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Two bromophenol compounds and application of pharmaceutically-acceptable salts of two bromophenol compounds in preparation of protection drug

A technology for reperfusion injury and myocardial ischemia, applied in the direction of drug combination, cardiovascular system diseases, ketone active ingredients, etc., can solve the problem of no relevant reports on the pharmacological effects of myocardial ischemia-reperfusion injury, and achieve the protection of myocardial ischemia Effects of reperfusion injury, increasing protein expression, and inhibiting apoptosis

Active Publication Date: 2012-04-25
SHANXI MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

[0006] But so far, the compound 2,3-dibromo-4,5-dihydroxybenzophenone and its pharmaceutically acceptable salts and the compound 2,3'-dibromo-4,5,6'-trihydroxydi There is no relevant report on the pharmacological effects of benzophenone and its pharmaceutically acceptable salts on myocardial ischemia-reperfusion injury protection at home and abroad

Method used

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  • Two bromophenol compounds and application of pharmaceutically-acceptable salts of two bromophenol compounds in preparation of protection drug
  • Two bromophenol compounds and application of pharmaceutically-acceptable salts of two bromophenol compounds in preparation of protection drug
  • Two bromophenol compounds and application of pharmaceutically-acceptable salts of two bromophenol compounds in preparation of protection drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] 1. Effects of M48 and M49 on different physiological parameters of rats

[0016] 1.1 Experimental animals: 60 SD rats, half male and half male, were randomly divided into 10 groups, one of which was the sham operation group, and the other nine groups established SD rat myocardial ischemia-reperfusion injury models.

[0017] 1.2 Experimental grouping: one group of experimental drugs is the sham operation group, that is, the ligation is only passed through without ligation; the second group is the model group; the third group is the solvent control group; the fourth group is the M48 low-dose group 5mg / Kg; M48 medium dose group is 10mg / Kg; six groups are M48 high dose group 15mg / Kg; seven groups are M49 low dose group 5mg / Kg; eighth groups are M49 medium dose group 10mg / Kg; nine groups are M49 high dose group 15mg / Kg; Ten groups used the positive control drug sodium fructose diphosphate 10ml / Kg.

[0018] 1.3 Experimental method: Anesthetized by intraperitoneal injection ...

Embodiment 2

[0032] 1. Effects of M48 and M49 on myocardial infarction size in rats with myocardial ischemia-reperfusion

[0033] 1.1 Specific experiments:

[0034] The experimental animals and experimental groupings are the same as in 1 in Example 1, and the experimental method is basically the same as in 1 in Example 1, the difference is that in this experiment, 1% EvansBlue is intravenously injected after reperfusion of the corresponding group of experimental drugs , to stain the myocardium. Then counterstain with 1% TTC to analyze the infarct size, the calculation formula is as follows:

[0035] Infarct size = (infarct area / total myocardial area) × 100%

[0036] 1.2 Experimental results (Table 3):

[0037] Table 3: Effects of M48 and M49 on myocardial infarct size of rat myocardial ischemia-reperfusion

[0038]

[0039] As can be seen from the experimental results in Table 3: the four to ten groups of medication have significantly improved myocardial infarction area than the m...

Embodiment 3

[0047] 1. Effects of M48 and M49 on NO in myocardial tissue during myocardial ischemia-reperfusion in rats

[0048] 1.1 Specific experiments:

[0049] The experimental animals and the experimental groupings are all the same as the method of 1 in Example 1, and the experimental method is basically the same as the method of 1 in Example 1, except that the corresponding group of experimental drugs is reperfused to detect the myocardial tissue after 3 hours. Nitric Oxide (NO) indicator.

[0050] 1.2 Experimental results (Table 5):

[0051] Table 5: Effects of M48 and M49 on NO in myocardial tissue during myocardial ischemia-reperfusion in rats

[0052]

[0053] From the experimental results in Table 5, it can be seen that the area of ​​myocardial infarction in groups 4 to 10 was significantly lower than that of the model control group (group 2), especially in the high-dose group, the level of NO was significantly reduced, indicating that M48 and M49 can inhibit myocardial inf...

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Abstract

The invention discloses two bromophenol compounds and a pharmaceutical application of their pharmaceutically-acceptable salts, specifically an application in the preparation of a myocardial ischemia-reperfusion injury protection drug. The two compounds and their pharmaceutically-acceptable salts can protect cardiomyocytes during rat heart acute ischemia so as to make rat heart functions complete.After routine intravenous administration, SOD activity after myocardial ischemia-reperfusion is raised, myocardial compliance is improved, serum LDH, serum CK, serum cTnT and MDA level after myocardial ischemia-reperfusion is remarkably reduced, myocardial injury is minimized, and FasmRNA after myocardial ischemia-reperfusion can be remarkably inhibited and reduced so as to inhibit cardiomyocyte apoptosis after myocardial ischemia-reperfusion. Therefore, the two bromophenol compounds and their pharmaceutically-acceptable salts have a clear myocardial ischemia-reperfusion injury protection function, thus providing a new method and means for the clinical treatment of myocardial ischemia-reperfusion injury and opening up a new direction for clinical medication.

Description

technical field [0001] The invention belongs to the field of application of brand-new compounds, specifically the compound 2,3-dibromo-4,5-dihydroxybenzophenone and its pharmaceutically acceptable salt and the compound 2,3'-dibromo-4,5,6' -Application of trihydroxybenzophenone and its pharmaceutically acceptable salts in the preparation of drugs for protecting myocardial ischemia-reperfusion injury. Background technique [0002] Myocardial ischemia-reperfusion injury (MIRI) refers to the recovery of blood supply within a certain period of time after myocardial ischemia, which will lead to more serious damage to the ischemic myocardium during the process of blood perfusion. At present, it is believed that the physiological changes of myocardial ischemia-reperfusion injury mainly include the massive production of oxygen free radicals (OFR), calcium overload, and activation of endothelial cells. Changes in the complement system and renin-angiotensin system, etc. The cellular b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/12A61P9/10
Inventor 李青山王义冯秀娥韩玲革
Owner SHANXI MEDICAL UNIV
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