Lee Miri, Park Hyeonji, Jeon Sea Wha, Bang JeongKyu, Chung Ka Young, Choi Dal Woong, Kim EunJoo, Lim Kyung-Min
College of Pharmacy, EwhaWomans University, 52 Ewhayeodae-gil, Seodaemun-gu, Seoul, 120-808, Korea.
Arch Dermatol Res. 2015 Apr;307(3):249-57. doi: 10.1007/s00403-015-1555-1. Epub 2015 Mar 10.
Diverse compound sources are being explored for de-pigmentation activities to develop novel therapeutic agents or functional cosmetic ingredients for hyper-pigmentation disorders. Peptoids are a class of peptidomimetics whose side chains are appended to the nitrogen atom of the peptide backbone, instead of α-carbon. Peptoids are more durable against proteolysis and are being actively investigated in drug discovery, but rarely studied as cosmetic ingredients. Here, we demonstrated that new hexa-peptoids, PAL-10 and PAL-12, can inhibit melanogenesis in B16F10 melanoma cells, a 3D pigmented human skin model (Neoderm(®)-ME, Tegoscience Co) and zebrafish. Anti-melanogenic effects of PAL-10 or PAL-12 as compared with arbutin, a positive control in B16F10 cells, Neoderm(®)-ME and zebrafish were statistically significant and concentration-dependent anti-melanogenic effects were manifested as determined by image, histology, and melanin contents. Anti-melanogenic effects of PAL-10 appeared to be from enzymatic inhibition of tyrosinase while mRNA expression of melanogenic enzymes was not affected. In conclusion, we demonstrated that PAL-10 and PAL-12 can be used as a new cosmetic ingredient with strong brightening efficacies.
人们正在探索多种化合物来源的美白活性，以开发用于色素沉着紊乱的新型治疗剂或功能性化妆品成分。类肽是一类肽模拟物，其侧链连接在肽主链的氮原子上，而不是α-碳原子上。类肽对蛋白水解更具耐受性，目前正在药物研发中积极研究，但作为化妆品成分的研究很少。在此，我们证明了新型六肽类化合物PAL-10和PAL-12能够抑制B16F10黑色素瘤细胞、一种三维色素沉着人类皮肤模型（Neoderm®-ME，Tegoscience公司）和斑马鱼中的黑色素生成。与熊果苷（B16F10细胞、Neoderm®-ME和斑马鱼中的阳性对照）相比，PAL-10或PAL-12的抗黑色素生成作用具有统计学意义，并且通过图像、组织学和黑色素含量测定显示出浓度依赖性的抗黑色素生成作用。PAL-10的抗黑色素生成作用似乎源于对酪氨酸酶的酶抑制作用，而黑色素生成酶的mRNA表达未受影响。总之，我们证明了PAL-10和PAL-12可作为具有强大提亮功效的新型化妆品成分。
