Application of baicalein to preparation of medicament for preventing and treating Parkinson's disease

A technology of baicalein and medicine, which is applied in the field of preparation of pharmaceutical preparations for the prevention and treatment of Parkinson's disease, can solve the problems of disease exacerbation, toxic side effects, and inability to delay the disease process, and achieve the goal of promoting reversal or recovery, inhibiting development, and protecting pathological changes Effect

Inactive Publication Date: 2016-08-31
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These drugs play a role in inhibiting the symptoms of Parkinson's patients through different channels, and can significantly improve the symptoms of Parkinson's disease, but cannot delay the progress of the disease, and cannot prevent the degeneration of dopaminergic neurons, and long-term use has serious side effects, even exacerbation of the disease

Method used

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  • Application of baicalein to preparation of medicament for preventing and treating Parkinson's disease
  • Application of baicalein to preparation of medicament for preventing and treating Parkinson's disease
  • Application of baicalein to preparation of medicament for preventing and treating Parkinson's disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Embodiment 1, the effect of baicalein on the behavioral improvement of MPTP-induced PD mice

[0070] Model building and grouping

[0071] C57BL / 6 mice were randomly divided into 3 groups, namely normal control group, MPTP model group and baicalein administration group (200mg / kg), 12 in each group. The control group and the model group were pre-administered with normal saline, and the administration group was given the above-mentioned dose of drugs. After continuous intragastric administration for one week, the model group and the administration group were intraperitoneally injected with MPTP (30 mg / kg) on ​​the 8th day, once a day , for 5 consecutive days, and observe the behavioral indicators of the mice on the 13th day.

[0072] Behavioral testing

[0073] 1. Spontaneous activity experiment uses mouse autonomic activity instrument (ZIL-2 type mouse autonomic activity instrument, Institute of Materia Medica, Chinese Academy of Medical Sciences) to measure and count t...

Embodiment 2

[0082] Example 2, the effect of baicalein on monoamine transmitters in the brain striatum of MPTP-induced PD mice

[0083] Model building and grouping are the same as above. Six mice were collected from each group, the brains were decapitated, and the substantia nigra and striatum were separated on ice trays and stored in liquid nitrogen. One side of the striatum was taken for the determination of neurotransmitters. Take striatum, weigh and record, homogenize in 0.2ml homogenate solution in ice bath for 40s, 80% ultrasonic energy, cycle=0.7, centrifuge at 12000rpm at 4°C for 30min, take the supernatant and detect it with high performance liquid phase electrochemical method The levels of dopamine (DA) and its metabolite dihydroxyphenylacetic acid (DOPAC), homovanillic acid (HVA), 5-hydroxytryptamine (5-HT) and its metabolite 5-hydroxyindoleacetic acid (5-HIAA), each Inject 20 μl each time. Mobile phase: 0.1mol / l NaH 2 PO 4 The aqueous solution contains 0.85mmol / l OSA, 0.5m...

Embodiment 3

[0085] Embodiment 3, the effect of baicalein on MPTP-induced PD mouse brain tyrosine hydroxylase (TH), dopamine transporter (DAT), glial-derived fibrin (GFAP) expression

[0086] Model building and grouping are the same as above. Six rats were taken from each group for immunohistochemical detection. Anesthetize and fix with 4% chloral hydrate, open the chest cavity, perfuse and fix with normal saline and 4% paraformaldehyde respectively, and take out the brain by craniotomy. After being fixed in 4% paraformaldehyde for 1 day, the cells were replaced with 0.01M PBS containing 30% sucrose. After the brain tissue sank, a 20 μm thick coronal slice of the brain was cut with a cryostat. The brain slices were shaken and rinsed 3 times with PBST (PH=7.4), 10 min each time; 2 o 2 Treat for 10 minutes, wash with PBST shaking 3 times, 10 minutes each time; incubate with blocking solution for 1 hour; add primary antibody (TH, 1:500; DAT, 1:200; GFAP, 1:400), and incubate overnight at ...

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Abstract

The invention discloses application of baicalein(chemical name:5,6,7-trihydroxy flavone;English name: baicalein) shown as a general formula (I) to preparation of a medicament for preventing and treating Parkinson's disease. The baicalein can lower the tremorfrequency and amplitude of the Parkinson's disease, and improve and treat Parkinson's disease symptoms; the baicalein can protect dopaminergic neurons from being injured, and can effectively prevent and treat pathological change of the Parkinson's disease and the development of the Parkinson's disease; through the anti-apoptosis, anti-inflammation and anti-oxidation functions of the baicalein, the effect of protecting thedopaminergic neurons and the effect of restraining the symptoms of the Parkinson's disease are achieved. The invention relates to separate use of the baicalein to preparation of the medicament for preventing and treating the Parkinson's disease and preparation of the baicalein into various preparations in combination with other substances. The general formula (I) is show in the description.

Description

technical field [0001] The invention relates to the use of baicalein in the preparation of medicines for preventing or treating Parkinson's disease or diseases characterized by symptoms related to Parkinson's disease. It also relates to the combination of baicalein, flavonoids and other substances for the preparation of pharmaceutical preparations for preventing and treating Parkinson's disease, which belongs to the field of pharmacy, Background technique [0002] Parkinson's disease (PD) has become the second most common age-related neurodegenerative disease in the world after Alzheimer's disease. The incidence rate of the elderly over 60 years old in the world is 1%, and the incidence rate increases with age. In my country, there are more than 1.7 million Parkinson's disease patients among the elderly over 55 years old. The current understanding of the main pathological features of PD is the progressive loss and death of dopaminergic neurons in the substantia nigra compa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P25/16
CPCA61K31/352
Inventor 杜冠华穆鑫何国荣李晓秀吕扬杨宁
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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