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Substance for protecting heart

A composition and myocardial ischemia technology, applied in the field of medicine, can solve problems such as inability to deduce ischemia-reperfusion myocardium

Inactive Publication Date: 2012-03-14
SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Administration of berbamine before the onset of myocardial ischemia can reduce the injury effect of ischemia-reperfusion myocardium (prevention), but it cannot be deduced from this whether berbamine administration at the beginning of reperfusion after myocardial ischemia can also reduce the damage of ischemia-reperfusion myocardium damage

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0068] The preparation method of berbamine can adopt methods known to those skilled in the art, such as chemical synthesis or extraction from plants. The berbamine is extracted from plants of Berberidaceae, Fangjiaceae or Ranunculaceae, Berberis genus, Mahonia, and genus Nectarina.

[0069] In the present invention, pharmaceutically acceptable salts of berbamine or derivatives of berbamine are also included. The present invention also includes pharmaceutically acceptable salts, hydrates or precursors of the above compounds, as long as they also have the effect of promoting myocardial contraction or treating heart failure. The "pharmaceutically acceptable salt" refers to a salt formed by reacting a class of compounds with inorganic acids, organic acids, alkali metals or alkaline earth metals. These salts include (but are not limited to): (1) salts formed with inorganic acids such as hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid; (2) salts formed with organic a...

Embodiment 1

[0107] Embodiment 1, the influence of berbamine on myocardial contractility

[0108] 1. Materials and methods

[0109] animal

[0110] Male Sprague-Dawlay (SD) rats, weighing 250-300 g, were purchased from Shanghai Slack Experimental Animal Center.

[0111] drug

[0112] Berbamine hydrochloride was purchased from Sigma Company, product number 547190, molecular weight 681.65; purity 99.99%, dissolved in double distilled water at 37°C.

[0113] PKCεV1-2, PKCε specific inhibitor, molecular weight 947.1, purchased from Anaspec, product number 62186, purity>98%, dissolved in double distilled water at 37°C.

[0114] ML-9, an inhibitor specific to MLCK, with a molecular weight of 361.3, was purchased from BIOMOL, product number E1-153, with a purity of 99%, dissolved in ethanol: double distilled water (1:1).

[0115] isolated heart perfusion

[0116] Perfusate

[0117] Modified Krebs-Henseleit (K-H) solution (mM): NaCl 118; KCl 4.7; NaHCO 3 2.5; MgSO 4 1.2; CaCl 2 2.55; K...

Embodiment 2

[0172] Example 2. Protection of ischemic / reperfused myocardium by berbamine after ischemia and its mechanism

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PUM

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Abstract

The invention relates to a substance for protecting cardiac muscle, and provides novel application of berbamine in heart diseases. Berbamine has positive inotropic action to an animal heart, and can be applied to enhance the normal myocardial contractility. Furthermore, when the berbamine is administrated at the early stage of myocardial ischemia / reperfusion, the myocardial ischemia / reperfusion injury can be lightened, and myocardial contraction after ischemia can be improved, so that the berbamine can be used for preparing a medicament for treating cardiac insufficiency (heart failure diseases).

Description

technical field [0001] The present invention belongs to the field of medicine; more specifically, the present invention relates to a heart-protecting substance. Background technique [0002] Berbamine (BM) is a bisbenzylisoquinoline alkaloid proposed from Berberidaceae plants, and its pharmacological effects have been studied to some extent. However, there are no literature reports on its effect on enhancing myocardial contractility. Berbamine has been used clinically as a drug for increasing blood leukocytes, and its long-term application is safe and effective. [0003] Heart failure (heart failure) refers to the severe weakening of myocardial contractile function, the reduction of cardiac output blood, which is not enough to meet the body's needs, thus causing a series of symptoms and signs. Acute cardiac insufficiency is seen in decompensation of chronic heart failure, systolic insufficiency after myocardial infarction, and myocardial stunning after cardiac surgery. Ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4748A61P9/04A61P9/10
Inventor 杨黄恬张彩梅高崚
Owner SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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