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Use of oleanane-type triterpenoid ester derivatives as anti-neurodegenerative drugs

A kind of technology of oleanane type and ester derivatives, which is applied in the field of medicine

Active Publication Date: 2017-04-12
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there have been no reports of such compounds having NGF-like activity

Method used

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  • Use of oleanane-type triterpenoid ester derivatives as anti-neurodegenerative drugs
  • Use of oleanane-type triterpenoid ester derivatives as anti-neurodegenerative drugs
  • Use of oleanane-type triterpenoid ester derivatives as anti-neurodegenerative drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The preparation method of compound I-1a and I-1b:

[0030]

[0031] Dissolve compound (1) [3β,23,28-trihydroxy-12-oleanene-3β-caffeate (3β,23,28-trihydroxy-12 -oleanene-3β-caffeate)] (10 mg), add 0.5 mg DMAP (4-dimethylaminopyridine), stir, add 100 μl acetic anhydride, spin dry the reaction solution, perform solvent distribution with water and ethyl acetate, recover the ester layer, and use The ester layer samples were purified by PTLC and HPLC to obtain compounds I-1a and I-1b.

[0032] Physicochemical properties of compound I-1a: white solid, high resolution mass spectrum shows that its molecular formula is C 47 h 64 o 10 (HRESI-TOF-MS m / z(M+Na) + Calcd.for C 47 h 64 o 10 Na: 811.4392, Found: 811.4422); 1 HNMR (500MHz, CDCl 3)δ7.57(d,J=16.0Hz,1H),7.39(dd,J=1.88,8.34Hz,1H),7.35(d,J=1.8Hz,1H),7.21(d,J=8.4Hz, 1H),6.34(d,J=16.0Hz,1H),5.21(brt,1H),4.94(dd,J=11.7,4.7Hz,1H),4.00(dd,J=25.5,11.3Hz,2H), 3.68(dd,J=11.3,8.3Hz,2H),2.30(s,3H),2.30(s,3H),2.07(s,6H),2.0...

Embodiment 2

[0049] In animal models of neurodegenerative diseases, studies have found that NGF can prevent or reduce the degeneration of neurons, prevent the progression of AD to a certain extent, and have the effects of promoting nerve growth and neuroprotection. Because PC12 cells have the general characteristics of nerve cells, PC12 cells will stop dividing under the action of NGF, grow protrusions, and transform into neuron-like cells. Therefore, using PC12 cells as an effective activity identification system to screen active active ingredients will become an effective drug for the treatment of senile dementia.

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PUM

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Abstract

The invention provides an application of an oleanane pentacyclic triterpene ester derivative in preparation for medicine for treating senile dementia, and the senile dementia comprises neurodegenerative disease. The medicine is prepared by the oleanane pentacyclic triterpene ester derivative and a pharmaceutically acceptable carrier or an excipient. The oleanane pentacyclic triterpene ester derivative has obvious activity analogous with a nerve growth factor, and can be used for preparing the neurodegenerative disease medicine for treating senile dementia. According to the invention, a structural formula of the oleanane pentacyclic triterpene ester derivative is shown as follows.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to oleanane-type pentacyclic triterpene ester derivatives and their application in the prevention and treatment of neurodegenerative diseases such as senile dementia. Background technique [0002] The rapid growth of the elderly population makes people pay more attention to the health status of this group, and Alzheimer's disease seriously affects the health of the elderly, and it has become one of the four main causes of death in adults. In the 2009 report of the International Alzheimer's Association, it was pointed out that in 2010, about 36 million people in the world suffered from dementia, and it will double every 20 years, reaching 66 million in 2030. In 2050, it will reach 115.4 million people, and the number of patients in low- and middle-income countries will account for 71% of the global total. In the 2010 report, the total social cost of Alzheimer's disease ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/56A61P25/28
Inventor 戚建华曹时宁向兰
Owner ZHEJIANG UNIV