title: N-Nicotinoyl tyramine, a novel niacinamide derivative, inhibits melanogenesis by suppressing MITF gene expression.
abstract: We synthesized and investigated the inhibitory effects of a novel niacinamide derivative, N-nicotinoyltyramine (NNT) on melanogenesis. NNT inhibited melanin production in B16F10 murine melanoma cells stimulated with α-melanocyte stimulating hormone (α-MSH), in human melanocyte and in three-dimensional cultured human skin model. NNT did not affect the catalytic activity of tyrosinase, but acted as an inhibitor of microphthalmia-associated transcription factor (MITF) and tyrosinase expressions in B16F10 cells. These findings suggest that the hypopigmentary effect of NNT results from the down-regulation of MITF and subsequently of tyrosinase, although NNT did not directly inhibit tyrosinase activity. In addition, safety of NNT was verified through performing neural stem cell morphology assay and Human repeated insult patch test as whitening agent. Our findings indicate that NNT may be a potential and non-skin irritant whitening agent for use in cosmetics and in the medical treatment of pigmentary disorders.
authors.affiliation: Skin & Bio Research, Ellead Co., Ltd., Gyeonggi 463-824, Republic of Korea.
authors.forename: Bora
authors.initials: B
authors.lastname: Kim
authors.affiliation: Translational Research Center for Protein Function Control, College of Life Science and Biotechnology, Yonsei University, Seoul 120-752, Republic of Korea.
authors.forename: Soung-Hoon
authors.initials: SH
authors.lastname: Lee
authors.affiliation: Translational Research Center for Protein Function Control, College of Life Science and Biotechnology, Yonsei University, Seoul 120-752, Republic of Korea.
authors.forename: Kang-Yell
authors.initials: KY
authors.lastname: Choi
authors.affiliation: Department of Food Science and Technology, Jungwon University, 85, Munmu-ro, Geosan-eup, Geosan-gun, Chungbuk 367-805, Republic of Korea. Electronic address: hyun1006@jwu.ac.kr.
authors.forename: Hyun-Soo
authors.initials: HS
authors.lastname: Kim
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D015536:Down-Regulation / Q000187:drug effects*; D006801:Humans; D008543:Melanins / Q000096:biosynthesis*; D008544:Melanocytes / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D051739:Microphthalmia-Associated Transcription Factor / Q000235:genetics*; D014442:Monophenol Monooxygenase / Q000235:genetics; D058953:Neural Stem Cells / Q000187:drug effects; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000633:toxicity; D009539:Nicotinic Acids / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D062327:Skin Lightening Preparations / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D014439:Tyramine / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000633:toxicity; D000521:alpha-MSH / Q000494:pharmacology
chemical_list: D008543:Melanins; D051739:Microphthalmia-Associated Transcription Factor; D009539:Nicotinic Acids; D062327:Skin Lightening Preparations; D009536:Niacinamide; D000521:alpha-MSH; D014442:Monophenol Monooxygenase; C000609187:N-nicotinoyl tyramine; D014439:Tyramine
keywords: Melanogenesis; Microphthalmia-associated transcription factor (MITF); N-Nicotinoyl tyramine; Pigmentation