• Genomics & Informatics
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• v.21 no.3
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• pp.43.1-43.13
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• 2023

Melanin is synthesized by tyrosinase to protect the skin from ultraviolet light. However, overproduction and accumulation of melanin can result in hyperpigmentation and skin melanoma. Tyrosinase inhibitors are commonly used in the treatment of hyperpigmentation. Natural tyrosinase inhibitors are often favoured over synthetic ones due to the potential side effects of the latter, which can include skin irritation, allergies, and other adverse reactions. Nuciferine, an alkaloid derived from Nelumbo nucifera, exhibits potent antioxidant and anti-proliferative properties. This study focused on the in silico screening of nuciferine for anti-tyrosinase activity, using kojic acid, ascorbic acid, and resorcinol as standards. The tyrosinase protein target was selected through homology modeling. The residues of the substrate binding pocket and active site pockets were identified for the purposes of grid box optimization and docking. Therefore, nuciferine is a potent natural tyrosinase inhibitor and shows promising potential for application in the treatment of hyperpigmentation and skin melanoma.

• KSBB Journal
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• v.29 no.3
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• pp.199-204
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• 2014

To investigate the effect of Plantago asiatica L. Root extract on skin care, we measured anti-oxidant activity and whitening action. As a result of measuring DPPH radical scavenging activity to examine independent anti-oxidation of PRE, there was slight scavenging activity. Fluorescent materials DHE, DCF-DA and DHR were each used to measure superoxide anion, hydrogen peroxide, and hydroperoxide created in RAW 264.7 cells, all concentrations were found to dependently prevent ROS production. Tyrosinase activation was found to be blocked dose-dependant. Melanin production was also prevented dose-dependant, but the effects were slight. Therefore, it is expected to be used effectively in development of functional cosmetic materials.

• The Korean Journal of Physiology and Pharmacology
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• v.26 no.2
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• pp.113-123
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• 2022

Diarylpropionitrile (DPN), a selective agonist for estrogen receptor β (ERβ), has been reported to regulate various hormonal responses through activation of ERβ in tissues including the mammary gland and brain. However, the effect of DPN on melanogenesis independent of ERβ has not been studied. The aim of this study is to examine the possibility of anti-melanogenic effect of DPN and its underlying mechanism. Melanin contents and cellular tyrosinase activity assay indicated that DPN inhibited melanin biosynthesis in alpha-melanocyte stimulating hormone-stimulated B16F10 melanoma cell line. However, DPN had no direct influence on in vitro tyrosinase catalytic activity. On the other hand, 17β-estradiol had no effect on inhibition of melanogenesis, suggesting that the DPN-mediated suppression of melanin production was not related with estrogen signaling pathway. Immunoblotting analysis showed that DPN down-regulated the expression of microphthalmia-associated transcription factor (MITF), a central transcription factor of melanogenesis and its down-stream genes including tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2. Also, DPN attenuated the phosphorylation of protein kinase A (PKA) and cAMP-response element-binding protein (CREB). Additionally, DPN suppressed the melanin synthesis in UVB-irradiated HaCaT conditioned media culture system suggesting that DPN has potential as an anti-melanogenic activity in physiological conditions. Collectively, our data show that DPN inhibits melanogenesis via downregulation of PKA/CREB/MITF signaling pathway.

• Journal of Mushroom
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• v.19 no.3
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• pp.150-159
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• 2021

Anti-melanogenesis and skin anti-wrinkle effects of methanol (ME) and hot water (HE) extracts from the fruiting bodies of Ganoderma applanatum were investigated in this study. The total phenolic contents of the ME and HE of the mushroom were 11.68 and 3.15 ㎍ GAEs/mg, respectively, whereas the total flavonoid contents of the ME and HE were 21.82 and 2.69 ㎍ QEs/mg, respectively. The survival rate of B16-F10 murine melanoma cells treated with 750 ㎍ ME and HE were 83.46% and 85.54%, respectively, thereby suggesting that mushroom extracts were slightly cytotoxic at the tested concentration. The in vitro tyrosinase inhibition by ME (83.15%) and HE (83.44%) was significantly lower than that of kojic acid (99.61%), the positive control, at 2.0 mg/mL. Although the inhibition of cellular melanin synthesis in B16-F10 melanoma cells by 2.0 mg/mL of ME (50.24%) and HE (51.24%) was lower than that of arbutin (64.84%), the inhibition by both ME and HE was higher than 50%. Collagenase inhibition by HE was comparable to 2.0 mg/mL epigallocatechin (EGCG), the positive control; however, elastase inhibition by ME and HE was lower than that of EGCG at the concentration tested. The results showed that the fruiting bodies of G. applanatum had good anti-tyrosinase, good anti-collagenase, and moderate anti-elastase activities, which might be useful for developing novel skin-whitening and anti-wrinkle agents.

• Journal of Applied Biological Chemistry
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• v.51 no.1
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• pp.7-12
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• 2008

The suitability of CPWs, by-products of the juice industry, was investigated as a source for the production of cosmeceuticals. Four kinds of CPWs, CW, CWE, CWER, and CWEA, were examined for their antioxidant potentials in terms of DPPH radical-scavenging ability for anti-wrinkle applications, inhibition of tyrosinase or melanin production for whitening products, and anti-inflammatory effects to treat various skin diseases such as atopic dermatitis and acne as well as for anti-bacterial activity against acne-inducing pathogens. Of the four extracts, CWER was the most potent tyrosinase inhibitor ($IC_{50}$ value: $109\;{\mu}g/mL$), and CWEA ($IC_{50}:\;167\;{\mu}g/mL$) showed good antioxidative effects. CWE and CWEA samples had dose-dependent inhibitory effects on the melanin production. The cytotoxic effects of the four CPWs were determined by colorimetric MTT assays using human keratinocyte HaCaT cells. Most extracts exhibited low cytotoxicity at $100\;{\mu}g/mL$. These results suggest CPWs are attractive candidates for topical applications on the human skin.

• Biomolecules & Therapeutics
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• v.22 no.1
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• pp.35-40
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• 2014

Resveratrol is a polyphenolic compound found in various natural products such as grapes and berries and possesses anti-cancer, anti-hyperlipidemia, and anti-aging properties. Recently, it has been reported that resveratrol inhibits ${\alpha}$-melanocyte-stimulating hormone signaling, viability, and migration in melanoma cells. However, these effects have not been confirmed in vivo, specifically brownish guinea pigs. To evaluate the potential of resveratrol as a regulator of melanin for hyperpigmentation therapy, the influence of resveratrol on pigmentation was investigated by ultraviolet B-induced hyperpigmentation in brownish guinea pig skin. We found that resveratrol reduced the expression of melanogenesis-related proteins tyrosinase, tyrosinase-related proteins 1 and 2, and microphthalmia-associated transcription factor in melanoma cells. Furthermore, topical application of resveratrol was demonstrated to significantly decrease hyperpigmentation on ultraviolet B-stimulated guinea pig skin in vivo. Based on our histological data, resveratrol inhibits melanin synthesis via a reduction in tyrosinase-related protein 2 among the melanogenic enzymes. This study is the first to provide evidence supporting resveratrol as a depigmentation agent, along with further clinical investigation of resveratrol in ultraviolet B-induced skin disorders such as hyperpigmentation and skin photoaging.

• Biomolecules & Therapeutics
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• v.29 no.1
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• pp.98-103
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• 2021

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.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.49 no.4
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• pp.307-312
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• 2023

Water chestnut is fruits of Trapa natans var. bispinosa grown wild in Korea. In this study, water chestnut was investigated for anti-pigmentation. Treatment with ethanolic extracts of water chestnut significantly reduced production of melanin in α-MSH simulated B16F10 cells. At 200 ㎍/mL ethanolic extracts of water chestnut, melanin contents were repressed by 43.26% compared to the control group. Additionally, ethanolic extracts of water chestnut reduced expression and activity of tyrosinase, key enzyme in melanogenesis, in α-MSH simulated B16F10 cells. Ethanolic extracts of water chestnut downregulated tyrosinase activity and expression to 23.65% and 62.35%, respectively. These results suggest that ethanolic extracts of water chestnut might be used as a promising whitening ingredients for inhibition of α-MSH-induced melanin synthesis and pigmentation.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.22 no.2
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• pp.82-91
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• 2009

Objectives : The purpose of this study is to investigate whitening effects and anti-wrinkle effects of a few 80% ethanol extracted herbal medicines. Methods : In the first study, a few 80% ethanol extracted herbal medicines were screened for their inhibitory activities against the tyrosinase. In the second study, a few 80% ethanol extracted herbal medicines were screened for their inhibitory activities against elastase. Results : 1. We showed 28%, 27% and 19% inhibitions of mushroom tyrosinase at 500 $\mu$g/ml concentration of ASR, AIF and ABR extracts and they were showed higher anti-tyrosinase activity than arbutin's. We also could observe that the decreased mushroom tyrosinase activities in RR, CML, LR, AGR and TH extracts. 2. RR, AF and ABR (final concentrstion 1 mg/ml) were appeared 60%, 98%, 83% of inhibitions of elastase activity, and they were showed higher anti-elastase activity than that of ursolic acid. We also could observe that the decreased elastase activities in AIF, AR, LR and CML extracts. Conclusions : These results suggest that ASR, AIF and ABR extracts contribute to the anti-melanin activities and represent potential sources of whitening agent, and RR, AF and ABR extracts contribute to the anti-elastase activities and represent potential sources of anti-wrinkle agent. These results suggest that some herbal medicines could be strong potential sources of inhibition about anti-aging and whitening effects for the skin.

• The Korea Journal of Herbology
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• v.32 no.2
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• pp.57-64
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• 2017

Objectives : Yam bean (Pachyrhizus erosus) possess various nutrients, it has been widely used as traditional cosmetic material in Indonesia. The aim of this study was to investigate the anti-oxidant activity and the anti-melanogenic effect of Yambean (Pachyrhizus erosus) extract and its fractions. Methods : The anti-oxidant activity of yam bean extract assessed based on total polyphenol, flavonoid contents, DPPH and ABTS radical scavenging assay. To evaluate anti-melanogenic effects and cytotoxicity of Yambean extract and its fractions, B16F10 melanoma cell was used. Results : In results, total polyphenol content of yam bean water extract (YW) and Yambean 70% ethanol extract (YE) were $1.18{\pm}0.03mg/g$ (mg of gallic acid/g of sample), $1.16{\pm}0.01mg/g$. Total flavonoid contents of YW, YE were $3.55{\pm}0.06mg/g$ (mg of naringin/g of sample), $1.78{\pm}0.03mg/g$. Moreover, YE scavenged DPPH and ABTS effectively in $4mg/m{\ell}$ compared to YW. Cytotoxicity of YE and its fractions in B16F10 melanoma cell was measured using MTT assays. It had no cytotoxicity up to $500{\mu}g/m{\ell}$. Melanin accumulation in B16F10 melanoma cell was induced using alpha-melanocyte stimulating hormone (${\alpha}-MSH$) and 3-isobutyl-1-methylxanthine (IBMX). B16F10 melanoma cell treated with $10-500{\mu}g/m{\ell}$ YE and hexane, ethyl acetate, butanol, $H_2O$ fractions for 24h. Non treated B16F10 melanoma cell (Control) markedly increased melanin contents. In contrast, YE ethylacetate fraction effectively suppressed melanin accumulation in a dose-dependent manner. Conclusion : In conclusion, these results suggest that Yambean extract has the potential as a cosmetic material which possess anti-oxidant and anti-melanogenic activities.