State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai 200237, PR China.
J Enzyme Inhib Med Chem. 2009 Oct;24(5):1154-60. doi: 10.1080/14756360802694252.
Tiliroside was found to inhibit both monophenolase and diphenolase activity of mushroom tyrosinase. The lag time of tyrosine oxidation catalyzed by mushroom tyrosinase was obviously lengthened; 0.337 mM of tiliroside resulted in the lag time extension from 46.7 s to 435.1 s. A kinetic analysis shown that tiliroside was a competitive inhibitor for monophenolase and diphenolase with K(i) values of 0.052 mM and 0.26 mM, respectively. Furthermore, tiliroside showed 34.5% (p < 0.05) inhibition of intracellular tyrosinase activity and 54.1% (p < 0.05) inhibition of melanin production with low cytotoxicity on B16 mouse melanoma cells at 0.168 mM. In contrast, arbutin displayed 9.1% inhibition of cellular tyrosinase activity and 29.5% inhibition of melanin production at the same concentration. These results suggested that tiliroside was a potent tyrosinase inhibitor and might be used as a skin-whitening agent and pigmentation medicine.
獐芽菜苷被发现能同时抑制蘑菇酪氨酸酶的单酚酶和二酚酶活性。蘑菇酪氨酸酶催化的酪氨酸氧化的延滞时间明显延长；0.337 mM 的獐芽菜苷使延滞时间从 46.7 s 延长至 435.1 s。动力学分析表明，獐芽菜苷对单酚酶和二酚酶分别为竞争性抑制剂，其 K(i)值分别为 0.052 mM 和 0.26 mM。此外，獐芽菜苷在 0.168 mM 时对 B16 小鼠黑色素瘤细胞的细胞内酪氨酸酶活性有 34.5%（p < 0.05）的抑制作用，对黑色素生成有 54.1%（p < 0.05）的抑制作用，同时对细胞的毒性较低。相比之下，熊果苷在相同浓度下对细胞酪氨酸酶活性的抑制率为 9.1%，对黑色素生成的抑制率为 29.5%。这些结果表明，獐芽菜苷是一种有效的酪氨酸酶抑制剂，可作为皮肤增白剂和色素沉着药物。
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