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Eucommia active monomer compound as well as preparation method, pharmaceutical composition and application thereof

A technology of active monomers and compounds, applied in the field of active monomers of traditional Chinese medicine and their preparation, can solve the problems of unclear active ingredients and action mechanism, and the application of Eucommia active monomer compounds has not yet been seen, and achieves stable and easy separation process, Abundant sources and positive effects

Inactive Publication Date: 2014-05-07
HENAN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, studies have shown that Eucommia bark and its seeds, leaves, and flowers have sedative and hypnotic effects, but the specific active ingredients and mechanism of action in Eucommia are still unclear, and no active monomeric compounds of Eucommia have been seen so far. Information on applications in the field of sedation and hypnosis

Method used

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  • Eucommia active monomer compound as well as preparation method, pharmaceutical composition and application thereof
  • Eucommia active monomer compound as well as preparation method, pharmaceutical composition and application thereof
  • Eucommia active monomer compound as well as preparation method, pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The preparation method of the eucommia active monomer compound shown in formula I, the steps are as follows:

[0033] (1) System solvent extraction process

[0034] Eucommia ulmoides leaves were picked and cleaned to remove impurities, dried in the shade, and lightly crushed. Take 2500g of it, soak it in 30L of ethanol with a mass percentage of 75%, soak it for two weeks, recover the soaking solution (65°C, 0.08 mp) in vacuum and low temperature, repeat three times, and combine , to obtain ethanol extract, dry weight 442g, and then use the system solvent method to extract and separate extracts of different polarities. Each solvent was repeatedly extracted four times, and each extract was concentrated respectively to obtain various solvent extracts, including 29.0 g of petroleum ether extract, 50.7 g of ethyl acetate extract, and 128.2 g of n-butanol extract. The remaining aqueous phase obtained 343.0 g of water extract;

[0035] (2) Chromatographic separation process ...

Embodiment 2

[0085] The health-care herbal tea provided in this example is composed of 4-hydroxy-3-(2-hydroxyethyl)-1-cyclopentene-1,2-dimethanol, black tea and compound sweetener, wherein 4-hydroxy- The weight percentage of 3-(2-hydroxyethyl)-1-cyclopentene-1,2-dimethanol is 3%.

[0086] The preparation method of the health-care herbal tea provided in this example: take 3 grams of 4-hydroxy-3-(2-hydroxyethyl)-1-cyclopentene-1,2-dimethanol, mix it with 50 grams of black tea leaves, Go to the pulverizer and pulverize to 15-30 mesh, add 47 kilograms of compound sweeteners, put into special paper bubble bag after mixing thoroughly, coat aluminum-plastic compound bag, seal, every bag 5-8 gram, make the health care of this embodiment herbal tea.

Embodiment 3

[0088] The health-care granule provided in this example is composed of 4-hydroxy-3-(2-hydroxyethyl)-1-cyclopentene-1,2-dimethanol, fruit juice powder and white sugar, in which 4-hydroxy-3- The weight percentage of (2-hydroxyethyl)-1-cyclopentene-1,2-dimethanol is 1%.

[0089] The preparation method of the health care granule provided in this example: take 1 gram of 4-hydroxy-3-(2-hydroxyethyl)-1-cyclopentene-1,2-dimethanol, mix it with 50 grams of fruit juice powder and 49 grams of white Granulated sugar is mixed, passed through a 12-mesh sieve, dried at 75° C., packaged into bags, and made into the health-care granule of this embodiment.

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Abstract

The invention discloses a eucommia active monomer compound, the structural formula of which is shown in the specification. The invention also discloses a preparation method of the compound, a pharmaceutical composition containing the compound and pharmaceutical application of the compound. The active monomer compound is extracted from eucommia and can be extracted from eucommia bark, eucommia leaves, eucommia male flowers, eucommia seeds or whole eucommia plants. The extracted active monomer compound is 4-hydroxy-3-(2-hydroethyl)-1-cyclopentene-1,2-dimethanol, and experiments prove that the compound has obvious sedation, hypnogenesis, anti-convulsion and other effects as well as no side effect and dependence, and can be taken for a long time. The active monomer compound extracted from eucommia and the effects of the compound in the aspects of sedation, hypnogenesis, anti-convulsion and the like are provided in the invention, thereby providing a novel natural active substance for researching and developing novel health-care food and novel sedative-hypnotic drugs.

Description

technical field [0001] The invention relates to the technical field of active monomers of traditional Chinese medicine and the preparation thereof, in particular to an active monomer compound of eucommia ulmoides, a preparation method, a pharmaceutical composition and its application. Background technique [0002] Insomnia is a clinical frequently-occurring disease with complex etiology and easy recurrence. Insomnia seriously affects people's life, work and physical and mental health. The incidence of serious accidents and trauma caused by long-term insomnia is significantly higher than that of normal sleepers. Insomnia, if left untreated, can lead to disturbances in metabolism and systemic function, causing significant changes in mood, behavior, and psychomotor function. [0003] Drug therapy is one of the most important means for the treatment of insomnia. The effect of sedative hypnotics can make the patient's tension, irritability, insomnia and other mental overexcite...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C33/12C07C29/76A61K31/047A61P25/20A61P25/08A23L1/29A23L33/00
Inventor 朱文学李欣樊金玲罗磊刘少阳白喜婷于明刘严
Owner HENAN UNIV OF SCI & TECH
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