Ortiz-Ruiz Carmen Vanessa, Berna Jose, Garcia-Molina Maria Del Mar, Tudela Jose, Tomas Virginia, Garcia-Canovas Francisco
GENZ: Grupo de Investigacion de Enzimologia, Departamento de Bioquimica y Biologia Molecular-A, Facultad de Biologia, Campus de Excelencia Internacional 'Mare Nostrum', Universidad de Murcia, E-30100, Espinardo, Murcia, Spain.
Grupo de Quimica Organica Sintetica, Departamento de Quimica Organica, Facultad de Quimica, Campus de Excelencia Internacional 'Mare Nostrum', Universidad de Murcia, E-30100, Espinardo, Murcia, Spain.
Bioorg Med Chem. 2015 Jul 1;23(13):3738-46. doi: 10.1016/j.bmc.2015.04.016. Epub 2015 Apr 10.
In recent years, the hydroxyalkylphenols p-hydroxybenzyl alcohol and tyrosol, and the compound phloretin and its derivate phloridzin have been described as inhibitors of the enzyme tyrosinase. When the monophenolase and the diphenolase activities of tyrosinase on its physiological substrates l-dopa and/or l-tyrosine are measured in the presence of these compounds, the rate of action of the enzyme decreases. These findings led to the identification of these compounds as inhibitors. However, these molecules show an unusual behavior as inhibitors of the enzyme indeed, in this study, we demonstrate that they are not true inhibitors but alternative substrates of the enzyme.
近年来,羟烷基酚对羟基苯甲醇和酪醇,以及化合物根皮素及其衍生物根皮苷已被描述为酪氨酸酶的抑制剂。当在这些化合物存在的情况下测量酪氨酸酶对其生理底物L-多巴和/或L-酪氨酸的单酚酶和二酚酶活性时,酶的作用速率会降低。这些发现导致将这些化合物鉴定为抑制剂。然而,这些分子作为该酶的抑制剂表现出一种不寻常的行为,实际上,在本研究中,我们证明它们不是真正的抑制剂,而是该酶的替代底物。