Different effects of five depigmentary compounds, rhododendrol, raspberry ketone, monobenzone, rucinol and AP736 on melanogenesis and viability of human epidermal melanocytes

@article{Lee2016DifferentEO,
  title={Different effects of five depigmentary compounds, rhododendrol, raspberry ketone, monobenzone, rucinol and AP736 on melanogenesis and viability of human epidermal melanocytes},
  author={Chang Seok Lee and Yung Hyup Joo and Heung Soo Baek and Miyoung Park and Jeong-Hwan Kim and Hong-Ju Shin and Nok-hyun Park and John Hwan Lee and Young-Ho Park and Song Seok Shin and Hae-Kwang Lee},
  journal={Experimental Dermatology},
  year={2016},
  volume={25}
}
Numerous medications are used to treat hyperpigmentation. However, several reports have indicated that repeated application of some agents, such as rhododendrol (RD), raspberry ketone (RK) and monobenzone (MB), can be toxic to melanocytes. Although these agents had severe side effects in human trials, no current in vitro methods can predict the safety of such drugs. This study assessed the in vitro effects of five depigmentary compounds including leukoderma‐inducing agents. In particular, we… 
Biochemical Mechanism of Rhododendrol-Induced Leukoderma
TLDR
It is found that the oxidation of racemic RD by mushroom tyrosinase rapidly produces RD-quinone, which gives rise to secondary quinone products and the results suggest two major mechanisms of cytotoxicity to melanocytes.
Protopanaxatriol inhibits melanin synthesis through inactivation of the pCREB–MITF–tyrosinase signalling pathway in melanocytes
TLDR
Protopanaxatriol significantly reduced intracellular and extracellular melanin content in a concentration‐dependent manner in B16 melanoma cells treated with α‐melanocyte‐stimulating hormone, and dramatically suppressed the expression of genes encoding the melanogenic proteins tyros inase, tyrosinase‐related protein‐1 and ‐2, and microphthalmia‐associated transcription factor.
Conjugation with Dihydrolipoic Acid Imparts Caffeic Acid Ester Potent Inhibitory Effect on Dopa Oxidase Activity of Human Tyrosinase
TLDR
Data point to 2-S-lipoyl caffeic acid methyl ester as a valuable candidate for further trials toward its use as a skin depigmenting agent and highlight the differential effects of tyrosinase inhibitors on the human and mushroom enzymes.
Glucose Exerts an Anti-Melanogenic Effect by Indirect Inactivation of Tyrosinase in Melanocytes and a Human Skin Equivalent
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It is concluded that glucose indirectly inhibits tyrosinase activity through conversion into lactic acid, explaining its anti-melanogenic effects in melanocytes.
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TLDR
The inhibition properties of the caffeic acid- dihydrolipoic acid S-conjugate, 2-S-lipoylcaffeic acid (LC) on mushroom tyrosinase would point to LC as a novel prototype of melanogenesis regulators for the treatment of pigmentary disorders.
Depigmentation efficacy of galacturonic acid through tyrosinase regulation in B16 murine melanoma cells and a three‐dimensional human skin equivalent
TLDR
The results support the utility of GA as an effective candidate antimelanogenic agent and significantly suppressed melanin synthesis and secretion in a concentration‐dependent manner in α‐melanocyte stimulating hormone‐treated B16 melanoma cells.
Rhododendrol‐induced leukoderma update II: Pathophysiology, mechanisms, risk evaluation, and possible mechanism‐based treatments in comparison with vitiligo
TLDR
This review investigates and evaluates the major considerations for developing rhododendrol‐induced leukoderma based on data from original or review articles published in the literature to provide a wide range of information regarding the pathophysiology, mechanisms, risk evaluation, and possible mechanism‐based treatments.
Rhododenol Activates Melanocytes and Induces Morphological Alteration at Sub-Cytotoxic Levels
TLDR
It is discovered that rhododenol treatment reduced the number of melanocytes in a pigmented 3D human skin model, Melanoderm™, confirming the melanocyte toxicity of RD and suggesting that RD not only induces cytotoxicity in melanocytes but also can lead to a profound perturbation of melanocyte integrity even at sub-cytotoxic levels.
Rhododendrol‐induced leukoderma update I: Clinical findings and treatment
TLDR
It is found that ultraviolet light therapy is the most effective treatment for RDL, and reports of the efficacy of oral vitamin D3 in RDL are summarized, and guidance is provided for patients using self‐tanning and skin‐whitening agents to improve their quality of life.
Keratinocyte-derived IL-36γ plays a role in hydroquinone-induced chemical leukoderma through inhibition of melanogenesis in human epidermal melanocytes
TLDR
Hydroquinone-induced IL-36γ from human keratinocytes plays a pivotal role in the development of chemical leukoderma by autocrinally or paracrinally modulating the crosstalk between keratinocyte and melanocytes.
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