胡椒碱及其衍生物对原代培养心肌细胞损伤的保护作用

背景：胡椒碱是滇产回心草心脏保护作用的主要物质基础，同时，其化学结构相对简单，可进行结构修饰，为进一步研发新型的抗心肌缺血的化合物奠定基础。目的：观察胡椒碱及其7个衍生物对异丙肾上腺素和过氧化氢损伤心肌细胞的保护作用。方法：采用异丙肾上腺素和H2O2诱导原代培养大鼠心肌细胞致心肌细胞损伤模型，MTT法检测不同剂量胡椒碱及其衍生物对损伤心肌细胞的影响。结果与结论：7×10-8 mol/L胡椒碱、7×10-8，7×10-7mol/L胡椒酸甲酯、7×10-8，7×10-7，7×10-6 mol/L吡咯烷产物、7×10-8，7×10-7，7×10-6 mol/L二乙胺产物可不同程度地提高异丙肾上腺素诱导的心肌细胞损伤模型中心肌细胞的存活比例(P < 0.05)，但未见剂量相关性； 7×10-8 mol/L胡椒碱(P < 0.05)、7×10-8，7×10-7 mol/L吡咯烷产物和7×10-8，7×10-7 mol/L二乙胺产物可提升过氧化氢诱导的心肌细胞损伤模型中心肌细胞存活比例，未见明显的剂量相关性。由此推测胡椒碱及其衍生物可显著缓解异丙肾上腺素和过氧化氢所致的心肌细胞损伤，且其吡咯烷产物和二乙胺产物作用效果优于胡椒碱。

Protective effect of piperine and its derivates on myocardial cells

BACKGROUND: Piperine is the lead compound of Rhodobryum roseum Limp that have protective effect on heart. Simultaneously, the chemical constitution of piperine is relative simple, which can provide a foundation for the further study of anti-myocardial ischemia. OBJECTIVE: To investigate the protective effect of piperine and its seven derivates on cardiocytes injured by isoproterenol or hydrogen peroxide (H2O2). METHODS: Injured cardiocyte model was induced by isoproterenol and H2O2. And then the influence of piperine and its seven derivates on injured cardiocytes was detected by MTT. RESULTS AND CONCLUSION: The 7×10-8mol/L piperine, 7×10-8, 7×10-7 mol/L methyl piperate, 7×10-8, 7×10-7, 7×10-6 mol/L 5-(3, 4-methylenedioxy phenyl)-2E, 4E-pentadienoic acid pyrrolidine amide and 7×10-8, 7×10-7, 7×10-6 mol/L 5-(3, 4- methylenedioxy phenyl)-2E, 4E-pentadienoic acid diethyl amide could significantly increased the survival of cardiocytes in the isoproterenol model group (P < 0.05), but there was no dose-dependent manner. And the survival of cardiocytes was also significantly higher in the H2O2 model group under the effect of 7×10-8mol/L piperine, 7×10-8, 7×10-7 mol/L 5-(3, 4-methylenedioxy phenyl)-2E, 4E-pentadienoic acid pyrrolidine amide and 7×10-8, 7×10-7mol/L 5-(3.4-methylenedioxy phenyl)-2E, 4E-pentadienoic acid diethyl amide. In a word, piperine and its derivates could protect the primary cultured cardiocytes from isoproterenol damage and H2O2 damage. 5-(3, 4-methylenedioxy phenyl)-2E, 4E-pentadienoic acid pyrrolidine amide and 5-(3, 4-methylenedioxy phenyl)-2E, 4E-pentadienoic acid diethyl amide showed better protective effect than piperine.