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Preparation method of traditional Chinese medicine manyflower tickclove herb extract and application in anti-senile dementia medicaments

A technology of hungry leeches and extracts, which is applied in the field of medicine, can solve the problems of large molecular weight, inability to pass through the blood-brain barrier, and difficulty in large-scale preparation, and achieve the effects of convenient material selection, significant neuromimetic growth factor activity, and wide sources

Active Publication Date: 2013-09-11
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is a polypeptide composed of more than 100 amino acids; due to its large molecular weight and strong polarity, it cannot pass through the Blood Brain Barrier (BBB), and it is difficult to prepare on a large scale, which limits its practical clinical application , NGF has not found a better treatment method other than direct administration of intracerebral surgery

Method used

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  • Preparation method of traditional Chinese medicine manyflower tickclove herb extract and application in anti-senile dementia medicaments
  • Preparation method of traditional Chinese medicine manyflower tickclove herb extract and application in anti-senile dementia medicaments
  • Preparation method of traditional Chinese medicine manyflower tickclove herb extract and application in anti-senile dementia medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Preparation of Hungry Leech Extract and its Active Components and Active Compounds

[0039] 1. Crushing and extraction:

[0040] After crushing 1000g of traditional Chinese medicine leeches, extract with 3L of ethanol at room temperature (occasionally shake). After suction filtration, concentration and drying, 50 g of the crude ethanol extract was obtained, which was alternately extracted and separated with water and ethyl acetate several times to obtain 10 g of the active component (A) of the ester layer.

[0041] 2. Separation and purification:

[0042] The active component (A) is first separated by a silica gel open column (200-300 mesh, the following solvent systems are all in volume ratio, and the first separation is chloroform:ethyl acetate=100:0,90:10,80:20 , 70:30, 50:50, 0:10), combined chloroform:ethyl acetate 90:10 to 50:50 eluted fractions to obtain active component (B) 1g; then, the active component was further Separation with ODS open column (...

Embodiment 1

[0044] Qualitative identification of physical and chemical characteristics and chemical structure of the compound obtained in embodiment 1:

[0045] The structures of compounds (1), (2) and (3) were confirmed by MS, 1 H NMR, 13 C NMR test, and confirmed after comparison with literature data.

[0046] Compound 1: white solid; (c1.0,MeOH);C 39 h 56 o 6 (HR ESI-TOF-MS m / z(M+Na) + Calcd.for C 39 h 56 o 6 Na: 643.3969, Found: 643.3981); 1 H NMR (500MHz, CD 3 OD)δ7.51(1H,d,J=15.8Hz),7.03(1H,d,J=2.0Hz),6.94(1H,dd,J=8.2,2.0Hz),6.78(1H,d,J= 8.2Hz),6.23(1H,d,J=15.8Hz),5.20(1H,brt),4.97(1H,dd,J=9.1,7.6Hz),3.52(2H,d,J=10.0Hz),3.35 (d,10Hz,1H),3.16(1H,d,J=12.7Hz),3.11(1H,d,J=11.8Hz),1.23(3H,s),1.07(3H,s),1.02(3H, s), 0.89(6H,s), 0.83(3H,s).

[0047] 13 C NMR (125MHz, CD 3 OD)δ169.2,149.5,146.7,146.6,145.8,127.7,123.4,122.9,116.5,115.6,115.1,75.8,69.8,64.7,49.1,47.9,47.8,43.8,43,43,41,39.2,38.1,37 35.3, 33.7, 33.1, 32.3, 31.8, 26.6, 26.6, 24.6, 24.1, 24, 22.9, 18.8, 17.3, ...

Embodiment 3

[0052] Biological activity of the extract of the traditional Chinese medicine Lelicus chinensis and its active components and active compounds.

[0053] 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 PC 12 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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Abstract

The invention provides a preparation method of a manyflower tickclove herb extract, as well as an active component and an active compound thereof. A pentacyclic triterpenoid type active compound can be obtained by crushing traditional Chinese medicine manyflower tickclove herb, then leaching and separating to obtain an ester layer active component, and further performing HPLC (high performance liquid chromatography) purification. According to the preparation method provided by the invention, PC12 cells are adopted as an effective activity identification system, and the manyflower tickclove herb ethanol extract, as well as the active component and the active compound thereof are found to be capable of inducing neurite outgrowth of the PC12 cells, have the significant activity of imitating a nerve growth factor and be capable of being applied in preparation of medicaments and health care foods for preventing senile dementia and other neurodegenerative diseases. As the sources of the manyflower tickclove herb are wide, and the material is convenient to take, the preparation method provided by the invention can enable the development of the new pharmaceutical application of the manyflower tickclove herb to be possible.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a preparation method of an extract of leech locust and its active components and active compounds, and its application in food and medicine for preventing and treating 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 201...

Claims

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Application Information

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IPC IPC(8): C07J63/00A61K31/56A61P25/28A23L1/30
Inventor 戚建华曹时宁向兰
Owner ZHEJIANG UNIV