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Preparation method and application of total steroidal saponin extracts of dwarf lilyturf roots

A technology of steroidal saponins and extracts, which is applied in the field of traditional Chinese medicine, can solve the problems of impermeability, large molecular weight, and high price, and achieve the effects of convenient material collection, simple preparation method, and wide sources

Inactive Publication Date: 2012-08-22
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

NGF may be an effective method for the treatment of AD, but there are still the following problems: (1) expensive; (2) relatively large molecular weight, impenetrable (Blood Brain Barrier, BBB)[25], only intracerebroventricular injection, there are many technical problems in long-term treatment

Method used

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  • Preparation method and application of total steroidal saponin extracts of dwarf lilyturf roots
  • Preparation method and application of total steroidal saponin extracts of dwarf lilyturf roots
  • Preparation method and application of total steroidal saponin extracts of dwarf lilyturf roots

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Preparation of Ophiopogon japonicus total steroidal saponins extract

[0033] 1) Crushing and extraction:

[0034] After crushing 9.5 kg of traditional Chinese medicine Ophiopogon japonicus, it was extracted with 50 L of methanol (industrial grade) by shaking at room temperature for 3 days. After suction filtration and concentration, 1.2 kg of crude methanol extract was obtained.

[0035] 2) Separation and purification:

[0036] The crude sample of the aqueous layer is first separated by an ODS open column (the solvent system is methanol: water = 50:50, 60:40, 70:30, 80:20, 90:10, methanol: chloroform = 1:1) ; Then, the sample (3.8 g) containing the active ingredient was separated again with a silica gel open column (200-300 mesh, the solvent system was methanol by volume ratio: chloroform=10:90, 15:85, 20:80, 25: 75 , 30:70); finally, the white extract of total steroidal saponins of Ophiopogon japonicus (1.1 g) was obtained.

[0037] The present invention...

Embodiment 1

[0039] Qualitative identification of the physical and chemical characteristics and chemical structure of compound 1-4 obtained in embodiment 1:

[0040] The structure of compound (1) was confirmed by MS, 1 H NMR, 13 C NMR test, and confirmed after comparison with literature data.

[0041] The structure of compound (2) was confirmed by HR MS, 1 H NMR, 13 C NMR, DEPT, COZY, HMBC, HSQC and HOHAHA determined after determination.

[0042] The structure of compound (3) was confirmed by MS, 1 H NMR, 13 C NMR test, and confirmed after comparison with literature data.

[0043] The structure of compound (4) was confirmed by MS, 1 H NMR, 13 C NMR test, and confirmed after comparison with literature data.

[0044] Physicochemical properties of compound (1): white solid, [α] -105.7 ( c 0.45, pyridine); 13 C NMR (125 MHz, in pyridine- d 5 ) : 139.5 (C-5), 124.7 (C-6), 109.2 (C-22), 106.6 (C-1′′′), 101.7 (C-1′′), 100.4 (C-1′), 85.4 (C-3′), 83.4 (C-1), 81.0 (C-16), 78.3 (...

Embodiment 3

[0056] Biological activity of the total steroidal saponins extract of Ophiopogon japonicus derived from the traditional Chinese medicine Ophiopogon japonicus.

[0057] In animal models of neurodegeneration, 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 total steroidal saponin extracts of dwarf lilyturf roots, which comprises the following steps: crushing traditional Chinese medicine dwarf lilyturf roots, leaching with methanol, concentrating through vacuum filtration, separating through an ODS column, and finally separating through a silica gel chromatography open column. Based on an anti-senile dementia in-vitro screening model, experiment on rat adrenal pheochromocytoma cells proves that the total steroidal saponin extracts of dwarf lilyturf roots have activity remarkably similar to that of anerve growth factor (NGF) and can promote nerve cells to grow out and protrude. Thus, the invention is applicable to the preparation of medicaments for preventing and treating senile dementia, especially medicaments for treating Alzheimer diseases and other neurodegenerative diseases. The invention expands the pharmaceutical application of the total steroidal saponin extracts of dwarf lilyturf roots; the preparation method is convenient; the extracted product has high purity; and dwarf lilyturf roots have extensive sources and can be acquired conveniently.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicines, and in particular relates to a preparation method of Ophiopogon japonicus total steroidal saponins extract and its application in the preparation of drugs for preventing and treating neurodegenerative diseases such as senile dementia. Background technique [0002] With the development of the global social population, the growth of the elderly population is a worldwide trend, and the prevalence and incidence of senile dementia are gradually increasing. Senile dementia is not only a medical problem, but will become a prominent social problem . At present, there are probably 17 million Alzheimer's patients worldwide. With the aging population, the incidence of Alzheimer's disease has risen to the third common cause of death, second only to cardiovascular and cerebrovascular diseases and cancer. Alzheimer's disease has gradually become a chronic disease that seriously threatens the healt...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J71/00A61K31/7048A61P25/28
Inventor 戚建华曲媛叶英李静
Owner ZHEJIANG UNIV
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