R & D Center, AmorePacific Corporation, Giheung-gu, Yongin, Korea.
Arch Dermatol Res. 2011 Apr;303(3):153-9. doi: 10.1007/s00403-010-1079-7. Epub 2010 Sep 17.
To find novel depigmenting agents, a new synthetic compound, N-adamantyl-3,4-dihydroxybenzamide (NADB) was produced and the effects on melanogenesis were investigated. Our results showed that NADB reduced melanin synthesis in a dose-dependent manner in melan-a cells. Tyrosinase activity was also reduced by NADB treatment in melan-a cells. However, NADB did not inhibit tyrosinase activity directly in a cell-free system. Treatment of melan-a cells with NADB caused a marked decrease in protein and mRNA levels of tyrosinase along with tyrosinase-related protein 1 and dopachrome tautomerase. To determine whether NADB reduces skin pigmentation, the dorsal skin of brown guinea pigs was shaved and irradiated with UV for 3 weeks using a solar simulator. Then NADB (2 or 1% in propylene glycol:ethanol:water = 5:3:2) was applied topically twice daily for 4 weeks. Visual inspection and Fontana-Masson staining both demonstrated that NADB resulted in lower skin pigmentation and total epidermal melanin in comparison to vehicle-treated areas. These findings suggest that NADB is useful in the treatment of hyperpigmentation.
为了寻找新型的脱色剂，我们合成了一种新的化合物，N-金刚烷基-3,4-二羟基苯甲酰胺（NADB），并研究了其对黑色素生成的影响。结果表明，NADB 能够剂量依赖性地减少黑色素-a 细胞中的黑色素合成。NADB 处理还能降低黑色素-a 细胞中的酪氨酸酶活性。然而，NADB 在无细胞体系中不能直接抑制酪氨酸酶活性。用 NADB 处理黑色素-a 细胞会导致酪氨酸酶及其相关蛋白 1 和多巴色素互变异构酶的蛋白和 mRNA 水平明显下降。为了确定 NADB 是否能减少皮肤色素沉着，我们用太阳模拟器对棕色豚鼠的背部皮肤进行了剃毛和 3 周的紫外线照射。然后用 NADB（2%或 1%，在丙二醇：乙醇：水 = 5:3:2 中）每天两次局部涂抹 4 周。肉眼观察和 Fontana-Masson 染色均表明，与载体处理区域相比，NADB 导致皮肤色素沉着和表皮黑色素总量降低。这些发现表明 NADB 可用于治疗色素沉着过度。
