Kim Kyuri, Leutou Alain S, Jeong Haein, Kim Dayoung, Seong Chi Nam, Nam Sang-Jip, Lim Kyung-Min
College of Pharmacy, Ewha Womans University, Seoul 03760, Korea.
Department of Chemistry and Nano Science, Global Top 5 Program, Ewha Womans University, Seoul 03760, Korea.
Mar Drugs. 2017 May 13;15(5):138. doi: 10.3390/md15050138.
Bioactivity-guided isolation of a crude extract from a culture broth of Bacillus sp. has led to the isolation of (-)-4-hydroxysattabacin (1). The inhibitory effect of (-)-4-hydroxysattabacin (1) was investigated on melanogenesis in the murine melanoma cell line, B16F10, and human melanoma cell line, MNT-1, as well as a pigmented 3D-human skin model. (-)-4-Hydroxysattabacin treatment decreased melanin contents in a dose-dependent manner in α-melanocyte stimulating hormone (α-MSH)-stimulated B16F10 cells. Quantitative real time PCR (qRT-PCR) demonstrated that treatment with (-)-4-hydroxysattabacin down-regulated several melanogenic genes, including tyrosinase, tyrosinase-related protein 1 (TRP-1), and tyrosinase-related protein 2 (TRP-2) while their enzymatic activities were unaffected. The anti-melanogenic effects of (-)-4-hydroxysattabacin were further demonstrated in a pigmented 3D human epidermal skin model, MelanodermTM, and manifested as whitening and regression of melanocyte activation in the tissue.
对芽孢杆菌属菌株培养液的粗提物进行生物活性导向分离，得到了（-）-4-羟基萨塔巴辛（1）。研究了（-）-4-羟基萨塔巴辛（1）对小鼠黑色素瘤细胞系B16F10、人黑色素瘤细胞系MNT-1以及一种有色素的三维人体皮肤模型中黑色素生成的抑制作用。（-）-4-羟基萨塔巴辛处理以剂量依赖的方式降低了α-黑素细胞刺激素（α-MSH）刺激的B16F10细胞中的黑色素含量。定量实时聚合酶链反应（qRT-PCR）表明，用（-）-4-羟基萨塔巴辛处理下调了几种黑色素生成基因，包括酪氨酸酶、酪氨酸酶相关蛋白1（TRP-1）和酪氨酸酶相关蛋白2（TRP-2），而它们的酶活性未受影响。（-）-4-羟基萨塔巴辛的抗黑色素生成作用在有色素的三维人体表皮皮肤模型MelanodermTM中得到进一步证实，并表现为组织中黑色素细胞活化的变白和消退。
