Radix ophiopogonis nerve growth factor activity simulating component and compound and preparation

A technology for active components and compounds, which is applied in the fields of steroids, organic active ingredients, food preparation, etc., can solve the problems of limited application and inability to pass the blood-brain barrier, etc., and achieves the effect of simple preparation method, high purity and optimized structure.

Inactive Publication Date: 2013-12-18
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, NGF is a protein containing more than 100 amino acids. Its large molecular weight and strong polarity prevent it from passing through the blood-brain barrier, which limits its clinical application.

Method used

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  • Radix ophiopogonis nerve growth factor activity simulating component and compound and preparation
  • Radix ophiopogonis nerve growth factor activity simulating component and compound and preparation
  • Radix ophiopogonis nerve growth factor activity simulating component and compound and preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 Extraction and Separation of Ophiopogon japonicus

[0041] (1) Crushing and extraction:

[0042] 10.0 kg of the traditional Chinese medicine Ophiopogon japonicus ( Ophiopogon japonicus (Thunb.) Ker-Gawl) crushed, leaching with 50.0 L of methanol (industrial grade) at room temperature for 3 days with shaking. After suction filtration and concentration, a crude sample of methanol extract was obtained. Then, the crude sample was dissolved with ethyl acetate and water, and both were transferred to a separatory funnel for solvent distribution. After the upper ester layer and the lower aqueous layer were concentrated respectively, the crude sample of ethyl acetate layer (15.9 g) and the crude sample of aqueous layer ( 2.9 kg).

[0043] (2) Separation and purification of the crude sample in the water layer:

[0044] First, the crude sample of the aqueous layer (2.9 kg) was evenly divided into 10 parts, and each part was separated by a reversed-phase silica g...

Embodiment 2

[0045] Embodiment 2 is to the qualitative identification of the physical and chemical characteristics of the compound 1-4 obtained in embodiment 1 and compound structure:

[0046] Compound 1: colorless solid; high resolution mass spectrometry shows its molecular formula is C 43 h 68 o 16 (HR ESI-TOF-MS m / z(M+H) + Calcd.for C 43 h 69 o 16 :841.4586,Found:841.4603).

[0047] Table 1 Compound 1 1 H and 13 C NMR data (solvent: pyridine-d 5 )

[0048]

[0049] a 500MHz, the coupling constant (Hz) is in brackets, b 125MHz.

[0050] Compound 2: Colorless solid; high-resolution mass spectrometry showed its molecular formula to be C 45 h 70 o 16 (HR ESI-TOF-MS m / z (M+H) + Calcd.for C 45 h 71 o 16 :867.4742,Found:867.4736).

[0051] Table 2 Compound 2 1 H and 13 C NMR data (solvent: pyridine-d 5 )

[0052]

[0053] a 500MHz, the coupling constant (Hz) is in brackets, b 125MHz.

[0054] Compound 3: a colorless solid; high-resolution mass spectrometry show...

Embodiment 3

[0059] Example 3 The active components in Ophiopogon japonicus and its compounds exhibited significant NGF-mimicking activity in PC12 cells, an in vitro screening model of senile dementia.

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PUM

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Abstract

The invention provides a preparation method of an active component extracted from traditional Chinese medicine, namely, radix ophiopogonis, an active saponin compound contained in the component, and a separation and preparation method of the compound. The identification result shows that the active component of the radix ophiopogonis contains four active compounds. According to the experiment for an anti-senile dementia in vitro screening model, namely, rat pheochromocytoma cells, the active component of radix ophiopogonis and the four active components show remarkable nerve growth factor simulating activity, namely, NGFmimics, which can promote the outgrowth and protuberance of nerve cells. The preparation method has the advantages that the medical application of the active component of radix ophiopogonis and the active compound contained in the component in prevention of senile dementia is created; and a new treatment medicine is provided for preventing and treating senile dementia and other neurodegenerative diseases.

Description

technical field [0001] The invention belongs to the field of medicine and food, and specifically relates to a method for separating, extracting and preparing active components from the Chinese medicinal material Radix Ophiopogon Applications in neurodegenerative diseases such as dementia and neurotrophic protection drugs and food. Background technique [0002] Alzheimer's disease (Alzheimer's disease, Alzheimer's disease) is a progressive and fatal neurodegenerative disease. Psychiatric symptoms and behavioral disturbances. At present, Alzheimer's disease has become the fourth leading cause of human death after heart disease, cancer, and stroke. The number of patients with Alzheimer's disease in my country has exceeded 5 million, accounting for about 1 / 4 of the total number of cases in the world. With the acceleration of population aging, the number of patients will be even greater, which will seriously affect the stability and development of society. Therefore, the devel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/7048A61P25/28A23L1/29A23L33/00
Inventor 戚建华叶英曲媛
Owner ZHEJIANG UNIV
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