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Correction published on 29 March 2016, see Int. J. Mol. Sci. 2016, 17(4), 468.

Open AccessArticle
Int. J. Mol. Sci. 2015, 16(9), 21759-21774; doi:10.3390/ijms160921759

A Novel Ligustrazine Derivative T-VA Prevents Neurotoxicity in Differentiated PC12 Cells and Protects the Brain against Ischemia Injury in MCAO Rats

1
School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China
2
Department of Pathology, Beijing University of Chinese Medicine, Beijing 100029, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Katalin Prokai-Tatrai
Received: 18 June 2015 / Revised: 24 August 2015 / Accepted: 31 August 2015 / Published: 9 September 2015
(This article belongs to the Collection Neuroprotective Strategies)
View Full-Text   |   Download PDF [6938 KB, uploaded 30 March 2016]   |  

Abstract

Broad-spectrum drugs appear to be more promising for the treatment of acute ischemic stroke. In our previous work, a new ligustrazine derivative (3,5,6-trimethylpyrazin-2-yl) methyl 3-methoxy-4-[(3,5,6-trimethylpyrazin-2-yl)methoxy]benzoate (T-VA) showed neuroprotective effect on injured PC12 cells (EC50 = 4.249 µM). In the current study, we show that this beneficial effect was due to the modulation of nuclear transcription factor-κB/p65 (NF-κB/p65) and cyclooxygenase-2 (COX-2) expressions. We also show that T-VA exhibited neuroprotective effect in a rat model of ischemic stroke with concomitant improvement of motor functions. We propose that the protective effect observed in vivo is owing to increased vascular endothelial growth factor (VEGF) expression, decreased oxidative stress, and up-regulation of Ca2+–Mg2+ ATP enzyme activity. Altogether, our results warrant further studies on the utility of T-VA for the potential treatment of ischemic brain injuries, such as stroke. View Full-Text
Keywords: ligustrazine derivative; neuroprotection; NF-κB/p65; VEGF; middle cerebral artery occlusion (MCAO) ligustrazine derivative; neuroprotection; NF-κB/p65; VEGF; middle cerebral artery occlusion (MCAO)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Li, G.; Tian, Y.; Zhang, Y.; Hong, Y.; Hao, Y.; Chen, C.; Wang, P.; Lei, H. A Novel Ligustrazine Derivative T-VA Prevents Neurotoxicity in Differentiated PC12 Cells and Protects the Brain against Ischemia Injury in MCAO Rats. Int. J. Mol. Sci. 2015, 16, 21759-21774.

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