Mechanisms of melanogenesis inhibition by propafenone

Abstract

Melanogenesis is a physiological process that results in the synthesis of melanin pigments, which play a crucial protective role against skin photocarcinogenesis. The present study was conducted to determine the inhibitory effects of propafenone on melanogenesis and to elucidate the molecular events involved in the inhibition of melanogenesis by propafenone. To accomplish this, several experiments were conducted using human epidermal melanocyte cells. The melanin content and cAMP production were evaluated, and western blots for proteins involved in melanogenesis were conducted. The melanin content was significantly inhibited by propafenone in a concentration-dependent manner. To clarify the mechanism of the depigmenting property of propafenone, we examined the involvement of propafenone in cAMP signaling. In the cAMP production assay, the intracellular cAMP level was reduced by propafenone. The level of microphthalmia-associated transcription factor (MITF) protein, the upstream transcription factor of tyrosinase, was also reduced by propafenone. In addition, propafenone inhibited the expression of tyrosinase, TRP-1, and TRP-2. Taken together, the results of our study show that propafenone inhibits melanogenesis by suppressing cAMP production, which is involved in the expression of melanogenesis-related proteins and suggests that propafenone may be an effective inhibitor of hyperpigmentation.

Inhibition of Melanogenesis by Gallic Acid: Possible Involvement of the PI3K/Akt, MEK/ERK and Wnt/β-Catenin Signaling Pathways in B16F10 Cells

“…A recent study reported that degradation of MITF is related to the suppression of the α-MSH-induced cAMP-dependent melanogenic pathway in melanoma cells [27]. Consequently, we theorized that gallic acid-induced MITF down-regulation is also involved in the cAMP signal transduction cascade.…”

Novel Application of Cultured Roots of Mountain Ginseng (Panax Ginseng Meyer) and Ginsenoside Re as Safe Antimelanogenic Cosmeceutical Components

“…To better understand the molecular mechanisms of Reinduced inhibitory effect, we further examined the effect of Re on the mRNA expression level of melanogenic transcription genes. It has been reported that MITF down-regulation is related to the suppression of the cyclic AMP-dependent signaling pathway stimulated by α-MSH in melanoma cells (Huh et al, 2010). However, in the current study, we did not evaluate the inhibitory activity of ginsenoside Re in the cyclic AMP-mediated melanin production.…”

Partially purified components of Nardostachys chinensis suppress melanin synthesis through ERK and Akt signaling pathway with cAMP down-regulation in B16F10 cells

“…It has recently been reported that MITF degradation is related to suppression of the cAMP-dependent melanogenic pathway stimulated by ␣-MSH in melanoma cells (Kim et al, 2008;Huh et al, 2010). Therefore, we hypothesized that PPNC-induced MITF down-regulation is involved in the cAMP signal transduction cascade.…”