Effects of certain resorcinol derivatives on the tyrosinase activity and the growth of melanoma cells

Methods Find Exp Clin Pharmacol. 1998 Mar;20(2):99-109. doi: 10.1358/mf.1998.20.2.485637.

Abstract

Effects of certain resorcinol derivatives on tyrosinase activity, melanin formation and some other biological activities were studied in order to develop a new, potent depigmentor and/or antimelanoma drug. NKO-09, having isopentyl group in position 6 of resorcinal, exhibited a more potent effect than the compounds which have methyl (NKO-10), ethyl (NKO-11), hexyl (KOM-14), octyl (NKO-14), decyl (NKO-19), dodecyl (NKO-15) and tetradecyl (NKO-16) group in inhibiting the tyrosinase activities (both tyrosine hydroxylation and dopa oxidation). NKO-09 was more potent than hydroquinone in inhibiting the tyrosine hydroxylation; furthermore, NKO-09 inhibited the dopa oxidation different from hydroquinone. In the studies on melanin formation, protein synthesis and the growth of the melanoma cells, NKO-09 caused the most potent effect among the test compounds, except for the growth of the melanoma cells. KOM-14 was more potent than NKO-09 in the antimelanoma activity, and its effect was superior than that of 5-fluorouracil. From these findings, it is suggested that NKO-09 and KOM-14 can be used as an efficacious depigmentor and antimelanoma drug, respectively.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / toxicity
  • Drug Screening Assays, Antitumor
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / toxicity
  • Melanins / metabolism
  • Melanoma, Experimental / enzymology*
  • Melanoma, Experimental / metabolism
  • Melanoma, Experimental / pathology
  • Mice
  • Mice, Inbred DBA
  • Monophenol Monooxygenase / antagonists & inhibitors*
  • Monophenol Monooxygenase / metabolism
  • Resorcinols / chemistry
  • Resorcinols / pharmacology*
  • Resorcinols / toxicity
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Melanins
  • Resorcinols
  • Monophenol Monooxygenase