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Application of 1,3,4,5-tetrahydro-2-benzo-cycloheptatriene compound to in vitro screening or drug preparation

A technology of dibenzoxepin and benzoxepatriene, which is applied in the field of traditional Chinese medicine, can solve the problems of restricting the scientific use of medicinal plants and hindering the wide application of pinnatifida, and achieve the protection of cardiomyocytes Injury, reduce the effect of cardiomyocyte injury

Active Publication Date: 2016-05-04
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] However, due to the large number of ingredients in Campanula, people know little about the effects of each component in Campanula, which limits the scientific use of such medicinal plants in Campanula to a certain extent, and hinders the scientific use of Campanula. wide application of

Method used

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  • Application of 1,3,4,5-tetrahydro-2-benzo-cycloheptatriene compound to in vitro screening or drug preparation
  • Application of 1,3,4,5-tetrahydro-2-benzo-cycloheptatriene compound to in vitro screening or drug preparation
  • Application of 1,3,4,5-tetrahydro-2-benzo-cycloheptatriene compound to in vitro screening or drug preparation

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Experimental program
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preparation example Construction

[0034]In a typical implementation of the present invention, the preparation method of the above-mentioned dibenzoxepin-based compounds comprises the following steps: using a solvent to reflux extract the aerial part of Campanula chinensis to obtain an extract; The first extraction solvent extracts the extract for the first time to obtain the first extract; preferably the first extraction solvent is selected from petroleum ether, dichloromethane or chloroform; the second extraction solvent is used to extract the petroleum ether extract for the second time , to obtain the second extract; preferably the second extraction solvent is selected from ethyl acetate or n-butanol; the second extract is subjected to silica gel column chromatography, and chloroform is used in the chromatographic process: Methanol is used for gradient washing of the second extract In the gradient elution process, the volume ratio of chloroform to methanol ranges from 100:0, 100:3 to 9 and 100:12 to 30; the e...

Embodiment 1

[0050] The preparation of embodiment 1 compound of the present invention

[0051]After crushing 15kg of the above-ground part of the spinach, extract twice with 70% ethanol under reflux, and recycle the ethanol to obtain about 1.8kg of extract. After dissolving the extract in 6000ml of water, extract three times with 6000ml of petroleum ether, 2000ml each time, recover the solvent under reduced pressure to obtain petroleum ether extract (FS, 100g); extract three times with 18000ml ethyl acetate, 6000ml each time, reduce The solvent was recovered under pressure to obtain an ethyl acetate extract (FY, 700 g), which was extracted three times with 18000 ml of n-butanol, 6000 ml each time, and the solvent was recovered under reduced pressure. Ethyl acetate extract (FY, 700g) was subjected to silica gel column chromatography with chloroform:methanol (100:0~100:100) for gradient elution, and was divided into FY-a (100:0, 5g), FY-b ( 100:3, 25g), FY-c(100:6, 50g), FY-d(100:9, 50g), F...

Embodiment 2

[0057] Example 2 Protective effect of viridescent acid B on H9c2 cardiomyocyte injury induced by hypoxia-reoxygenation

[0058] The experiment was divided into blank control group, hypoxia-reoxygenation model group and viridanic acid B pretreatment group. Among them, the blank control group was treated with serum-free culture medium during the experiment. The hypoxia-reoxygenation model group was cultured in serum-free medium for 2 hours, and then added with a final concentration of 200 μM hypoxia-reoxygenation for 2 hours. In the main active ingredient pretreatment group, the serum-free culture solution containing various active ingredients at the corresponding concentration was treated for 4 hours, the drug-containing culture solution was discarded, and a final concentration of 200 μM was added for hypoxia-reoxygenation for 2 hours.

[0059] Cells in the logarithmic growth phase were divided into 5×10 4 The density of cells / well was seeded in 96-well plate in 5v% CO 2 1. ...

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Abstract

The invention provides application of a 1,3,4,5-tetrahydro-2-benzo-cycloheptatriene compound to in vitro screening or drug preparation. The 1,3,4,5-tetrahydro-2-benzo-cycloheptatriene compound is a compound shown by the structural formula (I) or pharmaceutically-acceptable salt of the compound shown by the structural formula (I), wherein R1 (please see the formula in the description), R2 and R3 are independently selected from -OH, OCH3, H or C1-C3 alkyl groups, and R4 is C1-C3 alkyl groups, C1-C3 carboxyl groups, C1-C3 carbonyl groups, C1-C3 aldehyde groups or C1-C3 ester groups. The compound can reduce myocardial cell injuries caused by hpoxia and reoxygenation, has a remarkable effect on protecting myocardial cell injuries and is suitable for being applied to in vitro screening or preparing drugs for treating and / or preventing diseases relevant to myocardial cell injuries.

Description

technical field [0001] The invention relates to the field of traditional Chinese medicine, in particular to the application of a dibenzoxepin compound in in vitro screening or preparation of drugs for treating and / or preventing diseases related to myocardial cell damage. Background technique [0002] Cardiovascular disease has become the world's number one health killer due to its high incidence and high mortality rate. Tens of millions of people die from cardiovascular disease every year in the world, and cardiovascular disease seriously endangers human health. According to the latest research, new protective measures for patients with high cardiovascular risk can effectively prevent cardiovascular death and disability through drug intervention. As a major public health problem that needs to be solved more and more urgently, the research on cardiovascular disease has been highly valued for many years. [0003] Clinopodium chinense (Benth.) O. Kuntze is a plant of the genus...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/335A61P9/10C07D313/14
CPCA61K31/335C07D313/14
Inventor 许旭东朱寅荻余世春吴海峰马国需朱乃亮孙忠浩李朋飞
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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