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Application of epicatechin gallate and derivatives thereof for treating or preventing myocardial infarction and other ischemic heart diseases

A technology of epicatechin gallate and ischemic heart disease, applied in the field of natural medicine and medicine, can solve problems such as carcinogenicity and adverse reactions, and achieve the effect of improving cardiac contractility

Inactive Publication Date: 2011-03-16
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is very easy to produce tolerance with adenosine receptor agonists, and all PKC activity inducers have obvious carcinogenicity, K ATP Channel openers are prone to various adverse reactions, etc.

Method used

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  • Application of epicatechin gallate and derivatives thereof for treating or preventing myocardial infarction and other ischemic heart diseases
  • Application of epicatechin gallate and derivatives thereof for treating or preventing myocardial infarction and other ischemic heart diseases
  • Application of epicatechin gallate and derivatives thereof for treating or preventing myocardial infarction and other ischemic heart diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Protective Effect of ECG on Cardiac Ischemia / Reperfusion Injury

[0036] Objective: The inventor's previous studies have shown that ECG has the function of activating PKCε and increasing the contractility of isolated rat myocardial contractility. On the previous basis, the present invention uses the Langendorff in vitro rat heart perfusion system to study whether ECG still has the effect of activating PKCε in cardiac ischemia / reperfusion, and detects whether it has pre-adaptation in ischemia-reperfusion injury and post-adaptation protection.

[0037] Materials and methods:

[0038] 1) Reagents: TIP, a specific inhibitor of PKCε, was purchased from Calbiochem, and the mitochondrial ATP-sensitive potassium channel mKATP blocker 5-HD was purchased from Sigma.

[0039] 2) Experimental grouping: The group design of ECG ischemia / reperfusion preconditioning and postconditioning is as follows: figure 2 shown as the experimental treatment group and control group, ...

Embodiment 2

[0057]Example 2: Protective Effects of ECG Derivatives EGCG and TF4 on Cardiac Ischemia / Reperfusion Injury

[0058] Same as in Example 1, in the Langendorff isolated rat heart ischemia / reperfusion system in vitro, the ECG derivative EGCG or TF4 is used for preconditioning treatment, which can make the LVDP of the rat heart from 35.0±5.0% after ischemia Respectively increased to 87.0±6.2% (n=5, p<0.01) and 78.0±7.2% (n=6, p<0.01), the results indicated that EGCG and TF4 have protective effects on cardiac ischemia / reperfusion injury.

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Abstract

The invention relates to an application of natural compound epicatechin gallate obtained from tea and derivatives thereof for treating or preventing myocardial infarction and other ischemic heart diseases. The compound is used for preventing the myocardial injury of the heart caused by ischemia-reperfusion, and is a medicament for potentially treating or preventing the heart ischemia / reperfusion injury. Particularly, the compound has a novel effect on protecting the heart and has a function that the enhancement of the myocardial contractility does not depend on the increase of the concentration of calcium ions in myocardial cells. In the invention, it is discovered that the epicatechin gallate (ECG) and the derivatives thereof have pharmacological pre-adaptation functions and have pharmacological post-adaptation functions for the first time, thus the ECG and the derivatives thereof are possibly novel medicaments for treating or preventing myocardial infarction and other ischemic heart diseases. The ECG and the derivatives thereof not only can be used for clinically treating congestive heart diseases through pharmacological post-adaptation but also can be used for medically preventing the patient who suffers from myocardial infarction and then is cured from being subjected to myocardial infarction again through pharmacological pre-adaptation.

Description

technical field [0001] The invention belongs to the fields of natural medicine and medicine, and relates to the use of a class of natural compound epicatechin gallate derived from tea leaves and its derivatives in treating or preventing ischemic heart disease such as myocardial infarction. Background technique [0002] Ischemic heart disease (IHD) is myocardial damage caused by the imbalance between coronary blood flow and myocardial demand caused by changes in coronary circulation. It is the first enemy that threatens human life and health in the world today. IHD includes coronary heart disease, angina pectoris, myocardial infarction (myocardial infarction, MI), etc. Among them, coronary artery stenosis and occlusion caused by coronary atherosclerosis account for about 90% of IHD. Ischemic heart disease affects millions in the United States. In my country, with the improvement of people's living standards, ischemic heart disease has increasingly become the "first killer" t...

Claims

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Application Information

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IPC IPC(8): A61K31/353A61K31/7048A61P9/10A61P9/04
Inventor 谢子建宛晓春杨昌军李大祥
Owner ZHEJIANG HISUN PHARMA CO LTD
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