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Application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in preparing medicine for treating cerebrovascular diseases

A drug and ischemic stroke technology, applied in cardiovascular system diseases, drug combinations, nervous system diseases, etc.

Inactive Publication Date: 2014-02-26
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to provide a new application of the compound to solve the above-mentioned defects in the existing drugs for the treatment of cerebrovascular diseases

Method used

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  • Application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in preparing medicine for treating cerebrovascular diseases
  • Application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in preparing medicine for treating cerebrovascular diseases
  • Application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in preparing medicine for treating cerebrovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] compound Protective effect on glucose and hypoxia injury of neural cell line HT22 cells cultured in vitro. This compound is hereinafter referred to as IV 7 .

[0023] Nerve cell line HT22 cells were cultured for 24 hours and divided into non-glucose and hypoxia control group, glucose and hypoxia (OGD) group, and non-glucose and hypoxia IV group. 7 0.1, 1, 10, 50, 100μM groups and OGD+IV 7 0.1, 1, 10, 50 or 100 μM groups. After glucose and hypoxia for 12 hours, the degree of cell damage was detected by LDH method. According to the formula LDH leakage rate = A culture solution / (A culture solution + A cell homogenate) × 100%.

[0024] figure 1 The effect of compound IV7 0.1, 1, 10, 50, 100 μM alone on the LDH leakage rate of HT22 cells, mean±SD, n=6.

[0025] figure 1 Show that: compared with the control group, IV alone 7 0.1, 1, 10, 50, 100μM had no significant effect on the leakage rate of LDH, indicating that the above doses of IV 7 No toxic effect on H...

Embodiment 2

[0029] Example 2: Compound IV 7 Protection against permanent focal ischemic brain injury in rats.

[0030] Male SD rats were randomly divided into control group (sham operation group), model group, IV 7 High, medium and low dose groups (25mg / kg -1 , 5mg / kg -1 and 1mg / kg -1 ), 10 per group. The rat model of permanent middle cerebral artery occlusion (MCAO) was established by suture method. Inject IV intraperitoneally 1 hour after ischemia 7 , administered in equal volumes at different concentrations. After 24 hours of ischemia, a 5-point scoring method was used. The higher the score, the more obvious the neurological deficit. Nerve function was measured by grasping force method and observed by TTC staining method IV 7 Effect on infarct volume.

[0031] image 3 Compound IV7 reduced the neurological symptom score of rats with cerebral ischemia, mean±SD, n=10; compared with the model group, *p <0.05.

[0032] Figure 4 Compound IV 7 Improve the grip strength of ra...

Embodiment 3

[0037] (E)-2-(3,5-Dimethoxybenzylidene)-cyclopentanone compound (IV 7 ) preparation

[0038] Add cyclopentanone (4.43g, 0.05mol) and morpholine (5.20g, 0.06mol) to 20mL of benzene, install a water trap, and reflux to azeotrope until no water is formed. Benzene and morpholine were evaporated under reduced pressure to obtain enamine (1) with a yield of 100%.

[0039]Add compound 1 (6.54g, 0.043mol) and 3,5-dimethoxybenzaldehyde (5.40g, 0.033mol) into 20mL of benzene, install a water trap, and reflux azeotropically until no water is formed. Cool to room temperature, slowly add 6mol / L hydrochloric acid with stirring, and stir at room temperature. The benzene layer was separated, the aqueous layer was extracted with the benzene layer, the benzene layers were combined, and dried over anhydrous sodium sulfate. Evaporate to dryness, recrystallize from petroleum ether ethanol solution to obtain yellow needle-like crystals, yield 80.6%, mp: 98.2~99.3°C.

[0040] IR(KBr, cm -1 ): 17...

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Abstract

The invention discloses application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in preparing a medicine for treating cerebrovascular diseases. The related research indicates that the compound has an obvious cranial nerve protection effect, obviously reduces the focal cerebral ischemia rat cerebral infarction volume and remarkably improves the neurologic symptom. The (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone is used for preventing or treating the diseases such as ischemic brain injury, cerebral hemorrhage, cerebral thrombosis, cerebral embolism, cerebral infarction, cerebral apoplexy, lacunar infarction, transient ischemic attack, cerebral arteriosclerosis, diabetic cerebrovascular complications and the like.

Description

technical field [0001] The invention relates to the field of medicines, in particular to the application of (E)-2-(3,5-dimethoxybenzylidene)-cyclopentanone in the preparation of medicines for treating mammalian cerebrovascular diseases. Background technique [0002] Cerebral stroke is a group of diseases whose main clinical manifestations are cerebral tissue ischemia and hemorrhagic injury symptoms, also known as stroke or cerebrovascular accident. The disease has an acute onset, high disability rate and high mortality rate, and is one of the most important diseases that endanger human health in the world today. Stroke is mainly divided into two categories: hemorrhagic stroke (cerebral hemorrhage or subarachnoid hemorrhage) and ischemic stroke (ischemic brain injury, including cerebral infarction and cerebral thrombosis). Stroke is the most common. [0003] At present, the clinical treatment of ischemic stroke mainly adopts drug therapy, including thrombolysis, vasodilator...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/122A61P25/00A61P9/10
Inventor 张慧灵敖桂珍顾卫卫徐敏宋恒罗宇陈韶华
Owner SUZHOU UNIV
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