Cyclohexanediol bis-ethylhexanoate inhibits melanogenesis of murine B16 melanoma and UV-induced pigmentation in human skin
| Autor: | Myoung Rae Kim, Joo Hyuck Lim, So Hyun Park, Byoung Sam Yoo, Jung Hyun Kim, In Woo Cheong, Jae Chan Yang, Jin Hun Cho |
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| Rok vydání: | 2012 |
| Předmět: |
Stereochemistry
Ultraviolet Rays Tyrosinase Melanoma Experimental Pharmaceutical Science Human skin Skin Pigmentation Pregnancy Proteins Melanin Mice Western blot Cyclohexanes medicine Cytotoxic T cell Animals Humans Cyclohexanediol bis-ethylhexanoate RNA Messenger Inhibitory effect Caproates Pharmacology Melanins medicine.diagnostic_test Dose-Response Relationship Drug Chemistry Monophenol Monooxygenase General Medicine Molecular biology Intramolecular Oxidoreductases Interferon Type I B16 melanoma |
| Zdroj: | Biologicalpharmaceutical bulletin. 36(3) |
| ISSN: | 1347-5215 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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