异鼠李素对蘑菇酪氨酸酶二酚酶活力的抑制机理  

Inhibition mechanism of isorhamnetin on the activity of mushroom tyrosinase diphenolase

作　　者：刘敏 邵文祥[2] 张灵芝[2] 骆彩红 匡溢敏 左爱仁[2] LIU Min SHAO Wen-xiang ZHANG Ling-zhi KUANG Yi-min ZUO Ai-ren(School of Basis Medicine, Jiangxi Health Vocational College, Nanchang 330029 School of Basis Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang 330006)

机构地区：[1]江西卫生职业学院基础部,南昌330029 [2]江西中医药大学基础医学院,南昌330006

出　　处：《中国食品添加剂》2016年第12期73-77,共5页China Food Additives

基　　金：江西省卫生计生委中医药基金资助项目(2015A042);江西省普通本科高校大学生创新创业教育计划项目(201410412046;201610412020);江西中医药大学科技项目(2014ZR012);江西省自然科学基金资助项目(20161BAB205218)

摘　　要：异鼠李素是沙棘果实和美白类中草药白蒺藜、白鲜皮的主要黄酮类活性成分,具有广泛的药理活性。酪氨酸酶是人体细胞产生黑色素和果蔬褐变的关键酶。本文研究了异鼠李素对蘑菇酪氨酸酶二酚酶活力的抑制机理。以L-多巴为底物,测定异鼠李素对酪氨酸酶二酚酶活性的IC50、抑制类型和抑制常数。抑制类型由Lineweaver-Burk双倒数作图法来判断,并计算相应的抑制常数(KI和KIS)。实验结果显示,异鼠李素对蘑菇酪氨酸酶二酚酶活力抑制效果显著,IC50为25μmol/L,是混合型可逆抑制,抑制常数KI为20.1μmol/L,KIS为108.6 mol/L。总之,异鼠李素对蘑菇酪氨酸酶二酚酶活力有很好的抑制作用,是值得进一步研究的美白类候选药物和防止果蔬褐变的食品添加剂。Isorhamnetin is the main active flavonoid from the Hippophae rhamnoides Linn.,Tribulus terrestris L.and Dictamnus dasycarpus Turcz. Isorhamnetin has extensive pharmacological activities. Tyrosinase is the key enzyme to produce melanin in body cells and to produce the browning of fruit and vegetable. The main aim of this study is to examine the inhibition mechanism of isorhamnetin on the activity of mushroom tyrosinase diphenolase. The experiment examined the IC50 values,inhibitory type,and the values of KI and KIS of isorhamnetin on mushroom tyrosinase diphenolase for the oxidation of L-DOPA. Inhibition type and inhibition constants（KI and KIS）are determined by Lineweaver- Burk method. The experiment results showed that isorhamnetin had obvious inhibitory effects on the activity of mushroom tyrosinase diphenolase. Isorhamnetin was the reversible inhibitor and competitive-uncompetitive mixed type inhibitor. The IC50 value of isorhamnetin on diphenolase activity was 25μmol/L. KI was 20.1 μmol/L and KIS was 108.6 mol/L. In a word,isorhamnetin had obvious inhibitory effects on the diphenolase activity of mushroom tyrosinase. These results support the use of isorhamnetin as the new drug candidate of whitening agent and as the food additive of preventing the browning of fruit and vegetable.

关 键 词：酪氨酸酶二酚酶 异鼠李素 抑制机理 

分 类 号：TQ464.8[化学工程—制药化工]