Rhododenol Activates Melanocytes and Induces Morphological Alteration at Sub-Cytotoxic Levels

Kim, Minjeong; Lee, Chang-Suck; Lim, Kyung Min

doi:10.3390/ijms20225665

Cited by 10 publications

(7 citation statements)

References 35 publications

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“…RT-PCR results showed a decrease in the expression of melanogenesis-related genes. RD treatment has been reported to increase the gene and protein expression levels of Rab27A and TRP-2 (DCT), which are regulated by MITF (Chiaverini et al, 2008;Hoek et al, 2008;Kim et al, 2019). However, the dct mRNA levels were decreased by RD in our experiments.…”

Section: Discussioncontrasting

confidence: 78%

Zebrafish as a new model for rhododendrol‐induced leukoderma

Hayazaki

Hatano

Shimabayashi

et al. 2021

Pigment Cell Melanoma Res

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Rhododendrol (RD: 4-(4-Hydroxyphenyl)-2-butanol) is a melanogenesis inhibitor isolated from the stem bark of Acer nikoense MAXIM.Since RD is structurally similar to L-tyrosine, it competitively inhibits tyrosinase, a rate-limiting enzyme for melanin synthesis (Akazawa et al., 2006). RD was approved as an ingredient in cosmetics for skin lightening in Japan in 2008; however, 5 years later, cosmetic products containing RD were recalled because of the development of depigmentation (idiopathic leukoderma or vitiligo) in the skin. The total number of patients with leukoderma caused by RD was 19,605, accounting for 2%-2.5% of users of the RD-included cosmetic products (Nishigori et al., 2015). Although the symptoms of RD-induced leukoderma were improved or eliminated in 72% of patients, the remaining patients were resistant to conventional therapy (Watabe et al., 2018).A study with cultured melanocytes has reported that tyrosinase converts RD to cytotoxic metabolites, such as RD-catechol and RD-cyclic catechol, which cause melanocyte-specific cell death

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Section: Discussioncontrasting

confidence: 78%

Zebrafish as a new model for rhododendrol‐induced leukoderma

Hayazaki

Hatano

Shimabayashi

et al. 2021

Pigment Cell Melanoma Res

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“…MITF is one of the key regulators for melanogenesis and it controls the gene transcription of tyrosinase, TRP-1, TRP-2, Cdc42 and Rab27a ( Noguchi et al, 2016 ; Kim et al, 2019 ). We first examined the influence of J147 on MITF transcripts.…”

Section: Resultsmentioning

confidence: 99%

The Inhibitory Effect of Curcumin Derivative J147 on Melanogenesis and Melanosome Transport by Facilitating ERK-Mediated MITF Degradation

Yang

Jia

et al. 2021

Front. Pharmacol.

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The therapeutic use of curcumin and chemically modified curcumin (CMC) for suppressing melanogenesis and tyrosinase activity have been recognized. J147 is a modified version of curcumin with superior bioavailability and stability. However, there is no report about the effects of J147 on pigmentation in vitro and in vivo. In our studies, we investigated the hypopigmentary effects of J147 treatment on melanocytes and explored the underlying mechanism. The present studies suggested that J147 suppressed both basal and α-MSH-induced melanogenesis, as well as decreased melanocyte dendricity extension and melanosome transport. J147 played these roles mainly by activating the extracellular signal-regulated protein kinase (ERK) pathway. Once activated, it resulted in MITF degradation and further down-regulated the expression of tyrosinase, TRP-1, TRP-2, Myosin Va, Rab27a and Cdc42, ultimately inhibited melanin synthesis and melanosome transport. Furthermore, the hypopigmentary effects of J147 were demonstrated in vivo in a zebrafish model and UVB-induced hyperpigmentation model in brown guinea pigs. Our findings also suggested that J147 exhibited no cytotoxicity in vitro and in vivo. Taken together, these data confirmed that J147 may prove quite useful as a safer natural skin-whitening agent.

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“…Since tyrosinase is key in the melanogenesis inhibition in melanocytes, its inhibitors were considered promising candidates as skin whitening agents in cosmetics ( Pillaiyar et al ., 2017 ). However, tyrosinase inhibitors such as hydroquinone, rhododenol, or raspberry ketones can cause adverse effects such as leukoderma by affecting the melanocyte integrity ( Kim et al ., 2016 , 2017b , 2019 ). Therefore, novel skin whitening agents with a novel mode of action and new scaffolds are required.…”

Section: Discussionmentioning

confidence: 99%

Antaroide, a Novel Natural Nine-Membered Macrolide, Inhibits Melanin Biosynthesis in B16F10 Murine Melanoma Cells

Ryu

Baek

Kim

et al. 2021

Biomolecules & Therapeutics

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The demand for natural substances with anti-melanogenic activity is increasing due to the recent interest in skin whitening. Intensive investigation on the culture broth of Streptomyces sp. SCO-736, a marine bacterium from the Antarctica coast, has led to the isolation of a new natural product named antaroide (1). The chemical structure was established through the interpretation of MS, UV, and NMR spectroscopic data. Antaroide is a nine-membered macrolide with lactone and lactam moieties. To investigate its applicability in skin whitening cosmetics, its anti-melanogenic activity in B16F10 murine melanoma cells was examined. As a result, antaroide displayed strong inhibitory activities against melanin synthesis and also attenuated the dendrite formation induced by the α-melanocyte stimulating hormone (α-MSH). Antaroide suppressed the mRNA expression of the melanogenic enzymes such as tyrosinase, TRP-1 and TRP-2. This suggests that it may serve as a transcriptional regulator of melanogenesis. Collectively, the discovery of this novel natural nine-membered macrolide and its anti-melanogenic activity could give new insights for the development of skin whitening agents.

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Rhododenol Activates Melanocytes and Induces Morphological Alteration at Sub-Cytotoxic Levels

Cited by 10 publications

References 35 publications

Zebrafish as a new model for rhododendrol‐induced leukoderma

Zebrafish as a new model for rhododendrol‐induced leukoderma

The Inhibitory Effect of Curcumin Derivative J147 on Melanogenesis and Melanosome Transport by Facilitating ERK-Mediated MITF Degradation

Antaroide, a Novel Natural Nine-Membered Macrolide, Inhibits Melanin Biosynthesis in B16F10 Murine Melanoma Cells

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