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作 者:谢雪[1,2,3] 张宏达[1,2,3] 陈昱竹[1] 曹跃[1] 王丽[1] 许枬[1]
机构地区:[1]辽宁中医药大学,辽宁大连116600 [2]江苏康缘药业股份有限公司,江苏连云港222001 [3]中药制药过程新技术国家重点实验室,江苏连云港222001
出 处:《中国中药杂志》2012年第23期3585-3590,共6页China Journal of Chinese Materia Medica
基 金:国家"重大新药创制"科技重大专项(2009ZX09103-394)
摘 要:目的:对愈肾汤总黄酮的化学成分和活性进行研究,为处方的活性成分揭示和作用机制阐明奠定基础。方法:采用体外H2O2诱导人脐静脉内皮细胞(HUVEC)损伤实验评价愈肾汤总黄酮的活性。并采用硅胶柱、大孔吸附树脂、葡聚糖凝胶色谱和高效液相制备等方法分离纯化愈肾汤总黄酮的化学成分,根据理化性质和波谱数据鉴定其结构。结果:愈肾汤总黄酮具有明显的抗过氧化氢诱导的HUVEC损伤和下调PAI-1表达(P<0.05)的作用。从愈肾汤总黄酮部位分离得到9个黄酮类化合物分别为毛蕊异黄酮(1)、蒙花苷(2)、3',4'-二羟基-7-O-β-D-葡萄糖苷(3)、3'-羟基-4'-甲氧基-7-O-β-D-葡萄糖苷(4)、槲皮素(5)、山柰酚(6)、芦丁(7)、红车轴草异黄酮-7-O-β-D-葡萄糖苷(8)、4'-羟基二氢黄酮-7-O-β-D-葡萄糖苷(9)。结论:愈肾汤总黄酮具有抗HUVEC氧化损伤作用,所分离的9个黄酮化合物均为首次从该方中分离得到,化合物1,3,4,8,9可能来自于黄芪,化合物2,5~7可能来自于小蓟和仙鹤草,其中3,4和9为首次从组方的单味药中分离得到。] Objective: To study the chemical constituents and activity of total flavonoids contained in Yushen Tang,in order to lay a foundation for defining active consituents of the prescription and their mechanism. Method: The activity of total flavonoids contained in Yushen Tang were evaluated by in vitro H2O2 -induced human umbilical vein endothelial cell injury experiment. The chemical constituents were separated and purified by such methods as silica column chromatography, macroporous resin chromatography, sephadex and HPLC preparation, and their structures were identified on the basis of their spectral data and physicochemical properties. Result: Total flavonoids contained in Yushen Tang showed the effects in inhibiting hydrogen peroxide-induced human umbilical vein endothelial cell(HUVEC) injury and down-regulating PAI-1 expression(P 〈 0.05). Nine flavonoids were separated from total flavonoids contained in Yushen Tang and identified as calycosin ( 1 ), linarin (2), 3',4', 7 -trihydroxyflavone-7-O-β-D-glucopyranoside ( 3 ), 7,3'-dihydroxy- 4'-methoxyflavone -7-glucoside( 4 ), quercetin ( 5 ), kaempferol ( 6 ), rutin ( 7 ), pratensein-7-O-β-D-glucoside ( 8 ) and 7-O-glucosyl liquiritigenin(9). Conclusion: Total flavonoids contained in Yushen Tang showed the effect in inhibiting HUVEC injury. All of the nine flavonoids were separated from Yushen Tang for the first time, and compounds 1,3,4,8,9 may be derived from astragalus mongho- licus,while compounds 4,5-7 may be derived from herba cepbalanoplosis segeti and hairyvein agrimony. Among them, compounds 3,4 and 9 were seperated from single ingredient of the prescription for the first time.
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