Application of 5-bromo-2-(alpha-hydroxy amyl) sodium benzoate in medicine for curing cardiovascular disease

A technology of sodium benzoate and hydroxypentyl group is applied in the field of medicinal chemistry to achieve the effects of reducing the size of acute myocardial infarction, reducing myocardial damage and delaying myocardial hypertrophy

Inactive Publication Date: 2018-07-17
ZHENGZHOU UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The inventor found through detailed experiments in later research that BZP has obvious protective effects on acute and chronic myocardial ischemia-reperfusion injury, and there is no relevant literature report at present

Method used

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  • Application of 5-bromo-2-(alpha-hydroxy amyl) sodium benzoate in medicine for curing cardiovascular disease
  • Application of 5-bromo-2-(alpha-hydroxy amyl) sodium benzoate in medicine for curing cardiovascular disease
  • Application of 5-bromo-2-(alpha-hydroxy amyl) sodium benzoate in medicine for curing cardiovascular disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1: Protective effect of BZP on isolated heart ischemia-reperfusion injury in ICR mice

[0051] Experimental materials and methods

[0052] (1) Experimental materials

[0053] Select ICR mice, weighing 18-22 g, half male and half male, BZP (synthesized by our laboratory) was prepared with double distilled water; TTC was purchased from Sigma Company.

[0054] (2) Langendorff isolated heart perfusion: the isolated heart was perfused with the Powerlab Langendorff cardiac perfusion device of AD Instrument Company, and the animal was anesthetized by intraperitoneal injection of 10% chloral hydrate (300mg / Kg) by mass percentage, and 1000U / kg heparin was injected intraperitoneally at the same time Inject anticoagulation. Open the chest, quickly take out the heart along the root of the aorta, and immediately put it into K-H perfusate (composition mM: NaCl: 118, KCl 4.7, MgSO 4 1.2, KH 2 PO 4 1.2, EDTA.2Na 0.5, NaHCO 3 25, CaCl 2 2.5, Glucose 11, pH 7.4), wash t...

Embodiment 2

[0066] Example 2: Protective effect of BZP on whole animal heart ischemia-reperfusion injury in ICR mice

[0067] Experimental materials and methods

[0068] (1) Experimental materials

[0069] ICR mice were selected, weighing 18-22 g, half male and half male, and BZP (synthesized by our laboratory) was prepared with double distilled water; TTC was purchased from Sigma Company.

[0070] (2) Whole animal mouse myocardial ischemia and reperfusion model preparation: Animals were anesthetized with 2-3% isoflurane by mass percentage using the Viking Medical inhalation anesthesia system in the United States, and cut about 1.2 through the left 4-5 intercostal space. A cm incision was made to bluntly separate the pectoralis major and pectoralis minor muscles, and then the pleura and epicardium were cut open with Mosquito forceps to expose the heart, and then the heart was gently squeezed out to find the left anterior descending coronary artery located below the left atrial appendage ...

Embodiment 4

[0089] Example 4: The protective effect of BZP on delaying myocardial hypertrophy and heart failure after whole animal heart ischemia-reperfusion injury in ICR mice

[0090] experimental method:

[0091] (1) Experimental materials

[0092] ICR mice, half male and half male, BZP powder was prepared with double distilled water.

[0093] (2) Experimental grouping

[0094] A total of 4 groups, 12 in each group, half male and half male, 48 in total. They were sham operation group (sham); myocardial infarction model group (MI); BZP high (40 mg / kg), low dose group (20 mg / kg). Positive drug selection metoprolol succinate 10mg / kg.

[0095] (3) Long-term administration method

[0096] Treatment group: BZP was intragastrically administered after the MI model was established, the doses were 20mg / kg and 40mg / kg respectively. The dosing volume was 0.01 ml / g.

[0097] Positive drug group: after establishment of MI model, the rats were given metoprolol succinate by intragastric adminis...

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Abstract

The invention discloses application of compound 5-bromo-2-(alpha-hydroxy amyl) sodium benzoate (BZP) in medicine for curing cardiovascular disease, and belongs to the field of medicinal chemistry. Experiments prove that BZP has a protective effect for acute and chronic myocardial ischemia reperfusion injuries of a mouse, so that the overall animal acute myocardial infarction area is reduced through BZP oral administration and intravenous injection, the myocardial infarction area of the acute ischemia reperfusion injury of the isolated perfusion heart of the mouse is reduced through BZP, the function of myocardial contraction is improved, and the haematological myocardial injury markers are reduced; moreover, the invention also relates to application for delaying a process of the conversionfrom myocardial hypertrophy to cardiac failure after chronic orally taken administration of BZP for acute myocardial infarction of the mouse and reducing ventricular remodeling caused by ischemic heart disease of the mouse, the therapeutic action of the cardiac function is improved obviously; moreover, the invention also relates to the transient effect of the compound BZP for reducing the blood pressure of the hypertension mouse (SHR mouse), and these results indicate that the BZP has effective research and development prospects of myocardial damage protection medicine for clinically acute and chronic myocardial infarctions.

Description

technical field [0001] The present invention relates to the application of 5-bromo-2-(α-hydroxypentyl)sodium benzoate (abbreviated as BZP) in the preparation of medicines for treating cardiovascular diseases, in particular to the application of BZP in the prevention and treatment of ischemia-reperfusion injury after acute and chronic myocardial infarction The application in diseases belongs to the field of medicinal chemistry. Background technique [0002] Cardiovascular diseases, especially coronary atherosclerosis and the resulting ischemic heart disease are still common diseases that seriously plague human health. According to incomplete statistics, the number of deaths from cardiovascular diseases in the world accounts for 30% of the total number of deaths every year. %, of which ischemic heart disease accounts for more than 40% (about 7 million people), about 1.5 million people die of ischemic heart disease in China every year, and with the improvement of people's livin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61P9/00A61P9/10A61P9/04A61P9/08
CPCA61K31/192A61P9/00A61P9/04A61P9/08A61P9/10C07C51/09C07C65/03
Inventor 常俊标赵文宋传君
Owner ZHENGZHOU UNIV
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