Department of Biotechnology, Shivaji University , Kolhapur 416004, India.
J Agric Food Chem. 2014 Nov 26;62(47):11594-601. doi: 10.1021/jf5039585. Epub 2014 Nov 17.
Tyrosinase inhibitors have been used as whitening or antihyperpigment agents because of their ability to suppress dermal-melanin production. In the present study, screening and kinetic evaluation of various small molecules were performed on mushroom tyrosinase (MT) using surface plasmon resonance. The binding constant KD (M) values obtained for tannic acid, phloroglucinol, saffron, catechol, and pyrogallol are 1.213 × 10(-4), 7.136 × 10(-5), 3.111 × 10(-5), 1.557 × 10(-5), and 7.981 × 10(-6) M, respectively. Pyrogallol has been found to display high affinity for MT, whereas catechol, saffron, and phloroglucinol have been found to bind with low affinity. MT shows considerable changes in the secondary structure in the presence of inhibitors. The study reveals the Biacore/SPR sensor's ability in the rapid identification and characterization of inhibitors for MT. The methodology described here can be used to rapidly screen and optimize various lead compounds for other enzymes and elucidate structure function inter-relationships between various enzymes.
由于能够抑制皮肤黑色素的产生，酪氨酸酶抑制剂已被用作美白或抗色素沉着剂。本研究采用表面等离子体共振法对蘑菇酪氨酸酶（MT）进行了各种小分子的筛选和动力学评价。单宁酸、间苯三酚、藏红花、儿茶酚和焦儿茶酚的结合常数 KD（M）值分别为 1.213×10(-4)、7.136×10(-5)、3.111×10(-5)、1.557×10(-5)和 7.981×10(-6)M。结果表明，焦儿茶酚对 MT 具有高亲和力，而儿茶酚、藏红花和间苯三酚与 MT 的亲和力较低。MT 在抑制剂存在下其二级结构发生了明显的变化。该研究揭示了 Biacore/SPR 传感器在快速鉴定和表征 MT 抑制剂方面的能力。这里描述的方法可用于快速筛选和优化其他酶的各种先导化合物，并阐明各种酶之间的结构功能关系。
