阿魏酸乙酯的药理活性及其机制研究

目的: 观察阿魏酸乙酯的药理活性及其机制。方法: 在兔富含血小板血浆(PRP)中加入阿魏酸乙酯和阿魏酸,用ADP诱导血小板的集聚,用TYXN-91 智能血液凝集仪观察血小板聚集率,激光共聚焦显微镜观察血小板细胞聚集时细胞内钙离子的变化情况。制备CCl4 肝损伤小鼠模型,取血清测定谷丙转氨酶(ALT)、谷草转氨酶(AST)活性,取肝组织测定丙二醛(MDA)水平及超氧化物歧化酶(SOD)活性。结果: 不同浓度的阿魏酸乙酯,对ADP诱导的血小板聚集抑制百分数均显著高于等浓度的阿魏酸(n=8,P<0.05)。在阿魏酸乙酯作用下ADP诱导的血小板细胞内钙离子荧光强度的变化(ΔFI)为4.6 ±1.7,明显低于对照组ΔFI 值(10.3 ±2.6,n=8,P<0.01)。阿魏酸乙酯可使肝损伤小鼠组织MDA、血清ALT、AST 含量显著低于对照组,而肝组织的SOD 水平显著高于对照组。结论: 阿魏酸乙酯抑制ADP诱导的血小板聚集作用及对CCl4 引起的小鼠急性肝损伤的保护作用均比阿魏酸强。

Study of pharmacological effects and mechanism of ethyl ferulate

AIM: To investigate the pharmacological effects and mechanism of ethyl ferulate (EF).METHODS: The platelet congregate rate was observed by congregater TYXN-91 and the platelet intracellular calcium oscillation was observed by laser scanning.The acute liver injury model of mice was made by using the CCl4 156 mg·kg^-1, ip.Then the levels of ALT and AST were determined in serum and the levels of MDA and SOD in the liver.RESULTS: The inhibition rate of the platelet congregate were 26.3 %±3.3 %, 33.4 %±2.4 %, 73.4 %±3.1 %, and 94.9 %±2.7 %(n=8)in different concentration(0.1, 0.5, 1.5, and 3.0 mmol·L^-1)of ethyl ferulate, respectively.It was higher than those in the same concentrations of ferulic acid.The change of the fluctuation of calcium (ΔFI 4.6 ±1.7)in EF group was much lower than the rest level (10.3 ±2.6)(n=8, P <0.01).The levels of AST and ALT in serum andMDA in the liver tissue of EF group were obviously lower than those of the control group.It also showed that EF could significantly enhance the activities of SOD.CONCLUSION: The inhibition of ethyl ferulate on platelet congregation induced by ADP is much better than that of ferulic acid.Ethyl ferulate against the CCl4 acute liver injury is better than that of ferulic acid in mice.