川芎咔啉碱的合成及其对血管内皮细胞损伤的保护作用  

Synthesis of Chuanxiong Perlolyrine and its protective effect on injured vascular endothelial cells

作　　者：刘新泳[1] 赵全芹[2] 李朝武[3] 张蕊[1] 王兴坡[2] 徐文方[1] 

机构地区：[1]山东大学药学院药物化学研究所 [2]山东大学化学化工学院 [3]山东大学齐鲁医院

出　　处：《山东大学学报（医学版）》2003年第5期485-487,共3页Journal of Shandong University:Health Sciences

基　　金：山东省科委国际合作课题;中医药局资助课题

摘　　要：目的:探讨川芎咔啉碱的新合成方法及其对血管内皮细胞损伤的保护作用。方法:以色胺为原料,经Pictet-Spengler环合反应,脱氢芳化反应制得川芎咔啉碱。用过氧化氢诱导血管内皮细胞损伤,以MTT法检测细胞的活力,计算细胞增殖率。结果:川芎咔啉碱的化学结构由元素分析、红外光谱、核磁共振波谱分析证实。川芎咔啉碱对H2O2引起的人胎儿脐静脉内皮细胞(HUVECs)的损伤具有保护作用,当浓度达到1.2mmol/L时保护作用最大。在浓度0.1～1.2mmol/L范围内,存在剂量依赖性关系。结论:川芎咔啉碱对H2O2诱导的HUVECs的损伤具有保护作用,提示可能对内皮损伤时的修复具有重要的意义。Objective:To search for a new synthetic method of Chuanxiong Perlolyrine and to investigate its protective effect on human vascular endothelial cells(VECs).Methods:Chuanxiong Per-lolyrine was synthesized by the Pictet-Spengler cyclic reaction of tryptamine with5-acety loxymethyl fu-raldehyde and followed by the dehydrogenation with sulfur.The proliferation of human umbilical vein endothelial cells(HUVECs)was assessed by MTT assay.Results:The structure of Perlolyrine was confirmed by elemental and spectral analysis.With the favorite concentration of1.2mmol.L -1 ,Chuanxiong Perlolyrine exhibited high potent protective effect on HUVECs injured by hydrogen peroxide.There was a clear dosage-activity correlation at the concentration range of0.1-1.2mmol.L -1 .Conclusion:Chuanxiong Perlolyrine possesses highly protective effect on injured HUVECs,indicating the potential significance in repairing the injured endothelium as a new candidate for treatment of cardiovascular diseases.

关 键 词：川芎咔啉碱 血管内皮细胞 四甲偶氮唑蓝比色法 

分 类 号：R914.5[医药卫生—药物化学]