• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.1
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• pp.73-78
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• 2009

In order to investigate the potential of a Dayflower (Commelina communis L.) extract as an active in gredient for whitening cosmetics, we prepared aqueous Commelina communis L. extract We measured its mushroom tyrosinase inhibitory activity, cellular tyrosinase activity, and melanin synthesis inhibitory activity in B16 melanoma cells. It did not show inhibitory activity against mushroom tyrosinase but showed melanin synthesis inhibitory activity. In a melanin synthesis inhibition assay using mouse B16-F10 melanoma cell, it suppressed melanin production up to 32% at a concentration of $1,000{\mu}/mL$ without cytotoxicity, and also reduced cellular tyrosinase activity to above 50 % above the concentration of $250{\mu}g/mL$. In study on the melanogenic protein expressions, it had especially influence on expression of tyrosinase protein, which is a well-known key protein on melanogenesis, and tyrosinase expression was gradually decreased in a dose-dependent. Dayflower also blocked N-glycosylation of TRP-2, but affected on the expression of TRP-1 rather than on blocking of N-glycosylation processing. Therefore, this result suggests that aqueous Commelina communis L. extract could be used as an active ingredient for whitening cosmetics.

• Bulletin of the Korean Chemical Society
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• v.28 no.5
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• pp.758-762
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• 2007

A new alkyldithiocarbonate (xanthate), as sodium salts, C2H5OCS2Na, was synthesized by the reaction between CS2 with ethyl alcohol in the presence of NaOH. The new xanthate was characterized by 1H NMR, IR and elemental analysis. Then, the new synthesized compound was examined for functional study of cresolase activity of Mushroom Tyrosinase (MT) from a commercial source of Agricus bisporus in 10 mM phosphate buffer pH 6.8, at three temperatures of 10, 20 and 33℃ using UV spectrophotemetry. 4-[(4-methylphenyl)- azo]-phenol (MePAPh) was used as a synthetic substrate for the enzyme for cresolase reaction. The results show that ethyl xanthate can activate or inhibit the cresolase activity of mushroom tyrosinase depending to the concentration of ethyl xanthate. It was concluded that the enzyme has two distinct sites for ethyl xanthate. The first one is a high-affinity activation site and the other is a low-affinity inhibition site. Activation of the enzyme in the low concentration of ethyl xanthate arises from increasing the affinity of binding for the substrate as well as increasing the enzyme catalytic constant. The affinity of ligand binding in the activation site is decreased by increasing of the temperature, which is the opposite result for the inhibition site. Hence, the nature of the interaction of ethyl xanthate is different in two distinct sites. The binding process for cresolase inhibition is only entropy driven, meanwhile the binding process for cresolase activation is not only entropy driven but also enthalpy driven means that hydrophobic interaction is more important in the inhibition site.

• Natural Product Sciences
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• v.11 no.2
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• pp.89-91
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• 2005

Effect of the neolignans, honokiol (1) and magnolol (2), isolated from Magnoliae Cortex on mushroom tyrosinase activity was investigated in vitro using L-tyrosine as a substrate. Honokiol (1) inhibited tyrosinase activity significantly in a concentration-dependent manner, on the other hand, magnolol (2) did not show tyrosinase inhibitory effect. Honokiol exhibited tyrosinase inhibitory effect with $IC_{50}$ value of $67.9\;{\mu}M$, and proved to act as a non-competitive inhibitor by the analysis of Lineweaver-Burk plot.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.16 no.2
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• pp.96-118
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• 2003

The effect of Glycyrrhizae Radix water extract, known as depigmenting agent, on melanin biosynthesis was investigated in cellular level by using B16 mouse melanoma cells. The inhibitory effect of Glycyrrhizae Radix water extract on melanogenesis was determined by mushroom tyrosinase assay traditionally using in vitro screening test. To determine whether Glycyrrhizae Radix water extract suppress melanin synthesis in cellular level, B16 mouse melanoma cells were cultured in the presence of different concentrations of Glycyrrhizae Radix water extract. Effects on cell proliferation, melanin biosynthesis, tyrosinase activity, DOPAchrome tautomerase activity, and expression level of mRNA for tyrosinase were examined. The maximum concentration of Glycyrrhizae Radix water extract that was not inhibitory to growth of the cells was 2 mgml. At that concentration, melanin synthesis was significantly inhibited without cytotoxicity after 5 days, compared with untreated cells. The treatment with Glycyrrhizae Radix water extract reduced tyrosinase and DOPAchrome tautomerase activity in a dose-dependent manner. However, the treatment with Glycyrrhizae Radix water extract did not affect significantly mRNA levels for tyrosinase. These results suggest that the inhibitory effect of Glycyrrhizae Radix water extract on melanogenesis is correlated with the suppression of tyrosinase and DOPAchrome tautomerase activity more than altering mRNA levels of tyrosinase.

• Journal of Microbiology and Biotechnology
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• v.20 no.6
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• pp.988-994
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• 2010

The EtOAc fraction of Lespedeza cyrtobotrya showed mushroom tyrosinase inhibitory and radical scavenging activities. Four active compounds were isolated based on Sephadex LH-20 chromatography and HPLC, and the structures were elucidated, on the basis of their LC-MS and NMR spectral data, as 2-(2,4-dihydroxyphenyl)-6-hydroxybenzofuran (1), eriodictyol-7-O-glucopyranoside (2), haginin A (3), and dalbergioidin (4), respectively. Compound (1) showed mushroom tyrosinase inhibitory activity with an $IC_{50}$ value of $5.2\;{\mu}M$ and acted as a competitive inhibitor. Furthermore, $37.3\;{\mu}M$ of compound 1 reduced 50% of the melanin content on human melanoma (MNT-1) cells. The radical scavenging activities of compounds 1, 2, 3, and 4 were shown to have $IC_{50}$ values of 11.0, 24.5, 9.0, and $36.5\;{\mu}M$, respectively, in an ABTS system and $IC_{50}$ values of 42.7, 36.0, 37.7, and $61.7\;{\mu}M$, respectively, in a DPPH system. The mushroom tyrosinase inhibitory activity of the EtOAc fraction of Lespedeza cyrtobotrya was contributed by compounds 1, 3, and 4, and its radical scavenging activity was contributed by compounds 1-4.

• Journal of Microbiology and Biotechnology
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• v.29 no.8
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• pp.1204-1211
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• 2019

Fungal exopolysaccharides are important natural products having diverse biological functions. In this study, exopolysaccharides from Fomitopsis castanea mycelia (FEPS) were prepared, and the highest mushroom tyrosinase inhibitory activity was found. FEPS were prepared from cultivation broth by ethanol precipitation method. The extraction yield and protein concentration of FEPS were 213.1 mg/l and 0.03%, respectively. FEPS inhibited mushroom tyrosinase with the half maximal inhibitory concentration ($IC_{50}$) of 16.5 mg/ml and dose-dependently inhibited cellular tyrosinase activity (63.9% at $50{\mu}g/ml$, and 83.3% at $100{\mu}g/ml$) in the cell-free extract of SK-MEL-5 human melanoma cell and ${\alpha}$-melanocyte-stimulating hormone (${\alpha}-MSH$)-stimulated melanin formation in intact SK-MEL-5 human melanoma cell. The $IC_{50}$ of FEPS against NO production from RAW264.7 macrophage cells was $42.8{\pm}0.64{\mu}g/ml$. By in vivo study using a zebrafish model, exposure of FEPS at $400{\mu}g/ml$ to dechorionated zebrafish embryos for 18 h decreased the pigment density, compared to that without FEPS-treated control.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.32 no.3 s.58
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• pp.153-160
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• 2006

We synthesized 2',4'-dimethoxyflavone and investigated the effects on melanogenesis. To determine the effects as a whitening agent, various in uitro tests were performed such as free radical scavenging activity, melanin assay, tyrosinase activity and expression of tyrosinase, TRP-1 and TRP-2 (western blot and RT-PCR) in Bl6 melanoma cells. 2',4'-Dimethoxyflavone showed neither free radical scavenging activities against 1,1- diphenyl -2-picrylhydrazvl (DPPH) radical and inhibition of mushroom tyrosinase activity, 2',4'-dimethoxyflavone significantly inhibited melanin production in B16 melanoma cells. 2',4'-Dimethoxyflavone treatment (48h) suppressed the biosynthesis of melanin up to 27% at $5{\mu}g/mL$ and reduced tyrosinase activity up to 20% at $5{\mu}g/mL$ in B16 melanoma cells. 2',4'-Dimethoxyflavone was also able to significantly inhibit tyrosinase and TRP-1 expression in protein and mRNA level. These results suggest that 2',4'-dimethoxyflavone inhibits melanin biosynthesis at the level of enzyme activity and protein mRNA expression B16 melanoma cells. Therefore, 2',4'-dimethoxyflavone may be useful as a new whitening agent in cosmetics.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.1
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• pp.33-38
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• 2004

Melanin pigmentation in human skin is a major defense mechanism against ultraviolet light of the sun, but abnormal pigmentation such as freckles, liver spot could be a serious aesthetic problem. Nearly all studies are mainly concentrated on searching for the materials that have inhibitory activities on tyrosinase. In this work, to isolate phenolic compounds from Gastrodia elata, we purified the extract through solvent fractionation, column chromatography, and recrystallization. They were identified as 4-hydroxybenzyl alcohol 1, bis(4-hydroxyphenyl)methane 2, gastrodin (4-${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 on the base of spectroscopic evidences. In order to investigate their depigmentation effect, inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cells were evaluated in vitro. We have found that 4-hydroxybenzyl alcohol 1 and gastrodin (4- ${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 have no tyrosinase inhibitory activity, but inhibit the melanin synthesis in B16 melanoma cells. Tyrosinase inhibitory activities of bis(4-hydroxyphenyl)methane 2 (IC$\_$50/ = 400 $\mu\textrm{g}$/mL) and butanol fraction (IC$\_$50/ = 46 $\mu\textrm{g}$/mL) were lower/higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL), but inhibitory activities of melanin synthesis in B16 melanoma cells were much higher than that of arbutin. Especially, tyrosinase inhibitory activities of isolated phenolic fraction (IC$\_$50/ = 2.37 $\mu\textrm{g}$/mL) from butanol fraction was very higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL). Therefore, these results suggest that isolated phenolic compounds from Gastrodia elata have inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in 816 melanoma cells in vitro.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.22 no.2
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• pp.193-200
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• 1996

In eastern Asian region, cosmetic preparations containing the molecues possessing the whitening activity are promising. In this study, 100 plant extracts were screened in order to elucidate the whitening effects using in vitro tyrosinase assay and DOPA autooxidation. Several plant extracts such as Morus alba, Glycyrrhiza glabra showed the inhibitory activity (>50%) against mushroom tyrosinase at the concentration 333$mu extrm{m}$/ml. And plant extracts including Morus alba and Bupleurum falcatum showed the inhibitory activity (>50%) at the concentration of 500($\mu\textrm{g}$/ml against DOPA autooxidation. The IC50 values of the several extracts were also found.

• Natural Product Sciences
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• v.29 no.2
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• pp.59-66
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• 2023

The anti-melanogenic activity of 259 actinomycete strains was tested, and based on the results for the inhibition of mushroom tyrosinase activity and the reduction in melanin content, Micromonospora sp. JCS1 and JCS7 were selected as the strains with the highest anti-melanogenic potential. The activity-guided fractionation of extracts from JCS1 and JCS7 led to the isolation of the dipeptides cyclo(ʟ-Phenyl alanine (Phe)-ʟ-Proline (Pro)) (1) and cyclo(ʟ-Tryptophan (Trp)-ʟ-Proline (Pro)) (2). These two compounds were tested for their inhibition of mushroom tyrosinase by monitoring ʟ-DOPA levels and melanin production. Cyclo(ʟ-Phe-ʟ-Pro) (1) and cyclo(ʟ-Trp-ʟ-Pro) (2) were thus confirmed to have the potential for use in functional whitening cosmetics containing actinomycete-derived secondary metabolites.