连翘花中抑制酪氨酸酶活性成分研究

Activity-guided Isolation of Mushroom Tyrosinase Inhibitors from the Flower of Forsythia suspensa

本文首次对连翘花抑制酪氨酸酶活性成分进行了研究。首先,对连翘不同器官[叶、果实(青翘、老翘)、花]抑酶活性进行比较分析,发现连翘花对酪氨酸酶的抑制表现出了浓度依赖性;进而对连翘花不同溶剂提取物进行抑酶活性评价,结果表明95%乙醇提取物抑酶活性最高。然后根据活性导向分离方法,对连翘花95%乙醇提取物进行了化学成分分离,从中分离得到5个化合物,鉴定为:连翘酯苷A(1)、芦丁(2)、(+)-松脂素-β-D-葡萄糖苷(3)、(+)-甲基松脂素-β-D-葡萄糖苷(4)、连翘苷(5),其中化合物4是首次从连翘花中分离得到。酪氨酸酶抑制活性测试表明化合物均显示出一定的抑酶活性,同时各化合物之间表现出明显的协同作用,这表明这些成分可能是连翘花美白作用的物质基础。

This is the first time to investigate the chemical constitutes of Forsythia suspensa flower for tyrosinase-inhibition activity. First, different organs （flower,leaf,green Forsythiae Fructus and ripe Forsythiae Fructus） of F.suspensa were tested for the tyrosinase-inhibition activity,and the F.suspensa flower showed concentration-dependent on the inhibition of tyrosinase activity.Second,different extracts of F.suspensa flower were also tested for the tyrosinase-inhibition activity,and the 95% ethanol extract displayed the best inhibition of tyrosinase activity.Then,five compounds were obtained from 95% ethanol extract by the activity-guided isolation method,and their structures were identified as forsythiaside A （1）,rutin （2）,（＋）-pinoresinol-β-D-glucoside （3）,（＋）-pinoresinol monomethyl ether β-D-glucoside （4） and （＋）-phillyrin （5）,while compound 4was reported for the first time from F.suspensa flower.Four of them showed weak inhibition activity against tyrosinase but displayed obvious synergistic effect.The results implied that the 5 compounds were most likely to be the chemical substance foundation of the whitening effect of F.suspensa flower and its inhibitory effect was possibly produced by synergistic effect.