Novel anti-melanogenic hexapeptoids, PAL-10 and PAL-12.
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.
College of Pharmacy, EwhaWomans University, 52 Ewhayeodae-gil, Seodaemun-gu, Seoul, 120-808, Korea.
Miri
M
Lee
Hyeonji
H
Park
Sea Wha
SW
Jeon
JeongKyu
J
Bang
Ka Young
KY
Chung
Dal Woong
DW
Choi
EunJoo
E
Kim
Kyung-Min
KM
Lim
D000818:Animals; D001104:Arbutin / Q000008:administration & dosage; D003358:Cosmetics; D004549:Elastin / Q000737:chemistry; D006801:Humans; D017495:Hyperpigmentation / Q000188:drug therapy* / Q000473:pathology; D008543:Melanins / Q000378:metabolism*; D008546:Melanoma, Experimental; D051379:Mice; D014442:Monophenol Monooxygenase / Q000378:metabolism*; D009924:Organ Culture Techniques; D034444:Peptoids / Q000008:administration & dosage* / Q000138:chemical synthesis; D055550:Protein Stability; D012867:Skin / Q000187:drug effects* / Q000473:pathology; D015027:Zebrafish
D003358:Cosmetics; D008543:Melanins; D034444:Peptoids; D004549:Elastin; D001104:Arbutin; D014442:Monophenol Monooxygenase