Application of Pubescenoside C in preparation of drugs 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, achieve the effect of improving myocardial ischemia-reperfusion injury and myocardial tissue lesions, and reducing myocardial injury

Active Publication Date: 2021-06-04
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 C in preparation of drugs for preventing and treating myocardial ischemia-reperfusion injury
  • Application of Pubescenoside C in preparation of drugs for preventing and treating myocardial ischemia-reperfusion injury
  • Application of Pubescenoside C in preparation of drugs for preventing and treating myocardial ischemia-reperfusion injury

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] 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 ;

[0035] 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 with a concentration; the collection concentration is 60% % ethanol eluent was recovered under reduced pressure to obtain 566g of thick extract, 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 7:3, concentrate and pass through ODS column, use methanol:water 7:3 as eluent for elution, collect and concentrate the eluent and p...

Embodiment 2

[0037] The white amorphous powder obtained in Example 1 was positive for Liebermann-Burchard reaction, and finally showed a purple color, indicating that it was a triterpenoid. Mass Spectrum ESI-ME m / z:933[M+Na] + , combined with 13 C NMR and 1 H NMR deduces that its molecular formula is C 47 h 74 o 17 , degree of unsaturation Ω=11.

[0038] 1 H NMR spectrum (attached figure 1 ), the low field δ H 5.62(1H, br s) shows an ene hydrogen signal; δ H 6.32 (1H, d, J = 8.0Hz), 5.36 (1H, d, J = 7.6Hz) and 4.85 (1H, d, J = 7.6Hz) are the terminal hydrogen proton signals of 2 glucose and xylose, high Field δ H The seven A base signal, suggesting that the compound may be an ursane-type triterpene saponin.

[0039] 13 C NMR (with figure 2 ) and DEPT spectrum (attached image 3 ) shows that the compound has a total of 47 carbon signals. In the low field region δ C 175.3 is an ester carbonyl carbon signal, δ C 127.5, 139.1 and δ C 135.2 and 136.1 are 2 groups of olefi...

Embodiment 3

[0043] SD rat myocardial ischemia-reperfusion model was used to verify the effect of the compound on reducing myocardial ischemia-reperfusion injury by studying the effect of Pubescenoside C on myocardial infarction and myocardial injury markers in rats with myocardial ischemia-reperfusion injury.

[0044] 1. Animal dosing groups

[0045] Adult male Sprague-Dawley (SD) rats (WM: 250-280 g) were used for in vivo experiments. Four rats were housed in each cage, and a 12:12h light-dark cycle was performed at a temperature of 22±2°C in an SPF animal room, and the animals were allowed free access to standard rodent chow and distilled water.

[0046] Rats were divided into groups: Group 1: SHAM group, normal saline (i.p.); Group 2: MI / R group, normal saline (i.p.); Group 3: MI / R+Pubescenoside C (10mg / kg, i.p.) ; Group 4: MI / R+Pubescenoside C (30 mg / kg, i.p.). Male SD rats were subjected to left coronary artery ligation. Pubescenoside C was dissolved in absolute ethanol and diluted...

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Abstract

The invention provides application of a pubescent holly root triterpenoid saponin compound Pubescenoside C in preparation of drugs for preventing and treating myocardial ischemia-reperfusion injury. The triterpenoid saponin compound Pubescenoside C can mediate macrophage to be polarized from M1 type to M2 type by regulating and controlling interaction of HSP90 / GSK-3 beta, thereby having the effects of improving myocardial ischemia-reperfusion injury and myocardial tissue lesions and reducing myocardial injury. The pubescent holly root triterpenoid saponin compound Pubescenoside C can also be combined with other pharmaceutical excipients to prepare drugs of different dosage forms, and the prepared drugs 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 C, a triterpenoid saponin compound of Ilex pubescens, 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-rep...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/704A61K9/08A61K9/48A61K9/20A61K47/38A61K47/36A61K47/02A61K36/185A61P9/10A61K125/00
CPCA61K31/704A61K9/0019A61K9/08A61K47/02A61K9/4866A61K9/2059A61K36/185A61P9/10
Inventor 刘中秋程媛媛吴鹏周华廖国超张容容黄秋菊陈思璇
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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