title: Melanogenesis inhibition of β-lapachone, a natural product from Tabebuia avellanedae, with effective in vivo lightening potency.
abstract: β-Lapachone is an ortho naphthoquinone obtained from the bark of the lapacho tree (Tabebuia avellanedae), which has been used medicinally for centuries. The purpose of this study was to investigate the effects of β-lapachone on inhibitory mechanism of melanogenesis. β-Lapachone inhibited melanin synthesis and tyrosinase activity at 0.8 μM in melan-a cells. Also, β-lapachone reduced the expression of tyrosinase and tyrosinase-related protein-1 at transcriptional and translational levels. The decreased expression of tyrosinase and tyrosinase-related protein-1 might result from the reduced microphthalmia-associated transcription factor (MITF) level which regulates major melanogenic proteins. The reduced level of MITF was associated with delayed ERK activation by β-lapachone. Furthermore, β-lapachone reduced melanogenesis in the human 3D skin tissue culture; besides, it dramatically inhibited body pigmentation of zebrafish and decreased melanin content and tyrosinase activity. These results show that β-lapachone may be useful as a potential depigmentation agent for various hyperpigmentation disorders.
authors: College of Herbal Bio-industry, Daegu Haany University, Gyeongsan, 712-715, Korea.
authors: Jin Hee
authors: JH
authors: Kim
authors: Se Mi
authors: SM
authors: Lee
authors: Cheol Hwan
authors: CH
authors: Myung
authors: Kyung Rhim
authors: KR
authors: Lee
authors: Seung Min
authors: SM
authors: Hyun
authors: Ji Eun
authors: JE
authors: Lee
authors: Young Sun
authors: YS
authors: Park
authors: Se Rim
authors: SR
authors: Jeon
authors: Jong Il
authors: JI
authors: Park
authors: Sung Eun
authors: SE
authors: Chang
authors: Jae Sung
authors: JS
authors: Hwang
mesh_terms: D000818:Animals; D002454:Cell Differentiation / Q000187:drug effects; D002461:Cell Line, Transformed; D048049:Extracellular Signal-Regulated MAP Kinases / Q000378:metabolism; D006801:Humans; D008543:Melanins / Q000378:metabolism; D008544:Melanocytes / Q000187:drug effects* / Q000502:physiology; D051379:Mice; D008810:Mice, Inbred C57BL; D051739:Microphthalmia-Associated Transcription Factor / Q000235:genetics / Q000378:metabolism; D014442:Monophenol Monooxygenase / Q000235:genetics / Q000378:metabolism; D009285:Naphthoquinones / Q000494:pharmacology*; D009924:Organ Culture Techniques; D010088:Oxidoreductases / Q000235:genetics / Q000378:metabolism; D008517:Phytotherapy / Q000379:methods*; D010858:Pigmentation / Q000187:drug effects; D024301:Plant Bark; D012867:Skin / Q000187:drug effects* / Q000473:pathology; D029663:Tabebuia / Q000276:immunology*; D015027:Zebrafish
chemical_list: D008543:Melanins; D051739:Microphthalmia-Associated Transcription Factor; D009285:Naphthoquinones; C014638:beta-lapachone; D010088:Oxidoreductases; C064056:tyrosinase-related protein-1; D014442:Monophenol Monooxygenase; D048049:Extracellular Signal-Regulated MAP Kinases