Technology for inhibiting activity of acetylcholin esterase

An acetylcholinesterase, active technology, applied in the field of medicine, can solve the problems of large side effects, complex pathogenesis of AD, weak curative effect and the like

Active Publication Date: 2019-08-30
HKUST SHENZHEN RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The pathogenesis of AD is complicated. In modern clinical practice, acetylcholinesterase (AChE) inhibitors such as tacrine and galantamine are often used in the treatment. By reducing the hydrolysis of acetylcholine (ACh) by AChE, the effect of central cholinergic neurotransmission can be improved, and the clinical effect of AD can be improved. Symptoms may delay their further development, but most of them have the disadvantages of large side effects and weak curative effect
There is still no specific drug for the treatment of AD

Method used

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  • Technology for inhibiting activity of acetylcholin esterase
  • Technology for inhibiting activity of acetylcholin esterase
  • Technology for inhibiting activity of acetylcholin esterase

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Anti-acetylcholinesterase activity of fangchinoline, berberine and their combination (1:5)

[0031] 1 Materials and reagents

[0032] 1.1 Drugs and reagents

[0033] Fangchinoline (Lot S090409-10, purity 99%) and berberine hydrochloride (Lot S071016-5, purity 99%) were purchased from Chengdu Master Biotechnology Co., Ltd. DTNB (Lot 16262), acetylcholine iodide (ATCh, Lot BCBV4822), and tetraisopropyl pyrophosphoimide (iso-OMPA, Lot BCBW4257) were purchased from Sigma-Aldrich (USA); NP-40 (Lot C10297258) , Leupeptin (Lot C10079991), Aprotinin (Lot C10060365), Pepsin (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.

[0034] 1.2 Preparation of animal brain lysate

[0035]C57BL / 6 male mice (Hong Kong University of Science and Technology, Center for Animal and Plant Care) were selected....

Embodiment 2

[0060] Example 2 Anti-acetylcholinesterase activity of fangchinoline, berberine and their combination (1:2)

[0061] 1 Materials and reagents

[0062] 1.1 Drugs and reagents

[0063] With the 1.1 item medicine and reagent in embodiment 1.

[0064] 1.2 Preparation of animal brain lysate

[0065] With the 1.2 item method in embodiment 1.

[0066] 2 Experimental methods

[0067] 2.1 Drug preparation

[0068] Precisely weigh appropriate amount of Fangchinoline and Berberine Hydrochloride reference substances, and dissolve them in DMSO to 50mM and 25mM respectively.

[0069] Take an appropriate amount of mother solution of fangchinoline base, dilute it with DMSO, and serially dilute it into 7 gradients from a 2-fold gradient from an initial concentration of 2mM. Take an appropriate amount of berberine hydrochloride mother solution, dilute it with DMSO, and serially dilute it into 7 gradients from a 2-fold gradient from the initial concentration of 4mM. Get Fangchinoline and ...

Embodiment 3

[0086] Example 3 Anti-acetylcholinesterase activity of fangchinoline, berberine and their combination (1:1)

[0087] 1 Materials and reagents

[0088] 1 Materials and reagents

[0089] 1.1 Drugs and reagents

[0090] With the 1.1 item medicine and reagent in embodiment 1.

[0091] 1.2 Preparation of animal brain lysate

[0092] With the 1.2 item method in embodiment 1.

[0093] 2 Experimental methods

[0094] 2.1 Drug preparation

[0095] Precisely weigh appropriate amount of Fangchinoline and Berberine Hydrochloride reference substances, and dissolve them in DMSO to 50mM and 25mM respectively.

[0096] Take an appropriate amount of mother solution of fangchinoline base, dilute it with DMSO, and serially dilute it into 7 gradients from a 2-fold gradient from an initial concentration of 2mM. Take an appropriate amount of berberine hydrochloride mother solution, dilute it with DMSO, and serially dilute it into 7 gradients from a 2-fold gradient from the initial concentrat...

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Abstract

The invention provides a technology for inhibiting activity of acetylcholin esterase. The technology comprises a pharmaceutical composition for inhibiting the activity of acetylcholin esterase, an Alzheimer disease prevention and treatment medicine, a production method of the pharmaceutical composition and a production method of the Alzheimer disease prevention and treatment medicine. The pharmaceutical composition comprises fangchinoline and berberine at a mole ratio of 1:5-2:1. The inventors combine fangchinoline and berberine by reference to a clue and a method of compound compatibility oftraditional Chinese medicines; an obvious synergic compatibility effect can be generated in an aspect of inhibition of acetylcholin esterase; and the use dosage and toxicity of a single medicine are reduced.

Description

technical field [0001] The present invention relates to the field of medical technology, in particular to a technology for inhibiting the activity of acetylcholinesterase, which includes a pharmaceutical composition for inhibiting the activity of acetylcholinesterase, a drug for preventing and treating Alzheimer's disease and a production method thereof; specifically, The invention relates to a new application of fangchinoline in anti-acetylcholinesterase activity, and an application of a compatible composition of fangchinoline and berberine in anti-acetylcholinesterase activity. Background technique [0002] Alzheimer's disease (AD) is a common neurodegenerative disease with insidious onset and rapid disease progression. Neurodegenerative disease with high mortality. With the acceleration of population aging in my country, its incidence rate is increasing year by year. The pathogenesis of AD is complicated. In modern clinical practice, acetylcholinesterase (AChE) inhibito...

Claims

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Application Information

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