TY - JOUR
T1 - Effects of certain resorcinol derivatives on the tyrosinase activity and the growth of melanoma cells
AU - Tasaka, Kenji
AU - Kamei, Chiaki
AU - Nakano, Shinji
AU - Takeuchi, Yasuo
AU - Yamato, Masatoshi
PY - 1998/3/1
Y1 - 1998/3/1
N2 - 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 resorcinol, 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.
AB - 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 resorcinol, 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.
KW - 5- Fluorouracil
KW - Hydroquinone
KW - Melanoma cells
KW - Resorcinol derivatives
KW - Tyrosinase activity
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U2 - 10.1358/mf.1998.20.2.485637
DO - 10.1358/mf.1998.20.2.485637
M3 - Article
C2 - 9604851
AN - SCOPUS:0031921716
VL - 20
SP - 99
EP - 109
JO - Methods and Findings in Experimental and Clinical Pharmacology
JF - Methods and Findings in Experimental and Clinical Pharmacology
SN - 0379-0355
IS - 2
ER -