Abstract: Four pyridyl asymmetrical curcumin analogues were synthesized by 4-acetyl pyridine and appropriate aromatic aldehyde with alkaline and acid catalytic condensation respectively. Their inhibition activity on tyrosinase was evaluated. The results indicate that 3-(4-hydroxyl- 3,5-dimethoxyphenyl)-1-(4-pyridyl)-2-en-propanone has the strongest inhibition on tyrosinase，semi inhibitor concentration is 45.1 μmol/L which is 2.2 times of curcumin （IC50 = 97.1 μmol/L）. Study on inhibitive kinetics discovers that the inhibition on tyrosinase belong to competitive model.

Key words: curcumin analogues, synthesis, tyrosinase inhibitory activity, kinetic study

摘要： 通过芳香醛与4-乙酰基吡啶在酸碱条件下催化缩合，合成了4个单羰基姜黄素类似物A1～A4，并研究了其对酪氨酸酶的抑制活性。结果表明，3-(4-羟基-3,5-二甲氧基苯基)-1-(4-吡啶基)-2-烯-1-酮对酪氨酸酶具有强抑制活性，半数抑制浓度（IC50）为45.1μmol/L，是姜黄素（IC50= 97.1μmol/L）的抑制活性的2.2倍。抑制动力学研究表明，3-(4-羟基-3,5-二甲氧基苯基)-1-(4-吡啶基)-2-烯-1-酮对酪氨酸酶的抑制作用类型属于竞争性抑制。

关键词: 姜黄素类似物, 合成, 酪氨酸酶抑制活性, 抑制动力学