) every day. sodium aqueous solution), and the model group (APP / PS1 group) was orally administered 1% sodium carboxymethylcellulose aqueous solution of the same volume every day. Four months later, the Morris water maze test was used to evaluate the learning and memory levels of the two groups of animals: when the Morris water maze was trained for 5 days, the detection results of the mice's escape latency were as follows: figure 2 Shown; Morris water maze training for 6 days, the detection results of the number of tim...

Embodiment 3

[0033]Tangeretin can be made into different dosage forms or products, so as to make a drug for inhibiting the activity of β-secretase or a drug for treating diseases caused by enhanced activity of β-secretase.

[0034] Tangeretin can be made into tablets, which include the following components in parts by weight: 55 parts of Tangeretin, 44 parts of anhydrous lactose, and 1 part of magnesium stearate;

[0035] Tangeretin can be made into granules, which include the following components in parts by weight: 75 parts of Tangeretin and 25 parts of anhydrous lactose.

[0036] Tangeretin can be made into milk powder, which includes the following components in parts by weight: 20 parts of Tangeretin, 70 parts of skimmed milk powder, 5 parts of xylitol, and 5 parts of erythritol.

[0037] Tangeretin can be made into a solid drink, which includes the following components in parts by weight: 30 parts of Tangeretin, 30 parts of skimmed milk powder, 10 parts of Antarctic krill oil powder, ...

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Abstract

The invention discloses application of hesperetin in preparation of a drug for inhibiting the activity of beta secretase, and also discloses application of the hesperetin in preparation of a drug fortreating diseases caused by activity enhancement of the beta secretase. The invention explores that the action target of the hesperetin is the beta secretase for the first time. The invention discovers and verifies that the hesperetin has the capability of combining the beta secretase similar to that of a beta secretase inhibitor; the hesperetin is combined with the beta secretase and inhibits theactivity of the beta secretase, so that the error shearing of the beta secretase on amyloid precursor protein is reduced; and further the generation and error accumulation of amyloid A beta in the brain are reduced, and thus the effects of improving Alzheimer's disease and enhancing learning and memory abilities are achieved. Moreover, the hesperetin has the effect of inhibiting the activity of the beta secretase, so that any disease caused by the activity enhancement of the beta secretase can be improved and treated by the hesperetin.

Description

technical field [0001] The invention relates to the technical field of medicine and health products, in particular to the application of tangeretin in the preparation of drugs for inhibiting the activity of β-secretase. Background technique [0002] Alzheimer's disease (AD), also known as senile dementia, is a very harmful geriatric disease. According to statistics, the incidence of this disease is increasing year by year in our country. As the aging of our society continues to increase, Alzheimer's disease will bring huge medical expenditures and social burdens. Therefore, the development of drugs that can relieve or treat this disease has become a research hotspot. [0003] The current mainstream theory believes that one of the main causes of Alzheimer's disease is the wrong accumulation of amyloid Aβ in the brain, which produces neurotoxic senile plaques and eventually leads to the death of neurons. In the brain, amyloid precursor protein (Amyloid precursor protein, AP...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P25/28A23L33/10A23C9/152A23C9/156A23L2/39A23L2/52
CPCA61K31/352A61P25/28A23L33/10A23C9/152A23C9/156A23L2/39A23L2/52A23V2002/00
Inventor 舒细记包建梁征龚晓康柳威孙宾莲
Owner JIANGHAN UNIVERSITY
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