Cyclohexanediol Bis-Ethylhexanoate Inhibits Melanogenesis of Murine B16 Melanoma and UV-Induced Pigmentation in Human Skin

The role of cyclohexane diester analogues in the formation of melanin has been recently reported. In the present study, we investigated the inhibitory effect of cyclohexanediol bis-ethylhexanoate (CHEH) on melanogenesis in B16 melanoma cells and on UV-B-induced pigmentation in human skin. CHEH signi...

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Bibliographic Details
Published in:Biological & pharmaceutical bulletin 2013/03/01, Vol.36(3), pp.346-351
Main Authors: Lim, Joo Hyuck, Park, So-Hyun, Kim, Myoung Rae, Yoo, Byoung-Sam, Yang, Jae Chan, Cheong, In Woo, Kim, Jung Hyun, Cho, Jin Hun
Format: Article
Language:English
Subjects:
Animals
anti-melanogenesis
Caproates - pharmacology
cyclohexanediol bis-ethylhexanoate
Cyclohexanes - pharmacology
Dose-Response Relationship, Drug
Humans
Interferon Type I - genetics
Intramolecular Oxidoreductases - genetics
Melanins - antagonists & inhibitors
Melanins - biosynthesis
Melanoma, Experimental - metabolism
Mice
Monophenol Monooxygenase - antagonists & inhibitors
Monophenol Monooxygenase - genetics
Pregnancy Proteins - genetics
RNA, Messenger - analysis
Skin Pigmentation - drug effects
Skin Pigmentation - radiation effects
tyrosinase
Ultraviolet Rays - adverse effects
whitening
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Summary:The role of cyclohexane diester analogues in the formation of melanin has been recently reported. In the present study, we investigated the inhibitory effect of cyclohexanediol bis-ethylhexanoate (CHEH) on melanogenesis in B16 melanoma cells and on UV-B-induced pigmentation in human skin. CHEH significantly reduced the melanin content in a dose-dependent manner, without cytotoxic effects at the effective concentrations. Moreover, CHEH dose-dependently inhibited tyrosinase activity in B16 melanoma cells, as confirmed by Western blot analysis of the tyrosinase protein levels. However, tyrosinase transcript levels remained unchanged under the same experimental conditions. These results indicate that CHEH inhibited melanogenesis in B16 melanoma cells by regulating tyrosinase activity at the post-transcriptional level. On the other hand, in a cell-free system, CHEH did not inhibit tyrosinase activity. This indicated that CHEH suppressed the pigmentation of melanocytes by indirectly regulating tyrosinase activity. Finally, in a clinical trial, a cream containing 1.0% CHEH showed good whitening effect on UV-induced pigmented human skin without adverse effects. In conclusion, we suggest that CHEH may be an effective inhibitor of melanogenesis and useful effects in the treatment of hyperpigmented disorders.
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.b12-00585