Synthesis of dihydroresveratrol glycosides and evaluation of their activity against melanogenesis in B16F0 melanoma cells

Eur J Med Chem. 2014 Nov 24:87:862-7. doi: 10.1016/j.ejmech.2014.09.092. Epub 2014 Oct 2.

Abstract

Dihydroresveratrol glucoside 1 isolated from Camellia oleifera and its xyloside derivative 2 were synthesized for the first time in 5 steps from TBS-protected aldehyde 4. Natural product 1 is a potent melanogenesis inhibitor in B16F0 melanoma cells (approximately 40 fold more potent than kojic acid). In contrast, the synthetic product 2 stimulates melanogenesis, suggesting that a single hydroxymethyl group in the glycoside substituent of dihydroresveratrols is responsible for inhibition or activation of melanogenesis.

Keywords: Camellia oleifera; Dihydroresveratrol glycoside; Glycosylation; Melanogenesis activator; Melanogenesis inhibitor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Glycosides / chemistry
  • Magnetic Resonance Spectroscopy
  • Melanins / biosynthesis*
  • Melanoma, Experimental / metabolism*
  • Melanoma, Experimental / pathology
  • Mice
  • Spectrometry, Mass, Electrospray Ionization
  • Stilbenes / chemical synthesis*
  • Stilbenes / chemistry
  • Stilbenes / pharmacology

Substances

  • Glycosides
  • Melanins
  • Stilbenes
  • dihydroresveratrol