中国中药杂志

2017, v.42(24) 4716-4721

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银杏二萜内酯类化合物拮抗PAF诱导的血小板聚集及对神经细胞的保护作用
Antagonistic effect of ginkgolide homologues on PAF-induced platelet aggregation and neuroprotective effect

徐君;王奎龙;曹泽彧;曹亮;王振中;萧伟;
XU Jun;WANG Kui-long;CAO Ze-yu;CAO Liang;WANG Zhen-zhong;XIAO Wei;State Key Laboratory of New-tech for Chinese Medicine Pharmaceutical Process,Jiangsu Kanion Parmaceutical Co.,Ltd.;

摘要(Abstract):

该研究通过对银杏二萜内酯类化合物拮抗PAF诱导的血小板凝集和神经保护作用进行检测来探讨银杏内酯制剂治疗缺血性脑卒中的作用机制。实验以PAF作为血小板聚集诱导剂,将银杏二萜内酯分别加入采集的兔血中,采用比浊法检测各化合物对血小板凝集的抑制作用;在L-谷氨酸诱导的原代皮质神经细胞损伤模型上采用MTT检测细胞活率,使用荧光染料Fura-2 AM检测细胞内游离钙离子浓度,通过Hoechst 33258染色法检测银杏二萜内酯对神经细胞凋亡的抑制作用。结果发现银杏二萜内酯类化合物中抑制PAF诱导的血小板凝集活性大小依次为银杏二萜内酯K(GK)、银杏二萜内酯B(GB)、银杏二萜内酯A(GA)、银杏二萜内酯C(GC)、银杏二萜内酯M(GM)、银杏二萜内酯J(GJ)和银杏二萜内酯L(GL);其中GB和GK(1~100μmol·L~(-1))能显著减轻L-谷氨酸所致的细胞损伤,表现为神经细胞活率明显提高(P<0.05),细胞内钙离子浓度明显下降(P<0.05)和细胞凋亡率明显减少(P<0.05)。该研究明确了银杏二萜内酯各化合物在抑制PAF诱导的血小板凝集和神经细胞保护方面的活性与作用特征。
To study the antagonistic effect of ginkgolide homologues on platelet-activating factor(PAF)-induced platelet aggregation and investigate its neuroprotective effect. PAF was used as a coagulant,and ginkgolides were added to the rabbit blood samples respectively. The inhibitory effect of each compound on platelet aggregation was detected by turbidimetry. In L-glutamate induced primary cortical neuron cell injury model,MTT assay was used to detect cell viability. Intracellular free Ca2 +concentration in neurons was measured by using the fluorescent Ca2 +indicator Fura-2 AM. Morphological observation and Hoechst 33258 staining were used to detect the inhibitory effect of ginkgolide on neuronal apoptosis. The results showed that the inhibitory effect on PAF-induced platelet aggregation activity in ginkgolide homologues was ginkgolide K( GK),ginkgolide B( GB),ginkgolide A( GA),ginkgolide C( GC),ginkgolide M( GM),ginkgolide J( GJ) and ginkgolide( GL) from high to low. GB and GK( 1-100 μmol· L-1) could significantly reduce the cell damage caused by L-glutamate,with survival rate increasing,intracellular calcium concentration reducing and cell morphology restoring. This paper has identified the activities and characteristics of various compounds of ginkgolide homologues on PAF-induced platelet aggregation as well as its neuroprotective effect.

关键词(KeyWords): 银杏二萜内酯类化合物;拮抗PAF受体;神经保护;凋亡;Ca2+超载
ginkgolide homologues;antagonistic to PAF receptor;neuroprotection;apoptosis;Ca2+ overload

Abstract:

Keywords:

基金项目(Foundation): 国家“重大新药创制”科技重大专项(2013ZX09402203);; 江苏省科技成果转化项目(BA2010109)

作者(Author): 徐君;王奎龙;曹泽彧;曹亮;王振中;萧伟;
XU Jun;WANG Kui-long;CAO Ze-yu;CAO Liang;WANG Zhen-zhong;XIAO Wei;State Key Laboratory of New-tech for Chinese Medicine Pharmaceutical Process,Jiangsu Kanion Parmaceutical Co.,Ltd.;

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