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New Codonopsis Alcohol Compounds, Preparation Method, Application and Pharmaceutical Composition thereof

A technology of compound and Codonopsis pilosula, applied in the field of compound extraction and separation, can solve problems such as unstable curative effect, unclear mechanism of action, and complex components of traditional Chinese medicine

Inactive Publication Date: 2019-01-25
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 affects the clinical use and the entry of Chinese medicine into the international mainstream market. Drugs for the treatment of degenerative diseases are an urgent task for medical researchers for a long time to come

Method used

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  • New Codonopsis Alcohol Compounds, Preparation Method, Application and Pharmaceutical Composition thereof
  • New Codonopsis Alcohol Compounds, Preparation Method, Application and Pharmaceutical Composition thereof
  • New Codonopsis Alcohol Compounds, Preparation Method, Application and Pharmaceutical Composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: 5 kg of dried Codonopsis pilosula was crushed, soaked in 40 L of distilled water for 2 h, heated and refluxed for 3 times, 2 hours each time; Adsorption, after washing with pure water, then elute with 30%, 50%, 70%, 95% ethanol (each 2 times the amount of resin), receive the eluents of each section, concentrate under reduced pressure to obtain each extract; each extract Concentrate under reduced pressure to obtain 12 g, 60 g, 100 g, 160 g of 30 %, 50 %, 70 %, 95 % ethanol elution parts; silica gel (200-300 mesh, 500 g) column chromatography for 50 % ethanol elution parts , CH 2 Cl 2 -MeOH (100:1→1:1) gradient elution separation to obtain fractions Fr1-Fr10; Fr 6 (10g) was separated by medium pressure column chromatography (10-90% methanol gradient elution for 10 hours) 50 fractions (500 ml for 1 fraction) were obtained from Fr. 12 by preparative liquid phase to obtain a new codonopynol compound (5 mg).

Embodiment 2

[0028] Example 2: Application of Compound 1 in the preparation of drugs for the prevention and / or treatment of 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 alcohols 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 experiment

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

experiment example 1

[0033] Experimental example 1: Effect of the compound of the present invention on the survival state of rat cerebral cortex neurons and its protective effect in the model of neuron apoptosis induced by sodium nitroprusside

[0034] In the study of the effect of the compound on the survival state of neurons, the primary cultured rat cortical neurons (DIV-9) were divided into a control group and an 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) model group, sodium nitroprusside (350 μM) + ida Lavone (100 μM) administration group, sodium nitroprusside (350 μM) + compound (10 μM) administration group, n =6. After administration, the cells were placed in a cell incubator to continue culturing for 24 hours, and the cell viability was measured by MTT method (570 nm). Taking the absorbance of the control group as the standa...

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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 neocodonopsis alcohol and its preparation method, application and pharmaceutical composition. Background technique [0002] Codonopsis Codonopsis is a traditional and precious Chinese medicinal material in my country. Codonopisis pilosula (Franch) Nannf, Suhua Codonopsis Codonopsis pilosula Nannf .var .modesta (Nannf.) L .T .Shen or Sichuan Codonopsis Codonopisis tangshen The dry root of Oliv has a sweet and flat taste, and is mainly returned to the spleen and lung meridians. etc., mainly produced in Shanxi, Shaanxi, Gansu and other places. [0003] As my country's aging society accelerates, the number of elderly people continues to increase. According to statistics, by 2020, my country's aging level will reach 17.17%, and the number of patients with various geriatric diseases is also on the rise. In developed countries, Alzheimer's disease, as the most...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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