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Application of tanshinone IIA derivative in preparation of ischemic stroke drugs

A technology for ischemic stroke and tanshinone, applied in the field of medicine, can solve the problems of low bioavailability, insignificant protective effect of cerebral infarction and cerebral edema, poor water solubility of tanshinone IIA, etc., so as to improve water solubility and increase bioavailability. Effect

Active Publication Date: 2019-06-21
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The invention provides the application of a tanshinone IIA derivative in the preparation of cardiovascular and cerebrovascular drugs, specifically relates to the protective effect on cerebral infarction and cerebral edema caused by cerebral ischemia-reperfusion, so as to solve the problem of poor water solubility of tanshinone IIA and its bioavailability. Low, and the protective effect on cerebral infarction and cerebral edema caused by cerebral ischemia-reperfusion is not significant

Method used

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  • Application of tanshinone IIA derivative in preparation of ischemic stroke drugs
  • Application of tanshinone IIA derivative in preparation of ischemic stroke drugs
  • Application of tanshinone IIA derivative in preparation of ischemic stroke drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1: Primary Screening Experiment of Tanshinone IIA Derivatives

[0018] 1. Test method

[0019] 1. Establishment of the oxygen-glucose deprivation / reoxygenation (OGD / R) model of rat primary cortical neurons

[0020] Sodium dithionite (Na 2 S 2 o 4 ) dry powder fully dissolved, so that the final concentration of 20mM, with NaHCO 3 Adjust the pH to 7.2, which is the anoxic solution. The primary cortical neuron cells were cultured in a 24-well cell culture plate for 7-10 days, and the cells in good growth state were selected for experiments. Before administration, the medium in the 24-well plate was gently aspirated, washed twice with PBS buffer, and then cultured with drug-containing medium. The experiment included a blank control group, a model control group, a tanshinone IIA derivative group, and a tanshinone IIA group. After 24 hours, the drug-containing medium was removed and replaced with anoxic solution, and an equal volume of maintenance medium (Neuro...

Embodiment 2

[0028] Example 2: Determination of the protective effect of tanshinone IIA derivatives on cerebral ischemia-reperfusion injury

[0029] 1. Experimental purpose: To establish SD rat MCAO animal model, and to observe the protective effect of test drugs W-1~W-5 on cerebral infarction and cerebral edema caused by cerebral ischemia-reperfusion.

[0030] 2. Experimental method

[0031] 1. Focal cerebral ischemia / reperfusion model in rats

[0032] No food or water was allowed 24 hours before the modeling operation. Referring to the method of Longa et al., the middle cerebral artery occlusion (MCAO) model in rats was prepared by the internal carotid artery suture method: the rats were anesthetized by intraperitoneal injection (ip) of 3% chloral hydrate (300 mg / kg), and operated in supine position. On the stage, make a midline incision in the neck, expose the right common carotid artery, pull the digastric muscle and sternocleidomastoid muscle outwards, free from the bifurcation of t...

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Abstract

The invention relates to application of tanshinone IIA derivative in the preparation of ischemic stroke drugs and belongs to the field of medicine. The high-molecular tanshinone IIA derivative is synthesized herein; pharmacological experiment studies on animals are carried out; experimental results show that the high-molecular tanshinone IIA derivative can well protect cerebral ischemia-reperfusion injury in MCAO (middle cerebral artery occlusion) animal model of an SD (Sprague Dawley) rat; compared with positive controls, the high-molecular tanshinone IIA derivative can evidently improve neurological behaviors, cerebral infarction area and encephaledema of the rat with focal cerebral ischemia. The high-molecular tanshinone IIA derivative provided by the invention helps provide a new ideafor treating ischemic stroke, and has the potential of being developed into drugs to treat ischemic stroke.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the application of a tanshinone IIA derivative in the preparation of ischemic stroke medicine, and the compound has a protective effect on cerebral ischemia-reperfusion injury. Background technique [0002] In recent years, with the acceleration of the aging population in my country, the incidence of cerebrovascular diseases has been increasing year by year. The vast majority of cerebrovascular diseases are strokes caused by ischemia, which seriously endanger human health. At present, the main clinical treatment principles for ischemic stroke are: timely restore the blood flow and reperfusion of blood vessels, improve the blood circulation of the brain, and increase the supply of blood and oxygen in the ischemic area. The main purpose is to save the ischemic penumbra The surviving neurons in the zone reduce the size of the cerebral infarction. (Appelboom G, Strozyk D, Meyers PM, Higashi...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61P9/10A61P7/10
Inventor 王进欣宫志博
Owner CHINA PHARM UNIV
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