Lasiokaurin的合成与活性研究  

Study on the Synthesis and Activity of Lasiokaurin

作　　者：闫学斌[1] 李雯[2] 刘宏民[1] 

机构地区：[1]郑州大学新药研究开发中心,河南郑州450052 [2]郑州大学化学工程学院,河南郑州450002

出　　处：《郑州大学学报（工学版）》2006年第3期113-115,共3页Journal of Zhengzhou University（Engineering Science）

基　　金：国家"863"计划资助项目(2002AA2Z3242)

摘　　要：为了研究lasiokaurin的生物活性和冬凌草的构效关系,以提取的冬凌草甲素为原料,经选择性保护、乙酰化和脱保护三步反应以69.3%的收率合成了lasiokaurin,所合成的化合物经IR1、H-NMR、MS和元素分析等确证结构.测定了冬凌草甲素和lasiokaurin的抗原虫epimastigote活性,发现lasiokaurin的半数致死浓度为25μM,抗原虫活性高于冬凌草甲素,说明1位对冬凌草甲素的活性有明显的影响.To study bioactivities of lasiokaurin and stucture- activity ralationship of oridonin, desired compound lasiokaurin was successfully obtained in 69.3% overall yield via three steps, selective acetonide protection, acetylation and deprotection, using isolated oridonin as the starting material. The structures of the compounds were characterized by IR, ^1H- NMR, MS and Elemental analysis. The antiprotozoon activity of lasiokaurin and oridonin was determined. Median lethal concentration of lasiokauin is 25μM, which indicates 1 - hydroxyl has obvious effects on activity.

关 键 词：Lasiokaurin 冬凌草甲素 乙酰化 合成 活性 

分 类 号：R284.3[医药卫生—中药学]