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Application of sterides in preparing medicament for treating cardiovascular and cerebrovascular diseases

A technology for cardiovascular and cerebrovascular diseases and steroidal compounds, which is applied in the application field of steroidal compounds in the preparation of drugs for treating cardiovascular and cerebrovascular diseases. , resource-rich effect

Inactive Publication Date: 2008-05-07
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But fewer steroids for cardiovascular disease
However, there is no report about its development and utilization as a drug for the treatment of cardiovascular and cerebrovascular diseases.

Method used

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  • Application of sterides in preparing medicament for treating cardiovascular and cerebrovascular diseases
  • Application of sterides in preparing medicament for treating cardiovascular and cerebrovascular diseases
  • Application of sterides in preparing medicament for treating cardiovascular and cerebrovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Embodiment 1 steroid compound and its preparation

[0017] Asterias amurensis (Asterias amurensis) 4 kg, methanol reflux extraction 3 times (24L×3), methanol recovery under reduced pressure. The methanol extract was dispersed in 4 L of water, extracted three times with an equal volume of n-butanol, combined, and concentrated under reduced pressure to obtain 350 g of n-butanol extract. Get the above-mentioned n-butanol extract, through silica gel column chromatography (Φ30×80cm), chloroform methanol mixed solution (chloroform and methanol according to volume ratio 100:0, 50:1, 20:1, 10:1, 8:2, 7:3, 6:4 ratio) gradient elution, every 1000 milliliters was collected as a fraction, and then combined according to the results of thin layer chromatography to obtain 15 fractions (fraction A to O); fraction H (chloroform-methanol 8: 2 elution fractions) 20 grams of ODS medium and low pressure column chromatography, methanol-water (volume ratio 30%, 50%, 70%, 90%) gradient elutio...

Embodiment 2

[0023] Embodiment 2 promotes the detection of vasodilation activity

[0024] Accurately weigh the steroid compound obtained in Example 1, add DMSO, shake and dissolve to form 1mol L -1 solution. Take the rat thoracic aorta, cut it into a 3mm wide arterial ring, then hang the arterial ring in a bath filled with normal saline, with a volume of 20ml, and continuously pass it with 95% O 2 +5%CO 2 of mixed gas. One end of the arterial ring was fixed, and the other end was connected to the tension sensor of the BL-420 biological signal recording system with a thin wire, and a preload of 1 gram was given. Add norepinephrine after one hour of stabilization. After elution, stabilize for 20 minutes, add norepinephrine, add 10 μM steroid compound (coded as YLH-3) obtained in Example 1 at the peak of norepinephrine contraction, and record the tension curve. The tension curve against the effect of norepinephrine-induced vasoconstriction is shown in FIG. 1 .

[0025] It can be seen fr...

Embodiment 3

[0026] Example 3 Protective Effects on Calcium Overload in Cardiomyocytes Induced by KCl

[0027] Accurately weigh the steroid compound obtained in Example 1, add DMSO, shake and dissolve to form 1mol L -1 solution. Single rat ventricular myocytes were separated by enzymatic hydrolysis, and the cardiomyocytes were placed in 20 μmol·L -1 In the loading solution of Fluo-3 / AM, after Fluo-3 / AM passively diffuses into the cells, it is hydrolyzed by esterase to release Fluo-3, Fluo-3 and Ca 2+ Complexation, excited by 488nm laser to generate fluorescence, its fluorescence value is the same as [Ca 2+ ] i It is positively correlated, that is, it is expressed by the change of fluorescence value [Ca 2+ ] i Changes, the XY plane of the cell was scanned under the timeseries program of the laser scanning confocal microscope with an interval of 10s, and a total of 25 scans were performed. Calculate the average fluorescence intensity in the XY plane of the cell, and use the average flu...

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Abstract

The present invention provides an application of a steroid compound in the preparation of a drug for treating cardiovascular and cerebrovascular diseases, wherein the structure of the steroid compound is as follows: the drug prepared by the application of the present invention has the effect of promoting vasodilation and inhibiting cardiomyocytes induced by KCl The protective effect of internal calcium overload can treat cardiovascular and cerebrovascular diseases.

Description

technical field [0001] The invention relates to a steroid compound, in particular to the application of a steroid compound in the preparation of medicines for treating cardiovascular and cerebrovascular diseases. Background technique [0002] Cardiovascular and cerebrovascular diseases are the number one killer threatening human health, and the incidence of them is gradually getting younger, and the morbidity and mortality are also rising. The main cause of cardiovascular and cerebrovascular diseases is the changes in the structure and function of cardiovascular and cerebrovascular, central or peripheral blood vessels, such as abnormal increase of vascular tension. Currently on the market as drugs for the treatment of cardiovascular and cerebrovascular diseases, there are certain deficiencies, such as easy to produce drug resistance, as a drug for the treatment of arrhythmia itself leads to the generation of arrhythmia, and even some drugs have strong toxic and side effects,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61K9/08A61K9/10A61K9/16A61K9/48A61P9/00
Inventor 姚新生刘宏伟杨宝峰吕延杰戴毅
Owner JINAN UNIVERSITY
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