Effects of certain resorcinol derivatives on the tyrosinase activity and the growth of melanoma cells.
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.
Tasaka
K
K
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Okayama University, Japan.
Kamei
C
C
Nakano
S
S
Takeuchi
Y
Y
Yamato
M
M
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000633:toxicity; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000494:pharmacology* / Q000633:toxicity; D008543:Melanins / Q000378:metabolism; D008546:Melanoma, Experimental / Q000201:enzymology* / Q000378:metabolism / Q000473:pathology; D051379:Mice; D008811:Mice, Inbred DBA; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012118:Resorcinols / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D008543:Melanins; D012118:Resorcinols; D014442:Monophenol Monooxygenase