The inhibitory effect of arbutin, a naturally occurring beta-D-glucopy
ranoside derivative of hydroquinone, on melanogenesis was studied bioc
hemically by using human melanocytes in culture. Cells were cultured i
n the presence of different concentrations of arbutin. The maximum con
centration of arbutin that was not inhibitory to growth of the cells w
as 100 mu g/ml. At that concentration, melanin synthesis was inhibited
significantly by similar to 20% after 5 days, compared with untreated
cells. This phenotypic change was associated with the inhibition of t
yrosinase and DHICA polymerase activities, and the degree of inhibitio
n was dose dependent. No significant difference in DOPAchrome tautomer
ase (DT) activity was observed before or after arbutin treatment. West
ern blotting experiments revealed there were no changes in protein con
tent or in molecular size of tyrosinase, TRP-1 or TRP-2, indicating th
at inhibition of tyrosinase activity by arbutin might be due to effect
s at the post-translational level.