New codonopsis pilosula alkynol compound as well as preparation method and application thereof and pharmaceutical composition thereof

A technology of compound and Codonopsis pilosula, which is applied in the field of compound extraction and separation, can solve the problems of complex components of traditional Chinese medicine, unclear active ingredients, and unstable curative effect

Inactive Publication Date: 2017-06-13
NORTH CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the composition of traditional Chinese medicine is complex, the active ingredients are not clear, the curative effect is unstable, and the mechanism of action is not clear, which seriously affect...

Method used

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  • New codonopsis pilosula alkynol compound as well as preparation method and application thereof and pharmaceutical composition thereof
  • New codonopsis pilosula alkynol compound as well as preparation method and application thereof and pharmaceutical composition thereof
  • New codonopsis pilosula alkynol compound as well as preparation method and application thereof and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: 5 kg of dried Codonopsis pilosula, crushed, soaked in 40 L of distilled water for 2 hours, heated and refluxed for 3 times, 2 hours each time; after water extraction and alcohol precipitation, volatilized ethanol to have no alcohol smell, and mixed with AB-8 resin. Adsorption, after washing with pure water, eluting with 30%, 50%, 70%, 95% ethanol (each 2 times the amount of resin), receiving the eluents of each section, and concentrating under reduced pressure to obtain each extract; each extract Concentrated under reduced pressure to obtain 30%, 50%, 70%, and 95% ethanol elution fractions of 12 g, 60 g, 100 g, and 160 g; the 50 % ethanol elution fractions were subjected to silica gel (200-300 mesh, 500 g) column chromatography , CH 2 Cl 2 -MeOH (100:1→1:1) gradient elution separation gave fractions Fr1-Fr10;. Fr6 (10 g) was separated by medium pressure column chromatography (10 – 90% methanol gradient over 10 hours) In 50 fractions (1 fraction of 500 ml), ...

Embodiment 2

[0028] Example 2: Application of Compound 1 in the preparation of a medicament for preventing and / or treating neurodegenerative diseases. The neurodegenerative diseases are stroke, dementia, neuroinflammation, heavy metal poisoning, and nerve agent poisoning. The dementia is Alzheimer's disease and vascular dementia.

[0029] The physicochemical and spectral data of the new Codonopsis alkynols are as follows:

[0030] Yellow oil, ESI-MS m / z 217 [M+H] + . 1 H-NMR (500 MHz, CD 3 OD) δ : 6.23(1H, dt, J =11.0, 6.0Hz, H-2),6.28(2H, dd, J = 16.0, 5.0Hz, H-9), 5.83(1H, dt, J =15.5, 2.0Hz, H-8), 5.67(1H, dd, J = 11.0, 1.0Hz, H-3), 4.31(2H, dd, J = 6.5,1.5Hz, H-1) ; 13 C-NMR (125 MHz, CD 3 OD) δ : 149.1(C-2), 147.5(C-9), 109.5(C-3), 108.9(C-8), 82.1(C-8), 80.0(C-7), 78.4(C-1') , 77.9(C-6), 74.6(C-5), 69.5(C-5'), 61.3(C-1), 33.0(C-2'), 27.0(C-4'), 24.4(C- 3').

[0031] Pharmacological experiments

[0032]Test material 1. Test drug: the monomer compound of the ...

experiment example 1

[0033] Experimental Example 1: Influence of the compounds of the present invention on the survival state of neurons in rat cerebral cortex and protective effect in the model of neuronal apoptosis induced by sodium nitroprusside

[0034] In the study of the effects of compounds on neuronal survival, primary cultured rat cortical neurons (DIV-9) were divided into control group and administration group (10 μM), n = 6; In the study of the protective effect of the apoptosis model, the primary cultured rat cortical neurons (DIV-7) were divided into control group, sodium nitroprusside (350 μM) modeling group, sodium nitroprusside (350 μM) + Eda Ravone (100 μM) administration group, sodium nitroprusside (350 μM) + compound (10 μM) administration group, n =6. After administration, cells were incubated in a cell incubator for 24 hours, and cell viability was measured by MTT method (570 nm). Taking the absorbance of the control group as the standard, the ratio of the absorbance of each ...

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PUM

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Abstract

The invention discloses a new codonopsis pilosula alkynol compound 1 extracted from codonopsis pilosula, a preparation method thereof, a pharmaceutical composition containing a new codonopsis pilosula alkynol compound and application in a neuroprotective drug, especially senile dementia. Pharmacological experiments show that the compound embodies neuroprotection activity and has good neuroprotection activity in a sodium nitroprusside injury primary neuron model and a glutamic acid-induced primary neuron toxicity model. A structural formula of the compound 1 is as shown in the specification.

Description

technical field [0001] The invention relates to the field of compound extraction and separation, in particular to new Codonoprolol and its preparation method, application and pharmaceutical composition. Background technique [0002] Codonopsis is a traditional precious Chinese medicinal material in my country, which is a plant of the Campanulaceae family. Codonopisis pilosula (Franch) Nannf, Codonopsis Codonopsis pilosula Nannf .var .modesta (Nannf.) L.T.Shen or Sichuan Codonopsis Codonopis tangshen The dry root of Oliv, its nature is sweet and flat, mainly belongs to the spleen and lung meridians. Embolism, mainly produced in Shanxi, Shaanxi, Gansu and other places. [0003] With the acceleration of the aging society in my country, the number of elderly people is increasing. According to statistics, by 2020, the level of aging in my country will reach 17.17%, and the number of patients with various geriatric diseases is also on the rise. In developed countries, Al...

Claims

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Application Information

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IPC IPC(8): C07D309/06A61K31/351A61P9/10A61P25/28A61P25/00A61P29/00A61P39/02
CPCC07B2200/09C07D309/06
Inventor 王晓霞庄鹏宇陈金铭张丹阳林晓莹杨宇柯
Owner NORTH CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY
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