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Preparation method and application of marine-derived anti-senile dementia compound

A technology for senile dementia and compounds, which is applied in the directions of medical preparations containing active ingredients, organic chemistry, drug combinations, etc., can solve problems such as no anti-senile dementia reports, and achieve the effect that the preparation method is simple and easy to implement and easy to realize.

Inactive Publication Date: 2021-02-02
滨州医学院附属医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

It is reported that the compound has anti-tumor activity, but there is no report on the compound's anti-senile dementia

Method used

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  • Preparation method and application of marine-derived anti-senile dementia compound
  • Preparation method and application of marine-derived anti-senile dementia compound
  • Preparation method and application of marine-derived anti-senile dementia compound

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Embodiment

[0033] The anti-senile dementia compound of marine origin described in this example is isolated from the sponge Aaptos suberitoides, and its molecular formula is C 13 h 12 N 2 o 2 , the structural formula is:

[0034]

[0035] The compound is named: aaptamine.

[0036] The sponge Aaptos suberitoides was collected from the waters of Yongxing Island in Xisha in 2012, and it was stored frozen at -20°C.

[0037] The preparation method of the anti-senile dementia compound comprises the following steps:

[0038] 1. Raw material processing: After crushing the sponge sample with a wet weight of 2.5kg in freezer storage, use a pulverizer to extract 3 times with methanol dynamic cold immersion at room temperature, soaking for 5 days each time; combine the 3 extracts, and the temperature condition is 40 ℃ Concentrate under reduced pressure; then, dissolve and desalt 3 times with anhydrous methanol to obtain 162.5 g of extract (crude extract of sponge Aaptos suberitoides);

[003...

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Abstract

The invention relates to the technical field of marine organisms and medicines, in particular to a preparation method and application of an anti-senile dementia compound separated from marine sponge Aaptos suberitodes. The anti-senile dementia compound disclosed by the invention is an aaptamine compound separated from sponge Aaptos suberitodes, the preparation method of the compound is simple andeasy to implement, and artificial synthesis of the compound is also easy to realize. Meanwhile, the invention discloses that the compound has better activity of inhibiting acetylcholin esterase and butyrylcholin esterase for the first time, wherein the IC50 values of the compound are 6.071 [mu]g / mL and 1.492 [mu]g / mL respectively; the invention provides application of the compound having undergonestructural modification and optimization to a lead compound used for preparing acetylcholin esterase inhibiting medicines and butyrylcholin esterase inhibiting medicines for the first time; and a scientific basis is provided for development and utilization of marine biological resources in China and research and development of new anti-senile dementia compounds.

Description

technical field [0001] The invention relates to the technical fields of marine biology and medicine, in particular to a preparation method and application of an anti-senile dementia compound isolated from marine sponge Aaptossuberitoides. Background technique [0002] Alzheimer's disease, also known as Alzheimer's Disease (AD for short), is a complex neurodegenerative disease that mostly occurs in the elderly. With the rapid growth of the world's elderly population, the incidence of AD is increasing year by year, and it is currently the third leading cause of death in the elderly after cardiovascular diseases and tumors. The disease usually initially manifests as short-term memory loss and, as the disease progresses, eventually leads to loss of physical function and even death. At present, the anti-senile dementia drugs used clinically can only alleviate the progress of the disease but cannot completely cure the disease. Therefore, it is extremely urgent to develop new anti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61K31/4745A61P25/28
CPCA61P25/28C07D471/04
Inventor 宫凯凯苗双贺倩倩
Owner 滨州医学院附属医院
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