Inhibitory effect of 5-iodotubercidin on pigmentation.

Abstract

Melanin pigments are the primary contributors for the skin color. They are produced in melanocytes and then transferred to keratinocytes, eventually giving various colors on skin surface. Although many depigmenting and/or skin-lightening agents have been developed, there is still a growing demand on materials for reducing pigmentation. We attempted to find materials for depigmentation and/or skin-lightening using the small molecule compounds commercially available, and found that 5-iodotubercidin had inhibitory potential on pigmentation. When HM3KO melanoma cells were treated with 5-iodotubercidin, pigmentation was dramatically reduced. The 5-iodotubercidin decreased the protein level for pigmentation-related molecules such as MITF, tyrosinase, and TRP1. In addition, 5-iodotubercidin decreased the phosphorylation of CREB, while increased the phosphorylation of AKT and ERK. These data suggest that 5-iodotubercidin inhibits melanogenesis via the regulation of intracellular signaling related with pigmentation. Finally, 5-iodotubercidin markedly inhibited the melanogenesis of zebrafish embryos, an in vivo evaluation model for pigmentation. Together, these data suggest that 5-iodotubercidin can be developed as a depigmenting and/or skin-lightening agent.

• Authors: Kyung-Il Kim, Hae Bong Jeong, Hyunju Ro, Jeung-Hoon Lee, Chang Deok Kim, Tae-Jin Yoon
• Journal: Biochemical and biophysical research communications (Biochem Biophys Res Commun) Vol. 490 Issue 4 Pg. 1282-1286 (09 02 2017) ISSN: 1090-2104 [Electronic] United States
• PMID: 28684314 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2017 Elsevier Inc. All rights reserved.

Chemical References

• CREB1 protein, human
• Cyclic AMP Response Element-Binding Protein
• Enzyme Inhibitors
• MITF protein, human
• Microphthalmia-Associated Transcription Factor
• Skin Lightening Preparations
• 5-iodotubercidin
• Monophenol Monooxygenase
• Proto-Oncogene Proteins c-akt
• MAPK1 protein, human
• Mitogen-Activated Protein Kinase 1
• Mitogen-Activated Protein Kinase 3
• PRSS1 protein, human
• Trypsin
• Tubercidin

Topics

• Animals
• Cell Line, Tumor
• Cyclic AMP Response Element-Binding Protein (antagonists & inhibitors, genetics, metabolism)
• Embryo, Nonmammalian (drug effects)
• Enzyme Inhibitors (pharmacology)
• Gene Expression Regulation
• Humans
• Melanocytes (cytology, drug effects, metabolism)
• Microphthalmia-Associated Transcription Factor (antagonists & inhibitors, genetics, metabolism)
• Mitogen-Activated Protein Kinase 1 (genetics, metabolism)
• Mitogen-Activated Protein Kinase 3 (genetics, metabolism)
• Monophenol Monooxygenase (antagonists & inhibitors, genetics, metabolism)
• Phosphorylation (drug effects)
• Pigmentation (drug effects, genetics)
• Proto-Oncogene Proteins c-akt (agonists, genetics, metabolism)
• Signal Transduction
• Skin (drug effects, metabolism)
• Skin Lightening Preparations (pharmacology)
• Trypsin (genetics, metabolism)
• Tubercidin (analogs & derivatives, pharmacology)
• Zebrafish