Myricetin suppresses UVB-induced skin cancer by targeting Fyn

Cancer Res. 2008 Jul 15;68(14):6021-9. doi: 10.1158/0008-5472.CAN-08-0899.

Abstract

Skin cancer is currently the most common type of human cancer in Americans. Myricetin, a naturally occurring phytochemical, has potent anticancer-promoting activity and contributes to the chemopreventive potential of several foods, including red wine. Here, we show that myricetin suppresses UVB-induced cyclooxygenase-2 (COX-2) expression in mouse skin epidermal JB6 P+ cells. The activation of activator protein-1 and nuclear factor-kappaB induced by UVB was dose-dependently inhibited by myricetin treatment. Western blot and kinase assay data revealed that myricetin inhibited Fyn kinase activity and subsequently attenuated UVB-induced phosphorylation of mitogen-activated protein kinases. Pull-down assays revealed that myricetin competitively bound with ATP to suppress Fyn kinase activity. Importantly, myricetin exerted similar inhibitory effects compared with 4-amino-5-(4-chloro-phenyl)-7-(t-butyl)pyrazolo[3,4-d]pyrimidine, a well-known pharmacologic inhibitor of Fyn. In vivo mouse skin data also revealed that myricetin inhibited Fyn kinase activity directly and subsequently attenuated UVB-induced COX-2 expression. Mouse skin tumorigenesis data clearly showed that pretreatment with myricetin significantly suppressed UVB-induced skin tumor incidence in a dose-dependent manner. Docking data suggest that myricetin is easily docked to the ATP-binding site of Fyn, which is located between the N and C lobes of the kinase domain. Overall, these results indicated that myricetin exerts potent chemopreventive activity mainly by targeting Fyn in skin carcinogenesis.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Female
  • Flavonoids / pharmacology*
  • Mice
  • Mice, Inbred ICR
  • Models, Biological
  • NF-kappa B / metabolism
  • Neoplasms, Radiation-Induced / drug therapy*
  • Phosphorylation
  • Proto-Oncogene Proteins c-fyn / metabolism*
  • Skin Neoplasms / drug therapy*
  • Skin Neoplasms / etiology*
  • Transcription Factor AP-1 / metabolism
  • Ultraviolet Rays*

Substances

  • Antineoplastic Agents
  • Flavonoids
  • NF-kappa B
  • Transcription Factor AP-1
  • myricetin
  • Fyn protein, mouse
  • Proto-Oncogene Proteins c-fyn