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Application of bilobalide in preparing medicine for treating ischemic cardiomyopathy

A technology of ischemic cardiomyopathy and bilobalide, which is applied in drug combination, cardiovascular system diseases, pharmaceutical formulations, etc., can solve the problems that have not been seen or reported on the regulatory effect of bilobalide

Inactive Publication Date: 2012-09-19
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Bilobalide belongs to the sesquiterpene lactones in ginkgolides. It has been reported that ginkgolides are strong platelet activating factor antagonists and have a positive effect on ischemic cardiomyopathy. It has a therapeutic effect, but the reports are all reports on the mixture of ginkgolides (comprising ginkgolides A, B, C, J, M, etc. and bilobalide). Ischemic cardiomyopathy has been reported, and there is no report on the regulation of platelet activating factor by bilobalide

Method used

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  • Application of bilobalide in preparing medicine for treating ischemic cardiomyopathy
  • Application of bilobalide in preparing medicine for treating ischemic cardiomyopathy
  • Application of bilobalide in preparing medicine for treating ischemic cardiomyopathy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Bilobalide Improves Cell Survival Rate Test

[0023] Primary culture of SD suckling mice aged 1-3 days, under aseptic conditions, take the heart, wash it in PBS, cut it into pieces, transfer it to a Erlenmeyer flask containing 0.125% trypsin and digest it at 37°C for 10 minutes, and digest it 8 times under continuous magnetic stirring ;Collect the supernatant after each digestion, stop the digestion with serum, centrifuge at 2000rpm for 5 minutes, collect the cell pellet and adjust the cell density to 10 5 / ml, cultured in DMEM containing 10% calf serum, and used for the experiment on the third day; divided into normal control group (no drug intervention, normoxia and high glucose), model group (no drug intervention, lack of Oxygen and sugar deficiency for 6 h), bilobalide group (respectively pre-administered drugs 500ng / ml, 50ng / ml, 5ng / ml, 0.5ng / ml for 12h, followed by hypoxia and sugar deficiency for 6h) ginkgolide A 500ng / ml. The cell viability was detect...

Embodiment 2

[0024] Example 2 Observation of bilobalide on morphological changes of hypoxic cells

[0025] Implementation method is the same as embodiment 1. Fluorescein dye Hoechst 33258 was used to measure cardiomyocyte apoptosis: cells in each treatment group were fixed with 4% paraformaldehyde at room temperature for 20-30 min, and washed 3 times with PBS. Add fluorescein dye Hoechst 33258 (20 μg / ml), incubate at 37°C for 20 min, wash with PBS three times, 10 min each time. Mount the slides with 10% buffered glycerol, observe under a fluorescent microscope, and take pictures.

[0026] The result is as figure 2 As shown, bilobalide 50ng / ml and 5ng / ml groups can significantly reduce the apoptosis of cardiomyocytes.

Embodiment 3

[0028] Effects of various concentrations of bilobalide on gene expression of PAF-AH and PAFR in cardiomyocytes injured by hypoxia and glucose deficiency for 6 h

[0029] The specific implementation method is the same as in Example 1. The results showed that bilobalide could dose-dependently regulate the expression of PAFR and PAF-AH genes within a certain range.

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Abstract

The invention belongs to the pharmaceutical field, and relates to a novel medical application of bilobalide, particularly relates to an application of the bilobalide in preparing a medicine for treating ischemic cardiomyopathy, and in particular to an application of a medicine for treating ischemic myocardium injury. According to the invention, the results of the in vitro culture experiment for cardiac muscle cells and the in vivo animal experiment indicate that the bilobalide can increase the cell survival rate, regulate the platelet activating factor receptor and the platelet activating factor acetylhydrolase and reduce the myocardial apoptosis, and is embodied as the expression of regulating PAFR (platelet activating factor receptor) and PAF-AH (platelet activating factor-acetylhydrolase) genes in a dose-dependent form, specifically as the expression of up-regulating the PAFR and down-regulating the PAF-AH. The bilobalide can be applied to treating the myocardium injury in particular the hypoxic and ischemic cardiomyopathy of myocardium injury by being taken as a therapeutic medicine.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to the new medicinal application of bilobalide, in particular to the application of bilobalide in the treatment of target organ protection drugs, especially in the preparation of drugs for the treatment of ischemic myocardial injury. Background technique [0002] Ischemic cardiomyopathy is a sudden and temporary myocardial ischemia and hypoxia syndrome caused by insufficient coronary blood supply. Its typical clinical manifestation is paroxysmal substernal compression pain radiating to the left upper limb. The pathophysiological basis is the imbalance between supply and demand of myocardial tissue oxygen. At present, the drugs used clinically to treat ischemic cardiomyopathy mainly include nitrates, β-adrenoceptor blockers and calcium channel blockers, etc. Practice shows that the above three types of drugs are all effective for ischemic cardiomyopathy. Has a certain therapeutic effect. [0...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P9/10
Inventor 朱依谆玛丽·斯蒂芬妮郭薇刘春华
Owner FUDAN UNIV
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