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Oral crocin with protecting effect on cerebral ischemia reperfusion injury and application of oral crocin

A technology of ischemia-reperfusion and crocin, which is applied in the field of pharmacodynamics of crocin, can solve the problems of delayed clinical drug development and limited treatment options, etc.

Inactive Publication Date: 2017-08-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, although many new achievements have been made in the mechanism of cerebral ischemia and its prevention and treatment, its treatment options are still very limited, and the development of clinical therapeutic drugs is relatively lagging behind.

Method used

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  • Oral crocin with protecting effect on cerebral ischemia reperfusion injury and application of oral crocin
  • Oral crocin with protecting effect on cerebral ischemia reperfusion injury and application of oral crocin
  • Oral crocin with protecting effect on cerebral ischemia reperfusion injury and application of oral crocin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1 Crocin improves cerebral infarction volume and behavior

[0026] SD rats (50, male, purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd., weighing 240±20 g) were used for the experiment. Under the standard feeding environment (eating and drinking freely, alternation of day and night, each 12 hours), adaptive feeding was carried out for one week. Subsequently, they were randomly divided into 5 groups, namely the sham operation group, the model group, the positive drug group, the saffron intravenous injection group and the saffron oral administration group. All rats were fasted for more than 12 h before the experiment and had free access to water.

[0027] Establishment of the animal model: After the animals were anesthetized by intraperitoneal injection of 10% chloral hydrate (1 mL / 300 g), the model of middle cerebral artery occlusion was established according to the modified ZeaLonga suture method. In the sham operation group, no ...

Embodiment 2

[0030] Example 2 Effects of Crocin on MDA Content and Total Antioxidative Capacity in Brain Tissue

[0031] The establishment and grouping of experimental animals and models were the same as in Example 1. After 2 hours of cerebral ischemia in rats and 22 hours of reperfusion, they were anesthetized with chloral hydrate. into a 10% brain homogenate, and detect brain tissue malondialdehyde (MDA) content and total antioxidant capacity according to the kit instructions (the kit was purchased from Beyond Biotechnology Co., Ltd.).

[0032] The results of MDA detection showed that the MDA content of the model group was significantly different from that of the sham operation group (p=0.025). Compared with the model group, the positive drug group can significantly reduce the MDA level (p=0.029), there is no significant difference in the crocin intravenous injection group (p=0.070), and the MDA level of the crocin oral administration group is significantly reduced (p=0.070). 0.007)( ...

Embodiment 3

[0033] Example 3 Metabolomics Analysis of Brain Tissue After Administration of Crocin

[0034] The establishment and grouping of experimental animals and models were the same as in Example 1. After 2 hours of cerebral ischemia in rats and 22 hours of reperfusion, the brain tissue was anesthetized with chloral hydrate, and the brain tissue was taken after heart perfusion with physiological saline. 2- 13 C 2- Homogenate in 800 μL of 80% methanol solution (2.5 μg / mL) of myristic acid, let it stand in a refrigerator at 4° C. for 1 hour, and centrifuge at 20,000×g at 4° C. for 10 minutes. Take 200 μL of the supernatant in a GC sample bottle, evaporate to dryness under reduced pressure, then add 30 μL of methoxyamine pyridine solution (10 mg / mL), vortex for 3 min, and stand at room temperature for 16 h for oximation. Then add 30 μL of derivatization reagent MSTFA (containing 1% TMCS), vortex for 3 minutes, let stand at room temperature for 1 hour for silanization, and finally add ...

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Abstract

The invention provides an oral drug, namely crocin with a protecting effect on cerebral ischemia reperfusion injury. The crocin is from natural drugs, namely saffron crocus and jasmine, and an alternate name is crocin-I. An arterial ischemia reperfusion model in an animal brain is constructed through a suture method; and the crocin is subjected through gastric irrigation and static injection separately, so that the protecting effect of the crocin on the cerebral ischemia reperfusion injury is superior to that of an existing positive first-line drug edaravone injection during intragastric administration, and is obviously superior to that of an intravenous administration group. The oral crocin has a good protecting effect on the cerebral ischemia reperfusion injury, and a preferred drug is provided for clinical treatment and prevention of related diseases such as a cerebral injury and cerebral arterial thrombosis caused by ischemia reperfusion.

Description

technical field [0001] The invention relates to the pharmacological effect of crocin, especially the pharmacological protective effect on brain injury and ischemic stroke caused by ischemia-reperfusion. Background technique [0002] Stroke, also known as stroke or cerebrovascular accident, is mainly divided into two categories: ischemic stroke (cerebral infarction, cerebral thrombosis) and hemorrhagic stroke (cerebral hemorrhage, subarachnoid hemorrhage). Among them, ischemic stroke accounts for about 70%-80% of all strokes, has a very high mortality rate and disability rate, is extremely harmful to patients, often causes irreversible brain damage, and causes great harm to families and society. Big burden, and showing a younger trend. In recent years, although many new achievements have been made in the mechanism of cerebral ischemia and its prevention and treatment, its treatment options are still very limited, and the development of clinical therapeutic drugs is relativel...

Claims

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Application Information

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IPC IPC(8): A61K31/7024A61P9/10
CPCA61K31/7024
Inventor 王广基阿基业张悦
Owner CHINA PHARM UNIV
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