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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 study the chemical constituents of sugar esters and their anti-xanthine oxidase activities in Polygala sibirica var.megalopha and to analyze their structure-activity relationship. Methods The extract of 75% ethanol from Xiao Yuan Zhi was passed through D101 macroporous resin and eluted with water and 35%, 65% and 95% ethanol in turn. The highest anti-xanthine oxidase activity was detected by uric acid formation assay (IC50 = 10.83μg / m L). The fractions were separated and purified by a variety of column chromatography methods, and four activity-based sugar ester compounds with high inhibitory activity on xanthine oxidase were obtained. Results Four sugar ester compounds were identified as polygalactosidase A (1), 3,6’-alanylsucrose (2), 3’-E-3,4,5-trimethoxycinnamoyl-6 -phenyl sucrose (3) and 3’-E-3,4,5-trimethoxycinnamoyl-4-phenyl sucrose (4) were isolated from this plant for the first time. The IC50 of compound 1,3,4 for xanthine oxidase was 9.5, 10.2 and 7.7μmol / L, respectively, which was slightly stronger than that of allopurinol (IC50 = 11.2μmol / L) μmol / L) showed stronger anti-xanthine oxidase activity. It is presumed that the structural segment linking the styryl group and the glycosyl group in the sugar ester structure is an important group that exerts efficacy. Conclusion Sugar esters as new xanthine oxidase inhibitor, has the potential to develop into a drug against gout.