Lin Yin-Shiou, Wu Wen-Chung, Lin Shyr-Yi, Hou Wen-Chi
Graduate Institute of Pharmacognosy, Taipei Medical University, Taipei, Taiwan.
Amino Acids. 2015 Mar;47(3):617-25. doi: 10.1007/s00726-014-1895-8. Epub 2014 Dec 16.
Among the eight amino acid hydroxamates tested, Glycine hydroxamate (GH) was the best inhibitor of mushroom tyrosinase (TYR). With L-tyrosine as substrate, the GH inhibition of the monophenolase activity of the mushroom TYR was noncompetitive. GH decreased not only TYR protein expression, but also melanin content, tyrosinase-related protein (TRP)-1, TRP-2, and microphthalmia-associated transcription factor (MITF) expression in B16F10 melanoma cells while in the presence of α-melanocyte-stimulating hormone (α-MSH). GH also significantly decreased the isobutylmethylxanthine (IBMX)-induced increase in melanin content, which was not prevented by the ERK inhibitor PD98059. These results suggest GH has the potential for use in cosmetic hypopigmentation.
在所测试的八种氨基酸异羟肟酸中，甘氨酸异羟肟酸（GH）是蘑菇酪氨酸酶（TYR）的最佳抑制剂。以L-酪氨酸为底物时，GH对蘑菇TYR单酚酶活性的抑制作用是非竞争性的。在α-黑素细胞刺激激素（α-MSH）存在的情况下，GH不仅降低了B16F10黑色素瘤细胞中TYR蛋白的表达，还降低了黑色素含量、酪氨酸酶相关蛋白（TRP）-1、TRP-2以及小眼畸形相关转录因子（MITF）的表达。GH还显著降低了异丁基甲基黄嘌呤（IBMX）诱导的黑色素含量增加，而ERK抑制剂PD98059并不能阻止这种增加。这些结果表明GH具有用于化妆品美白的潜力。
