• Microbiology and Biotechnology Letters
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• v.44 no.1
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• pp.19-25
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• 2016

Sargassum micracanthum (SM) is a member of the family Sargassaceae and commonly occurs along the coast of Korea. Extracts from SM were evaluated for their antioxidant and collagenase and tyrosinase inhibitory activities based on their total phenolic concentration (TPC), 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging effect, and metal-chelating effect. The TPC of SM ethanol and water extracts used in the study was 11.20 and 11.70 mg/g of dry sample, respectively. Both SM ethanol and water extracts had high DPPH radical-scavenging effect. The metal-chelating effect of SM ethanol extract (40.47% at 0.5 mg/ml) was higher than that of water extract (23.28% at 0.5 mg/ml). With regard to the anti-wrinkling effect, SM ethanol extract showed collagenase inhibitory activity with an $IC_{50}$ value of $488.20{\mu}g/ml$. Lastly, regarding the anti-melanogenesis effect, SM ethanol extract showed higher tyrosinase inhibitory activity (45.08% at 5 mg/ml) than that shown by the water extract (21.29% at 5 mg/ml). These results suggest that SM has the potential to be a resource with natural anti-melanogenesis, anti-wrinkle, and anti-oxidant effects.

• Journal of Life Science
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• v.28 no.6
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• pp.745-752
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• 2018

Melanogenesis is involved in the pigmentation of the hair, eyes, and skin in living organisms. Various signaling pathways stimulated by ${\alpha}-MSH$, SCF/c-Kit, $Wnt/{\beta}-catenin$, nitric oxide and ultraviolet activate melanocyte, leading to melanin production by tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2 expressed via the microphthalmia-associated transcription factor (MITF). However, the abnormal regulation of melanogenesis causes dermatological issues such as graying hair and vitiligo. Therefore, the activators that promote melanogenesis are crucial for the prevention of graying hair and the treatment of hypopigmentary disorders. Many melanogenesis stimulators have been studied for the development of novel drugs derived from synthesized compounds and natural products. Here, in addition to providing a description of a common signaling pathway in the melanogenesis of graying hair and the vitiligo process for the development of novel anti-hair graying agents, this article reviews natural herbs and the active ingredients that promote melanin synthesis as a pharmaceutical agent for the treatment of vitiligo. In particular, compounds such as Imatinib and Sugen with a stimulating effect on melanogenesis as a side effect of the drugs, are also introduced. Recent advances in research on natural plant extracts such as Polygonum multiflorum, Rhynchosia Nulubilis, Black oryzasativa, and Orysa sartiva, widely known as traditional and medicinal extracts, are also reviewed.

• Natural Product Sciences
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• v.22 no.3
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• pp.193-200
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• 2016

This study describes the anti-inflammatory, anti-oxidant, and melanogenesis inhibition activities of methanol extract and various organic solvent fractions of Arecae Pericarpium. We examined the inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, 1,1-diphenyl-2-picrylhydrazine (DPPH) scavenging activity, mushroom tyrosinase inhibition activity and melanin contents. The study showed that, among all tested fractions, methylene chloride fraction showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells ($IC_{50}$ value $8.89{\mu}g/mL$) and DPPH radical scavenging activity ($EC_{50}$ value $21.39{\mu}g/mL$). Methylene chloride and ethyl acetate fractions similarly inhibited mushroom tyrosinase activity. Methanol extract exhibited strongest reduction of melanin content in B16F10 melanoma cells. Based on the bioactivity assay results, methylene chloride and ethyl acetate fractions were further separated. Eight phenolic compounds were isolated, which are dimeric syringol (1), catechol (2), 4-hydroxybenzaldehyde (3), vanillin (4), 4-hydroxyacetophenone (5), apocynin (6), protocatechuic acid (7) and 4-hydroxybenzoic acid (8). Among the isolated compounds tested, catechol showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells. Catechol also showed the concentration-dependent NF-${\kappa}B$ inhibition activity. Arecae Pericarpium might have potentials to be developed as anti-inflammatory agent or dermatological product for skin-whitening agent.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.20 no.1
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• pp.1-13
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• 1994

An antioxidative compound was isolated from pine needles. This compound was identified as 4-hydroxy-5-methyl-3[2H]-furanone on the basis of spectroscopic evidences. It scavenged 1,1-diphenyl-2-picrylhydrazyl free radicals more efficiently than maltol and tocopherol did. It exhibited an inhibitory effect on the lipid peroxidation of rat liver microsome induced by Fe(ll)/ascorbate, and the protective effect against UV cytotoxicity in cultured human fibroblasts. In addition, HMF appeared to prevent the cellular melanogenesis in the cultured murine melanoma cells, more effectively than kojic acid, a well known inhibitor of melanogenesis, while the former was not so effective as the latter for the inhibilion of the tyrosinase. Considering that cellular melanogenesis is a metabolic process triggered by oxidative stress, it was tentatively deduced that the antioxidative property of HMF may afford the effect against cellular pigmentation by alleviating the causative stress. This study provided a novel inhibitor of melanogenesis, that might be useful for the cosmetic applications.

• Biomolecules & Therapeutics
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• v.24 no.1
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• pp.85-93
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• 2016

We already reported that genetically engineered resveratrol-enriched rice (RR) showed to down-regulate skin melanogenesis. To be developed to increase the bioactivity of RR using calli from plants, RR was adopted for mass production using plant tissue culture technologies. In addition, high-pressure homogenization (HPH) was used to increase the biocompatibility and penetration of the calli from RR into the skin. We aimed to develop anti-melanogenic agents incorporating calli of RR (cRR) and nanoparticles by high-pressure homogenization, examining the synergistic effects on the inhibition of UVB-induced hyperpigmentation. Depigmentation was observed following topical application of micro-cRR, nano-calli of normal rice (cNR), and nano-cRR to ultraviolet B (UVB)-stimulated hyperpigmented guinea pig dorsal skin. Colorimetric analysis, tyrosinase immunostaining, and Fontana-Masson staining for UVB-promoted melanin were performed. Nano-cRR inhibited changes in the melanin color index caused by UVB-promoted hyperpigmentation, and demonstrated stronger anti-melanogenic potential than micro-cRR. In epidermal skin, nano-cRR repressed UVB-promoted melanin granules, thereby suppressing hyperpigmentation. The UVB-enhanced, highly expressed tyrosinase in the basal layer of the epidermis was inhibited by nano-cRR more prominently than by micro-cRR and nano-cNR. The anti-melanogenic potency of nano-cRR also depended on pH and particle size. Nano-cRR shows promising potential to regulate skin pigmentation following UVB exposure.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.43 no.1
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• pp.35-41
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• 2017

Melanin synthesis inhibition activities were investigated for the extracts prepared from the leaves of Carpinus turczaninowii (C. turczaninowii) by using B16F10 melanoma cells. As a result, the ethanol extract ($100{\mu}g/mL$) showed 72.2% inhibition activities without cell toxicities in MTT assays. For the solvent fractions (n-hexane, ethyl acetate, n-butanol, water), the most potent activities were observed at the ethyl acetate fraction. To isolate the active constituents, the ethyl acetate fraction was further purified to afford four compounds; ethyl gallate (1), quercetin rhamnose (2), kaempferol rhamnose (3) and quercetin galloylrhamnose (4). The identification of the isolates was made by spectroscopic data including NMR spectra, and all of the compounds 1-4 were isolated for the first time from the leaves of C. turczaninowii. Anti-melanogenesis activities were studied for the isolates 1-4, and the compound 4 was determined to decrease the melanin synthesis dose-dependently without causing cell toxicities. ELISA measurement indicated that the isolate 4 decreased the contents of cell tyrosinase, a critical enzyme in melanogenesis. Based on these results, the extracts of C. turczaninowii were found to be applicable as whitening ingredients in cosmetic formulations.

• Mycobiology
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• v.40 no.2
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• pp.117-123
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• 2012

Nuruk contributes to the unique characteristics of Korean alcoholic beverages. In this study, the effects of nuruk extracts (NE) on anti-oxidant characters, melanogenesis, and anti-photoaging activity were investigated. NEs were obtained from the 70% ethanol extracts of six types of nuruk, which have been used in brewing of fermented alcohol beverages in Korea. First, various antioxidant characteristics were identified in terms of 2,2'-azino-bis(3-ethylbenzthiozoline-6-sulphonic acid) (ABTS) radical scavenging activity, superoxide dismutase (SOD) expression, and inhibition of xanthine oxidase activity. NE#4 exhibited potent ABTS radical scavenging activity ($IC_{50}$ = 19.51 ${\mu}g$/mL). Compared with NE#4, relatively lower levels of activity were observed for NE#3 and NE#6, with $IC_{50}$ values of 90.99 and 76.88 ${\mu}g$/mL, respectively. According to results of western blot analysis for determination of SOD expression in $H_2O_2$-treated HepG2 cells, NE#5 and NE#6 induced a dramatic increase in the expression ratio of SOD, compared to the group treated with $H_2O_2$ only. Activity of xanthine oxidase, which converts xanthine into uric acid, generating superoxide ions, was inhibited by NE#4 and NE#6 in a dose-dependent manner. NE#4 induced significant inhibition of mushroom tyrosinase activity. A reduction in cellular melanin contents of 80% was observed in B16F1 melanocytes treated with NE#5 and NE#6; these effects were similar to those of arbutin at 100 ${\mu}M$. In addition, gelatin zymography and reverse transcription-PCR analysis were performed for assessment of anti-photoaging activity of Nuruk. Treatment with NE#6 resulted in dramatically inhibited activities of matrix metalloproteinase (MMP)-2/-9, suppressed expression of MMP-1, and increased expression of type-1 procollagen. Results of gelatin zymography for NE#4 and NE#5 were similar, to a slightly lesser degree. These results suggest the potential of NE#4 and NE#6 as natural ingredients for use in functional foods and cosmetics.

• Journal of the Korean Society of Food Science and Nutrition
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• v.43 no.11
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• pp.1695-1700
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• 2014

Oriental herbal liquor (Yakju) is a type of Korean traditional alcoholic beverage that uses Nuruk and oriental herbs for fermentation. The purpose of this study was to develop cosmetic ingredients using Jubak, which is a by-product of alcoholic fermentation of oriental herbal liquor. To investigate antioxidant, whitening, and anti-aging effects of Jubak, we prepared extract of Jubak and its solvent fractions. Ethyl acetate fraction (KSD E4-3) showed the most prominent free radical [1,1-diphenyl-2-picrylhydrazyl (DPPH)] scavenging activity ($SC_{50}$: 0.75 mg/mL). KSD E4-3 significantly inhibited in vitro mushroom tyrosinase activity ($IC_{50}$: 0.82 mg/mL) and reduced the melanin contents in mouse melanoma melanocyte, B16F10 cells. KSD E4-3 down-regulated protein expression of tyrosinase related proteins (TRP)-1, -2, which play key roles in melanogenesis. For anti-aging effects, inhibition of matrix metalloproteinase (MMPs) expression was evaluated using human keratinocyte, HaCaT cells. Treatment of HaCaT cells with KSD E4-3 reduced expression of MMP-1, -2, -9 and inhibited proteolytic activities of MMP-2, -9. These results suggest that KSD E4-3 induces down-regulation of cellular melanogenesis and protects against photoaging induced by UVB-induced damage. Thus KSD E4-3 could potentially be a valuable cosmetic ingredient.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.1
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• pp.57-63
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• 2009

UV irradiated skin cells produce reactive oxygen species (ROS). ROS is known to be the primary cause of skin inflammation that is eventually leading to skin aging through decrease of collagen in the dermis. In this study, we evaluated basic efficacy of anti-aging, anti-inflammation and anti-melanogenesis using two antioxidative mineral-bio waters (Mineral-bio water 1 (MIBA-W1) and Mineral-bio water 2 (MIBA-W2)). Both antioxidative mineral-bio waters reduced TNF-${\alpha}$ expression which was induced upon UV irradiation. MIBA-W 1 increased collagen synthesis from UVB irradiated fibroblast at 0.01 % concentration but MIBA-W2 shows slight, but linear increase. Stimulation of melanogenesis by ${\alpha}$-MSH treatment in the cultured B16-F1 melanoma was significantly reduced by the treatment of MIBA-W2 in a dose dependent manner. Taken together, antioxidative MIBA-W1 and 2 seem to have potential applications as functional cosmetic materials.

• Preventive Nutrition and Food Science
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• v.2 no.4
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• pp.285-290
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• 1997

Previously, a 50% aqueous methanol extract of Galla rhois was shown to be the most potent tyrosinase inhibition activity with an {TEX}$IC_{50}${/TEX}(the concentration causing 50% inhibition of tyrosinase activity) of 0.2mg/ml of 205 crude drug extracts. To isolate tyrosinase inhibitors, the methanol extract was evaporated to a small volume in vacuo, and then partitioned stepwise with benzene and ethyl acetate(EtOAc). the EtOAc fraction was solubilized in 10% MeOH solution, and then fractionated successively by Diaion HP-20 and Sephadex LH-20 column chromatography, and preparative HPLC. Three phenolic compounds were isolated, and characterized as gallic acid(GA), methyl gallate(MG) and 1,2,3,4,6-penta-O-galloyl-$\beta$-D-glucose(PGG) by UV, IR, {TEX}${1}^H${/TEX}-&{TEX}${13}^C${/TEX}-NMR, and FAB-MS spectroscopy, PGG({TEX}$IC_{50}${/TEX}=50$\mu\textrm{g}$/ml) showed a considerable inhibitory effect against mushroom tyrosinase, while GA({TEX}$IC_{50}${/TEX}=1.6mg/ml) and MG({TEX}$IC_{50}${/TEX}=234$\mu\textrm{g}$/ml) did not show an appreciable effect. Meanwhile, MG inhibited greatly melanogenesis in a murine melanocyte cell line, Mel-Ab. MG and PGG showed typical noncompetitive inhibition patterns against mushroom tyrosinase. These results suggest that PGG and MG may be potentially useful as either anti-browning or anti-melanogenic agents in foods and cosmetics.