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Costunolide, dehydrogenized costunolide, and function of derivative thereof in preparing protective medicine for preventing and treating anoxic cardiac muscle

A technology for dehydroxylan and xylolide, which is applied in the field of medicine and can solve the problems of abnormal heart failure, atrioventricular conduction block, clinical application limitation and the like

Active Publication Date: 2020-02-04
樊鹏程
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are many contraindications in practical application, including airway blockage, atrioventricular block and abnormal heart failure, etc., and the clinical application is limited.

Method used

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  • Costunolide, dehydrogenized costunolide, and function of derivative thereof in preparing protective medicine for preventing and treating anoxic cardiac muscle
  • Costunolide, dehydrogenized costunolide, and function of derivative thereof in preparing protective medicine for preventing and treating anoxic cardiac muscle
  • Costunolide, dehydrogenized costunolide, and function of derivative thereof in preparing protective medicine for preventing and treating anoxic cardiac muscle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] (1) Preparation of ethanol extract

[0049] The electronic balance weighs 100g of muxiang decoction pieces, pulverizes it into powder by a pulverizer, and puts it in a 1000ml beaker. Add 70% ethanol with a mass ratio of 8 times to the woody powder, mix well, soak for 12 hours, ultrasonic machine for 45 minutes, stand and separate layers, the upper layer is orange-red solution, and the lower layer is precipitated as insoluble medicinal material powder. Separate the liquid, collect the supernatant, add the same volume of 70% ethanol as in the previous step to the remaining precipitate, mix well, continue to soak for 12 hours, ultrasonically sonicate for 45 minutes, let stand and separate into layers, the upper layer is orange-red solution, and the lower layer is precipitated as insoluble medicinal material powder. Split, collect supernatant and combine all supernatants. All the supernatant was concentrated to 80 ml by vacuum rotary evaporation at 45° C. to obtain solutio...

Embodiment 2

[0059] Example 2 Anti-hypoxic efficacy screening of effective active ingredients, anti-hypoxic efficacy of coynelide and dehydrocorylidene

[0060] According to the preparation method of Example 1, according to the experimental results, 2kg of medicinal materials obtained coynelide and dehydrocoyne lactone 33.0g, wherein, coynelide 17.6g, dehydrocoyne lactone 15.4g ; The extraction rate of coynelide and dehydrocoynelide is 1.65%.

[0061] The obtained parts were firstly dried by rotary evaporation, and then dried under reduced pressure to obtain dry brown powders of ethanol extract, petroleum ether part extract, ethyl acetate part and extracted liquid part (ie ethyl acetate layer) respectively. Balb / c mice (♂) were intragastrically administered into groups according to the doses in Table 2, and the airtight hypoxia experiment at normal pressure was carried out. The corynelide and dehydrocorylidene monomers prepared by separation and purification from the ethyl acetate part of...

Embodiment 3

[0068] Example 3 Effects of couscous lactone on blood pressure in acute hypoxic rats

[0069] Low-pressure hypoxic experimental warehouse (Guizhou Fenglei), BP-2010 intelligent non-invasive blood pressure monitor (Beijing Soft Dragon), XT-2000i animal whole blood cell analyzer (Japan Sysmex), BX-3010 animal automatic biochemical analyzer (Japan) Sysmex), blood gas analyzer (ABL90 FLEX analyzer).

[0070] A total of 40 SPF grade Wistar rats, half male and half male, weighing 210±20g. Divide into 4 groups at random according to male and female half and half, every group 10, according to the result of experiment before, the costunolide (Costunolide, CTL) group dosage of preparation of embodiment 1 is 250mg / kg, continuous intragastric administration 3 day; the positive control group was given acetazolamide (Acetazolamide, ACZ) 300mg / kg by intragastric administration for 3 consecutive days, and the administration volume was 20ml / kg; the normal control (Normal) group and the hypoxi...

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Abstract

The invention provides costunolide, dehydrogenized costunolide, and application of a derivative thereof in preparing a protective medicine for preventing and treating anoxic cardiac muscle. Anti-myocardial anoxia functions of the costunolide and the dehydrogenized costunolide are researched through an atmospheric pressure airtight anoxia experiment and acute decompression anoxia model, the resultshows that the costunolide and the derivative dehydrogenized costunolide have an anti-anoxia function, and an action mechanism can be realized through antioxidant stress injury. The costunolide can protect the activity of SOD and CAT in anoxia mice cardiac muscle tissues, enhance an anoxia body brain ROS and free radical scavenging capacity, and reduce MDA, H2O2 and OH levels in mice cardiac muscle caused by ROS after anoxia so as to achieve the effect on resisting myocardial anoxia.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to the method and application of coynelide, dehydrocoynelide and derivatives thereof in the preparation of cardioprotective drugs for the prevention and treatment of hypoxia. Background technique [0002] Heart disease is one of the diseases that seriously threaten human health. Myocardial ischemia is the cause of most cardiovascular diseases. Myocardial infarction, which is common clinically, is mostly caused by hypoxia, which will cause a series of pathological changes in the body. Common therapeutic drugs for myocardial ischemia include nitrate coronary vasodilators, β-blockers, and calcium ion antagonists, among which β-blockers are widely used. However, there are many contraindications in practical application, including airway blockage, atrioventricular block and abnormal heart failure, etc., and the clinical application is limited to a certain extent. Therefore, it is very ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365C07D307/93A61P9/10A61P39/06
CPCA61K31/365C07D307/93A61P9/10A61P39/06A61K36/285
Inventor 郝颖樊鹏程靳婉君赵彤苗路伟
Owner 樊鹏程
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