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., Lianyungang 222001, China.
Zhongguo Zhong Yao Za Zhi. 2017 Dec;42(24):4716-4721. doi: 10.19540/j.cnki.cjcmm.2017.0206.
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.
研究银杏内酯同系物对血小板活化因子(PAF)诱导的血小板聚集的拮抗作用,并探讨其神经保护作用。以PAF作为凝聚剂,分别向兔血样中加入银杏内酯。采用比浊法检测各化合物对血小板聚集的抑制作用。在L-谷氨酸诱导的原代皮质神经元细胞损伤模型中,采用MTT法检测细胞活力。利用荧光Ca2+指示剂Fura-2 AM测量神经元细胞内游离Ca2+浓度。采用形态学观察和Hoechst 33258染色检测银杏内酯对神经元凋亡的抑制作用。结果表明,银杏内酯同系物对PAF诱导的血小板聚集活性的抑制作用由高到低依次为银杏内酯K(GK)、银杏内酯B(GB)、银杏内酯A(GA)、银杏内酯C(GC)、银杏内酯M(GM)、银杏内酯J(GJ)和银杏内酯(GL)。GB和GK(1 - 100 μmol•L⁻¹)可显著减轻L-谷氨酸引起的细胞损伤,提高细胞存活率,降低细胞内钙浓度,恢复细胞形态。本文明确了银杏内酯同系物各化合物对PAF诱导的血小板聚集的活性及特点以及其神经保护作用。