Application of SB202190 in preparation of medicines for treating intractable epilepsy

A technology of 1.SB202190 and 2.SB202190 is applied in the application field of SB202190 in the preparation of drugs for the treatment of refractory epilepsy, and can solve the problems of decreased drug concentration in the brain, drug resistance and the like

Inactive Publication Date: 2015-05-13
JINSHAN HOSPITAL FUDAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because it can recognize a variety of AEDs with different mechanisms of action, it actively pumps drugs through the blood-brain barrier, causing a decrea

Method used

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  • Application of SB202190 in preparation of medicines for treating intractable epilepsy
  • Application of SB202190 in preparation of medicines for treating intractable epilepsy
  • Application of SB202190 in preparation of medicines for treating intractable epilepsy

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Embodiment Construction

[0021] The specific embodiments provided by the present invention will be described in detail below in conjunction with the accompanying drawings.

[0022] 1 Materials and methods

[0023] 1.1 Experimental materials and equipment

[0024] Rabbit anti-p38MAPK monoclonal antibody: CST Company;

[0025] Mouse anti-p-p38 antibody monoclonal antibody: Santa Cruz Company;

[0026] Mouse anti-PGP monoclonal antibody: Abcam;

[0027] Goat anti-mouse, goat anti-rabbit DyLight TM Secondary antibody: Jackson company;

[0028] DAPI, phenytoin (PHT), sodium valproate, lamotrigine, SB202190: Sigma;

[0029] Microdialysis probe and casing: Sweden CMA company;

[0030] CMA / 100 Micro Syringe Pump: Sweden CMA Company;

[0031] MonEL510 high performance liquid chromatography: American syltech company.

[0032] 1.2 Establishment and grouping of epilepsy animal models

[0033] 1.2.1 Experimental animals

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Abstract

The invention relates to application of SB202190 in preparation of medicines for treating intractable epilepsy. By utilizing an intractable epilepsy animal model, due to a series of researches, the SB202190 can reduce the expression of multidrug transporter-P glycoprotein (PGP) related to drug tolerance in the brain of an intractable epilepsy rat, the drug concentration of antiepileptic drugs (AEDs) in hippocampus cell extracellular fluid of the intractable epilepsy rat is improved, the AEDs is assisted to improve the electrophysiological activity of the rat, and the ignition post-attack classification is reduced, namely the drug tolerance of the intractable epilepsy can be improved by the SB202190. The application of the SB202190 is widened, and an effective way is provided for treatment of the intractable epilepsy.

Description

technical field [0001] The present invention relates to the new application of SB202190, in particular, the application of SB202190 in the preparation of drugs for treating intractable epilepsy. Background technique [0002] SB202190 (FHPI, English chemical name [0003] 4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)-1H-imidazole) is a potent p38MAPK inhibitor with molecular formula C 20 h 14 FN 3 O, molecular weight 331.3, CAS number 152121-30-7. Current in vitro studies have shown that SB202190 significantly inhibits endogenous background and anti-Fas antibody-induced MAPKAPK 2 activity, and the inhibitory effect is dose-dependent. SB202190 alone is sufficient to induce death in Jurkat and Hela cells: Bcl-2 expression is blocked by activating the CPP32-like cysteine ​​protease. p38β alleviates and p38α exacerbates apoptosis induced by SB202190. SB202190 strongly inhibited UV-induced cox-2 protein expression and mRNA levels in HaCaT cells. Treatment of renal tu...

Claims

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Application Information

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IPC IPC(8): A61K31/4439A61P25/08C07D401/04
Inventor 陈英辉王翠翠邵一叶
Owner JINSHAN HOSPITAL FUDAN UNIV
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