金属配合物增强曲酸-苯丙氨酸酰胺的细胞通透性。
Enhanced cell permeability of kojic acid-phenylalanine amide with metal complex.
机构信息
School of Chemical and Biological Engineering, Seoul National University, Seoul 151-744, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2010 Jan 15;20(2):738-41. doi: 10.1016/j.bmcl.2009.11.069. Epub 2009 Dec 3.
Kojic acid-phenylalanine amide (KA-F-NH(2)), which showed an excellent tyrosinase inhibitory activity, did not inhibit melanogenesis in melanocyte due to its low cell permeability. To enhance its cell permeability by increasing lipophilicity, we prepared metal coordination compounds of KA-F-NH(2) and characterized them by FT-IR and ICP analysis. The metal complex of KA-F-NH(2) inhibited mushroom tyrosinase activity as much as KA-F-NH(2) and reduced melanin contents in melanocyte efficiently.
曲酸-苯丙氨酸酰胺（KA-F-NH(2)）具有优异的酪氨酸酶抑制活性，但由于其低细胞通透性，在黑素细胞中不能抑制黑色素生成。为了通过增加亲脂性来提高其细胞通透性，我们制备了 KA-F-NH(2)的金属配位化合物，并通过傅里叶变换红外光谱（FT-IR）和电感耦合等离子体分析（ICP）对其进行了表征。KA-F-NH(2)的金属配合物与 KA-F-NH(2)一样抑制蘑菇酪氨酸酶活性，并有效地减少黑素细胞中的黑色素含量。
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