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Preparation method of 1,5,8-Trihydroxy-3-methoxy?ketone

A technology of methoxy ketone and trihydroxy, which is applied in the field of preparation of 1,5,8-trihydroxy-3-methoxy* ketone to achieve the effects of improving extraction efficiency, simplifying operation steps and saving reagents

Inactive Publication Date: 2014-05-28
李旻辉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, about 1,5,8-trihydroxy-3-methoxy The effect of ketone (bellidifolin) in the treatment of arrhythmia has not been reported in the literature

Method used

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  • Preparation method of 1,5,8-Trihydroxy-3-methoxy?ketone
  • Preparation method of 1,5,8-Trihydroxy-3-methoxy?ketone
  • Preparation method of 1,5,8-Trihydroxy-3-methoxy?ketone

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Experimental program
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Embodiment 1

[0026] Monomeric compound 1,5,8-trihydroxy-3-methoxy from Pseudogentiana acuminate Study on Pharmacological Action of Bellidifolin

[0027] 1 Materials and methods

[0028] 1.1 Animals SD rats, weighing 200±20g, were provided by the Experimental Animal Center of Inner Mongolia University.

[0029] 1.2 Drug 1,5,8-trihydroxy-3-methoxy Ketone (self-made, purity greater than 98% by HPLC); verapamil hydrochloride injection 5mg / support (batch number 5E12002, Shanghai Hefeng Pharmaceutical Co., Ltd.); barium chloride (analytical pure, Tianjin Jinbei Fine Chemical Factory) ; Sodium pentobarbital (imported by Foshan Experimental Chemical Factory, batch number 060901).

[0030] 1.3 Instrument BL-420F biological function experiment system, Chengdu Taimeng Technology Co., Ltd., China.

[0031] 1.4 Method

[0032] Get 80 healthy SD rats, half male and half male, randomly divided into 5 groups (wherein three groups are test groups with different concentrations, one group is verapamil...

Embodiment 2

[0043] 1,5,8-trihydroxy-3-methoxy Preparation method of ketone compound and its extract

[0044] 1 Materials and methods

[0045] 1.1 Materials Pseudogentian apicalis was collected from Genhe City, Inner Mongolia Autonomous Region in July 2008. The sample was identified as Gentianaceae plant Pseudomonas apicalis by Mr. Wang Zhenwang from the Medicinal Plant Teaching and Research Office of Baotou Medical College; thin layer of silica gel G, column layer Analytical silica gel (100-200, 200-300 mesh) was purchased from Qingdao Ocean Chemical Factory; the reagents used (absolute ethanol, ethyl acetate, petroleum ether) were of analytical grade.

[0046] 1.21,5,8-trihydroxy-3-methoxy Extraction of ketone: crush and dry 500g of the aerial part of Pseudomonas acuminate, reflux and extract with 95% ethanol for 3 times, combine the extracts and concentrate to the extract to obtain 107g of extract; mix the extract with diatomaceous earth 1:1, place In a Soxhlet extractor, extract w...

Embodiment 3

[0051] (1) Crush and dry the above-ground part of Pseudogenus acuminate, extract with reflux 3 times with 95% ethanol, combine the extracts and concentrate to extract. Mix the extract and diatomaceous earth 1:1, place in a Soxhlet extractor, extract with 60-90°C petroleum ether and ethyl acetate successively until it is colorless, and concentrate the ethyl acetate extract under reduced pressure to After 300mL, an equal volume of absolute ethanol solution was added, a yellow precipitate appeared, allowed to stand, and filtered to obtain 1,5,8-trihydroxy-3-methoxy Ketone 88.5% extract.

[0052] (2) After dissolving the precipitate with ethyl acetate, take an equal amount of 100-200 mesh silica gel and mix until it is dry and uniform particles; dry the sample, and use 6 times the amount of 200-300 mesh silica gel column chromatography wet Separation by method, eluting with petroleum ether-ethyl acetate 7:3 in volume ratio, and recovering the solvent under reduced pressure to ob...

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Abstract

The present invention relates to application of bellidifolin and an extract thereof in preparations of drugs for prevention and treatment of cardiacarrhythmia. The present invention further discloses a drug composition, wherein the drug composition comprises bellidifolin adopted as an active ingredient or a pharmaceutically-acceptable carrier thereof, and an excipient or a diluent. Results of pharmacological experiments show that: the bellidifolin and the extract thereof have anti-cardiacarrhythmia effects, provide strong cardiacarrhythmia prevention activities compared with the control group, and provide the similar pharmacological properties compared with the positive control group of verapamil. In addition, the experimental study results of the present invention provide strong experimental supports for reasonable application of gentianella acuta traditional Chinese drug.

Description

[0001] The invention is funded by the National Science and Nature Foundation Project (81160504), the Science and Technology Research Project of the Inner Mongolia Education Department (NJ09161), and the Baotou Medical and Health Fund Project (2009S1001-31). technical field [0002] The present invention relates to the novel use of the monomer compound bellidifolin in Pseudogentiana acuminate, more specifically 1,5,8-trihydroxy-3-methoxy Application of ketone (bellidifolin) and its extract in the preparation of drugs for preventing and treating arrhythmia. Background technique [0003] According to the relevant literature of traditional Chinese medicine, the medicinal plants of the genus Pseudogentian often replace some medicinal plants of the genus Swertia and Sternia for the treatment of hepatitis and biliary colic. From the perspective of plant phylogeny, Pseudogentian is closely related to Swertia and Costa; from the perspective of chemical composition, the phytochemical...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P9/06
Inventor 李旻辉吕丽娟
Owner 李旻辉
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