Multiple-target effects of isoflavone derivative and its application in improvement of learning and memory

A technology for learning and memory impairment and function, which can be applied to medical preparations containing active ingredients, drug combinations, organic active ingredients, etc., and can solve the problem that single-target drugs are difficult to achieve ideal therapeutic effects.
CN104095849AActive Publication Date: 2014-10-15INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
Publication Date
2014-10-15

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Abstract

The invention discloses multiple-target effects of an isoflavone derivative and its application in improvement of learning and memory. Specifically, the invention discloses that a compound J39136 has the effects of: upregulating the expression of SIRT1 protein with damage repair and neuroprotective effects; inhibiting the activity of acetylcholinesterase and butyrylcholinesterase, and dose-dependently inhibiting the acetylcholinesterase activity of cells under a safe dose; protecting nerve cells, inhibiting abnormal expression of beta-APP, and reducing Abeta1-42 secretion; and regulating neuroinflammation. Animal experimental results prove that J39136 has low toxicity, can penetrate the blood-brain barrier, and can significantly improve scopolamine caused mouse dementia and strengthen learning and memory functions. Preclinical study results prompt that J39136 is expected to become the drug for prevention and / or treatment of learning and memory disorder and Alzheimer's disease.
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Description

technical field

[0001] The invention relates to a natural product derivative with double cholinesterase inhibitory effect, nerve cell protection effect and anti-inflammation effect, and the application of the compound in the treatment / prevention of learning and memory impairment and senile dementia. It belongs to the field of medical technology. technical background

[0002] Alzheimer's disease (AD) is a degenerative disease of the central nervous system characterized clinically by behavioral, cognitive and memory dysfunction, and its characteristic pathological changes are: neuron loss, neuron fiber tangle ( neurofibrillary tangles (NFTs), senile plaques (SPs). The incidence of AD in people aged 65-74 is about 3%, the incidence rate can rise to 19% in people aged 75-84, and the incidence rate of AD in people over 84 years old can be as high as 47%. AD is the fourth major killer of the elderly after cardiovascular disease, tumor, and cerebrovascular disease, and seriously ...

Claims

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