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Application of sunitinib in preparation of acetylcholinesterase inhibitor

A technology of acetylcholinesterase and sunitinib, which is applied in the field of anti-tumor drugs and can solve the problems such as sunitinib that have not yet existed

Inactive Publication Date: 2012-08-29
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Acetylcholinesterase plays an important role in the transmission of nerve impulses in the body. It is a choline ester hydrolase and belongs to a completely different target category from tyrosine kinase receptors. There is no sunitinib in the prior art. Related reports on acetylcholinesterase inhibitors

Method used

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  • Application of sunitinib in preparation of acetylcholinesterase inhibitor
  • Application of sunitinib in preparation of acetylcholinesterase inhibitor
  • Application of sunitinib in preparation of acetylcholinesterase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0017] Detection of sunitinib (compound 1) inhibiting acetylcholinesterase activity

[0018] The sunitinib (compound 1) used in the test of the present invention was prepared according to the method reported in the literature: WO 99 / 48868 (publication date: September 30, 1999).

[0019]

[0020] Inhibition of acetylcholinesterase activity detection test:

[0021] Fresh acetylcholinesterase, purchased from Sigma company;

[0022] Thioacetylcholine salt (ATOH) was purchased from Sigma as a substrate;

[0023] 5,5-dithiobis(2-nitrobenzoic acid) (DTNB) is a chromogen, purchased from Sigma;

[0024] 0.01M phosphate buffer (pH=7.0);

[0025] Sunitinib was made into DMSO solution (both 20 μmol / mL).

[0026] Detection method:

[0027] (1) Acetylcholinesterase and substrate are mixed with 0.01M phosphate buffer to prepare a suitable concentration solution. 1ml of the initial reaction system contains 0.02 units of enzyme, 0.1 μmol of substrate, 0.1 μmol of chromogen, and 10 μL o...

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Abstract

The invention discloses an application of sunitinib in preparation of an acetylcholinesterase inhibitor. Sunitinib used as an antineoplastic agent in the prior art is applied to the preparation of the acetylcholinesterase inhibitor in the technical solution provided by the invention and is used as a medicine for treating the Alzheimer's disease.

Description

technical field [0001] The present invention relates to a new application of an antineoplastic drug, sunitinib (Sunitinib, trade name: Sutent). Background technique [0002] Acetylcholine (Ach) is a neurotransmitter that mainly exists in the presynaptic cholinergic nerve endings. In the brain, maintaining a certain level of acetylcholine plays an important role in human memory and recognition functions; in the motor nervous system, acetylcholine exists at the neuromuscular junction and controls muscle contraction; in the sympathetic nerve, acetylcholine is released by the preganglionic nerve Neurotransmitters play an important role in maintaining normal physiological functions in the body. Acetylcholinesterase (AchE) mainly exists in the neuromuscular junction and cholinergic nervous system, and its physiological function in the body is to hydrolyze and inactivate acetylcholine. Acetylcholinesterase inhibitors can block the activity of AchE, delay the hydrolysis rate of ac...

Claims

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Application Information

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IPC IPC(8): A61K31/404A61P25/28A61P21/04A61P27/06
Inventor 杨永亮牛铭山毛磊
Owner DALIAN UNIV OF TECH