Graduate School of East-West Medical Science, Kyung Hee University, Yongin-si, Gyeonggi-do, Republic of Korea.
J Pharm Pharmacol. 2010 Mar;62(3):352-9. doi: 10.1211/jpp.62.03.0010.
Increased production and accumulation of melanin leads to many hyperpigmentation disorders such as melasma, freckles and geriatric pigment spots. Thus, there is a need for the development of depigmenting agents. Based on our previous reports, selenium derivatives as anti-melanogenic lead compounds could be very important. The aim of this study was to investigate the depigmenting effect of novel selenium-containing compounds.
The inhibitory effects of 5-chloroacetyl-2-piperidino-1,3-selenazole (CS1), a novel selenium-containing compound, on melanogenesis were investigated in B16F10 melanoma cells and cultured brownish guinea pig skin tissue with alpha-melanocyte-stimulating hormone stimulation.
We found that CS1 inhibited melanin production in B16F10 cells by suppressing tyrosinase activity and its protein expression. In addition, Western blotting analysis revealed that CS1 suppressed the expression of tyrosinase-related protein (TRP)-1 and TRP-2. Therefore, the depigmenting effect of CS1 might have been due to inhibition of tyrosinase activity and expression of melanogenic enzymes. Furthermore, CS1 had inhibitory effects on melanin biosynthesis of primary cultured skin of brownish guinea pig.
The results suggested that CS1 could be a useful candidate for the treatment of skin hyperpigmentation.
黑色素的过量产生和积累会导致多种色素沉着紊乱，如黄褐斑、雀斑和老年色素斑。因此，需要开发脱色剂。基于我们之前的报告，硒衍生物作为抗黑色素生成的先导化合物可能非常重要。本研究旨在研究新型含硒化合物的脱色作用。
用 5-氯乙酰基-2-哌啶基-1,3-硒唑（CS1），一种新型含硒化合物，在α-黑色素细胞刺激素刺激下，对 B16F10 黑色素瘤细胞和培养的棕色豚鼠皮肤组织中的黑色素生成进行抑制作用研究。
我们发现 CS1 通过抑制酪氨酸酶活性及其蛋白表达来抑制 B16F10 细胞中的黑色素生成。此外，Western 印迹分析显示 CS1 抑制了酪氨酸酶相关蛋白（TRP）-1 和 TRP-2 的表达。因此，CS1 的脱色作用可能是由于抑制了酪氨酸酶活性和黑色素生成酶的表达。此外，CS1 对棕色豚鼠原代培养皮肤的黑色素生物合成也有抑制作用。
结果表明，CS1 可能是治疗皮肤色素沉着过度的一种有用的候选药物。
