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本研究系统评价了20个9-取代小檗碱类似物的糖消耗活性,结果表明,在9位引入乙氧基有利于体外糖消耗活性的增加。9-乙氧小檗碱化合物2a在多个剂量水平下显示出高于阳性对照小檗碱的活性,在1.25μmol·L~(-1)剂量下,2a的活性达到小檗碱的5.4倍。同时,2a激活AMPK的活性是小檗碱的2.8倍。因此,化合物2a可成为进一步改造的母核。
The present study systematically evaluated the activity of sugar consumption of 20 9-substituted berberine analogs. The results showed that introduction of ethoxy group at position 9 was beneficial to increase the activity of sugar consumption in vitro. 9-Ethoxyberberine Compound 2a showed higher activities than the positive control berberine at multiple dose levels and the activity of 2a reached 5.4 times that of berberine at a dose of 1.25 micromol x L (-1) . At the same time, 2a activated AMPK activity is 2.8 times that of berberine. Therefore, compound 2a can be the mother core for further modification.