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Application of mulberone H in preparation of anti-Alzheimer's disease medicine

A technology of Alzheimer's and mulberry, which is applied in the field of medicine and can solve the problems such as no reports of butyrylcholinesterase inhibitory activity.

Pending Publication Date: 2021-07-30
SOUTHWEST UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Sulpione H has good potential for lowering blood pressure, antibacterial and anti-osteoporosis, but there is no report on its inhibitory activity against butyrylcholinesterase

Method used

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  • Application of mulberone H in preparation of anti-Alzheimer's disease medicine
  • Application of mulberone H in preparation of anti-Alzheimer's disease medicine
  • Application of mulberone H in preparation of anti-Alzheimer's disease medicine

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] The applicant will Sulperone H (structural formula sees Figure 4 ) was compared with other flavonoid-related activities with similar structures, and the results are shown in Table 1.

[0020] Concretely include: Morusin (Morusin, structural formula sees figure 1 ), mulperin C (Kuwanon C, structural formula see figure 2 ), Kuwanon G (Kuwanon G, structural formula see image 3 ).

[0021] IChE inhibition by the modified Ellman method 50 Value was tested, 40 μL of PBS (0.1M, PH 8.0), 20 μL of DTNB (5,5'-dithiobis(2-nitrobenzoic acid), 2mM), 10 μL of BChE (0.75u / mL) and 10 μL of samples with different concentrations were mixed, and then 20 μL of BTC (S-butyrylthiocholine iodide, 2 mM) was quickly added to start the reaction, and read at 405 nm using a microplate reader after 2 min.

[0022] Table 1. IC of prenylflavones with similar structures in Morus twig to BChE 50 value

[0023]

[0024] It can be seen from Table 1 that the inhibitory activity of mulperione ...

Embodiment 2

[0026] The in vitro inhibitory activity of BChE was tested by the modified Ellman method, 40 μL of PBS (0.1M, pH8.0), 20 μL of DTNB (5,5'-dithiobis(2-nitrobenzoic acid), 2mM) , 10 μL of BChE (0.75u / mL) and 10 μL of different concentrations of samples were mixed, and then quickly added 20 μL of BTC (S-butyrylthiocholine iodide, 2mM) to start the reaction. After 2 minutes, use a microplate reader at 405nm reading. The inhibition rate was calculated according to the following formula:

[0027]

[0028] Among them, A1 is the absorbance value of the sample group, A2 is the absorbance value of the blank without enzyme group, and A0 is the negative absorbance value without adding the sample. All experiments were repeated three times and the mean and standard deviation were calculated.

[0029] Experimental results (table 2): by in vitro inhibition of butyrylcholinesterase activity assay found that mulperione H has a good inhibitory activity to butyrylcholinesterase, and with the...

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Abstract

The invention discloses an application of mulberone H in preparation of an anti-Alzheimer's disease medicine. Through experimental screening, the applicant finds that mulberrin H has a good inhibition effect on butyrylcholine esterase, the inhibition effect is enhanced along with the increase of the drug concentration, and compared with a positive drug, the inhibition rate of butyrylcholine esterase is obviously higher, so that mulberrin H has the prospect of being developed into an anti-Alzheimer's disease drug.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the application of mulperidone H in the preparation of anti-Alzheimer's disease medicine. Background technique [0002] Alzheimer's disease (AD) is a common degenerative disease of the central nervous system, which is mainly manifested as memory, cognitive dysfunction, and decreased ability of daily life. AD has become one of the major diseases that seriously threaten the health of the elderly in modern society after cardiovascular diseases and tumors. [0003] At present, the pathogenesis of AD is still unclear, and the most widely accepted theory is the cholinergic hypothesis (cholinergic hypothesis), that is, changes in the cholinergic system are closely related to the degree of cognitive impairment in AD. Therefore, improving the cholinergic system and increasing the level of acetylcholine (ACh) in the brain is an important way to treat AD. Acetylcholinesterase (AChE) and bu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K36/605A61P25/28
CPCA61K31/352A61K36/605A61P25/28
Inventor 徐立向伟
Owner SOUTHWEST UNIVERSITY
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