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Application of coptisine in preventing and curing myocardial ischemic diseases

A technique for myocardial ischemia and coptisine, which is used in cardiovascular system diseases, applications, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2011-04-06
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have found that berberine has the same effect, but GI 50 The value is 95.1μM (35.4μg / ml), while palmatine has no similar effect (in vitro experiment)

Method used

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  • Application of coptisine in preventing and curing myocardial ischemic diseases
  • Application of coptisine in preventing and curing myocardial ischemic diseases
  • Application of coptisine in preventing and curing myocardial ischemic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0096] Embodiment 1: the preparation method of Chinese medicine monomer coptisine.

[0097] Take 3.95 kg of Coptis chinensis, extract 7 times with 95% ethanol in a water bath, combine the ethanol extracts, recover the solvent to about 2000 ml, add 350 ml of water, extract 2 times with petroleum ether, recover the lower solvent to form a paste, add water to dissolve, and use ethyl acetate Extract 3 times, add appropriate amount of NaCl to the aqueous solution, a yellow precipitate precipitates out, filter the precipitate, add about 4500ml of methanol to dissolve it, filter with suction, recrystallize, filter out the solid, and evaporate the mother liquor to dryness to obtain the solid 240. The solid was dissolved in methanol, mixed with an appropriate amount of silica gel (the silica gel was mixed in several times, the amount was relatively large, without weighing), and separated by column chromatography through 200-300 mesh silica gel. Perform gradient elution. The combined e...

experiment example 1

[0101] Experimental Example 1: Establishment of a rat model of myocardial ischemia injury.

[0102] Isoproterenol (Iso) can enhance myocardial contractility, accelerate heart rate, increase myocardial oxygen consumption, continuous use can cause experimental myocardial injury. In this example, the animal model of rat myocardial ischemia injury caused by intraperitoneal injection of Iso, the electrocardiogram of the rat was observed, the serum enzymes of the experimental rat, the range of myocardial ischemia, the damage degree of the myocardial mitochondria, and the histomorphological observation were determined to determine the degree of damage of coptisine. The protective effect on myocardial ischemia in rats and the pharmacological effect and application of prevention and treatment of myocardial ischemic diseases.

[0103] 105 male SD rats with a body weight of 200-220 g were selected as experimental animals, and were randomly divided into 7 groups, 15 in each group, normal ...

experiment example 2

[0104] Experimental Example 2: Improvement effect of coptisine on electrocardiogram in rats with myocardial ischemia injury.

[0105] The rats in each of the above groups were fasted overnight after the last administration, anesthetized with pentobarbital sodium 50 mg / kg the next day, needle electrodes were inserted subcutaneously in the front and rear limbs, and the electrocardiogram of lead II of the rats was recorded, and the ST segment of the electrocardiogram was observed. Changes. The results show (attached figure 1 ), the electrocardiogram of normal rats was in a normal state, and isoproterenol caused the shift of the ST segment in the electrocardiogram of the rats, the elevation of the T wave, and myocardial ischemic changes. Two positive drugs, fasudil and isosorbide dinitrate, can significantly improve the ECG changes induced by isoproterenol in rats. Coptisine can improve the ECG changes induced by isoproterenol in rats, and significantly reduce the range of myocar...

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PUM

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Abstract

The invention discloses an application of coptisine or physiologically acceptable salt thereof in preparing medicines for preventing and curing myocardial ischemic diseases. The coptisine or the physiologically acceptable salt thereof has pharmacological actions of protecting myocardial ischemic injury as well as preventing and curing myocardial ischemic diseases, has an effect of protecting myocardial mitochondria function, and has pharmacological actions of eliminating superoxide anion radical and protecting cardiocytes from being injured by free radicals. The invention discloses a compound containing the coptisine or physiologically acceptable salt and a pharmaceutically acceptable carrier and / or accessory. The coptisine is a monomeric compound extracted from rhizoma coptidis and other commonly used traditional Chinese medicines or folk herbs, which has the advantages of low toxicity and wide raw material resources.

Description

technical field [0001] The invention relates to natural medicine chemistry and new pharmacological action of coptisine, in particular to the application of coptisine or its physiologically acceptable salt in preventing and treating myocardial ischemic diseases. technical background [0002] As we all know, cardiovascular and cerebrovascular diseases are the diseases with the highest mortality rate in the world. Ischemic cardiomyopathy is a special type or advanced stage of coronary heart disease, which refers to long-term myocardial ischemia caused by coronary atherosclerosis, resulting in diffuse myocardial fibrosis, causing cardiac enlargement or stiffness, congestive heart failure, cardiac rhythm A syndrome with a series of clinical manifestations such as abnormalities. With the increasing incidence of coronary heart disease, the harm caused by ischemic cardiomyopathy to human health is becoming more and more serious. [0003] Myocardial ischemia can cause myocardial dy...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61P9/00A61P9/10A23L1/29A23L33/00
Inventor 秦海林方莲花宫丽丽邓安珺李志宏王夙博孙加琳杜冠华
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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