钒取代硅钨氧酸盐对酪氨酸酶的抑制作用  

Inhibition Effect of Vanadate-replaced Polyoxometalates on Mushroom Tyrosinase

作　　者：郑阿萍[1] 陈丙年[2] 陈发河[1] 王力[1] 

机构地区：[1]集美大学生物工程学院,厦门361021 [2]厦门大学附属中山医院演武分院,厦门361005

出　　处：《应用化学》2013年第2期165-170,共6页Chinese Journal of Applied Chemistry

基　　金：国家自然科学基金(20871054);福建省自然科学基金(JK2011027;2012J01045)资助项目

摘　　要：测定了自制的α-1,2,3-K6H[SiW9V3O40]、α-1,2-K6[SiW10V2O40]和α-K5[SiW11VO40](以下分别简写为α-SiW9V3、α-SiW10V2和α-SiW11V)钒取代多金属氧酸盐对蘑菇酪氨酸酶活性的抑制作用。结果表明,在pH=6.8的NaH2PO4-Na2HPO4缓冲溶液中,α-SiW9V3对酪氨酸酶有较强的抑制作用,表现为对酶稳态活力的抑制作用和对迟滞时间的延长作用,在DMSO溶液中,其IC50为0.6841 mmol/L,0.7 mmol/Lα-SiW9V3可使单酚酶的迟滞时间由235 s延长至650 s,增加了2.77倍。α-SiW9V3对酪氨酸酶单酚酶的抑制为可逆作用过程,抑制类型为混合型,其抑制常数KI、KIS分别为4.22和2.39 mmol/L。α-SiW10V2不溶于DMSO,故未研究其对酶的抑制作用,α-SiW11V对酪氨酸酶抑制作用很弱。Three kinds vanadate-replaced polyoxometalates, α-1,2,3-K6H[ SiW9V3O40], α-1,2-K6 [ SiW10V2O40 ] and α-K5 [ SiW]]VO40 ] （abbreviated as α-SiW9V3, α-SiW10V2, α-SiWllV） were synthesized and evaluated as tyrosinase inhibitors using the enzymological kinetic method. The results demonstrate that α-SiW9 V3 can inhibit tyrosinase strongly, as demonstrated by the inhibition of the steady-state activity of the enzyme and the lengthening of the lag time. The IC50 of α-SiW9V3 was estimated to be 0. 6841 mmol/L for the inhibition of mushroom tyrosinase. It resulted in the lag time of the monophenolase extension from 235 s to 650 s with 0.7 mmol/L of α-SiW9V3. The inhibition of α-SiW9V3 on monophenolase of mushroom tyrosinase proceeds as reversible process, and the inhibition of α-SiW9 V3 is a competitive-uncompetitive mixed-II type due to the oxidation of L-tyrosine. The inhibition constants （K1 and K1s ） are determined to be 4. 22 mmol/L and 2. 39 mmol/L, respectively. As for the α-SiW10V2, however, it is unsoluble in DMSO buffer, and its effect on the mushroom tyrosinase cannot be studied. While the inhibition ability of α-SiW11V on tyrosinase activity is rather weak.

关 键 词：多金属氧酸盐 酪氨酸酶 单酚酶活力 抑制作用 

分 类 号：O614.5[理学—无机化学]