3,4,5-Trimethoxycinnamate thymol ester inhibits melanogenesis in normal human melanocytes and 3D human epidermal equivalents via the PGC-1α-independent PPARγ partial agonism

Ko, Hyejin; Choi, Hyunjung; Han, Yujia; An, Seungchan; Min, Daejin; Park, Won-Seok; Sun, Jing; Kim, Hyoung-June; Noh, Minsoo

doi:10.1016/j.jdermsci.2022.02.010

Cited by 3 publications

(3 citation statements)

References 33 publications

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“…However, epidermal hyperdifferentiation was also observed through histological observation (Figure 5D). This is a unique feature of MelanoDerm that we have observed in previous studies [10,[23][24][25]. However, it is also necessary to comprehensively examine whether this phenomenon affected the epidermal pigmentation.…”

Section: Discussionmentioning

confidence: 70%

2,4,6-Triphenyl-1-hexene, an Anti-Melanogenic Compound from Marine-Derived Bacillus sp. APmarine135

Kim,

Do,

Park

et al. 2024

Marine Drugs

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Although melanin protects against ultraviolet radiation, its overproduction causes freckles and senile lentigines. Recently, various biological effects of metabolites derived from marine microorganisms have been highlighted due to their potential for biological and pharmacological applications. In this study, we discovered the anti-melanogenic effect of Bacillus sp. APmarine135 and verified the skin-whitening effect. Fractions of APmarine135 showed the melanin synthesis inhibition effect in B16 melanoma cells, and 2,4,6-triphenyl-1-hexene was identified as an active compound. The melanogenic capacity of 2,4,6-triphenyl-1-hexene (1) was investigated by assessing the intracellular melanin content in B16 cells. Treatment with 5 ppm of 2,4,6-triphenyl-1-hexene (1) for 72 h suppressed the α-melanocyte-stimulating hormone (α-MSH)-induced intracellular melanin increase to the same level as in the untreated control group. Additionally, 2,4,6-triphenyl-1-hexene (1) treatment suppressed the activity of tyrosinase, the rate-limiting enzyme for melanogenesis. Moreover, 2,4,6-triphenyl-1-hexene (1) treatment downregulated tyrosinase, Tyrp-1, and Tyrp-2 expression by inhibiting the microphthalmia-associated transcription factor (MITF). Furthermore, 2,4,6-triphenyl-1-hexene (1) treatment decreased the melanin content in the three-dimensional (3D) human-pigmented epidermis model MelanoDerm and exerted skin-whitening effects. Mechanistically, 2,4,6-triphenyl-1-hexene (1) exerted anti-melanogenic effects by suppressing tyrosinase, Tyrp-1, and Tyrp-2 expression and activities via inhibition of the MITF. Collectively, these findings suggest that 2,4,6-triphenyl-1-hexene (1) is a promising anti-melanogenic agent in the cosmetic industry.

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Section: Discussionmentioning

confidence: 70%

2,4,6-Triphenyl-1-hexene, an Anti-Melanogenic Compound from Marine-Derived Bacillus sp. APmarine135

Kim,

Do,

Park

et al. 2024

Marine Drugs

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“…In terms of the application and expansion of skin models. H. Ko et al [63] confirmed the whitening efficacy of the melaninogenic inhibitor TCTE by L* detection using MelanoDerm™ (MatTek), a dark skin donor-derived melanogenic skin model, and identified the target at the molecular level through a 3D epidermal model, revealing that the molecular mechanism of TCTE against melanin production is partial inhibition of PGC-1a-dependent PPARr.…”

Section: Whitening Effectmentioning

confidence: 94%

Progress in the Application of 3D Skin Models for Cosmetic Assessment

Shuxian,

Qin,

Yunlian

et al. 2024

Preprint

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With the development of organizational biology and forced from the EU Cosmetic Regulation (EU/1223/2009) with the complete ban of animal testing for cosmetic purposes, 3D skin models have been widely developed due to their similar physiological structure and metabolic function to native human tissue. 3D skin models for in vitro cosmetic evaluation are still promising alternative methods for evaluating phototoxicity, corrosivity and irritation. These models have been used for early screening and later validation of toxicity and efficacy evaluation by many well-known cosmetic companies. 3D skin models have become an important tool in cosmetic evaluation research. This article reviews the development of 3D skin models and their application in cosmetic evaluation. An outlook on the current application and future technological development directions in the cosmetic field is also presented.

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“…The adiponectin-secretion-promoting activity of 1 was more potent than that of aspirin (ASA), although its effect was weaker compared to antidiabetic GLI. Since antimelanogenic activity of adiponectin has been reported in several clinical experiments, compound 1 was also evaluated for the antimelanogenic activity. In result, 1 exhibited significant antimelanogenic activity in the human melanoma MNT-1 cell line (Figure C).…”

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confidence: 99%

Daldipyrenones A–C: Caged [6,6,6,6,6] Polyketides Derived from an Endolichenic Fungus Daldinia pyrenaica 047188

Lee,

Park,

Choi

et al. 2023

Org. Lett.

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polyketides featuring a spiro-azaphilone unit, were discovered from an endolichenic fungus, Daldinia pyrenaica 047188. The structures of 1−3 were determined by using spectroscopic analysis and chemical derivatization. Daldipyrenones are likely derived by combining a chromane biosynthesis intermediate, 1-(2,6-dihydroxyphenyl)but-2-en-2-one, and a spiro-azaphilone, pestafolide A, via radical coupling or Michael addition to form a bicyclo[2.2.2]octane ring. Genome sequencing of the strain revealed two separate biosynthetic gene clusters responsible for forming two biosynthetic intermediates, suggesting a proposed biosynthetic pathway. Daldipyrenone A (1) exhibited significant antimelanogenic activity with lower EC 50 's than positive controls and moderate adiponectin-secretion promoting activity.

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3,4,5-Trimethoxycinnamate thymol ester inhibits melanogenesis in normal human melanocytes and 3D human epidermal equivalents via the PGC-1α-independent PPARγ partial agonism

Cited by 3 publications

References 33 publications

2,4,6-Triphenyl-1-hexene, an Anti-Melanogenic Compound from Marine-Derived Bacillus sp. APmarine135

2,4,6-Triphenyl-1-hexene, an Anti-Melanogenic Compound from Marine-Derived Bacillus sp. APmarine135

Progress in the Application of 3D Skin Models for Cosmetic Assessment

Daldipyrenones A–C: Caged [6,6,6,6,6] Polyketides Derived from an Endolichenic Fungus Daldinia pyrenaica 047188

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