In vitro Dermal Absorption of Hydroquinone: Protocol Validation and Applicability on Illegal Skin-Whitening Cosmetics

Desmedt, Bart; Ates, Gamze; Courselle, P.; Beer, Jacques O. De; Rogiers, Vera; Hendrickx, Benoit; Deconinck, Éric; Paepe, Kristien De

doi:10.1159/000454719

Cited by 8 publications

(8 citation statements)

References 22 publications

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“…HQ containing cosmetic products are usually compounded 2% to 4% concentrations; the 2% concentrations of HQ available over the counter are not as efficacious as the 4% prescription formulations, as their onset of action is later than with the higher concentrations 21 . Because of the equivalence of the dermal absorption of HQ under a semisolid formulation (oil-in-water creams) and a liquid formulation, HQ is formulated in various topical forms: cream, emulsion, gel, or solution 22 . The efficacy of 4% HQ cream has been elucidated in several clinical trials [23][24][25] .…”

Section: Discussionmentioning

confidence: 99%

Melanogenesis inhibitory effect of Perilla Frutescens (L.) Britt on a hyperpigmentation model in rabbit

Nguyen¹,

Hao²,

Nguyen³

et al. 2022

Pharm Sci Asia

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The study aims to evaluate the melanogenesis inhibitory action of the ethyl acetate (EA) extract from Perilla frutescens (L.) Britt on a hyperpigmented rabbit model induced by UVA-exposure combined to progesterone injection. The dorsal shaved skin of the experimental rabbits was exposed to UVA radiation (386 nm, 147 uW/cm 2 ) in 30 minutes each day for 28 days. Progesterone was intramuscularly injected every other day at the dose of 5 mg/kg. EA extract was topically applied daily from the first day of melasma appearance until the end of the experiment. Morphometric observation based on color thresholder application on MATLAB software. Moreover, melanin determination and histological analysis were also performed. The morphometric observation on the surface of melasma areas as well as the histological analysis from 5% EA-treated group are similar to these of 4% Hydroquinone-treated group at day 14, 21, 28. Melanin concentration in 5% EA-treated group was significantly decreased as compared to the hyperpigmentation group. In conclusion, EA extract of Perilla leaves clearly exhibited the inhibitory effect on melanogenesis in the hyperpigmented rabbit-induced by UVA exposure combined to progesterone injection.

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Section: Discussionmentioning

confidence: 99%

Melanogenesis inhibitory effect of Perilla Frutescens (L.) Britt on a hyperpigmentation model in rabbit

Nguyen¹,

Hao²,

Nguyen³

et al. 2022

Pharm Sci Asia

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“…1 H NMR (500 MHz, CDCl3) δ 7.55 (s, 1H), 7.45 (d, J = 7.9 Hz, 1H), 7.37 (s, 2H), 7.31 (t, J = 6.9 Hz, 2H), 7.26 -7.15 (m, 9H), 7.13 (d, J = 7.7 Hz, 1H), 7.02 (d, J = 8.1 Hz, 2H), 6.87 (t, J = 7.3 Hz, 1H), 4.58 (d, J = 12.2 Hz, 1H), 3.97 (d, J = 14.1 Hz, 1H), 3.67 (s, 2H), 3.37-3.23 (m, 2H), 3.13 (d, J = 13.5 Hz, 1H), 2.51 (t, J = 10.3 Hz, 1H). 13…”

Section: Synthesis Procedures Of Pyrazolo[43c]pyridine (5) Figure 2 S...mentioning

confidence: 99%

“…Check for updates cosmetic and pharmaceutical industries [13,14,15]. However, very few inhibitors qualify for clinical use.…”

mentioning

confidence: 99%

Synthesis and Tyrosinase Inhibitory Activity of (E)-5-Benzyl-7- (3-Bromobenzylidene)-3-(3-Bromophenyl)-2-Phenyl-3,3a, 4,5,6,7-Hexahydro-2H-Pyrazolo[4,3-c]Pyridine

Oscifiani

Herfindo²,

Rahayu

et al. 2022

J. Kim. Sains Apl.

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The tyrosinase enzyme plays an essential role in the pigmentation of human skin, fruits, and vegetables. It has been tied with several human skin diseases and post-harvest problems. Hence, the tyrosinase enzyme becomes an excellent therapeutic target to overcome these issues. This study aimed to screen tyrosinase inhibitors by synthesizing halogen-substituted pyrazolopyridine derivatives. The pyrazolopyridine compound was obtained through two stages of synthesis. First, the intermediate compound, a derivative of 3,5-bis(arylidene)-4-piperidone, was synthesized through the Cleisen-Schmidt condensation reaction of 4-piperidone and benzaldehyde derivatives. Furthermore, the intermediate compound was reacted with phenylhydrazine through a cyclocondensation reaction to produce the titled compound with an 11% yield. The chemical structure of the target compound was identified through the interpretation of UV, FTIR, NMR, and HRMS spectra. Then an in vitro assay was conducted on the tyrosinase enzyme of the fungus Agaricus bisporus by detecting the presence of dopachrome at a wavelength of 492 nm. As a result, the in vitro assay showed that the titled compound had a weak inhibitory activity, and the IC50 value was > 500 µM. Thus, the synthesized compound is considered inactive.

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“…These agents inhibit melanogenesis by controlling TYR activity (Desmedt et al, 2016). However, hydroquinone has been banned or restricted as a cosmetic agent in many countries due to its toxic effects on mammalian cells, including contact dermatitis, irritation, burning, and hypopigmentation (Chang et al, 2017).…”

Section: Introductionmentioning

confidence: 99%

Anti‐melanogenic effect of exosomes derived from human dermal fibroblasts (BJ‐5ta‐Ex) in C57BL/6 mice and B16F10 melanoma cells

Lee,

Kim

et al. 2023

Pigment Cell Melanoma Res

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Exosomes are involved in intercellular communication by transferring cargo between cells and altering the specific functions of the target cells. Recent studies have demonstrated the therapeutic effects of exosomes in several skin diseases. However, understanding of the effects of exosomes on anti‐pigmentation is limited. Therefore, we investigated whether BJ‐5ta exosomes (BJ‐5ta‐Ex) derived from human foreskin fibroblasts regulate melanogenesis and delineated the underlying mechanism. Interestingly, treatment with BJ‐5ta‐Ex induced decreased melanin content, tyrosinase (TYR) activity, and expression of melanogenesis‐related genes, including microphthalmia‐related transcription factor (MITF), TYR, tyrosinase‐related protein‐1 (TRP1), and tyrosinase‐related protein‐2 (TRP2). In addition, BJ‐5ta‐Ex downregulated the cAMP/PKA and GSK‐3β/β‐catenin signaling pathways and upregulated the MAPK/ERK signaling pathway. Notably, treatment with BJ‐5ta‐Ex inhibited α‐melanocyte‐stimulating hormone‐induced melanosome transport and decreased the expression of key proteins involved in melanosome transport, namely, rab27a and melanophilin (MLPH). To further confirm the depigmenting effects of BJ‐5ta‐Ex, we conducted experiments using a three‐dimensional reconstituted human full skin model and ultraviolet B (UVB)‐irradiated mouse model. Treatment with BJ‐5ta‐Ex improved tissue brightness and reduced the distribution of melanosomes. In UVB‐irradiated mouse ears, BJ‐5ta‐Ex reduced the number of active melanocytes and melanin granules. These results demonstrate that BJ‐5ta‐Ex can be useful for the clinical treatment of hyperpigmentation disorders.

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In vitro Dermal Absorption of Hydroquinone: Protocol Validation and Applicability on Illegal Skin-Whitening Cosmetics

Cited by 8 publications

References 22 publications

Melanogenesis inhibitory effect of Perilla Frutescens (L.) Britt on a hyperpigmentation model in rabbit

Melanogenesis inhibitory effect of Perilla Frutescens (L.) Britt on a hyperpigmentation model in rabbit

Synthesis and Tyrosinase Inhibitory Activity of (E)-5-Benzyl-7- (3-Bromobenzylidene)-3-(3-Bromophenyl)-2-Phenyl-3,3a, 4,5,6,7-Hexahydro-2H-Pyrazolo[4,3-c]Pyridine

Anti‐melanogenic effect of exosomes derived from human dermal fibroblasts (BJ‐5ta‐Ex) in C57BL/6 mice and B16F10 melanoma cells

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