摘要
Four series of derivatives of vanillin,anisaldehyde,genistein and aloe emodin were prepared.The single crystal of （E）-1-（5-（4-methoxyphenyl）-3-（4-methoxystyryl）-4,5-dihydro-1H-pyrazol-1-yl）ethanone,which was synthesized from vanillin, was obtained by spontaneous evaporation method.All the compounds were tested for the tyrosinase inhibitory activities.The results demonstrated that the IC_（50）values of vanillin,anisaldehyde,genistein and aloe emodin against mushroom tyrosinase activity are 68,49,343 and 160μM,respectively.Among the twelve derivatives,（E）-1-（5-（4-methoxyphenyl）-3-（4-methoxystyryl）-4,5- dihydro-1H-pyrazol-1-yl）ethanone from vanillin and 4,5-dimethoxy-9,10-dioxo-9,10-dihydroanthracene-2-carboxylic acid from aloe emodin showed good inhibition against the tyrosinase with IC_（50）values of 18μM and 21μM,respectively.
以香草醛、茴香醛、染料木素和芦荟大黄素为原料合成一系列的衍生物,测定了衍生物(E)-1-(5-(4-甲氧基苯基)-3-(4-甲氧基苯乙烯基)-4,5-二氢-1H-吡唑-1-基)乙酮的晶体结构,并对这些化合物的酪氨酸酶抑制活性进行了测定。研究结果表明,香草醛、茴香醛、染料木素和芦荟大黄素的IC_(50)值分别为68μM,49μM,343μM和160μM。与标准对照品曲酸(IC_(50)=35μM)相比,香草醛衍生物(E)-1-(5-(4-甲氧基苯基)-3-(4-甲氧基苯乙烯基)-4,5-二氢-1H-吡唑-1-基)乙酮和芦荟大黄素衍生物4,5-二甲氧基-9,10-二氢蒽醌-2-甲酸具有更好的酪氨酸酶抑制活性,其IC_(50)值分别为18μM和21μM。
基金
National Key Technology R&D Program of China (Grant No.2007BAI27B05).
