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Anti-Melanogenic Activity of Gagunin D, a Highly Oxygenated Diterpenoid from the Marine Sponge Phorbas sp., via Modulating Tyrosinase Expression and Degradation

Tyrosinase is the rate-limiting enzyme critical for melanin synthesis and controls pigmentation in the skin. The inhibition of tyrosinase is currently the most common approach for the development of skin-whitening cosmetics. Gagunin D (GD), a highly oxygenated diterpenoid isolated from the marine sp...

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Autores principales: Lee, Ho Yeon, Jang, Eun Jeong, Bae, Song Yi, Jeon, Ju-eun, Park, Hyen Joo, Shin, Jongheon, Lee, Sang Kook
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5128755/
https://www.ncbi.nlm.nih.gov/pubmed/27869664
http://dx.doi.org/10.3390/md14110212
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author Lee, Ho Yeon
Jang, Eun Jeong
Bae, Song Yi
Jeon, Ju-eun
Park, Hyen Joo
Shin, Jongheon
Lee, Sang Kook
author_facet Lee, Ho Yeon
Jang, Eun Jeong
Bae, Song Yi
Jeon, Ju-eun
Park, Hyen Joo
Shin, Jongheon
Lee, Sang Kook
author_sort Lee, Ho Yeon
collection PubMed
description Tyrosinase is the rate-limiting enzyme critical for melanin synthesis and controls pigmentation in the skin. The inhibition of tyrosinase is currently the most common approach for the development of skin-whitening cosmetics. Gagunin D (GD), a highly oxygenated diterpenoid isolated from the marine sponge Phorbas sp., has exhibited cytotoxicity toward human leukemia cells. However, the effect of GD on normal cells and the molecular mechanisms remain to be elucidated. In the present study, we identified for the first time the anti-melanogenic activity of GD and its precise underlying mechanisms in mouse melan-a cells. GD significantly inhibited melanin synthesis in the melan-a cells and a reconstructed human skin model. Further analysis revealed that GD suppressed the expression of tyrosinase and increased the rate of tyrosinase degradation. GD also inhibited tyrosinase enzymatic activity. In addition, GD effectively suppressed the expression of proteins associated with melanosome transfer. These findings suggest that GD is a potential candidate for cosmetic formulations due to its multi-functional properties.
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spelling pubmed-51287552016-12-06 Anti-Melanogenic Activity of Gagunin D, a Highly Oxygenated Diterpenoid from the Marine Sponge Phorbas sp., via Modulating Tyrosinase Expression and Degradation Lee, Ho Yeon Jang, Eun Jeong Bae, Song Yi Jeon, Ju-eun Park, Hyen Joo Shin, Jongheon Lee, Sang Kook Mar Drugs Article Tyrosinase is the rate-limiting enzyme critical for melanin synthesis and controls pigmentation in the skin. The inhibition of tyrosinase is currently the most common approach for the development of skin-whitening cosmetics. Gagunin D (GD), a highly oxygenated diterpenoid isolated from the marine sponge Phorbas sp., has exhibited cytotoxicity toward human leukemia cells. However, the effect of GD on normal cells and the molecular mechanisms remain to be elucidated. In the present study, we identified for the first time the anti-melanogenic activity of GD and its precise underlying mechanisms in mouse melan-a cells. GD significantly inhibited melanin synthesis in the melan-a cells and a reconstructed human skin model. Further analysis revealed that GD suppressed the expression of tyrosinase and increased the rate of tyrosinase degradation. GD also inhibited tyrosinase enzymatic activity. In addition, GD effectively suppressed the expression of proteins associated with melanosome transfer. These findings suggest that GD is a potential candidate for cosmetic formulations due to its multi-functional properties. MDPI 2016-11-17 /pmc/articles/PMC5128755/ /pubmed/27869664 http://dx.doi.org/10.3390/md14110212 Text en © 2016 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Lee, Ho Yeon
Jang, Eun Jeong
Bae, Song Yi
Jeon, Ju-eun
Park, Hyen Joo
Shin, Jongheon
Lee, Sang Kook
Anti-Melanogenic Activity of Gagunin D, a Highly Oxygenated Diterpenoid from the Marine Sponge Phorbas sp., via Modulating Tyrosinase Expression and Degradation
title Anti-Melanogenic Activity of Gagunin D, a Highly Oxygenated Diterpenoid from the Marine Sponge Phorbas sp., via Modulating Tyrosinase Expression and Degradation
title_full Anti-Melanogenic Activity of Gagunin D, a Highly Oxygenated Diterpenoid from the Marine Sponge Phorbas sp., via Modulating Tyrosinase Expression and Degradation
title_fullStr Anti-Melanogenic Activity of Gagunin D, a Highly Oxygenated Diterpenoid from the Marine Sponge Phorbas sp., via Modulating Tyrosinase Expression and Degradation
title_full_unstemmed Anti-Melanogenic Activity of Gagunin D, a Highly Oxygenated Diterpenoid from the Marine Sponge Phorbas sp., via Modulating Tyrosinase Expression and Degradation
title_short Anti-Melanogenic Activity of Gagunin D, a Highly Oxygenated Diterpenoid from the Marine Sponge Phorbas sp., via Modulating Tyrosinase Expression and Degradation
title_sort anti-melanogenic activity of gagunin d, a highly oxygenated diterpenoid from the marine sponge phorbas sp., via modulating tyrosinase expression and degradation
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5128755/
https://www.ncbi.nlm.nih.gov/pubmed/27869664
http://dx.doi.org/10.3390/md14110212
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