高等学校化学学报 ›› 2014, Vol. 35 ›› Issue (3): 476-481.doi: 10.7503/cjcu20131010

• 研究论文: 无机化学 • 上一篇    下一篇

两种多酸型酪氨酸酶抑制剂的性能研究

郑阿萍1, 王芳2, 邢蕊1, 蒋爱华2, 王力1()   

  1. 1. 集美大学生物工程学院, 厦门 361021
    2. 泉州师范学院化学与生命科学学院, 泉州 362002
  • 收稿日期:2013-10-15 出版日期:2014-03-10 发布日期:2019-08-01
  • 作者简介:联系人简介: 王 力, 女, 博士, 教授, 主要从事多酸化学和酶学研究. E-mail: wanglimerry@jmu.edu.cn
  • 基金资助:
    国家自然科学基金(批准号: 20871054, 21371072)资助

Functionality Research of Keggin-type Polyoxotungstate as Potent Mushroom Tyrosinase Inhibitors

ZHENG Aping1, WANG Fang2, XING Rui1, JIANG Aihua2, WANG Li1,*()   

  1. 1. College of Bioengineering, Jimei University, Xiamen 361021, China
    2. College of Chemistry and Life Science, Quanzhou Normal College, Quanzhou 362000, China
  • Received:2013-10-15 Online:2014-03-10 Published:2019-08-01
  • Contact: WANG Li E-mail:wanglimerry@jmu.edu.cn
  • Supported by:
    † Supported by the National Natural Science Foundation of China(Nos.20871054, 21371072)

摘要:

以H3PW12O40和H4SiW12O40(简写为PW12和SiW12)为效应物, 测定其对酪氨酸酶活力的抑制作用. 通过非变性聚丙烯凝胶(Native-PAGE)电泳确定酪氨酸酶是多家族基因编码, 其分子量为3×104~3.4×104, 4.2×104~4.6×104, 6.4×104~6.8×104, 且均具有活性, 测定PW12和SiW12对酪氨酸酶的抑制效果, 并结合酶动力学法研究其抑制机理. 结果表明, 当PW12和SiW12浓度分别达到13和25 mmol/L时, 酪氨酸酶的活力完全被抑制, 即PW12和SiW12对酪氨酸酶二酚酶具有不同程度的抑制效果. 当所加酶量为0.0173 mg/mL时, PW12和SiW12对酪氨酸酶二酚酶活力的半抑制率 (IC50)分别为1.57和2.31 mmol/L, 它们对酪氨酸酶二酚酶的抑制均为可逆过程. 其中, PW12对二酚酶的抑制类型为混合型, 其KIKIS分别为0.34和0.43 mmol/L, SiW12对二酚酶的抑制类型表现为竞争型, 其KI为0.59 mmol/L. 综合考虑IC50值和抑制常数等参数, PW12对酪氨酸酶二酚酶的抑制能力优于SiW12.

关键词: 多金属氧酸盐, 酪氨酸酶, 非变性聚丙烯凝胶电泳, 抑制作用

Abstract:

H3PW12O40 and H4SiW12O40(abbreviated as PW12 and SiW12) were taken as inhibitors and their inhibitory effects and mechanisms on mushroom tyrosinase were evaluated by Native polyacrylamide gel electrophoresis(PAGE) electrophoresis method and kinetic enzymatic method. The Native-PAGE electrophoresis results show that tyrosinase are encoded by a multigene family, their molecular weight are mainly 3×104—3.4×104, 4.2×104—4.6×104 and 6.4×104—6.8×104, which were all active.The inhibitory effects of Kiggin-type polyoxotungstates, H3PW12O40 and H4SiW12O40 on mushroom tyrosinase were evaluated, and then the inhibitory mechanisms were further studied combined with the kinetic enzymatic method. The results indicated that the enzyme was inactive when the concentration of PW12 and SiW12 was 13 and 25 mmol/L, respectively. More-over, the kinetic enzymatic method suggested that both PW12 and SiW12 exhibited potent inhibitory activities with IC50 value of 1.57 and 2.31 mmol/L, respectively. PW12 was found to be a mixed-type inhibitor with KI=0.34 mmol/L and KIS=0.43 mmol/L, while SiW12 was suggested to be competitive inhibitor of tyrosinase with KI of 0.59 mmol/L. Based on a comprehensive consideration of IC50 and inhibitory constants, PW12 was more effective against mushroom tyrosinase than SiW12.

Key words: Polyoxometalate, Mushroom tyrosinase, Native polyacrylamide gel electrophoresis(PAGE), Inhibition effect

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