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New uses of 20(S)-protopanaxadiol

A technology of protopanaxadiol and myocardial ischemia, applied in the application field of medicine, can solve the problems such as no report on myocardial protection effect, and achieve the effects of low cost, small side effects and simple production process

Active Publication Date: 2014-01-15
SHANGHAI INNOVATIVE RESEARCH CENTER OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the saponins of the diol group can be rapidly converted into various metabolites in the body after oral administration, including Rg3, Rh2, compound-K and PPD, these metabolites are significantly different from the saponins of the protopanaxadiol group in mechanism, and their myocardial protection The effect has not been reported

Method used

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  • New uses of 20(S)-protopanaxadiol
  • New uses of 20(S)-protopanaxadiol
  • New uses of 20(S)-protopanaxadiol

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0037] Experimental example 1: Effect on in vitro cultured cardiomyocytes treated with hydrogen peroxide

[0038] In order to investigate the cardioprotective function of metabolite 20(S)-protopanaxadiol saponin (PPD) of protopanaxadiol group saponins, this experiment selected the main diol group saponin Rb1 in the protopanaxadiol group saponin group to compare PPD and Rb1 protect cardiomyocytes treated with hydrogen peroxide in vitro.

[0039] 1. Test material

[0040] 1.1 Test samples: 20(S)-protopanaxadiol (PPD), Rb1 are provided by Shanghai Traditional Chinese Medicine Innovation Research Center;

[0041] 1.2 Experimental equipment:

[0042] Clean bench, Shanghai Dianshan Lake Purification Equipment Factory;

[0043] constant temperature CO 2 Incubator, American Forma company;

[0044] Enzyme-linked immunoassay instrument, American BioTek company;

[0045] Inverted biological microscope, Chongqing Optical Instrument;

[0046] Desktop constant temperature shaker, Tai...

experiment example 2

[0063] Experimental Example 2: Effects on Myocardial Ischemia and Ischemia-Reperfusion Injury Models

[0064] In order to further confirm the effect of 20(S)-protopanaxadiol on myocardial protection, the following example is a pharmacological and pharmacological study of 20(S)-protopanaxadiol on animal models of myocardial ischemia and ischemia-reperfusion injury.

[0065] 1. Test material

[0066] 1.1 Test samples

[0067] 20(S)-protopanaxadiol (PPD), provided by Shanghai Innovation Research Center of Traditional Chinese Medicine; prepare 20(S)-protopanaxadiol into a suspension according to the following method: Weigh 100mg sample, add 10ml 0.5% Grind CMC-Na and make a 10mg / ml suspension

[0068] 1.2 Positive control samples

[0069] Name: Nifedipine Tablets, provided by Shanghai Pharmaceutical (Group) Co., Ltd. Xinyi Pharmaceutical General Factory, specification: 10mg / tablet, batch number: Guoyao Zhunzi H31021222; properties: film-coated tablets; storage method: store at ...

Embodiment 1

[0145] Embodiment 1: The preparation method of 20(S)-protopanaxadiol

[0146] 1. Add 5.0 kg of notoginseng leaf glycosides, add n-butanol and sodium ethylate, put it into the reaction kettle, stir, feed oxygen, keep the bubbles in the bubbles continuously emerging, heat up, and react for 72 hours; add n-butanol after cooling down Saturated water was washed twice, the water layer was separated, n-butanol was concentrated under reduced pressure and recovered to dryness, n-butanol was recovered, the residue was stirred with water, extracted three times with ethyl acetate, the water layer was discarded, and the ethyl acetate layers were combined and used Wash twice with saturated saline, and remove the water layer;

[0147] 2. Add anhydrous sodium sulfate to the ethyl acetate layer, dry it, concentrate the ethyl acetate layer to dryness under reduced pressure, recover the ethyl acetate, and obtain the crude product of protopanaxadiol;

[0148] 3. Add ethyl acetate to the crude pr...

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Abstract

The present invention relates to a new use of 20(S)-protopanoxadiol, and in particular, to an application of 20(S)-protopanoxadiol in preparing the medicines for preventing and treating ischemic heart diseases. Pharmacodynamics studies have found that 20(S)-protopanoxadiol can reduce myocardial histological damages caused by ischemia and ischemia reperfusion, reduce enzyme indicators related to infarct size and myocardial necrosis, and reduce the drift of J-spot on an electrocardiogram.

Description

technical field [0001] The present invention relates to a new application of 20(S)-protopanaxadiol, in particular to the application of 20(S)-protopanaxadiol in the preparation of medicines for preventing and treating ischemic heart disease. Background technique [0002] In my country, cardiovascular disease (including hypertension and coronary heart disease) has become a major disease that endangers human health and life. In 2002, the mortality rate of heart disease among residents in big cities in my country was 75.68 per 100,000 people, ranking the third cause of death after malignant tumors and cerebrovascular accidents. [0003] Myocardial ischemic heart disease, also known as coronary heart disease, refers to heart disease caused by myocardial ischemia or hypoxia caused by coronary atherosclerosis, which narrows or blocks the lumen, and is caused by coronary atherosclerosis. The most common type of organ disease. Clinical manifestations include stable angina, unstabl...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61P9/10
CPCA61K31/575A61P9/10
Inventor 许长江张文静潘欣萍汪沁琳杨子荣
Owner SHANGHAI INNOVATIVE RESEARCH CENTER OF TRADITIONAL CHINESE MEDICINE
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