• YAKHAK HOEJI
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• v.44 no.6
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• pp.601-606
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• 2000

Recently, studies on missile antitumor drugs, which selectively act on tumor cell and display drug effects, have been performed. These missile antitumor drugs which can increase drug effects and decrease side effects, are ideal medication method. Lectin has been reported as tumor cell specific binding protein and tannin as antitumor substance. In this study, we studied inhibition of melanoma metastasis by lectin-conjugated ellagitannin and used praecoxin A as ellagitannin source. Mouse melanoma cell, B16-F10, was injected into the sole of forefoot of C57BL/6 mouse, and after administration with drug, the number of pulmonary tumor colony was counted. The administration of praecoxin A, lectin-praecoxin A mixiture, and lectin-conjugated praecoxin A was started after amputation of established tumor foci at right forefoot of mice and continued for 3 weeks with i.p. injection of one of those drugs A every 24 hours. Lectin-praecoxin A mixture, and lectin-conjugated praecoxin A significantly reduced the number of spontaneous pulmonary metastasis. Exposure to 5 mg/kg of lectin-praecoxin A mixiture and lectin-conjugated praecoxin A produced a statistically significant 38.3%, 41.8% reduction in the number of remaining pulmonary metastasis. These results suggest that metastasis inhibition by lectin-praecoxin A mixiture and lectin-conjugated praecoxin A are better than that of praecoxin A.

• Animal cells and systems
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• v.8 no.2
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• pp.117-123
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• 2004

The purpose of this study was to analyze inhibitory effects of anti-4-1BB monoclonal antibody on melanoma metastasis The 4-1BB (CD137) T cell molecule is a member of the TNF receptor family and its activation by either 4-1BB ligand or antibody induces T cell activation and growth. In the present study, administration of anti-4-1BB mAb induced inhibition of melanoma metastasis. Agonistic anti-4-1BB mAb induced not only CD$8^+$4-1BBT cells but also CD$8^+$IFN-${\gamma}$$^{+}$ T cell population. In the presence of anti-CD3 antibody, lymphocytes produced high levels of IFN-${\gamma}$ and low levels of IL-4 in anti-4-1BB mAb treated group. Exposure of melanoma cells to IFN-${\gamma}$ induced expression of MHC-I molecules. Thus, the increase in number of CD$8^+$T cells and enhanced MHC-I expression on B16F10 cells by augmented IFN-${\gamma}$ production in response to anti-4-1BB mAb may result in suppression of tumor growth and metastasis.s.

• Journal of Physiology & Pathology in Korean Medicine
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• v.33 no.5
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• pp.267-274
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• 2019

This study aims to evaluate the effects of Shengmaisan (SMS) and three types of ShengmaisanJiaweifang on the inhibitory effect of melanin synthesis in B16F10 cells, the mechanism of action through tyrosinase, and the antioxidant effect through superoxide dismutase (SOD) activity. In this study, we used ShengmaisanJiaweifangs (SMS, SMSRR, SMSAD, SMSAR) to research the whitening effects in B16F10 cell lines. Shengmaisan (SMS) was a herbal medicine composed of Ginseng Radix, Liriopis Tuber, and Schisandrae Fructus. ShengmaisanJiaweifangs included SMSRR (SMS added with Rehmanniae Radix), SMSAD (SMS added with Asparagi Radix) and SMSAR (SMS added with Astragali Radix). We measured the cell viability, the inhibition rate of the melanin biosynthesis, and the activity of tyrosinase and SOD in malignant melanoma, B16F10 cells, to survey the whitening effect and the mechanism of the impact on the sample. As a result, SMSRR significantly suppressed the cell viability of B16F10 at more than $500{\mu}g/m{\ell}$ and significantly inhibited the generation of melanin induced by ${\alpha}$-MSH at more than $250{\mu}g/m{\ell}$. SMSRR ($500{\mu}g/m{\ell}$) decreased the activity of tyrosinase while increased the activity of SOD. Therefore, we considered that the SMSRR would be able to produce high value-added products more SMS if used as a commercial.

• 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.

• Herbal Formula Science
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• v.21 no.1
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• pp.91-98
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• 2013

Objective : The purpose of this study was to investigate the synergistic effect of Angelicae gigantis Radix (AG) and Lycii fructus (LF) ethanol extracts on skin-whitening effects. Method : LFAG extracts were prepared by extracting with 80% ethanol. The efficacy of LFAG was judged by measurement of cell viability, tyrosinase activity, melanin production, tyrosinase and microphthalmia-associated transcription factor (MITF) expression in B16F10 murine melanoma cells by lipopolysaccharides (LPS) treatment. Results : Each extract (LF or AG) inhibited the tyrosinase activity in a dose-dependent manner. The co-treatment of LFAG extracts ($25{\mu}g/mL$ LF plus $25{\mu}g/mL$ AG) markedly suppressed the LPS-induced cellular tyrosine activity, melanin production, tyrosinase and MMP-1 expression in B16F10 murine melanoma cells. These suppressive effects were synergistically increased by their combination. Conclusions : With these observations, we suggest that the extracts from Lycii fructus and Angelica gigantis Radix could be potent natural materials for whitening skin.

• Journal of Microbiology and Biotechnology
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• v.31 no.12
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• pp.1692-1700
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• 2021

Glycosylation of resveratrol was carried out by using the amylosucrase of Deinococcus geothermalis, and the glycosylated products were tested for their solubility, chemical stability, and biological activities. We synthesized and identified these two major glycosylated products as resveratrol-4'-O-α-glucoside and resveratrol-3-O-α-glucoside by nuclear magnetic resonance analysis with a ratio of 5:1. The water solubilities of the two resveratrol-α-glucoside isomers (α-piceid isomers) were approximately 3.6 and 13.5 times higher than that of β-piceid and resveratrol, respectively, and they were also highly stable in buffered solutions. The antioxidant activity of the α-piceid isomers, examined by radical scavenging capability, showed it to be initially lower than that of resveratrol, but as time passed, the α-piceid isomers' activity reached a level similar to that of resveratrol. The α-piceid isomers also showed better inhibitory activity against tyrosinase and melanin synthesis in B16F10 melanoma cells than β-piceid. The cellular uptake of the α-piceid isomers, which was assessed by ultra-performance liquid chromatography (UPLC) analysis of the cell-free extracts of B16F10 melanoma cells, demonstrated that the glycosylated form of resveratrol was gradually converted to resveratrol inside the cells. These results indicate that the enzymatic glycosylation of resveratrol could be a useful method for enhancing the bioavailability of resveratrol.

• 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.

• Korean Journal of Plant Resources
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• v.35 no.6
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• pp.704-712
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• 2022

Research on whitening materials using natural alternatives is actively being conducted. The aim of this study was to investigate the in vitro inhibitory effects of Ranunculus chinensis Bunge (RCB) on melanogenesis and associated enzymes, such as tyrosinase, tyrosinase-related protein (TRP)-1, and TRP-2 in B16F10 murine melanoma cells. We found that RCB extract significantly attenuated melanin synthesis and reduced the activity of intracellular tyrosinase, a rate-limiting melanogenic enzyme. Western blot analysis showed that RCB extract decreased the protein expression of tyrosinase and TRP-1. In addition, it significantly decreased the expression of microphthalmia-associated transcription factor (MITF), a key regulator of melanogenesis. Extracellular signal-regulated kinase (ERK) activation has been reported to be involved in the inhibition of melanogenesis. Thus, we investigated whether the hypopigmentary effects of RCB extract were related to the activation of ERK. RCB extract induced ERK phosphorylation in a dose-dependent manner. Furthermore, it markedly inhibited body pigmentation in a zebrafish model. Our results suggest that RCB extract inhibits melanogenesis by activating ERK pathway-mediated suppression of MITF and its downstream target genes, including tyrosinase. Therefore, RCB extract can be used as a whitening agent in the development of functional cosmetics.

• Natural Product Sciences
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• v.18 no.2
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• pp.89-96
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• 2012

Ligularia stenocephala has been used as a traditional medicine for the treatment of asthma, arthritis, jaundice, and hyperpiesia. In this study, we investigated the anti-metastatic and hypnotic effects of the methanolic extract of L. stenocephala (MLS). Gelatin zymographic analysis revealed that MLS suppresses matrix metalloproteinase-2 (MMP-2) and MMP-9 activities in B16F10 cells. The gene expressions of MMPs were also down-regulated by MLS treatment in a dose-dependent manner. In addition, cancer cell invasion and migration were attenuated by MLS via suppression of NF-${\kappa}B$ activation. The in vivo lung metastasis of B16F10 melanoma cells was also inhibited by the treatment of MLS. These findings show that MLS has anti-metastatic properties, and, therefore, it might be applicable as a valuable anti-metastatic agent.

• Korean Journal of Pharmacognosy
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• v.34 no.1 s.132
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• pp.70-74
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• 2003

Cornis fructus has been traditionally used for treating allergy, asthma, hepatitis, and chronic nephritis. It major chemical constituents have been saponins, phenolic acids and loganin. The main aim of the present study was to examine the effect of methanol extract from Cornis fructus on melanogenesis. Cell were cultured in the presence of methanol extracts from Cornis fructus for 48 h, and there were estimated total melanin content as a final product and activity of tyrosinase, a key enzyme, in melanogenesis. Methanol extract from Cornis fructus increased the melanin content and tyrosinase activity in a dose-dependent manner. Particularly, it was observed that only methanol extract $200\;{\mu}g/ml$ stimulated the melanin secretion in B16/F10 melanoma cells by 152% at 48 h treatment and the activity of tyrosinase was increased by 261% in the presence of same concentration.