CAS: 20188-85-6; 5-Hydroxy-2-(3-Hydroxy-4-Methoxyphenyl)-7-Methoxy-3-(((2S,3R,4S,5S,6R)-3,4,5-Trihydroxy-6-((((2R,3R,4R,5R,6S)-3,4,5-Trihydroxy-6-Methyltetrahydro-2H-Pyran-2-yl)Oxy)Methyl)Tetrahydro-2H-Pyran-2-yl)Oxy)-4H-Chromen-4-One

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diazomethane rutin dimethyl sulfateβ-D-glucose L-rhamnose ombuin O2,O3,O4-triacetyl-O6-(tri-O-acetyl-α-L-rhamnopyranosyl)-β-D-glucopyranosyloxy]-chromen-4-one5-acetoxy-2-(3-acetoxy-4-methoxy-phenyl)-7-methoxy-3-[O2,O3,O4-triacetyl-O6-(tri-O-acetyl-α-L-rhamnopyranosyl)-β-D-glucopyranosyloxy]-chromen-4-one

重氮甲烷,芦丁 以 甲醇,乙醚作为反应溶剂,反应 1.0H,以33%的收率获得2-(3,4-Dimethoxyphenyl)-5-Hydroxy-7-Methoxy-3-[(2S,3R,4S,5S,6R)-3,4,5-Trihydroxy-6-[[(2R,3R,4R,5R,6S)-3,4,5-Trihydroxy-6-Methyloxan-2-Yl]Oxymethyl]Oxan-2-Yl]Oxychromen-4-One
参考文献:Structural Requirements Of Flavonoids And Related Compounds For Aldose Reductase Inhibitory Activity.
标题:Structural Requirements Of Flavonoids And Related Compounds For Aldose Reductase Inhibitory Activity.
摘要:发现,几种天然药材和药用食品的甲醇提取物对大鼠晶状体醛糖还原酶显示抑制作用.在大多数情况下,通过生物测定指导的分离方法,分离得到黄酮类化合物作为活性成分,其中,槲皮苷(Ic50=0.15 μm),愈创木脂苷(0.18 μm)和去甲基芸香糖苷-1(0.082 μm)显示出强的抑制活性.去甲基芸香糖苷-1显示了最强的活性,相当于商品化合成醛糖还原酶抑制剂依帕司他(0.072 μm)的活性.为了阐明黄酮类化合物对醛糖还原酶抑制活性的结构要求,检测了各种黄酮类化合物及相关化合物.结果表明,黄酮类化合物的以下结构要求是:1)具有7-羟基和/或邻苯二酚结构的黄酮和黄酮醇(在b环上的3′,4′-二羟基结构)显示出强的活性;2)5-羟基结构并不影响活性;3)3-羟基和7-O-葡糖基结构降低活性;4)2-3双键增强活性;5)具有邻苯二酚结构的黄酮和黄酮醇显示出比具有连苯三酚结构(3′,4′,5′-三羟基结构)的化合物更强的活性.
Doi:10.1248/Cpb.50.788