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Preparation and anti-Alzheimer's disease uses of Ilex kudingcha C.J.Tseng leaf extract

A kind of Kudingcha extract and the technology of Kudingcha, applied in the field of medicine, can solve the problems of large molecular weight, inability to pass through the blood-brain barrier, and limited clinical application. Effect

Active Publication Date: 2016-12-21
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it is a polypeptide composed of more than 100 amino acids; due to reasons such as large molecular weight and strong polarity, it cannot pass the Blood Brain Barrier (Blood Brain Barrier), and it is difficult to prepare on a large scale, which limits its actual clinical application.
At present, there is no better treatment method for NGF other than direct administration of intracerebral surgery.

Method used

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  • Preparation and anti-Alzheimer's disease uses of Ilex kudingcha C.J.Tseng leaf extract
  • Preparation and anti-Alzheimer's disease uses of Ilex kudingcha C.J.Tseng leaf extract
  • Preparation and anti-Alzheimer's disease uses of Ilex kudingcha C.J.Tseng leaf extract

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The preparation of embodiment 1 Kudingcha active component and active compound

[0036] (1) Crushing and extraction:

[0037] After 100g of traditional Chinese medicine Kudingcha was pulverized, it was leached with 1L of methanol at room temperature for 3 times, each time for 24 hours. After the filtrate was concentrated and dried, it was alternately extracted and separated with water and ethyl acetate for several times to obtain the active component of the ester layer (A )7g;

[0038] (2) Separation and purification:

[0039] 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 then separated by normal hexane:ethyl acetate (100:0,70:30,50:50,0 :100) eluting, finally rinse with methanol, combine n-hexane: the elution fraction of ethyl acetate 70:30, obtain active component (b) 2g; Merge the elution fraction of methanol, obtain active component (B ) 2.2g.

[0040] 2 g of act...

Embodiment 1

[0043] Qualitative identification of physical and chemical characteristics and chemical structure of the compound obtained in embodiment 1:

[0044] The structures of compounds (1)-(4) were analyzed by LC-MS, 1 H NMR, 13 Confirmed after comparison of C NMR and literature data.

[0045] Compound 1: white solid, C 30 h 50 O(HRESI-TOF-MS m / z(M+H) + calcd for 427.3934,C 30 h 51 O), 1 H-NMR (500MHz, CDCl 3 ):δ0.76(s,3H),0.79(s,3H),0.83(s,3H),0.94(s,3H),0.97(s,3H),1.03(s,3H),1.68(s, 3H),4.69(1H,d,J=1.98Hz,H-29a),4.57(1H,d,J=2.03Hz,H-29b)3.19(1H,dd,J=11.40,4.85Hz,3-H ).

[0046] 13 C-NMR (125MHz, CDCl 3 ): Δ151.13,109.47,79.16,55.45,50.59,48.46,48.14,42.99,40.99,40.16,38.86,37.32,34.44,30,27.0,27.37.37,57,57,57,57,57,57,57,57,57,57,57,57.37.5.37.5. 18.47, 18.16, 16.27, 16.13, 15.52, 14.70.

[0047] Compound 2: white solid, C 30 h 50 O(HRESI-TOF-MS m / z(M+H) + calcd for 427.3934,C 30 h 51 O), 1 H-NMR (500MHz, CDCl 3 ):δ0.80(m,9H),0.91(s,3H),0.95(s,3H),1.00(s,3H),1....

Embodiment 3

[0061] Biological activities of active components (A), (b)-(f), (B)-(E), and active compounds (1)-(5) of traditional Chinese medicine Kudingcha.

[0062] 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, under the action of NGF, they will stop dividing, grow protrusions, and transform into neuron-like cells. Therefore, using PC 12 cells as an effective activity identification system to screen compounds with neuromimetic activity may become an effective drug for the treatment of Alzheimer's disease.

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Abstract

The invention provides a preparation method of an Ilex kudingcha C.J.Tseng leaf extract, wherein a traditional Chinese medicine Ilex kudingcha C.J.Tseng leaf is crushed, leached, separated and purified to obtain the Ilex kudingcha C.J.Tseng leaf extract, wherein the Ilex kudingcha C.J.Tseng leaf extract comprises active components (A), (b)-(f) and (B)-(E), and active compounds (1)-(5), and the active components (A), (b)-(f) and (B)-(E), and the active compounds (1)-(5) have the significant nerve growth factor simulation activity so as to be used for preparation of drugs and health food for prevention of Alzheimer's disease and other neurodegenerative diseases. According to the present invention, the traditional Chinese medicine Ilex kudingcha C.J.Tseng leaf has characteristics of wide source, easy obtaining and low cost, such that the development of the traditional Chinese medicine Ilex kudingcha C.J.Tseng leaf into the drugs and health food for prevention of Alzheimer's disease and other neurodegenerative diseases has important significance.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a preparation method of Kudingcha extract, its active components and active compounds, and its use in food and medicine for the prevention and treatment of neurodegenerative diseases such as Alzheimer's disease Applications. Background technique [0002] The rapid growth of the elderly population has made people more concerned about the health status of this group. According to the statistics of health organizations in various countries, only in Europe and the United States, 20% of people will be troubled by brain dysfunction diseases in their lifetime, and the total annual expenditure is as high as 2 trillion US dollars, which exceeds the cost of cardiovascular diseases, cancer, and diabetes. total, and this number is expected to continue to increase as human longevity increases. In particular, Alzheimer's disease (Alzeimer's disease, AD) has become a major factor ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/185A61P25/28A23L33/105
Inventor 戚建华曹雪丽長田裕之向兰
Owner ZHEJIANG UNIV
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