第 44 卷第 2 期Vol. 44 No. 2
2014 年 4 月Apr 2014

所属栏目:医药及中间体

鹰嘴豆芽素A 7-O-β-D-吡喃木糖苷的合成与抗缺氧活性研究
景临林1,范小飞1,2,马慧萍1,樊鹏程1,贾正平1* (1. 兰州军区兰州总医院药剂科,甘肃 兰州 730050; 2. 兰州大学 药学院,甘肃 兰州 730000)
摘 要:以乙酰溴代木糖和鹰嘴豆芽素A为原料,采用相转移催化法在鹰嘴豆芽素A 7位羟基处引入糖苷,合成得到了鹰嘴豆芽素A 7-O-β-D-吡喃木糖苷,方法简单,条件温和,收率较高。产物结构通过1H NMR、IR和ESI-MS分析确认。通过小鼠常压密闭耐缺氧实验和化学物质中毒实验对其抗缺氧活性进行评价,结果表明:鹰嘴豆芽素A 7-O-β-D-吡喃木糖苷表现出了较高的抗缺氧活性。
关键词:鹰嘴豆芽素A;糖苷;相转移催化;抗缺氧活性
中图分类号:TQ463.5  文献标识码:A  文章编号:1009-9212(2014)02-0025-03
Synthesis and Anti-hypoxia Activity of Biochanin A-7-O-β-D-xylopyranoside
JING Lin-lin1, FAN Xiao-fei1,2, MA Hui-ping1, FAN Peng-cheng1, JIA Zheng-ping1* (1. Department of Pharmacy, Lanzhou General Hospital, Lanzhou Command of CPLA, Lanzhou 730050, China; 2. Department of Medicinal Chemistry, Lanzhou University, Lanzhou 730000, China)
Abstract:Using α-D-xylopyranosyl bromide and biochanin A as the starting materials, biochanin A-7-O-β-D-xylopyranoside was synthesized by means of phase transfer catalysis. This route has advantages of mild reaction conditions, simple procedures and high yield. The structure was characterized by 1H NMR, IR and EI-MS spectra. The anti-hypoxic activities of the title compound were examined using the normobaric hypoxia and chemistry poisoning hypoxia model of mice. The results indicate that the title compound exhibits high anti-hypoxic activity.
Key words:biochanin A; glucoside; phase transfer catalysis; anti-hypoxia activity
基金项目:国家自然科学基金项目(81202458),全军医药科研“十二五”面上项目(CLZ12JA04),中国博士后科学基金(2012M521926)。
作者简介:景临林(1982-),男,山西临汾人,主管药师,博士,研究方向:药物合成研究(E-mail:lfjinglinlin@163.com)。
联 系 人:贾正平,男,主任药师,博士,研究方向:药物合成与药理研究(E-mail:zhengping_jia@yahoo.cn)。