The Glutathione Derivative, GSH Monoethyl Ester, May Effectively Whiten Skin but GSH Does Not
by
Bo Young Chung 1, So Ra Choi 2, Ik Jun Moon 2
, Chun Wook Park 1, Young-Hoon Kim 3,*,† and Sung Eun Chang 2,*,†
Bo Young Chung 1, So Ra Choi 2, Ik Jun Moon 2, Chun Wook Park 1, Young-Hoon Kim 3,*,† and Sung Eun Chang 2,*,†
1
Department of Dermatology, College of Medicine, Hallym University Kangnam Sacred Heart Hospital, Seoul 07441, Korea
2
Department of Dermatology, Asan Medical Center, University of Ulsan College of Medicine, 88 Olympic-ro 43-gil, Songpa-gu, Seoul 05505, Korea
3
Department of Pharmacology, University of Ulsan College of Medicine, 88 Olympic-ro 43-gil, Songpa-gu, Seoul 05505, Korea
*
Authors to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Academic Editor: Terrence Piva
Int. J. Mol. Sci. 2016, 17(5), 629; https://doi.org/10.3390/ijms17050629
Received: 14 March 2016 / Revised: 18 April 2016 / Accepted: 21 April 2016 / Published: 27 April 2016
(This article belongs to the Section Bioactives and Nutraceuticals)
Glutathione in its reduced form (GSH) is an antioxidant and also is involved in pheomelanin formation. Thus, it has been long believed that GSH has a skin whitening effect. However, its actual or direct effect is unproven. We evaluated the anti-melanogenic effects of GSH and its derivatives in vitro. We examined change of melanogenesis and its related proteins by GSH itself and its derivatives, including GSH monoethyl ester (GSH-MEE), GSH diethyl ester (GSH-DEE) and GSH monoisopropyl ester (GSH-MIPE) in Melan-A cells, Mel-Ab cells, and B16F10 cells. GSH and GSH-MEE did not display cytotoxic activity, but GSH-MIPE and GSH-DEE did. Intriguingly, GSH itself had no inhibitory effect on melanin production or intracellular tyrosinase activity. Rather, it was GSH-MEE and GSH-MIPE that profoundly reduced the amount of melanin and intracellular tyrosinase activity. Thus, GSH-MEE was selected as a suitable candidate skin-whitening agent and it did not alter melanogenesis-associated proteins such as microphthalmia-associated transcription factor (MITF), tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2, but it did increase the amount of suggested pheomelanin and suggested pheomelanin/eumelanin ratio. GSH-MEE was effective for anti-melanogenesis, whereas GSH itself was not. GSH-MEE could be developed as a safe and efficient agent for the treatment of hyperpigmentation skin disorders.
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
MDPI and ACS Style
Chung, B.Y.; Choi, S.R.; Moon, I.J.; Park, C.W.; Kim, Y.-H.; Chang, S.E. The Glutathione Derivative, GSH Monoethyl Ester, May Effectively Whiten Skin but GSH Does Not. Int. J. Mol. Sci. 2016, 17, 629.
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