• Journal of Physiology & Pathology in Korean Medicine
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• v.22 no.3
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• pp.649-653
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• 2008

The aqueous extract from Asiasari radix (AEAR) was used to investigate the effect of ${\alpha}$-melanocyte stimulating hormone induced melanogenesis in B16F10 mouse melnoma cells. The treatment with AEAR at the 1.0 and 2.0 mg/ml level significantly inhibited the biosynthesis of melanin without changes of cell growth and morphology compared with untreated control. The AEAR-treated cells at the 2.0 mg/ml level were more efficient than commercial arbutin at 0.1 mg/ml. The tyrosinase activity also significantly decreased in AEAR-treated cells at the 1.0 and 2.0 mg/ml level. The Western analyses confirmed the slightly decreased expression of tyrosinase by AEAR treatment. These results indicate that AEAR may contribute to the inhibition of melanin biosynthesis through regulating tyrosinase activity and expression and serve as a new candidate in the design of new skin-whitening or therapeutic agents.

• Natural Product Sciences
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• v.14 no.1
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• pp.1-11
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• 2008

Peroxynitrite ($(ONOO^-)$ is a cytotoxic species formed from nitric oxide and superoxide anion, which are highly implicated in the pathogenesis of oxidative stress-mediated diseases. The aim of this study was to investigate the scavenging effects of Phellinus linteus on authentic $ONOO^-$, and further phytochemical studies are planned that will attempt to identify the active principles. From the active EtOAc fraction, a mixture of fungisterol and 5-dihydroergosterol (1), a mixture of betulin and 1,2-benzenedicarboxylic acid bis (2-methyl heptyl) ester (2), protocatechualdehyde (3), protocatechuic acid (4), cirsiumaldehyde (5), hispidin (6), caffeic acid (7), phelligridin D (8), uracil (9), gallic acid (10), 2,5-dihydroxybenzoic acid (11), ferulic acid (12), 2,3-dihydroxybenzaldehyde (13), arbutin (14), isoferulic acid (15), guanosine (16), and ellagic acid (17) were isolated, and their structures were characterized based on spectroscopic data. All compounds except 3, 6, 7 and 16 were isolated for the first time from P. linteus. Compounds 3, 4, 6-8, 10-15, and 17 showed potent scavenging activity on $ONOO^-$, with $IC_{50}$ values of $2.06\;{\pm}\;0.10$, $3.45\;{\pm}\;0.57$, $0.71\;{\pm}\;0.05$, $2.78\;{\pm}\;0.36$, $5.42\;{\pm}\;0.26$, $1.13\;{\pm}\;0.02$, $1.82\;{\pm}\;0.17$, $0.91\;{\pm}\;0.19$, $1.59\;{\pm}\;0.09$, $1.88\;{\pm}\;0.07$, $1.22\;{\pm}\;0.37$, and $2.01\;{\pm}\;0.02\;{\mu}M$, respectively, as compared to the positive control, DL-penicillamine, with an $IC_{50}$ value of $5.04\;{\pm}\;0.06\;{\mu}M$.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.25 no.1
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• pp.69-88
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• 1999

Several solvent extracts from Alpinia katsumudai were prepared and their various anti-inflammatory activities were evaluated. Alpinia katsumadai extract showed high various anti-inflammatory effects among the 8 medicinal plant extracts, Butanol extract from Alpinia katsumndai showed a potent anti-oxidative and free radical scavenging activities, Free radical scavenging effect of butanol fraction of Alpinia katsumadai($IC_{50}$/ : 50$\mu$g/m$\ell$) was higher than butylated hydroxytoluene($IC_{50}$/ : 50$\mu$g/m$\ell$) and ascorbic acid($IC_{50}$/ : 22$\mu$g/m$\ell$). Alpinia katsumadai butanol fraction exhibited relatively high antioxidative activity($IC_{50}$/ : 335$\mu$g/m$\ell$) compared to ascorbic acid. The inhibitory effect of Alpinia katsumadal ethanol extract on elastase exhibited 10 to 78% at 100 to 1000$\mu$g/m$\ell$ concentration , tile $IC_{50}$/ values with 465.7$\mu$g/m$\ell$ for porcine pancreatic elastase(PPE) and 481.9$\mu$g/m$\ell$ for human leukocyte elastase(HLE), respectively The Alpinta katsumadai extract inhibited effectively hyaluronidase activity($IC_{50}$/ 335$\mu$g/m$\ell$), and showed inhibition in vitro on delayed hypersensitivity when it was topically applied. These results suggest that Alpinia katsumadai extract may reduce inflammatory skin trouble. The Alpinia katsumadai extract also showed higher Inhibitory effect of melanin biosynthesis on cultured melanoma cell compared to arbutin and kojic acid.

• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1226-1232
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• 2004

Extracts from seventeen seaweeds were determined for tyrosinase inhibitory activity using mushroom tyrosinase with L-tyrosine as a substrate. Only one of them, Ecklonia stolonifera OKAMURA (Laminariaceae) belonging to brown algae, showed high tyrosinase inhibitory activity. Bioassay-guided fractionation of the active ethyl acetate (EtOAc) soluble fraction from the methanolic extract of E. stolonifera, led us to the isolation of phloroglucinol derivatives [phloroglucinol (1), eckstolonol (2), eckol (3), phlorofucofuroeckol A (4), and dieckol (5)]. Compounds 1~5 were found to inhibit the oxidation of L-tyrosine catalyzed by mushroom tyrosinase with $IC_{50}$ values of 92.8, 126, 33.2, 177, and 2.16 ${\mu}g$ /mL, respectively. It was compared with those of kojic acid and arbutin, well-known tyrosinase inhibitors, with $IC_{50}$ values of 6.32 and 112 ${\mu}g$ / mL, respectively. The inhibitory kinetics analyzed from Lineweaver-Burk plots, showed compounds 1 and 2 to be competitive inhibitors with $K_i$ of $2.3{\times}10^{-4}\;and\;3.1{times}10^{-4}$ M, and compounds 3~5 to be noncompetitive inhibitors with $K_i$ of $1.9{\times}10^{-5},\;1.4{\times}10^{-3}\;and\;1.5{\times}10^{-5}$ M, respectively. This work showed that phloroglucinol derivatives, natural compounds found in brown algae, could be involved in the control of pigmentation in plants and other organisms through inhibition of tyrosinase activity using L-tyrosine as a substrate.

• Archives of Pharmacal Research
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• v.22 no.4
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• pp.335-339
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• 1999

The oxidation-reduction potentials of cosmetic raw materials, showing tyrosinase inhibitory action, and phenolic compounds structurally similar to L-tyrosine were determined by cylcic voltammetry. The voltammograms obtained could be classified ito 4 patterns (patterns 1-4). Patterns 1, characterized by oxidation and reduction peaks as a pair, was observed with catechol, hydroquinone or phenol, and pattern 2 exhibiting another oxidation peak in addition to oxidation and reduction peaks as a pair was found with arbutin, kojic acid, resorcinol, methyl p-hydroxybenzoate and L-tyrosine as the substrate of tyrosinase. Pattern 3 with an independent oxidation peak only was expressed by L-ascorbic acid, and pattern 4 with a reduction peak only at high potentials, by hinokitiol. The tyrosinase inhibitory activity of these compounds was also evaluated using the 50% inhibitory concentration ($IC_{50}$) and the inhibition constant (Ki) as parameters. Hinokitiol, classified as patterns 4, showed the highest inhibitory activity (lowest $IC_{50}$ and Ki). Hydroquinone showing the second highest activity belonged to pattern 1, which also included compounds exhibiting pattern 2 was relatively low with Ki values being in the order of 10-4 M. Although there was no consistent relationship between oxidation-reduction potentials and tyrosinase inhibitory action, the voltammetry data can be used as an additional index to establish the relationship between the structure and the tyrosine inhibitory activity.

• Preventive Nutrition and Food Science
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• v.15 no.3
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• pp.213-220
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• 2010

To examine the potential of Terminalia chebula as a whitening agent, we measured antioxidant activity using DPPH$\cdot$, ABTS${\cdot}^+$ assays and ferric-reducing antioxidant power (FRAP) assays, and depigmenting activity using B16F10 melanoma cells. The intracellular reactive oxygen species (ROS) level was monitored by $H_2DCFDA$ fluorescence labeling, and melanin contents in B16F10 melanoma cells by 960 $J/m^2$ dose of UVA-induced oxidative stress. The radical-scavenging activities of T. chebula extract (TCE) were measured in terms of $EC_{50}$ values using DPPH$\cdot$, ABTS${\cdot}^+$ assays and FRAP value were 280.0 ${\mu}g/mL$, 42.2 ${\mu}g/mL$ and 113.1 ${\mu}mol$ $FeSO_4{\cdot}7H_2O/g$, respectively. We found that ROS and melanin concentrations were reduced by TCE treatments of 25 ${\mu}g/mL$ under UVA-induced oxidative stress. Tyrosinase activity and melanin contents in $\alpha$-melanocyte stimulating hormone (MSH)-induced melanoma cells both decreased dose-dependently in the treatment groups. TCE similarly reduced melanogenesis in B16F10 melanoma cells stimulated by $\alpha$-MSH as compared to arbutin as a positive control. T. chebula may prove to be a useful therapeutic agent for hyperpigmentation and an effective component in skin whitening and.or lightening cosmetics.

• Journal of Microbiology and Biotechnology
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• v.30 no.9
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• pp.1436-1442
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• 2020

Amylosucrase (ASase, E.C. 2.4.1.4) is capable of efficient glucose transfer from sucrose, acting as the sole donor molecule, to various functional acceptor compounds, such as polyphenols and flavonoids. An ASase variant from Deinococcus geothermalis, in which the 226^th alanine is replaced with asparagine (DgAS-A226N), shows increased polymerization activity due to changes in the flexibility of the loop near the active site. In this study, we further investigated how the mutation modulates the enzymatic activity of DgAS using molecular dynamics and docking simulations to evaluate interactions between the enzyme and phenolic compounds. The computational analysis revealed that the A226N mutation could induce and stabilize structural changes near the substrate-binding site to increase glucose transfer efficiency to phenolic compounds. Kinetic parameters of DgAS-A226N and WT DgAS were determined with sucrose and 4-methylumbelliferone (MU) as donor and acceptor molecules, respectively. The k_cat/K_m value of DgAS-A226N with MU (6.352 mM^-1min^-1) was significantly higher than that of DgAS (5.296 mM^-1min^-1). The enzymatic activity was tested with a small phenolic compound, hydroquinone, and there was a 1.4-fold increase in α-arbutin production. From the results of the study, it was concluded that DgAS-A226N has improved acceptor specificity toward small phenolic compounds by way of stabilizing the active conformation of these compounds.

• Journal of the Korean Society of Food Science and Nutrition
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• v.44 no.6
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• pp.832-839
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• 2015

The study analyzed the antioxidant and whitening activities of fractions from hot-air-dried Allium hookeri (HADAH). The total polyphenol contents in fractions from HADAH extract showed the highest value ($171.07{\pm}7.55mg/g$ GAE) in ethyl acetate fraction of roots. Antioxidant activities of leaf and root parts were significantly higher in the ethyl acetate fraction. HADAH showed higher whitening activity (n-hexane fraction of leaf; 52.22% melanin production) than arbutin (65.82% melanin production), which is known as a whitening ingredient. These results suggest that HADAH extracts can be used as antioxidant and whitening materials. Thus, study of HADAH extracts showing effective whitening and physiological activities can provide efficient data for industrial use of Allium hookeri.

• Korean Journal of Plant Resources
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• v.28 no.2
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• pp.153-157
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• 2015

In this study, we investigated the applicability of functional materials by examining a variety of physiological activities with the extract of Cleyera japonica leaf. Cleyera japonica extract showed a low cytotoxicity against murine melanoma B16F10 cells. In little or no cytotoxicity at concentrations, we showed that the treatment with Cleyera japonica extract resulted in a significant increase in the DPPH radical scavenging activity (IC₅₀, 22.90 ㎎/L), similar to ascorbic acid (IC₅₀, 18.65 ㎎/L) and anti-microbial activities against Bacillus subtilis, Escherichia coli, and Candida albicans. In particular, anti-microbial activities against Gram-positive bacteria was high. These results suggest that Cleyera japonica extract could be used as a natural preservative. Additionally, Cleyera japonica extract showed the inhibition of tyrosinase activity (IC₅₀, 178.90 ㎎/L), similar to kojic acid (IC₅₀, 89.13 ㎎/L) and decreased melanin content (IC₅₀, 101.90 ㎎/L) higher than the control arbutin level (IC₅₀, 100.65 ㎎/L), especially. Therefore, these results indicate that Cleyera japonica extract may be an effective material for functional cosmetics such as skin whitening materials.

• ALGAE
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• v.34 no.2
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• pp.177-185
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• 2019

Ecklonia cava is popular in Korea as a marine functional materials. E. cava is generally collected and used on the coast of Jeju Island. However, the continuous use of collected natural E. cava may be limited because difficult to secure throughout the year and may be exposed to environmental pollution. Jeju magma seawater (MSW) was known to be significant advantages such as safety, cleanness, stability, and functional improvement. Attempts have been reported on application of MSW to the culturing of macro- and microalgae and showed improved results. Thus, the objective of the present study was to explore the anti-melanogenesis activity of brown seaweed E. cava (E. cava cultured with MSW [MSWE]) extract cultured in tanks with MSW of Jeju Island to evaluate the possibility of cosmeceutical industrial application. MSWE extract showed the higher polyphenolic and dieckol contents than natural E. cava (NE) extract. Anti-melanogenesis activity of MSWE extract and NE extract are tested and compared using tyrosinase and dihydroxyphenylalanine (DOPA) oxidation inhibition assay. MSWE extracts evidenced more effective tyrosinase and DOPA oxidation inhibition activity than that of the NE extracts and the commercial whitening agent, arbutin. MSWE extracts also markedly inhibited melanin synthesis and decreased the expression of melanogenesis-related protein in ${\alpha}$-melanocyte stimulating hormone-stimulated B16F10 melanoma cells without cytotoxicity. These results suggest that MSW cultivation process would be more effective in releasing bioactive compounds with whitening effect from seaweed such as E. cava at an industrial scale.