Application of Pubescenoside A in preparation of medicine for preventing and treating myocardial ischemia reperfusion injury

A technology for reperfusion injury and myocardial ischemia, applied in the field of biomedicine, can solve problems such as unsatisfactory results, and achieve the effects of reducing myocardial infarct size and CK-MB level, inhibiting damage, and preserving structure

Inactive Publication Date: 2021-06-01
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For myocardial ischemia-reperfusion injury, drugs such as calcium ion antagonists, receptor antagonists and oxygen free radical scavengers are commonly used in experiments to prevent and control arrhythmia, cardiac stunning and cardiac arrest induced by myocardial ischemia-reperfusion injury. Sudden death and other cardiovascular diseases occur, but the clinical effect is not satisfactory

Method used

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  • Application of Pubescenoside A in preparation of medicine for preventing and treating myocardial ischemia reperfusion injury
  • Application of Pubescenoside A in preparation of medicine for preventing and treating myocardial ischemia reperfusion injury
  • Application of Pubescenoside A in preparation of medicine for preventing and treating myocardial ischemia reperfusion injury

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] 1. Take the roots of Ilex pubescens, extract with 12, 10 and 8 times the concentration of 70% ethanol in turn for 2 hours, combine the ethanol extracts, recycle the ethanol after filtration and concentrate under reduced pressure until there is no alcohol smell, to obtain 2.2 kg of total extract ;

[0032] 2. The obtained total extract is dissolved in water, passed through a D-101 type macroporous resin column, and successively eluted with 30% ethanol, 60% ethanol and 95% ethanol; the collection concentration is 30% % ethanol eluent was recovered under reduced pressure to obtain a thick extract 341g, which was passed through a 200-300 mesh silica gel column, using chloroform-methanol as a solvent, with a gradient of 100:1-0:1 in chloroform:methanol Carry out elution; collect the eluent with chloroform:methanol ratio of 4:1, concentrate and pass through ODS column, use methanol:water 3:2 as eluent for elution, collect and concentrate the eluent and pass through Sephadex L...

Embodiment 2

[0034] Identification of the hollylic phenylpropanoid Pubescenoside A (PBA) prepared by the preparation method of Example 1.

[0035] Light yellow oil, mass spectrum HR-ESI-ME m / z:443.1548[M+H] + . combine 1 H NMR (with figure 1 )with 13 CNMR (attached figure 2 ) deduces that its molecular formula is C 20 h 26 o 11 , degree of unsaturation Ω=8. IR spectrum shows hydroxyl absorption (3338cm -1 ), carbonyl absorption (1688cm -1 ) and benzene ring absorption (1599, 1520, 1446cm -1 ). 1 δ in H NM spectrum H 7.60(1H,d,J=15.8Hz) and δ H 6.33 (1H, d, J = 15.9Hz) is a group of trans-alkene hydrogen proton signals. δ H 7.08(1H,d,J=1.8Hz), δ H 6.96(1H,dd,J=1.8,8.2Hz), δ H6.83 (1H, d, J=8.2Hz) is the ABX system on the benzene ring, which are the hydrogen proton signals of H-2, H-5, and H-6, respectively. δ H 5.37(1H,s) and δ H 5.37(1H,s) is the signal of two protons on another double bond. δ H 4.37 (1H, d, J=7.7Hz) is the terminal hydrogen proton signal of glu...

Embodiment 3

[0040] On the OGD / R model of rat cardiomyocyte H9c2 and the LAD-induced mouse myocardial ischemia-reperfusion model, it is verified that the compound can protect cardiomyocytes and have a protective effect on the heart.

[0041] 1. Determination of cell viability

[0042] Cell viability was determined by MTT assay. RAW264.7 and H9c2 cells (with or without OGD / R treatment) were treated with different doses of PBA for 48 hours. At the end of the experiment, MTT at a concentration of 0.5 mg / mL was added to each well and incubated at 37°C for 3 hours. After 3 hours, the supernatant was discarded, and 150 μL of DMSO was added to each well to dissolve the formazan in the cells, and then the absorbance of the solution at 570 nm was measured by a spectrophotometer (Thermo Fisher Scientific, Massachusetts, USA).

[0043] The results are attached Figure 4 As shown in B, in RAW264.7 and H9c2 cells, PBA did not have any cytotoxicity below 240 μM concentration. Therefore, in the next ...

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Abstract

The invention provides an application of a pubescent holly root phenylpropanoid compound Pubescenoside A in preparation of a medicine for preventing and treating myocardial ischemia reperfusion injury. The phenylpropanoid compound Pubescenoside A can inhibit H9c2 cell injury induced by OGD / R, the myocardial infarction area and the CK-MB level can be remarkably reduced on the animal level, the structure of myofibril is reserved, recruitment and myolysis of inflammatory cells are reduced, the phenylpropanoid compound Pubescenoside A can be combined with other medicine auxiliary materials to be prepared into medicines of different dosage forms, and the prepared medicine can be used for preventing and treating myocardial ischemia reperfusion injury.

Description

technical field [0001] The invention belongs to the field of biomedicine. More specifically, it relates to the application of Pubescenoside A, a phenylpropanoid compound in Radix Ilex, in the preparation of drugs for preventing and treating myocardial ischemia-reperfusion injury. Background technique [0002] Myocardial ischemia-reperfusion injury (MIRI) refers to the pathological process in which blood supply is restored within a certain period of time after myocardial ischemia, and more serious damage occurs to the ischemic myocardium during blood perfusion. Ischemia-reperfusion injury can account for all infarctions. 50% of the area of ​​the myocardium. At present, it is believed that myocardial ischemia-reperfusion injury is mainly caused by massive production of oxygen free radicals (OFR), intracellular calcium overload, activation of endothelial cells, inflammatory response, etc., and its cellular basis is cardiomyocyte apoptosis. For myocardial ischemia-reperfusion ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7032A61K36/185A61P9/10A61K125/00
CPCA61K31/7032A61K36/185A61P9/10
Inventor 刘中秋程媛媛吴鹏周华廖国超吴锦俊冯潜
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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