小远志中糖酯类成分及其体外抗黄嘌呤氧化酶活性研究  

Glycolipids from Polygala sibirica var. megalopha and their in vitro inhibitory activity on xanthine oxidase

作　　者：周凌云[1,2] 李盼盼[2] 余小红[2] 王军民[2] 鲁斌[2] 华燕[2] 

机构地区：[1]皖南医学院药学院,安徽芜湖241002 [2]西南林业大学西南山地森林资源保育与利用重点实验室,云南昆明650224

出　　处：《中草药》2016年第23期4146-4150,共5页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(31260083);皖南医学院校重点科研项目培育基金(WK2016Z06)

摘　　要：目的研究小远志Polygala sibirica var.megalopha中的糖酯类化学成分及其抗黄嘌呤氧化酶活性,并分析其构效关系。方法小远志75%乙醇提取物通过D101大孔树脂,依次用水和35%、65%、95%乙醇洗脱,采用尿酸生成法检测出65%乙醇洗脱部分抗黄嘌呤氧化酶活性最高(IC50=10.83μg/m L),对该部分采用多种柱色谱方法进行分离纯化,结合活性追踪,得到4个对黄嘌呤氧化酶具有高抑制活性的糖酯类化合物。结果 4个糖酯类化合物分别鉴定为远志寡糖酯A(1)、3,6′-二芥子酰基蔗糖(2)、3′-E-3,4,5-三甲氧基肉桂酰基-6-苯基蔗糖(3)、3′-E-3,4,5-三甲氧基肉桂酰基-4-苯基蔗糖(4),均为首次从该植物中分离得到。化合物1、3、4对黄嘌呤氧化酶的IC50分别为9.5、10.2、7.7μmol/L,比对照品别嘌呤醇(IC50=11.2μmol/L)抑制作用略强,而化合物2(IC50=1.3μmol/L)则显示出更强的抗黄嘌呤氧化酶活性,推测该类糖酯结构中苯乙烯基与糖基相连的结构片段是发挥药效的重要基团。结论糖酯类化合物作为新的黄嘌呤氧化酶高效抑制剂,具有开发成为抗痛风药的潜力。Objective To investigate the glycolipids from Polygala sibirica var. megalopha and their structure-activity relationship of xanthine oxidase （XO） inhibitory activity.Methods The 75% EtOH extract of P.sibirica var. megalopha was chromatographied with D101 macroporous resins column by water,35% EtOH,65% EtOH,and 95% EtOH,successively.Compared to other elution parts,the 65% EtOH elution part exhibited stronger XO inhibition.Further bioassay-guided separation led to the isolation of four known glycolipids,which demonstrated potent XO inhibition.Results Four compounds were identified to be tenuifoliside A （1）,3,6＇-disinapoyl sucrose （2）,3＇-E-3,4,5-trimethoxycinnamoyl-6-benzoyl sucrose （3）,and 3＇-E-3,4,5-trimethoxycinnamoyl-4-benzoyl sucrose （4） through spectroscopic data analysis.All compounds were obtained from this plant for the first time.This enzyme inhibition was dose dependent and the IC50 values of compounds 1,3,and 4 were 9.5,10.2,and 7.7 μmol/L,respectively.Among them,compound 2 had significantly higher XO inhibitory activity than that of the control allopurinol （IC50=11.2 μmol/L）.It was speculated that the styryl side chain linking with sugar base played an important role on the XO inhibitory activity.Conclusion Glycolipides as a novel series of XO inhibitors,may be developed into a promising remedy for human gout.

关 键 词：小远志 糖酯类成分 抗黄嘌呤氧化酶活性 3’-E-3 4 5-三甲氧基肉桂酰基-4-苯基蔗糖 3 6’-二芥子酰基蔗糖 

分 类 号：R284.1[医药卫生—中药学]