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.