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The edaravone and 3-n-butylphthalide ring-opening derivative 10b effectively attenuates cerebral ischemia injury in rats

  
@article{APS9365,
	author = {Kai Hua and Xiao Sheng and Ting-ting Li and Lin-na Wang and Yi-hua Zhang and Zhang-jian Huang and Hui Ji},
	title = {The edaravone and 3- n -butylphthalide ring-opening derivative 10b effectively attenuates cerebral ischemia injury in rats},
	journal = {Acta Pharmacologica Sinica},
	volume = {36},
	number = {8},
	year = {2017},
	keywords = {},
	abstract = {Aim: Compound 10b is a hybrid molecule of edaravone and a ring-opening derivative of 3-n-butylphthalide (NBP). The aim of this study was to examine the effects of compound 10b on brain damage in rats after focal cerebral ischemia.
Methods: SD rats were subjected to 2-h-middle cerebral artery occlusion (MCAO). At the onset of reperfusion, the rats were orally treated with NBP (60 mg/kg), edaravone (3 mg/kg), NBP (60 mg/kg)+edaravone (3 mg/kg), or compound 10b (70, 140 mg/kg). The infarct volume, motor behavior deficits, brain water content, histopathological alterations, and activity of GSH, SOD, and MDA were analyzed 24 h after reperfusion. The levels of relevant proteins in the ipsilateral striatum were examined using immunoblotting.
Results: Administration of compound 10b (70 or 140 mg/kg) significantly reduced the infarct volume and neurological deficits in MCAO rats. The neuroprotective effects of compound 10b were more pronounced compared to NBP, edaravone or NBP+edaravone. Furthermore, compound 10b significantly upregulated the protein levels of the cytoprotective molecules Bcl-2, HO-1, Nrf2, Trx, P-NF-κB p65, and IκB-α, while decreasing the expression of Bax, caspase 3, caspase 9, Txnip, NF-κB p65, and P-IκB-α.
Conclusion: Oral administration of compound 10b effectively attenuates rat cerebral ischemia injury.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/9365}
}