Application of piceatannol in preparing medicine for preventing and treating neurodegenerative diseases

文档序号:1678339 发布日期:2020-01-03 浏览:37次 中文

阅读说明:本技术 白皮杉醇在制备预防和治疗神经退行性疾病的药物方面的应用 (Application of piceatannol in preparing medicine for preventing and treating neurodegenerative diseases ) 是由 续旭 蔡楠 顾粮 李梅婷 吴志兵 于 2019-09-17 设计创作,主要内容包括:本发明提供了白皮杉醇在制备预防和治疗神经退行性疾病的药物方面的应用。与现有技术相比,本发明直接将具备高生物活性,低生物毒性的白皮杉醇应用于新的领域也就是预防和治疗神经退行性疾病领域,取得了良好的效果;一方面保留了其优点;另一方面由于是现有的天然产物,无需额外研发成本,且原料易得。因此适合做进一步的开发和深入研究应用。(The invention provides an application of piceatannol in preparing a medicament for preventing and treating neurodegenerative diseases. Compared with the prior art, the invention directly applies the piceatannol with high biological activity and low biological toxicity to a new field, namely the field of preventing and treating neurodegenerative diseases, and obtains good effect; on one hand, the advantages are kept; on the other hand, because the natural product is the existing natural product, additional research and development cost is not needed, and the raw materials are easy to obtain. Therefore, the method is suitable for further development and deep research application.)

1. Application of piceatannol in preparing medicine for preventing and treating neurodegenerative diseases is provided.

2. The use of piceatannol as claimed in claim 1, wherein: the neurodegenerative disease includes Alzheimer's disease, amyotrophic lateral sclerosis/Parkinson syndrome-dementia complex, silvery particle dementia, corticobasal degeneration, Creutzfeldt-Jakob disease, dementia pugilistica, diffuse neurofibrillary tangles with calcification, Down's syndrome, frontotemporal dementia with Parkinson's syndrome linked to chromosome17, Gerstmann-Straussler disease, Hallervorden-Spatz disease, myotonic dystrophy, Niemann-pick disease type C, non-synaptania motor neuron disease with neurofibrillary tangles, pick disease, postencephalitic parkinsonism, prion protein amyloid angiopathy, progressive subcortical gliosis, progressive supranuclear palsy, subacute sclerosing panencephalitis, neurofibrillary tangle dementia only, whole brain glial cell Tau proteinopathy, Alzheimer's disease, Parkinson disease, Cerebral amyloid angiopathy.

3. The use of piceatannol as claimed in claim 1, wherein: the medicament for preventing and treating the neurodegenerative diseases is a medicament for inhibiting the abnormal aggregation of Tau protein.

4. Use of piceatannol as claimed in claim 3, wherein: the Tau protein abnormal aggregation comprises oligomerization or fibrosis caused by gene mutation or abnormal modification.

5. The use of piceatannol as claimed in claim 1, wherein: the medicine for preventing and treating neurodegenerative diseases is a medicine for inhibiting the overexpression of Tau protein in cells.

6. The use of piceatannol as claimed in claim 1, wherein: the medicament for preventing and treating neurodegenerative diseases is a medicament for inhibiting hyperphosphorylation of Tau protein in cells.

7. Use of piceatannol according to claim 6, wherein: the drug for inhibiting the intracellular Tau protein hyperphosphorylation is a drug for activating PP2A expression.

Technical Field

The invention belongs to the field of medicines, and particularly relates to application of piceatannol in preparation of medicines for preventing and treating neurodegenerative diseases.

Background

Piceatannol, also known as Bixateol, is a polyphenol hydroxyl compound extracted from fructus Vitis Viniferae, fructus Myrtilli, and Passion fruit, and has chemical name of 3,3,4, 5' -tetrahydroxy trans-stilbene and molecular formula C14H12O4The relative molecular mass is 244.24, and the structural formula is shown in figure 1. Piceatannol can better inhibit the generation of low-density lipoprotein induced by copper ions, and has stronger scavenging capacity on stable free radical 1, 1-diphenyl-2-m-trinitrophenyl hydrazyl. Pharmacological research of the piceatannol shows that the piceatannol has the functions of resisting cancer, resisting cell proliferation, resisting inflammation, regulating immunity, resisting hyperlipidemia, resisting bacteria and inhibiting H in stomach+-K+ATP enzyme, etc. The paclitaxel has obvious effects on the treatment of cardiovascular diseases and the protection of myocardial ischemia-reperfusion injury, can obviously reduce the myocardial infarction area, reduce the generation of superoxide anions and enhance the coronary blood flow function, and is considered to be a good antioxidant and cardiovascular protective agent.

Due to the high biological activity of piceatannol, many properties and functions are yet to be researched and developed.

Disclosure of Invention

The invention aims to provide a new application of piceatannol, and solve the technical problem that the prior art is insufficient in the application and development of piceatannol.

In order to solve the technical problems, the invention provides the application of piceatannol in preparing the medicine for preventing and treating neurodegenerative diseases.

Preferably, the neurodegenerative disease includes alzheimer's disease, amyotrophic lateral sclerosis/parkinsonism-dementia complex, silvery particle dementia, corticobasal degeneration, creutzfeldt-jakob disease, dementia pugilistica, diffuse neurofibrillary tangles with calcification, down's syndrome, frontotemporal dementia with parkinsonism linked to chromosome17, gerstmann-straussler-scheinker disease, hallewden-shappers disease, myotonic dystrophy, niemann-pick C disease, non-kangaroo motor neuron disease with neurofibrillary tangles, pick's disease, postencephalitic parkinsonism, prion protein brain amyloid angiopathy, progressive subcortical gliosis, progressive supranuclear palsy, subacute sclerosing panencephalitis, dementia with neurofibrillary tangles only, dementia tangles with dementia, Whole brain glial cell Tau protein disease, cerebral amyloid angiopathy.

Preferably, the agent for preventing and treating neurodegenerative disease is an agent for inhibiting abnormal aggregation of Tau protein.

Further preferably, the abnormal aggregation of Tau protein includes oligomerization or fibrosis caused by gene mutation or abnormal modification.

Further preferably, the drug for preventing and treating neurodegenerative diseases is a drug that inhibits overexpression of Tau protein in cells.

Preferably, the agent for preventing and treating neurodegenerative disease is an agent that inhibits hyperphosphorylation of Tau protein in cells.

Further preferably, the drug inhibiting hyperphosphorylation of Tau protein in cells is a drug activating the expression of PP 2A.

Compared with the prior art, the invention directly applies the piceatannol with high biological activity and low biological toxicity to a new field, namely the field of preventing and treating neurodegenerative diseases, and obtains good effect; on one hand, the advantages are kept; on the other hand, because the natural product is the existing natural product, additional research and development cost is not needed, and the raw materials are easy to obtain. Therefore, the method is suitable for further development and deep research application.

Drawings

FIG. 1 is a chemical structural formula of piceatannol according to an embodiment of the present invention;

FIG. 2 is a graph showing the effect of piceatannol on Tau protein aggregation in vitro according to an embodiment of the present invention;

FIG. 3 is a transmission electron micrograph of piceatannol inhibiting Tau protein fibrosis in accordance with an embodiment of the present invention;

FIG. 4 is a graph showing the docking results of piceatannol with Tau protein molecules according to an embodiment of the present invention;

FIG. 5 is a graph showing the change of cell viability of piceatannol after it acts on SH-SY5Y/Tau cells according to an embodiment of the present invention;

FIG. 6 is a graph showing the expression level changes of total Tau protein, pT205-Tau, pT231-Tau, pS396-Tau and pS404-Tau protein after piceatannol is applied to SH-SY5Y/Tau cells and the results of statistical analysis according to an embodiment of the present invention;

FIG. 7 is a diagram showing the changes in the expression levels of PP2A α and PP2A α + β proteins after piceatannol is applied to SH-SY5Y/Tau cells and a statistical analysis result chart according to an embodiment of the present invention.

Detailed Description

In order to make the technical problems, technical solutions and advantageous effects to be solved by the present invention more clearly apparent, the present invention is further described in detail below with reference to the following embodiments. It should be understood that the specific embodiments described herein are merely illustrative of the invention and are not intended to limit the invention.

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