吴茱萸碱的合成及其结构表征和体内抗肿瘤作用  

Synthesis as well as structural characterization and in vivo antitumor activity evaluation of evodiamine

作　　者：杨云云[1] 郭惠[1] 王昌利[1] 张拴[1] 

机构地区：[1]陕西中医学院药学系,陕西咸阳712046

出　　处：《化学研究》2011年第3期22-25,共4页Chemical Research

基　　金：国家自然科学基金青年基金项目(81001669);陕西省教育厅专项科研计划项目(09JK393);陕西中医学院中药制药重点学科资助课题

摘　　要：以色胺和N-甲基靛红酸酐作为起始原料合成了吴茱萸碱;利用元素分析仪、红外光谱仪、核磁共振谱仪、质谱仪等对合成产物进行了结构表征,并研究了其对小鼠移植性肉瘤S180和小鼠肝癌H22的体内抗肿瘤作用.结果表明,所合成的吴茱萸碱在高、中、低剂量(20 mg.kg-1、10 mg.kg-1、5 mg.kg-1)下均对S180和H22的生长具有抑制作用;同环磷酰胺相比,吴茱萸碱对脾脏和胸腺损伤较小,甚至具有一定的保护作用.Evodiamine was synthesized by using tryptamine and N-methylisatoic anhydride as the starting materials.The composition and structure of as-synthesized product were analyzed by means of elemental analysis,infrared spectrometry,1H-nuclear magnetic resonance spectroscopy,and mass spectrometry.The in vivo antitumor activity of evodiamine for S180 and H22 in mice was evaluated.Results showed that high,medium and low dose of evodiamine（20 mg · kg-1,10 mg · kg-1 and 5 mg · kg-1） could all effectively inhibit the growth of S180 and H22.In the meantime,as compared with cyclophosphamide,as-synthesized evodiamine had little damage to spleen and thymus,and even possessed protective effect.

关 键 词：吴茱萸碱 合成 结构表征 体内抗肿瘤作用 

分 类 号：O626[理学—有机化学] R282.71[理学—化学]