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Melanogenesis inhibition of β-lapachone, a natural product from Tabebuia avellanedae, with effective in vivo lightening potency

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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.

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Acknowledgments

This study was supported by a grant of the Korean Health Technology R&D Project, Ministry of Health and Welfare, Republic of Korea (Grant No: HN11C0045), and Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology (NRF-2013R1A1A2007330).

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Authors and Affiliations

  1. College of Herbal Bio-industry, Daegu Haany University, Gyeongsan, 712-715, Korea

    Jin Hee Kim

  2. Department of Genetic Engineering and Graduate School of Biotechnology, Kyung Hee University, Yongin, 446-701, Korea

    Se Mi Lee, Cheol Hwan Myung, Kyung Rhim Lee, Seung Min Hyun, Ji Eun Lee, Young Sun Park, Se Rim Jeon, Jong Il Park & Jae Sung Hwang

  3. Department of Dermatology and Research Institute of Dermatology, Asan Medical Center, University of Ulsan College of Medicine, Seoul, Korea

    Sung Eun Chang

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  1. Jin Hee Kim
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Correspondence to Jae Sung Hwang.

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Kim, J.H., Lee, S.M., Myung, C.H. et al. Melanogenesis inhibition of β-lapachone, a natural product from Tabebuia avellanedae, with effective in vivo lightening potency. Arch Dermatol Res 307, 229–238 (2015). https://doi.org/10.1007/s00403-015-1543-5

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  • DOI: https://doi.org/10.1007/s00403-015-1543-5

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