Triterpenoid compounds, and preparation and application thereof

A compound and technology of triterpenoids, applied in the field of structure and preparation of triterpenoids, to achieve the effect of simple preparation method, high purity and optimized structure

Inactive Publication Date: 2013-10-23
ZHEJIANG UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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  • Triterpenoid compounds, and preparation and application thereof
  • Triterpenoid compounds, and preparation and application thereof
  • Triterpenoid compounds, and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Preparation of Compound A and Compound B

[0035] A preparation method for obtaining compounds A and B with significant NGF-mimicking activity from Motherwort Motherwort, the specific steps are:

[0036] (1) Grinding and extraction: After 300 g of Motherwort, a traditional Chinese medicine, was crushed, it was extracted with 1L of methanol (industrial grade) at room temperature for 5 days (shaking). After suction filtration and concentration, a crude sample of the methanol extract was obtained, and the solvent was partitioned with water and ethyl acetate to obtain a total of 6 grams of a crude sample of the ethyl acetate layer and 14 grams of a crude sample of the aqueous layer.

[0037](2) Separation and purification: separate the crude ethyl acetate layer through a silica gel open column (200-300 mesh, the following is the solvent volume ratio, n-hexane:chloroform=2:8,1:9,0:10, chloroform : Methanol=98:2, 96:4, 94:6, 92:8, 90:10), collect and combine chlo...

Embodiment 2

[0041] Example 2 Qualitative identification of the physical and chemical characteristics and compound structure of compound A, B obtained in embodiment 1:

[0042] The chemical structures of compounds A and B were determined by mass spectrometry (including high-resolution mass spectrometry) and nuclear magnetic resonance.

[0043] Compound A, a colorless solid, is easily soluble in methanol. When analyzed by TLC, using chloroform:methanol (8:2) as the developing solvent, the Rf value is 0.5 on a forward silica plate with a height of 5 cm. This sample has significant UV absorption at 228 nm.

[0044] Compound B, a colorless solid, is easily soluble in methanol. When analyzed by TLC, using chloroform:methanol (9:1) as developing solvent, on a forward silica plate with a height of 5 cm, the Rf value is 0.5. This sample has significant UV absorption at 228 nm.

[0045] Compound A, the molecular formula is C 36 h 56 o 11 ; HR FT-ICR MS: m / z 687.3707[M+Na] + , theoretical ...

Embodiment 3

[0047] Example 3 The compound exhibits significant NGF-mimicking activity in PC12 cells, an in vitro screening model of senile dementia.

[0048] experiment method:

[0049] 1) Culture of PC12 cells: inoculate 20×10 4 Each cell was placed in a 100 mm culture dish, containing 10 ml of DMEM medium (containing 10% horse serum, 5% fetal bovine serum), and the medium was replaced every two days, and subculture was carried out when the cell density reached the requirement. First wash the cells twice with PBS, then add 10 ml PBS to the culture dish, at 37 ℃, 5% CO 2 Let it stand in the incubator for 10 minutes, take it out and wash it, transfer the PBS with suspended cells to a 15 ml disposable centrifuge tube, count with a hemocytometer after centrifugation, and add 1 ml of serum to each well of the 24-well plate DMEM medium, after cell counting, each well was inoculated with 2×10 4 cells, mixed well, in CO 2 Samples were added after 24 hours in the incubator.

[0050] 2) A...

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PUM

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Abstract

The invention provides triterpenoid compounds, which are prepared by the following steps: pulverizing and leaching a traditional Chinese medicine Lindernia crustacea, separating the extract through a silica gel column, and purifying by high performance liquid chromatography. The in-vitro cytoactive experiment proves that the separated compounds have nerve growth factor NGF-like activity, and the in-vivo animal experiment proves that the separated compounds B have the effect of enhancing the senile dementia model mouse memory function; and therefore, the compounds can be applied to preparation of medicines or foods for preventing and treating senile dementia and other neurodegenerative diseases, and especially to preparation of medicines or foods for treating Alzheimer's disease (AD) and other neurodegenerative diseases. The preparation method provided by the invention is reasonable and simple to operate. The invention provides new therapeutic medicines for treating senile dementia and other neurodegenerative diseases. The structural general formula is disclosed in the specification.

Description

technical field [0001] The invention belongs to the fields of medicine and food, and specifically relates to a method for separating, extracting and preparing a class of natural compounds from Motherwort, a Chinese medicinal material, in particular to the structure and preparation method of triterpenoids, and the role of such compounds in preventing and treating senile dementia and other neurological diseases. Applications in degenerative diseases 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 acceler...

Claims

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Application Information

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IPC IPC(8): C07J17/00C07J9/00A61K31/704A61K31/575A61P25/28A23L1/30A23L1/09A23L33/105A23L33/125
Inventor 戚建华叶英陈欢向兰王彦
Owner ZHEJIANG UNIV
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