CAJ | 학술논문

研究表明,含三氟甲基1,2,3-三氮唑衍生物(TF-TZ)对蘑菇酪氨酸酶具有很强的抑制性:不仅抑制单酚酶活性,而且对二酚酶活性也是可逆性抑制,其半抑制浓度IC_(50)分别为30.4和34.5 μmol·L~(-1),并且单酚酶延滞时间随着TF-TZ浓度增加而延长.TF-TZ对二酚酶的抑制为抛物线型竞争性抑制,表明一分子的酶可以和两分子的TF-TZ相结合,从而形成两种酶-抑制剂复合物:EI和EI_2,其抑制常数分别为76.9和9.71 μmol·L~(-1).紫外-可见光谱表明,TF-TZ和酶相互作用后产成特征的"肩峰",说明TF-TZ能够作用于酶的活性中心.
연구표명,함삼불갑기1,2,3-삼담서연생물(TF-TZ)대마고락안산매구유흔강적억제성:불부억제단분매활성,이차대이분매활성야시가역성억제,기반억제농도IC_(50)분별위30.4화34.5 μmol·L~(-1),병차단분매연체시간수착TF-TZ농도증가이연장.TF-TZ대이분매적억제위포물선형경쟁성억제,표명일분자적매가이화량분자적TF-TZ상결합,종이형성량충매-억제제복합물:EI화EI_2,기억제상수분별위76.9화9.71 μmol·L~(-1).자외-가견광보표명,TF-TZ화매상호작용후산성특정적"견봉",설명TF-TZ능구작용우매적활성중심.
In this study,we demonstrate that the trifluoromethyl-containing 1,2,3-triazole derivative (TF-TZ)inhibits mushroom tyrosinase.TF-TZ could inhibit the monophenolase and diphenolase activities and the inhibition is reversible.IC_(50) values of 30.4 and 34.5 μmol·L~(-1)were estimated for the monophenolase activity and the diphenolase activity,respectively.TF-TZ could extend the lag period of the monophenolase activity.Kinetic analysis showed that parabofic-competitive inhibition of TF-TZ occurred on diphenolase.We proposed that two TF-TZ molecules combined with free tyrosinase to form enzyme-inhibitor complexes(EI and EI_2),and the inhibition constants(K_(i1) for EI and K_(i2) for EI_2)were 76.9 and 9.71 μmol·L~(-1).respectively.Moreover,the UV-Visible spectrum of a mixture of tymsinase and TF-TZ exhibited a characteristic shoulder peak that could be assigned to chelation of TF-TZ to the active site.