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Application of novel maca amine A in preparation of drug for preventing Alzheimer disease

A technology for Alzheimer's disease and macasine, which is applied in the field of pharmaceutical applications, and can solve the problems of no reports of macasine A inhibitory activity.

Inactive Publication Date: 2021-01-01
南京奥赛斯生物科技有限公司
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  • Abstract
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Problems solved by technology

[0005] No report on the inhibitory activity of macasine A on acetylcholinesterase

Method used

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  • Application of novel maca amine A in preparation of drug for preventing Alzheimer disease
  • Application of novel maca amine A in preparation of drug for preventing Alzheimer disease
  • Application of novel maca amine A in preparation of drug for preventing Alzheimer disease

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Embodiment Construction

[0015] The following examples are in order to specify the substantive technical content of the present invention, and the specific routine details recorded in the following examples cannot limit the protection scope of the present invention.

[0016] 1. Materials and methods

[0017] The Ellman method was used to test the AChE in vitro inhibitory activity. The specific method was as follows: dissolve the drugs to be tested (macacinamine A and positive drug huperzine A, with a purity ≥ 98%) with an appropriate amount of DMSO and add PBS buffer (pH 8.0 ) solution, prepared into mother liquor, and then diluted into different concentrations of drug solutions for subsequent use. During the test, 100 μL of PBS buffer, 20 μL of acetylcholinesterase solution (50 U / L, dissolved in PBS), 20 μL of drug solution (final concentrations of 0.025, 0.05, 0.1, 0.2, 0.4 μg / mL) were sequentially added to the 96-well plate ) and 20 μL of 1.2 mM iodothioacetylcholine (ATCh) as the enzyme reaction ...

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Abstract

The invention discloses an application of a novel maca amine A in preparation of a drug for preventing an Alzheimer disease. A research of the application disclosed by the invention found that novel maca amines A with different concentrations all have an inhibitory activity on acetylcholin esterase, and the inhibitory activity is enhanced with an increase of a drug concentration, and the novel maca amine A has an activity intensity similar to that of a positive drug. Compared with a positive drug, the inhibitory activity of the novel maca amine A on the acetylcholin esterase within a low-concentration range is lower than that of a positive drug, and is higher than that of the positive drug within a high-concentration range. Therefore, the novel maca amine A has a potential of becoming a drug for preventing an Alzheimer disease.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to the application of macacinamine A in the preparation of anti-Alzheimer's disease medicines. Background technique [0002] In recent years, Alzheimer's disease (AD) has become the fourth leading killer of the elderly after heart disease, cancer and stroke, seriously endangering human health. Cholinergic neurotransmission defects are the main cause of the disease, and acetylcholinesterase inhibitors (AChEI) are the most successfully studied class of drugs that can enhance cholinergic function. AChE is a multi-molecular glycoprotein consisting of 537 amino acids consisting of 14 α-helices and 12 β-sheets. It is a serine hydrolase. Human AChE is mainly distributed in nerve tissues. Under physiological conditions, the physiological function of AChE located on the postsynaptic membrane is mainly to catalyze the hydrolysis of acetylcholine (ACh), which is realized through the catal...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165A61P25/28
CPCA61K31/165A61P25/28
Inventor 不公告发明人
Owner 南京奥赛斯生物科技有限公司
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