Application of tanshinone IIA sodium sulfonate as blood-brain barrier protecting agent in cerebral diseases

A technology for blood-brain barrier and blood-brain barrier damage, which is applied to nervous system diseases, medical preparations containing active ingredients, and pharmaceutical formulas to achieve the effect of small dosage and long effective maintenance time

Inactive Publication Date: 2008-02-13
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, for the application of tanshinone IIA sulfonic acid sodium salt in the preparation of cerebral ischemic stroke, Parkinson's disease, multiple sclerosis and other brain diseases, especially for tanshinone IIA sulfonic acid sodium salt as a blood-brain barrier protective agent There is no report on the application of the treatment of the above diseases

Method used

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  • Application of tanshinone IIA sodium sulfonate as blood-brain barrier protecting agent in cerebral diseases
  • Application of tanshinone IIA sodium sulfonate as blood-brain barrier protecting agent in cerebral diseases
  • Application of tanshinone IIA sodium sulfonate as blood-brain barrier protecting agent in cerebral diseases

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Example 1: Protective effect of tanshinone IIA sulfonic acid sodium salt on blood-brain barrier damage caused by oxidative stress in vitro

[0025] 1.1 Culture of rat brain microvascular endothelial cells in vitro

[0026] The 1-week-old SD rats were sacrificed by cervical dislocation and then soaked and disinfected in ice-cold 75% ethanol solution for 5 minutes. The bilateral cerebral hemispheres were washed with ice-cold PBS until there was no blood stains. The pia mater, surface blood vessels and white matter were removed, and the remaining brain tissue was used After cutting into pieces with scissors, digest with 0.05% trypsin at 37°C for 20 minutes, add culture solution containing 20% ​​serum to stop the digestion, blow and disperse the cells with a pipette, filter the digestion solution with 150 μm and 74 μm nylon meshes successively, and collect the 74 μm nylon mesh The microvascular fragments were centrifuged at 25% BSA density (4000r / min, 10min) to remove tissu...

Embodiment 2

[0037] Example 2: Cerebral protection of sodium tanshinone IIA sulfonate on focal cerebral ischemia-reperfusion injury in rats

[0038] Get male SD rats and divide into 5 groups at random, namely sham operation group, model group, STS low-dose group (2mg / kg), STS high-dose group (5mg / kg) and positive control nimodipine group (1mg / kg), Each group was intraperitoneally injected with the corresponding drugs 1 hour after the operation, and the control group was injected with the same volume of normal saline. The rat model of focal cerebral ischemia-reperfusion injury was reproduced by the known suture method (Longa EZ, et al: Reversible middle cerebral artery occlusion without craniectomy in rats. Stroke, 1989; 20: 84-91), ischemia After 2 hours of reperfusion for 24 hours, the following indicators were measured: 1) Nervous deficit behavior score: score according to Longa's 5-level scoring method: level 0, no dysfunction; level 1, unable to extend the right forelimb; level 2, rota...

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Abstract

The present invention belongs to pharmaceutical field, which relates to the application of the sodium tanshinone IIA sulfonate as a protective agent for the blood brain barrier in mental diseases. The present invention provides the new function of the sodium tanshinone IIA sulfonate as a protective agent for the blood brain barrier in mental disease prevention and treatment. The in vitro and in vivo studies display that the sodium tanshinone IIA sulfonate possesses definite protection function for the blood brain barrier. The present invention also possesses definite prevention and treatment function for metal disease related to the blood brain barrier injury, which comprises ischemic cerebral apoplexy. The present invention skillfully takes the blood brain barrier as the therapy target for mental diseases, which breaks through the restriction that the treatment medicine should reach the effective drug therapy concentration in accordance with the pharmacokinetic characteristics. Medicine provided in the present invention can protect the brain when the drug reaches effective intravascular concentration. Therefore better choice for treatment of the mental disease is provided.

Description

technical field [0001] The invention belongs to the field of pharmacy and relates to the application of tanshinone IIA sulfonic acid sodium salt in the preparation and treatment of brain diseases related to blood-brain barrier damage. Background technique [0002] The blood-brain barrier is an important physiological barrier to protect brain tissue. It is mainly composed of vascular endothelial cells, glial cells and pericytes. The vascular endothelial cells located in the blood-brain barrier have tight junctions, and the pinocytic vesicles are much less than other vascular endothelial cells. cell. The specific physiological protective structure of the blood-brain barrier only allows a very small amount of water-soluble substances to enter the brain tissue through the cell bypass, but compounds with suitable fat solubility can freely diffuse into the brain tissue. The blood-brain barrier plays an important physiological role in maintaining the brain microenvironment. In ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/343A61P25/00A61P25/28A61P25/16A61P35/00
Inventor 郝海平王广基崔楠吴晓兰
Owner CHINA PHARM UNIV
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