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Application of 5-(3', 5'-dimethoxybenzylidene)-2-sulfo-imidazole-4-one to preparation of drug for treating cerebrovascular disease

A technology for cerebrovascular diseases and drugs, applied in the field of drugs, can solve the problems of low clinical efficacy, side effects, blood stealing, etc.

Active Publication Date: 2013-10-02
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The common characteristics of the above-mentioned drugs for the treatment of ischemic cerebral apoplexy are: strong pertinence and clear targets, but the curative effect is single, can only provide partial protective effect, the clinical curative effect is small, and there are different degrees of toxic and side effects
For example, it is difficult for thrombolytic drugs to enter the damaged brain tissue through the blood-brain barrier to exert their effects, so the curative effect is uncertain, and there are side effects of causing reperfusion injury and bleeding; vasodilator drugs can dilate blood vessels in normal parts, resulting in abnormal The blood flow to the normal brain tissue, resulting in the so-called "steal blood" phenomenon

Method used

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  • Application of 5-(3', 5'-dimethoxybenzylidene)-2-sulfo-imidazole-4-one to preparation of drug for treating cerebrovascular disease
  • Application of 5-(3', 5'-dimethoxybenzylidene)-2-sulfo-imidazole-4-one to preparation of drug for treating cerebrovascular disease
  • Application of 5-(3', 5'-dimethoxybenzylidene)-2-sulfo-imidazole-4-one to preparation of drug for treating cerebrovascular disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] compound In vitro cultured neural cell line HT 22 Protective effect of cellular glucose and hypoxia injury. This compound is hereinafter referred to as IV 4 .

[0026] Nervous cell line HT 22 The cells were cultured for 24 hours and divided into non-glucose and hypoxia control group, glucose and hypoxia (OGD) group, non-glucose and hypoxia (non-OGD)+IV 4 0.1, 1, 10, 50, 100μM groups and OGD+IV 4 0.1, 1, 10, 50 or 100 μM groups. After glucose and hypoxia for 12 hours, the degree of cell damage was detected by lactate dehydrogenase (LDH) method. According to the formula LDH leakage rate = A culture solution / (A culture solution + A cell homogenate) × 100%.

[0027] attached figure 1 Compound IV for single use 4 0.1, 1, 10, 50, 100μM for HT 22 Effect diagram of cell LDH leakage rate, mean ± SD, n=6.

[0028] figure 1 Show that: compared with the control group, IV alone 4 0.1, 1, 10, 50, 100μM had no significant effect on the leakage rate of LDH, indica...

Embodiment 2

[0031] Example 2: Compound IV 4 Protection against permanent focal ischemic brain injury in rats.

[0032] Male SD rats were randomly divided into control group (sham operation group), model group, IV 4 High, medium and low dose groups (10mg / 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. Intravenously administered 3 hours after ischemia 4 , 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 4 Effect on infarct volume.

[0033] attached image 3 for compound IV 4 Score chart of neurological symptoms of cerebral ischemia rats, mean ± SD, n=10; compared with model group, *p <0.05.

[0034] attached Figure 4 for compound IV 4 Improve the ...

Embodiment 3

[0037] Example 3: Nervous cell line HT 22 The cells were cultured for 24 hours and divided into non-glucose and hypoxia control group (non-OGD group), glucose and hypoxia (OGD) group, non-glucose and hypoxia IV group 4 0.1, 1, 10, 50, 100μM groups and OGD+IV 4 0.1, 1, 10, 50 or 100 μM groups. After 6 hours of glucose and hypoxia, the expression of cathepsin B was detected by Western Blotting.

[0038] attached Figure 6 HT 22 Expression map of cathepsin B in cells. Figure 6 A is a representative Western Blotting diagram; Figure 6 B is a Western Blotting statistical graph; mean±SD, n=3; compared with the control group ## p <0.01; compared with the model group, **p<0.01.

[0039] Figure 6 showed that compared with the non-glucose-hypoxic group, 6 h of glucose-deficient hypoxia significantly induced HT 22 The expression of cathepsin B in cell activity increased; 4 Can significantly inhibit OGD-induced HT 22 Increased expression of cellular active cathepsin B, il...

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Abstract

The invention discloses application of 5-(3', 5'-dimethoxybenzylidene)-2-sulfo-imidazole-4-one to preparation of drugs for treating cerebrovascular diseases. According to relevant researches disclosed by the invention, the compound has a remarkable cerebral nerve protection effect, can obviously reduce the volume of cerebral infarction of a focal cerebral ischemia rat and can obviously improve neurological signs; and moreover, the protection effect of an IV4 compound to cerebral ischemic injuries is related to the inhibition of the activation of lysosomal enzyme cathepsin B, so that the compound can be used for preparing drugs for preventing or treating diseases such as ischemic brain injuries, cerebral hemorrhage, cerebral thrombosis, cerebral embolism, cerebral infarction, cerebral stroke, lacunar infarction, transient ischemia attacks, cerebral arteriosclerosis and diabetic cardiovascular complications.

Description

technical field [0001] The invention relates to the field of medicines, in particular to the application of 5-(3',5'-dimethoxybenzyl)-2-thio-imidazol-4-one 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, vasodilat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4166A61P9/10A61P7/02
Inventor 张慧灵敖桂珍顾卫卫陈洁茹荣加国贺园园
Owner SUZHOU UNIV
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