title: Novel inhibitory effect of N-(2-hydroxycyclohexyl)valiolamine on melanin production in a human skin model.
abstract: Hyper-pigmentation causes skin darkness and medical disorders, such as post-inflammatory melanoderma and melasma. Therefore, the development of anti-melanogenic agents is important for treating these conditions and for cosmetic production. In our previous paper, we demonstrated that the anti-diabetic drug voglibose, a valiolamine derivative, is a potent anti-melanogenic agent. In addition, we proposed an alternative screening strategy to identify valiolamine derivatives with high skin permeability that act as anti-melanogenic agents when applied topically. In this study, we synthesized several valiolamine derivatives with enhanced lipophilicity and examined their inhibitory effects in a human skin model. N-(2-hydroxycyclohexyl)valiolamine (HV) possesses a stronger inhibitory effect on melanin production than voglibose in a human skin model, suggesting that HV is a more potent anti-melanogenic agent for the skin.
authors.affiliation: AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do 446-729, Korea. bbh82429@amorepacific.com.
authors.forename: Bum-Ho
authors.initials: BH
authors.lastname: Bin
authors.affiliation: AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do 446-729, Korea. yhjoo@amorepacific.com.
authors.forename: Yung Hyup
authors.initials: YH
authors.lastname: Joo
authors.affiliation: Department of Dermatology, Dongguk University Ilsan Hospital, 814 Siksa-dong, Ilsandong-gu, Goyang-si, Gyenoggi-do 410-773, Korea. leeay@duih.org.
authors.forename: Ai-Young
authors.initials: AY
authors.lastname: Lee
authors.affiliation: AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do 446-729, Korea. ssshin@amorepacific.com.
authors.forename: Song Seok
authors.initials: SS
authors.lastname: Shin
authors.affiliation: AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do 446-729, Korea.
authors.forename: Eun-Gyung
authors.initials: EG
authors.lastname: Cho
authors.affiliation: AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do 446-729, Korea. trlee@amorepacific.com.
authors.forename: Tae Ryong
authors.initials: TR
authors.lastname: Lee
mesh_terms: D002478:Cells, Cultured; D003511:Cyclohexanols / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D007294:Inositol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008543:Melanins / Q000096:biosynthesis*; D008544:Melanocytes / Q000187:drug effects* / Q000378:metabolism; D014442:Monophenol Monooxygenase / Q000235:genetics / Q000378:metabolism; D050111:Imino Sugars
chemical_list: D003511:Cyclohexanols; D007294:Inositol; D008543:Melanins; D014442:Monophenol Monooxygenase; C000596540:N-(2-hydroxycyclohexyl)valiolamine; C043270:valiolamine; D050111:Imino Sugars; C102817:voglibose