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

Abstract
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.
AuthorsMiri Lee, Hyeonji Park, Sea Wha Jeon, JeongKyu Bang, Ka Young Chung, Dal Woong Choi, EunJoo Kim, Kyung-Min Lim
JournalArchives of dermatological research (Arch Dermatol Res) Vol. 307 Issue 3 Pg. 249-57 (Apr 2015) ISSN: 1432-069X [Electronic] Germany
PMID25753002 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Cosmetics
  • Melanins
  • Peptoids
  • Elastin
  • Arbutin
  • Monophenol Monooxygenase
Topics
  • Animals
  • Arbutin (administration & dosage)
  • Cosmetics
  • Elastin (chemistry)
  • Humans
  • Hyperpigmentation (drug therapy, pathology)
  • Melanins (metabolism)
  • Melanoma, Experimental
  • Mice
  • Monophenol Monooxygenase (metabolism)
  • Organ Culture Techniques
  • Peptoids (administration & dosage, chemical synthesis)
  • Protein Stability
  • Skin (drug effects, pathology)
  • Zebrafish

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