• Journal of Life Science
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• v.33 no.2
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• pp.115-128
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• 2023

The fruit of Vaccinum oldhami was separated and purified to obtain the compounds chlorogenic acid (CA), quercetin (QT), and quercitrin (QR). The electron-donating abilities of CA, QT, and QR at 1,000 ㎍/ml were 91.9%, 89.9%, and 77.4%, respectively QT and QR showed 99.5% and 91.4% ABTS⁺ radical scavenging ability at a 1,000 ㎍/ml concentration, respectively, and CA showed a 95% ability or higher at 100 ㎍/ml. Regarding tyrosinase inhibitory activity, CA, QT, and QR exhibited 29.5%, 34.7%, and 23.7% efficacy, respectively, at 1,000 ㎍/ml. Regarding the cell viability for melanoma cells (B16F10) assessed through MTT assay, CA, QT, and QR showed cell a viability of 80% or more at 100 ㎍/ml. To measure the deterrent of protein expression, CA affected TRP-1 and TRP-2 in accordance with increases in concentration. The protein expression inhibition rate of QT was excellent for TRP-1, TRP-2, and tyrosinase. CA was confirmed to have an excellent mRNA expression inhibitory effect against MITF, and the amount of mRNA expression of TRP-1, TRP-2, and tyrosinase decreased with an increase in the CA concentration. As the concentration of QT increased, the mRNA expression of MITF, TRP-2, and tyrosinase decreased. QR decreased the amount of mRNA as the QR concentration increased. The excellent antioxidant and whitening effects of CA, QT, and QR were thus confirmed.

• Journal of Pharmaceutical Investigation
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• v.38 no.3
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• pp.163-169
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• 2008

Liposomes are spherical vesicles composed of lipid bilayer membranes. However, the conventional liposomes have been found to be plagued by rapid opsonization and taken up by the reticuloendothelial system (RES), resulting in shortened circulation time and limited intracellular uptake to target cell. In this study, polyethyleneglycol-cationic liposomes (PCL) containing cationic lipid and DSPE-mPEG were prepared by thin film cast-hydration method. The PEG liposomes had approximately $97.0{\pm}1.3\;nm$ of mean particle diameter and $-21.7{\pm}1.2\;mV$ of zeta potential value. PCL had $96.4{\pm}1.8\;nm$ of mean particle diameter and $-8.7{\pm}1.1\;mV$ of zeta potential value with a decrease of about 10 mV compared to the PEG liposomes. Loading of model drug, doxorubicin (DOX), in liposomes were carried out by using remote loading method and the loading efficiency of DOX in liposomes was about $95.0{\pm}1.9%$. Intracellular uptake and cytotoxicity of PCL were higher than that of PEG liposomes to murine B16F10 melanoma cells. In addition, anti-tumor activity of PCL was similar to that of PEG liposomes on growth of A549 human lung carcinoma in BALB/c mice. Consequently, PCL modified with cationic lipid may be applicable as anticancer drug carriers that can increase intracellular uptake and therapeutic efficacy.

• The Journal of Korean Obstetrics and Gynecology
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• v.35 no.3
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• pp.24-36
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• 2022

Objectives: Excessive melanin production leads to skin pigmentation, which causes various cosmetic and health problems. Citrus unshiu Markovich peel (CS) and Cimicifuga dahurica (CD) have long been widely used as a oriental medicinal plant because of their pharmacological properties including anti-ulcer, anti-oxidant, and anti-inflammatory properties. Methods: In this study, we investigated the inhibitory effects of CS, CD extracts or CS:CD=1:2 mixture on melanogenesis according to the various extraction methods. CS and CD extracted were prepared by ethanol extraction (EE), ultrasonification extraction (USE), Supercritical extraction (SCE), reflux extraction (RE), respectively. Results: DPPH radical scavenging and tyrosinase inhibitory activity of CD extracts or CS:CD=1:2 mixture were increased in dose-dependent manners. In addition, we evaluated the effect of CS, CD extracts or CS:CD=1:2 mixture on tyrosinase activity and melanogenesis in α-melanocyte stimulating hormone-induced B16-F10 melanoma cells. CS, CD extracts or CS:CD=1:2 mixture significantly inhibited tyrosinase activity and melanogenesis at 10-200 ㎍/mL. Conclusions: Therefore, our study suggests that CS and CD extracts have potential as a safe treatment for excessive pigmentation or as a natural ingredient in cosmetics.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.4
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• pp.309-315
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• 2009

In our search for the natural cosmetic ingredients, we found that Euryale ferox seed extract exhibited the strong antioxidative activity. Five active compounds were isolated from the ethyl acetate extract through various chromatographic methods and their structures were determined by NMR and MS spectral analysis. These compounds were identified as fucosterol (1), 3-(4-hydroxy-3-methoxybenzyl)-4-[(7'R),5'-dihydroxy-3'-methoxybenzyl]tetrahydrofuran (2), resorcinol (3), pyrogallol (4) and 4-O-methylgallic acid (5).We evaluated the antioxidative, antielastase activities and melanogenesis inhibitory effects of these compounds. The $SC_{50}$ values of compounds 2 ~ 5 for free radical scavenging activity were $17.0\;{\sim}\;100.2\;{\mu}M$ and especially compounds 4 and 5 were 6-fold more effective than ferulic acid as a positive control. And compounds 2 ~ 4 inhibited human neutrophil elastase with $IC_{50}$ values of $18.8\;{\sim}\;78.2\;{\mu}M$ and compound 3 also inhibited melanin synthesis in B16F10 melanoma cells with an $IC_{50}$ value of $492.8\;{\mu}M$. These results suggest that Euryale ferox extract having a lot of various active ingredients may be useful as a natural multi-functioning agent.

• Journal of Life Science
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• v.27 no.2
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• pp.139-148
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• 2017

The inhibition of tyrosinase, a key enzyme in mammalian melanin synthesis, plays an important role in preventing skin pigmentation and melanoma. Therefore, tyrosinase inhibitors are very important in the fields of medicine and cosmetics. However, only a few tyrosinase inhibitors are currently available because of their toxic effects on skin or lack of selectivity and stability. Therefore, we synthesized a novel series of (E)-2-(substituted benzylidene)-2,3-dihydro-1H-cyclopenta[a]naphthalen-1-one derivatives and evaluated their inhibitory effects on mushroom tyrosinase, with the aim of discovering a novel tyrosinase inhibitor. Among 19 derivatives, MHY3655 ($IC_{50}=0.1456{\mu}M$) showed the strongest inhibitory effect on tyrosinase activity compared to kojic acid ($IC_{50}=17.2{\mu}M$), a well-known tyrosinase inhibitor. In addition, MHY3655 showed competitive inhibition on Lineweaver-Burk plots. We confirmed that MHY3655 strongly interacts with mushroom tyrosinase residues through the docking simulation. Substitutions with a hydroxy group at both R2 and R4 in the phenyl ring indicated that these groups play a major role in the high binding affinity to tyrosinase. Further, MHY3655 did not show cytotoxicity at the concentrations tested in B16F10 melanoma cells. In conclusion, the novel compound MHY3655 potentially shows tyrosinase inhibitory activity, and it could be used as an ingredient in whitening cosmetics.

• Food Science and Preservation
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• v.22 no.2
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• pp.261-266
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• 2015

In this study, we investigated the applicability of functional materials by examining various physiological activities with an extract from the Agrimonia pilosa root. The A. pilosa extract showed low cytotoxicity against murine melanoma B16F10 cells. With little or no cytotoxicity at various concentrations, the A. pilosa extract showed high levels of DPPH radical scavenging activity ($ID_{50}$, 20.70 mg/L) and anti-microbial activity against Bacillus subtilis, Escherichia coli, and Candida albicans. In particular, it had a high level of anti-microbial activities against Gram-positive bacteria. These results suggest that the A. pilosa extract can be used as a natural preservative. It also showed inhibition of tyrosinase activity ($ID_{50}$, 90.18 mg/L), as does kojic acid ($ID_{50}$, 89.13 mg/L), and especially, a higher decrease in melanin content ($ID_{50}$, 62.5 mg/L) than the arbutin level ($ID_{50}$, 100.7 mg/L) as a positive control. These findings suggest that the A. pilosa extract inhibits melanin synthesis by suppressing the intracellular tyrosinase expression. These results indicate that the A. pilosa extract may be an effective material for functional cosmetics, such as skin whitening materials.

• The Journal of Korean Medicine
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• v.38 no.4
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• pp.62-81
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• 2017

Objectives: As interests in the beauty of skin is growing continuously, more people are focusing on white and clean skin. Melanin is the major factor that determines skin color. The abnormal concentration of melanin causes various skin diseases such as vitiligo, freckles, and melasma. This study investigated the inhibitory effect of Eriobotryae Folium extracts (EF) with phreatic water (PW) on the melanin synthesis. Methods: The effect of EF on melanin synthesis was evaluated by using mouse melanoma cells (B16F10). To define the mechanisms, real-time PCR and western blot were used. We also evaluated the inhibitory effects of EF and PW on melanin synthesis by using HRM-2 melanin-possessing hairless mice. After UVB irradiation, melanin differences between the skin parts that were treated and untreated with EF and PW. Levels of mRNA were measured by real-time quantitative PCR and histological analysis of the dorsal skin was conducted by hematoxylin and eosin staining. Results: EF inhibited various mechanisms of melanogenesis, and the effect was increased when combined with PW. In vitro experiments have shown that EF inhibited the expressions of tyrosinase related protein-1 (TRP-1) mRNA, tyrosinase mRNA, microphthalmia-associated transcription factor (MITF) mRNA and the tyrosinase inhibitory activation, but it stimulated the extracellular regulated kinase (ERK) mRNA expression. In vivo experiments have shown that EF prevented melanogenesis in the mice dorsal skin and inhibited TRP-1 mRNA expression. Also these effects were increased when combined with PW. Conclusions: EF and PW might be a new and effective treatment for whitening and treating pigmentation of skin.

• Journal of Physiology & Pathology in Korean Medicine
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• v.30 no.1
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• pp.47-53
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• 2016

Kaempferia galanga L. is one of the plants in Zingiberaceae family. It is used by people in many regions of Asia and Africa for relieving toothache, abdominal pain, muscular swelling and rheumatism. Tyrosinase is a key enzyme for melanogenesis, and hyperpigmentation is associated with abnomal accumulation of melanin pigment. This study aimed to investigate the inhibition of melanogenesis by hexane extract of Kaempferia galanga L. (HKG) in B16F10 melanoma cells. Cell-free tyrosinase, melanin contents, intracellular tyrosinase activity and western blot analysis were performed to elucidate the effects on anti-melanogenesis. Cytotoxicity of the extracts was measured using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and determined the concentration of 12.5, 25 μg/ml. HKG significantly inhibited to activities of intracellular tyrosinase and melanin synthesis in the absence or presence of α-melanocyte stimulating hormone (α-MSH) with dose-dependent manner. And HKG inhibited the expression of tyrosinase, tyrosinase-related protein 1 (TRP-1) and tyrosinase-related protein 2 (TRP-2), regardless of the presence or absence of α-MSH. HKG also down-regulated phosphorylation of p38 and JNK, and up-regulated phosphorylation of Akt. These effects were not related to its cytotoxicity action. These results indicate that HKG has the potential to be a useful therapeutic agent for treating hyperpigmentation disorders and as a beneficial additive in whitening agents in cosmetics industry.

• Journal of Microbiology and Biotechnology
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• v.28 no.7
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• pp.1061-1067
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• 2018

The anti-melanogenic effects of the extract of Angelica tenuissima (AT) root and the extract of AT root fermented by Aspergillus oryzae (FAT) were investigated. These effects were determined by measuring the inhibitory activity of AT and FAT on melanin production in B16F10 melanocytes and with in vitro tyrosinase activity assays. The AT extract inhibited melanin production at concentrations above $250{\mu}g/ml$, and this inhibitory effect was significantly enhanced by the fermentation process with A. oryzae. HPLC analysis resulted in the isolation of two active compounds from both the AT and FAT extracts. Their chemical structures were identified as decursin and Z-ligustilide through comparison with previously reported NMR data. The decursin and Z-ligustilide contents were increased in the FAT extract and could be responsible for its enhanced inhibitory effects on melanin production and tyrosinase activity compared with that of the AT extract.

• Korean Journal of Medicinal Crop Science
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• v.22 no.5
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• pp.331-338
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• 2014

Dendrobium moniliforme (DM) is a valuable and versatile herbal medicine with the anecdotal claims of antioxidant and anti-inflammation. In the present study, we investigated the whitening and anti-wrinkling effects of DM under various conditions with B16F10 melanoma cells and human dermal fibroblasts. The DM extract inhibited melanin contents and tyrosinase activity in a dose-dependent manner, compared with untreated group. Treatment of the DM extract effectively suppressed the ${\alpha}$-MSH-stimulated melanin formation, tyrosinase activity and dendrite outgrowth. Moreover, the ${\alpha}$-MSH-induced mRNA expressions of tyrosinase-related protein-1 (TRP-1) and tyrosinase-related protein-2 (TRP-2) and protein expression of tyrosinase were significantly attenuated by DM treatment. We also investigated the DM increased the production of type I procollagen and inhibited TNF-${\alpha}$-induced mRNA expressions of MMP-1, -3 in the human dermal fibroblast. These results indicate that DM may be a great cosmeceutical ingredient for its whitening and anti-wrinkle effects.