Cyclohexanediol bis-ethylhexanoate inhibits melanogenesis of murine B16 melanoma and UV-induced pigmentation in human skin

Joo Hyuck Lim, So Hyun Park, Myoung Rae Kim, Byoung Sam Yoo, Jae Chan Yang, In Woo Cheong, Jung Hyun Kim, Jin Hun Cho

Research output: Contribution to journalArticle

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Abstract

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.

Original languageEnglish
Pages (from-to)346-351
Number of pages6
JournalBiological and Pharmaceutical Bulletin
Volume36
Issue number3
DOIs
Publication statusPublished - 2013 Mar 1

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Experimental Melanomas
Pigmentation
Monophenol Monooxygenase
Skin
Melanins
Cell-Free System
cyclohexanediol bis-ethylhexanoate
Melanocytes
Western Blotting
Clinical Trials

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmaceutical Science

Cite this

Lim, Joo Hyuck ; Park, So Hyun ; Kim, Myoung Rae ; Yoo, Byoung Sam ; Yang, Jae Chan ; Cheong, In Woo ; Kim, Jung Hyun ; Cho, Jin Hun. / Cyclohexanediol bis-ethylhexanoate inhibits melanogenesis of murine B16 melanoma and UV-induced pigmentation in human skin. In: Biological and Pharmaceutical Bulletin. 2013 ; Vol. 36, No. 3. pp. 346-351.
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Cyclohexanediol bis-ethylhexanoate inhibits melanogenesis of murine B16 melanoma and UV-induced pigmentation in human skin. / Lim, Joo Hyuck; Park, So Hyun; Kim, Myoung Rae; Yoo, Byoung Sam; Yang, Jae Chan; Cheong, In Woo; Kim, Jung Hyun; Cho, Jin Hun.

In: Biological and Pharmaceutical Bulletin, Vol. 36, No. 3, 01.03.2013, p. 346-351.

Research output: Contribution to journalArticle

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