Novel anti-melanogenic hexapeptoids, PAL-10 and PAL-12

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• 作者：Miri Lee ; Hyeonji Park ; Sea Wha Jeon ; JeongKyu Bang…
• 关键词：Peptoid ; Melanogenesis ; Zebrafish ; 3D human skin models ; Tyrosinase
• 刊名：Archives of Dermatological Research
• 出版年：2015
• 出版时间：April 2015
• 年：2015
• 卷：307
• 期：3
• 页码：249-257
• 全文大小：1,716 KB
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• 刊物类别：Medicine
• 刊物主题：Medicine & Public Health
  Dermatology
  
• 出版者：Springer Berlin / Heidelberg
• ISSN：1432-069X

文摘

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.