摘要
以常见单糖作为取代基,采用固-液相转移催化法合成了9-O-小檗碱糖苷系列产物,合成化合物分子结构分别通过紫外光谱和核磁共振分析等方法进行了确认.通过对清洁级SD大鼠尾静脉注射四氧嘧啶获得实验性高血糖大鼠模型,分组对大鼠灌胃给药9-O-小檗碱葡萄糖苷、小檗碱与二甲双胍阳性对照药15d,并检测期间空腹血糖值.结果显示9-O-小檗碱葡萄糖苷具有明显体内降血糖能力,给药15d后高血糖大鼠血糖下降超过56%,优于小檗碱.
9-O-glycosyl-berberine derivatives were synthesyzed with berberine as the lead compound and common monosaccharide as the substituent groups according to solid-liquid phase transfer catalysis. The structures of the 9-O-glycosyl-berberine homologues synthesized were affirmed with ultraviolet spectrosco- py and 1 H NMR. To evaluate the hypoglycemic ability of 9-O-glycosyl berberine in vivo, a hyperglycemic rat model was established by tail vein injection of alloxan, and FBG （fasting blood-glucose） was assayed after intragastrical （ig）administration of 9-O-glucosyl-berberine upon hyperglycemic rats, compared with berberine and metformin. The results showed that after 15 days＇ ig administration, 9-O-glucosyl-berberine had significant in vivo hypoglycemic activity, the hypoglycemic rate being up to over 56%.
出处
《西南大学学报（自然科学版）》
CAS
CSCD
北大核心
2012年第5期146-151,共6页
Journal of Southwest University(Natural Science Edition)
基金
重庆市攻关项目(CSTC
2008AA5021
CSTC
2010AC5007)
重庆市医学科研计划项目(2011-1-114)
西南大学研究生科技创新基金项目(kb2009017)
关键词
小檗碱
结构修饰
体内降糖活性
9-O-小檗碱糖苷同系物
berberine
structural modification
in vivo hypoglycemic activity
9-O-glycosyl-berberine derivative
