Inhibitory Effect of Miconazole on Melanogenesis

Abstract

Miconazole (MIC), a regional antifungal agent, has been used worldwide in the treatment of superficial mycosis. However, the effect of MIC on skin pigmentation is not known. In this study, we investigated the inhibitory effect of MIC on melanogenesis in B16 melanoma cells. Tyrosinase activity and melanin content were dose dependently decreased by MIC as compared with untreated cells. The level of tyrosinase protein expression was reduced with treatment MIC. A decrease in cell proliferation was observed in B16 cells treated with MIC 30 m mM, indicating that the MIC-induced depigmenting effect was caused by inhibition of melanin synthesis and not by destruction of B16 cells. Furthermore, MIC markedly suppressed a a-melanocyte stimulating hormone or forskolin-induced tyrosinase activity in B16 cells. Therefore the depigmenting effect of MIC might be due to the inhibition of tyrosinase activity and tyrosinase expression, which eventually slows melanin biosynthesis. These results indicate that MIC may be a useful inhibitor of melanogenesis in B16 cells and suggest that it may have beneficial effects in the treatment of hyperpigmentation disorders such as ephelis and melasma.

Inhibitory Effects of Kurarinol, Kuraridinol, and Trifolirhizin from Sophora flavescens on Tyrosinase and Melanin Synthesis

“…These results indicate that compounds 1-3 can inhibit cAMP-mediated melanin production because IBMX is an elevator of intracellular cAMP 29) ; cAMP is shown to be a key messenger in the regulation of skin pigmentation. 30) Our data are consistent with others, 31,32) where the inhibition of melanogenesis was characterized by the inhibition of tyrosinase.…”

Antimelanogenic Activity of 3,4-Dihydroxyacetophenone: Inhibition of Tyrosinase and MITF

“…11) In the present study, we documented that 3,4-DHAP suppresses melanogenesis and tyrosinase activity by modulating the protein amounts of tyrosinase and MITF A B ( Fig. 3).…”

Inhibitory Effects of 2-Amino-3H-phenoxazin-3-one on the Melanogenesis of Murine B16 Melanoma Cell Line

“…Cellular tyrosinase activities were determined using a procedure slightly modified from that described previously. 21) Briefly, B16 cells were cultured in RPMI 1640 medium containing 10% FBS and then washed with ice-cold PBS. Cells were collected and lysed with Whole Cell Extraction Reagents (Chemicon, Temecula, CA) containing protease inhibitor cocktail (CompleteÔ, Roche Diagnostics, Mannheim, Germany), and the lysate was then centrifuged at 8,000 g for 30 min at 4 C. The supernatant was assayed for cellular tyrosinase activity.…”