Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China.
Molecules. 2012 Sep 6;17(9):10667-74. doi: 10.3390/molecules170910667.
Scutellarein, the main metabolite of scutellarin in vivo, has relatively better solubility, bioavailability and bio-activity than scutellarin. However, compared with scutellarin, it is very difficult to obtain scutellarein from Nature. Therefore, the present study focused on establishing an efficient route for the synthesis of scutellarein by hydrolyzing scutellarin. Neurological deficit score and cerebral infarction volume with the administration of scutellarein were then used to compare its neuroprotective effects on focal cerebral ischemia/reperfusion in rats induced by middle cerebral artery occlusion (MCAO) with those of scutellarin. The results showed that scutellarein had better protective effect on focal cerebral ischemia/reperfusion than scutellarin, which laid the foundation for further research and development of scutellarein as a promising candidate for ischemic cerebro-vascular disease.
灯盏乙素是灯盏花乙素在体内的主要代谢物,其水溶性、生物利用度和生物活性均优于灯盏花乙素。然而,与灯盏花乙素相比,从自然界中获得灯盏乙素非常困难。因此,本研究旨在建立一种高效的水解灯盏花乙素合成灯盏乙素的方法。然后,用灯盏乙素处理大鼠大脑中动脉闭塞(MCAO)诱导的局灶性脑缺血再灌注引起的神经功能缺损评分和脑梗死体积来比较其对大鼠局灶性脑缺血再灌注的神经保护作用与灯盏花乙素的作用。结果表明,灯盏乙素对脑缺血再灌注的保护作用优于灯盏花乙素,为进一步将灯盏乙素作为缺血性脑血管疾病的候选药物进行研究和开发奠定了基础。