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Application of Calycosin Derivatives in Preparation of Drugs for Treating Cerebral Ischemia-Reperfusion Injury

A technology of cerebral ischemia reperfusion and drugs, applied in the field of medicine, can solve problems such as inconsistency, high drug concentration, and retention

Active Publication Date: 2019-11-15
GUILIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the research on the protective effect of calycosin on cerebral ischemia-reperfusion injury is still in the preliminary pharmacodynamic stage, the concentration of the drug used is relatively high, and there is no clear target, and the results are often inconsistent.

Method used

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  • Application of Calycosin Derivatives in Preparation of Drugs for Treating Cerebral Ischemia-Reperfusion Injury
  • Application of Calycosin Derivatives in Preparation of Drugs for Treating Cerebral Ischemia-Reperfusion Injury
  • Application of Calycosin Derivatives in Preparation of Drugs for Treating Cerebral Ischemia-Reperfusion Injury

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1: the synthesis of the compound shown in the formula (I) used in the following each experimental examples of the application:

[0031] Synthesized according to the following synthetic route:

[0032]

[0033] Among them, the chemical name of compound 1 is: 7-hydroxy-3-(3-hydroxy-4-methoxy)-4H-benzopyran-4-one, and the chemical name of compound 2 is: 1,2-di Bromoethane, the chemical name of intermediate product 3 is: 7-(2-bromoethoxy)-3-(3-(2-bromoethoxy)-4-methoxyphenyl)-4H-benzo Pyran-4-one, the chemical name of compound 4 is: morpholine; the chemical name of compound 5 is: 3-(4-methoxy-3-(2-morpholinoethoxy)phenyl)-7 -(2-Morpholinoethoxy)-4H-benzopyran-4-one.

[0034] The specific synthesis method is:

[0035]1) Take 7-hydroxy-3-(3-hydroxy-4-methoxy)-4H-benzopyran-4-one (300mg) and 1,2-dibromoethane in a molar ratio of 1:8 Dissolve in 13mL of acetone, then use triethylamine to adjust the pH of the system to 10, react at room temperature for 8h, spin...

experiment example 1

[0047] Experimental example 1: neurological function score

[0048] After postoperative anesthesia, the behavioral deficits of the animals were scored according to the method of Bederson. 0 points: no neurological symptoms were observed; 1 point: when the tail was suspended in the air, the contralateral forelimb of the animal showed wrist and elbow flexion, elbow abduction, and was close to the chest wall; 2 points: the animal was placed on a smooth surface, and the operated side was pushed When the shoulder moves to the opposite side, the resistance decreases; 3 points: the animal walks around or circles to the opposite side of the operation; 4 points: flaccid paralysis, no spontaneous movement of the limbs. The higher the score, the more severe the behavioral disorder. Weed out unsuccessful models

[0049] The results showed that CAG002 can dose-dependently reduce the cerebral ischemia-reperfusion injury score in rats. The effect is most obvious when the drug concentratio...

experiment example 2

[0053] Experimental example 2: TCC detection of cerebral infarction area

[0054] After 2 hours of cerebral ischemia and 24 hours of reperfusion, the brain was decapitated and taken out. The brain was sliced ​​into 2 mm coronal slices, totaling 5 slices. Then the slices were placed in 2% TTC phosphate buffer and incubated at a constant temperature of 37°C for 30 min. Normal brain tissue was stained as Red, with white infarcts. Calculate the mass percentage of the infarcted part in the brain slice to reflect the infarct volume ratio.

[0055] The results showed that CAG002 could dose-dependently reduce the volume of cerebral infarction in rats with cerebral ischemia-reperfusion injury. Among them, when the drug concentration is 60mg / kg, the effect is the most obvious. Compared with the positive group, CAG002 is also significantly better than the calycosin group (p<0.05), as shown in Table 2.

[0056] Table 2 Effects of different concentrations of CAG002 and calycosin on cereb...

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Abstract

The invention discloses application of a calycosin derivative in preparing a medicine for treating cerebral ischemia reperfusion injury. Through experiments, an applicant discovers that the calycosin derivative can up-regulate expression levels of ERalpha and GPR30, and can be more beneficial to reducing a neurological function score, reducing a cerebral infarction volume and reducing a cerebral oedema degree compared with calycosin; the calycosin derivative can dose-dependently up-regulate an ERK1 / 2 and Akt phosphorylation level, and plays a role in protecting an ischemia reperfusion injury nerve cell. The calycosin derivative has a structure as shown in the formula (I) which is shown in the description.

Description

technical field [0001] The invention relates to the application of a calycosin derivative in the preparation of a medicine for treating cerebral ischemia-reperfusion injury, which belongs to the technical field of medicine. Background technique [0002] Stroke has attracted much attention due to its high morbidity, disability and mortality. Cerebral ischemia is the main cause of cerebral apoplexy. Research shows that 87% of strokes are caused by cerebral ischemia. The development and promotion of thrombolytic therapy has benefited more and more patients, but the ensuing reperfusion injury is a recognized pathophysiological change after the blood supply of ischemic brain tissue is restored, which can cause cell damage Aggravation, that is, secondary damage to neurons. Epidemiological surveys show that the incidence of ischemic stroke in premenopausal women is significantly lower than that of men of the same age, and the degree of cerebral ischemic damage is lighter than tha...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5377C07D311/36A61P9/10
CPCA61K31/5377C07D311/36
Inventor 陈健王勇夏春波王文波任倩瑶
Owner GUILIN MEDICAL UNIVERSITY
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