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Neutron capture therapeutic system for eliminating beta amyloid protein depositing plaque

A technology of amyloid protein and treatment system, applied in the field of neutron capture therapy system, can solve the problem of reducing or eliminating β-amyloid protein deposition plaque, which has not been found yet

Active Publication Date: 2017-10-31
NEUBORON MEDTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Neutron capture therapy is a treatment technology with strong pertinence, good effect and less damage to normal tissues. At present, no method that can effectively reduce or eliminate β-amyloid deposition plaques has been found, and no effective method has been found yet. Study reports application of neutron capture therapy in the treatment of Alzheimer's disease

Method used

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  • Neutron capture therapeutic system for eliminating beta amyloid protein depositing plaque
  • Neutron capture therapeutic system for eliminating beta amyloid protein depositing plaque
  • Neutron capture therapeutic system for eliminating beta amyloid protein depositing plaque

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] containing 10 The preparation method of the compound of B

[0074] The present invention contains 10 The preparation steps of the compound of B are as follows:

[0075] Step 1: 90mmol of 2-acetylfuran was dissolved in 40mL of dimethylformamide (DMF), and 108mmol of N-bromosuccinimide (NBS) was added thereto at 0°C, and the mixture was After stirring overnight at room temperature, the reaction mixture contained 1-(5-bromo-2-furyl)ethanone.

[0076] The reaction mixture described in step 1 was diluted with ethyl acetate, and filtered, and the organic phase in the filtrate was washed with saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate, concentrated, and then separated by chromatography to obtain 1- (5-Bromo-2-furyl)ethanone.

[0077] 1 H NMR (500MHz, CDCl 3 ,δ,ppm):2.46(3H.s),6.49(1H,d,J=3.4Hz),7.12(1H,d,J=3.4Hz).MS m / z 188(M+H) + .

[0078] Step 2: Add 5.3mmol of 1-(5-bromo-2-furyl)ethanone and 5.3mmol of 4-(di Methylamino) pheny...

Embodiment 2

[0089] containing 10 Application of the compound of B in the preparation and specific binding of β-amyloid protein

[0090] Due to the existence of the blood-brain barrier (BBB), it is difficult for most compounds to enter the brain through the blood stream. For many drugs, they cannot exert their efficacy if they cannot pass through the blood-brain barrier. In general, water-soluble drugs are difficult to pass through the blood-brain barrier, while fat-soluble drugs have better permeability than water-soluble drugs. The dissolution, absorption, distribution, and transport of drugs in the body are related to the water solubility and fat solubility of the drug, that is, the oil-water partition coefficient (logP). The oil-water partition coefficient is the logarithmic value of the ratio of the partition coefficient of the drug in n-octanol and water phase. The larger the logP value, the more lipophilic the substance is, and vice versa, the more soluble in water.

[0091] It i...

Embodiment 3

[0097] Simulation Test of Neutron Capture Therapy System Eliminating β-Amyloid Deposition Plaques

[0098] This embodiment uses boric acid (H 3 10 BO 3 ) instead of containing 10 The compound of B (including compound I and compound II), wherein boronic acid (H 3 10 BO 3 ) in the boron element is 10 B, Bovine serum albumin (BSA) is used to simulate β-amyloid protein, and the mixed solution composed of boric acid and bovine serum albumin is placed in the neutron beam environment generated by the neutron capture therapy device, and analyzed by SDS-PAGE gel electrophoresis The effect of neutrons on bovine serum albumin and its effect on H 3 10 BO 3 Effect of neutron beams on bovine serum albumin in the presence of conditions.

[0099] (1) The effect of neutrons on bovine serum albumin

[0100] Use ultrapure water to prepare a BSA solution with a concentration of 0.01% (w / w), store the prepared solution at 4°C and perform experimental operations. Take 1mL of the BSA sol...

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Abstract

The invention provides a neutron capture therapeutic system for eliminating beta amyloid protein depositing plaque. The system comprises a neutron capture therapeutic device and a 10B-containing compound capable of specifically combining with beta amyloid protein depositing plaque, and the structure of a beta amyloid protein depositing plaque can be destroyed by energy generated when a neutron beam generated by the neutron capture therapeutic device is illuminated on 10B element. The neutron capture therapeutic system has the beneficial effect that that the beta amyloid protein depositing plaque can be specifically and efficiently destroyed.

Description

technical field [0001] The invention relates to a neutron capture therapy system, in particular to a neutron capture therapy system that can be used to eliminate beta amyloid protein. Background technique [0002] Alzheimer's disease (AD) is a latent, progressive and irreversible brain disease with a high incidence in people over 65 years old. The current goal of AD treatment is to maintain physical function and capacity while slowing or delaying symptoms. Medications for mild to moderate AD include the acetylcholinesterase inhibitors donepezil, rivastigmine, and galantamine. Donepezil is also used to treat moderate to severe AD, alone or in combination with the N-methyl-D-aspartate receptor antagonist memantine. These neurotransmitter-modulating drugs temporarily improve symptoms, but patients still experience progressive cognitive deterioration, as well as psychosis, agitation, depression, and sleep disturbances. [0003] In 1984, scientists purified and measured the am...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61N5/10A61K41/00A61P25/28
CPCA61K31/69A61N5/103A61N5/1048A61N5/1077A61N2005/109A61K41/0095A61P25/28C07D207/00C07D207/02C07D207/04C07F5/02A61N5/1042A61N2005/1094A61N2005/1095A61N2005/1098
Inventor 陈瑞芬何静刘渊豪
Owner NEUBORON MEDTECH