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Acetylcholinesterase inhibitor, drug for preventing and treating Alzheimer's disease and production method thereof

A technology for acetylcholinesterase and Alzheimer's disease, which is applied in the field of acetylcholinesterase inhibitor, the compatible composition of fangchinoline and coptisine, and can solve the problems of deficiency, large side effects, weak curative effect and the like

Active Publication Date: 2021-01-05
HKUST SHENZHEN RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned therapeutic drugs can only partially alleviate the clinical symptoms of AD patients, and most of them have the disadvantages of large side effects and weak curative effect. Currently, there is still a lack of specific drugs for the treatment of AD.

Method used

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  • Acetylcholinesterase inhibitor, drug for preventing and treating Alzheimer's disease and production method thereof
  • Acetylcholinesterase inhibitor, drug for preventing and treating Alzheimer's disease and production method thereof
  • Acetylcholinesterase inhibitor, drug for preventing and treating Alzheimer's disease and production method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Study on anti-acetylcholinesterase activity of fangchinoline, coptisine and their combination (1:5)

[0032] 1 Materials and reagents

[0033] 1.1 Drugs and reagents

[0034] Fangchinoline (Lot S090409-10, purity 99%) and coptisine hydrochloride (Lot DST170711-003, purity 99%) were purchased from Chengdu Master Biotechnology Co., Ltd. DTNB (Lot16262), acetylcholine iodide (ATCh, Lot BCBV4822), and tetraisopropyl pyrophosphoimide (iso-OMPA, Lot BCBW4257) were purchased from Sigma-Aldrich (USA); NP-40 (Lot C10297258), Leupeptinin (Lot C10079991), Aprotinin (Lot C10060365), Pepsin inhibitor (Lot B10084382), 4-Hydroxyethylpiperazineethanesulfonic acid (HEPES, Lot B10094032), benzamidine hydrochloride ( Lot C10089171) and other analytical reagents were purchased from Shanghai Macklin Biochemical Technology Co., Ltd.

[0035] 1.2 Preparation of animal brain lysate

[0036] C57BL / 6 male mice (Hong Kong University of Science and Technology, Center for Animal and Pla...

Embodiment 2

[0059] Example 2 Study on anti-acetylcholinesterase activity of fangchinoline, coptisine and their combination (1:2)

[0060] 1 Materials and reagents

[0061] 1.1 Drugs and reagents

[0062] With the 1.1 item medicine and reagent in embodiment 1.

[0063] 1.2 Preparation of animal brain lysate

[0064] With the 1.2 item method in embodiment 1.

[0065] 2 Experimental methods

[0066] 2.1 Drug preparation

[0067] Precisely weigh appropriate amount of reference substances of fangchinoline and coptisine hydrochloride, and dissolve them in DMSO to 50mM and 25mM respectively.

[0068] Take an appropriate amount of fangchinoline base mother solution, dilute it with DMSO, and serially dilute it into 7 gradients from a 2-fold gradient from an initial concentration of 1 mM. Take an appropriate amount of mother liquor of coptisine hydrochloride, dilute it with DMSO, and serially dilute it into 7 gradients from a 2-fold gradient from the initial concentration of 2mM. Take Fangch...

Embodiment 3

[0084] Example 3 Study on anti-acetylcholinesterase activity of fangchinoline, coptisine and their combination (1:1)

[0085] 1 Materials and reagents

[0086] 1.1 Drugs and reagents

[0087] With the 1.1 item medicine and reagent in embodiment 1.

[0088] 1.2 Preparation of animal brain lysate

[0089] With the 1.2 item method in embodiment 1.

[0090] 2 Experimental methods

[0091] 2.1 Drug preparation

[0092] Precisely weigh appropriate amount of reference substances of fangchinoline and coptisine hydrochloride, and dissolve them in DMSO to 50mM and 25mM respectively.

[0093] Take an appropriate amount of Fangchinoline base and Coptisine hydrochloride mother solution, dilute them with DMSO respectively, and serially dilute into 7 gradients from the 2-fold gradient of the initial concentration of 2mM. Get Fangchinoline and Coptisine Hydrochloride mother liquor of appropriate volume respectively and mix, obtain the Fangchinoline, Coptisine Hydrochloride composition s...

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Abstract

The invention provides an acetylcholinesterase inhibitor and a production method thereof, a medicine for preventing and treating Alzheimer's disease and a production method of the medicine. The acetylcholinesterase inhibitor comprises Fangchinoline and coptisine, wherein the mole ratio of the Fangchinoline to the coptisine is (1 to 5) to (2 to 1). The thought and the method of the compatibility ofa Chinese herbal compound are used for reference, and the Fangchinoline and the coptisine are combined, so that the acetylcholinesterase inhibitor can generate obvious synergistic compatibility effects in the respect of acetylcholinesterase inhibition, and the usage dosage of a single medicine and the toxin are reduced.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular to an acetylcholinesterase inhibitor, a medicine for preventing and treating Alzheimer's disease and a production method thereof, wherein both the acetylcholinesterase inhibitor and the medicine for preventing and treating Alzheimer's disease use Fangchinoline The compatibility composition of alkali and coptisine. Background technique [0002] Acetylcholinesterase is a hydrolase of the neurotransmitter acetylcholine, which is abundant in the brain and is also a major target for the development of drugs for neurodegenerative diseases such as Alzheimer's disease (AD). At present, the AD clinical treatment drugs targeting this target mainly include tacrine, donepezil, galantamine and rivastigmine and other acetylcholinesterase inhibitors, which can improve the brain synaptic transmission effect of AD patients, improve Cognitive dysfunction in AD patients can delay the further...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4748A61K31/4375A61P25/28
CPCA61K31/4375A61K31/4748A61P25/28A61K2300/00
Inventor 詹华强孔祥鹏董婷霞陈志从王怀友刘韵乐任海琴吴启韵黄荣蕾
Owner HKUST SHENZHEN RES INST
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