The Institute of Chinese Medicinal Sciences, Guangdong Pharmaceutical University, Guangzhou Higher Education Mega Centre, Guangzhou, PR China.
J Ethnopharmacol. 2009 Oct 29;126(1):134-42. doi: 10.1016/j.jep.2009.07.034. Epub 2009 Aug 7.
Flavonoids, extracted from the leaves of Diospyros kaki, are the main therapeutic components of NaoXingQing (NXQ), a potent and patented Chinese herbal remedy widely used in China for the treatment of apoplexy syndrome.
To investigate the neuroprotective effects of FLDK-P70, a standardized flavonoid extract, using in vivo rat models of both focal ischemia/reperfusion (I/R) injury induced by middle cerebral artery occlusion (MCAO) and on transient global brain ischemia induced by four-vessel occlusion (4-VO). We also aim to examine the effects of FLDK-P70 on glutamate-induced cell injury of hippocampal neurons as well as on hypoxia-induced injury of cortical neurons in primary cell culture.
Administration of FLDK-P70 for 12 days (40, 80 mg/kg body weight, p.o., 5 days before and 7 days after 4-VO) increased the survival of hippocampal CA1 pyramidal neurons after transient global brain ischemia. Similarly, administration of FLDK-P70 for 7 days (40, 80 mg/kg body weight, p.o., 3 days before and 4 days after MCAO) significantly reduced the lesion of the insulted brain hemisphere and improved the neurological behavior of rats. In primary rat hippocampal neuronal cultures, pretreatment with FLDK-P70 (5, 10 microg/ml) protected neurons from glutamate-induced excitotoxic neuronal death in a dose-dependent manner. In primary rat cerebral cortical neuronal culture, pretreatment with FLDK-P70 (25, 100 microg/ml) also reduced hypoxia-reoxygen induced neuronal death and apoptosis in a dose-dependent manner.
These in vivo and in vitro results suggest that FLDK-P70 significantly protects rats from MCAO and 4-VO ischemic injury in vivo and protects hippocampal neurons from glutamate-induced excitotoxic injury as well as cortical neurons from hypoxia-induced injury in vitro. The mechanisms of these effects may be due to the antioxidative activity of the flavonoids. These results convincingly demonstrate that FLDK-P70 may be useful for the prevention and treatment of ischemia/reperfusion injury and other related neurodegenerative diseases.
类黄酮从柿叶中提取，是一种强效专利中草药的主要治疗成分，名为脑心清（NXQ），在中国被广泛用于治疗中风综合征。
使用体内大脑中动脉阻塞（MCAO）诱导的局灶性缺血/再灌注（I / R）损伤和四血管阻塞（4-VO）诱导的短暂全脑缺血的大鼠模型，研究 FLDK-P70（一种标准化类黄酮提取物）的神经保护作用。我们还旨在研究 FLDK-P70 对谷氨酸诱导的海马神经元细胞损伤以及原代细胞培养中缺氧诱导的皮质神经元损伤的影响。
FLDK-P70 给药 12 天（40、80mg / kg 体重，口服，4-VO 前 5 天和后 7 天）增加了短暂全脑缺血后海马 CA1 锥体神经元的存活。同样，FLDK-P70 给药 7 天（40、80mg / kg 体重，口服，MCAO 前 3 天和后 4 天）可显著减少受影响大脑半球的病变并改善大鼠的神经行为。在原代大鼠海马神经元培养物中，FLDK-P70（5、10μg / ml）预处理以剂量依赖性方式保护神经元免受谷氨酸诱导的兴奋性神经元死亡。在原代大鼠皮质神经元培养物中，FLDK-P70（25、100μg / ml）预处理也以剂量依赖性方式减少缺氧-复氧诱导的神经元死亡和细胞凋亡。
这些体内和体外结果表明，FLDK-P70 可显著保护大鼠免受体内 MCAO 和 4-VO 缺血性损伤，保护海马神经元免受谷氨酸诱导的兴奋性毒性损伤以及皮质神经元免受缺氧诱导的损伤。这些作用的机制可能是由于类黄酮的抗氧化活性。这些结果令人信服地证明，FLDK-P70 可能可用于预防和治疗缺血/再灌注损伤和其他相关的神经退行性疾病。
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