• Biomolecules & Therapeutics
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• v.30 no.5
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• pp.465-472
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• 2022

Melanoma is one of the most aggressive skin cancers. Hypoxia contributes to the aggressiveness of melanoma by promoting cancer growth and metastasis. Upregulation of cyclin D1 can promote uncontrolled cell proliferation in melanoma, whereas stimulation of cytotoxic T cell activity can inhibit it. Epithelial mesenchymal transition (EMT) plays a critical role in melanoma metastasis. Hypoxia-inducible factor-1α (HIF-1α) is a main transcriptional mediator that regulates many genes related to hypoxia. CoCl₂ is one of the most commonly used hypoxia-mimetic chemicals in cell culture. In this study, inhibitory effects of IDF-11774, an inhibitor of HIF-1α, on melanoma growth and metastasis were examined using cultured B16F10 mouse melanoma cells and nude mice transplanted with B16F10 melanoma cells in the presence or absence of CoCl₂-induced hypoxia. IDF-11774 reduced HIF-1α upregulation and cell survival, but increased cytotoxicity of cultured melanoma cells under CoCl₂-induced hypoxia. IDF-11774 also reduced tumor size and local invasion of B16F10 melanoma in nude mice along with HIF-1α downregulation. Expression levels of cyclin D1 in melanoma were increased by CoCl₂ but decreased by IDF-11774. Apoptosis of melanoma cells and infiltration of cytotoxic T cells were increased in melanoma after treatment with IDF-11774. EMT was stimulated by CoCl₂, but restored by IDF11774. Overall, IDF-11774 inhibited the growth and metastasis of B16F10 melanoma via HIF-1α downregulation. The growth of B16F10 melanoma was inhibited by cyclin D1 downregulation and cytotoxic T cell stimulation. Metastasis of B16F10 melanoma was inhibited by EMT suppression.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.16 no.2
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• pp.57-77
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• 2003

Objectives: The aim of this study was to investigate the depigmentation effects of Barley, Unpolished rice, Job's-tear. Metbods: We investigated that the extracts of Barley, Unpolished rice, Job's-tear inhibit activity of tyrosinase, the enzyme which convert ts 3-(3,4-dihydroxyphenyl) alanine to dopachrom in the biosynthetic process of melanin, the UV absorbance of the extracts in the UV-A region and UV-B region was measured by UV scanning, the effect of extracts on cell viability and melanin production in cultured B16 mouse melanoma cells were measured, and cytoprotective effects of extracts on PC12 cells injured by hydrogen peroxide measured by MTT assay. Results: The extracts of Barley, Unpolished rice, Job's-tear inhibited activity of tyrosinase in low density. The Barley, Job's-tear extracts not only showed inhibitory effects on melanin production in cultured B16 mouse melanoma cells, but also exhibited cytoprotective effects on PC12 cells injured by hydrogen peroxide in low density. Unpolished rice extract showed inhibitory effect on melanin production in cultured B16 mouse melanoma cells, but did not showed cytoprotective effect Barley, Unpolished rice, Job's-tear extracts did not showed an absorbance effect in the UV-A region and UV-8 region. Conclusions: These results suggest that Barley, Unpolished rice, Job's-tear inhibit melanin biosynthesis which is involved in hyperpigmentation and could be used as a whitening agent.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.22 no.2
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• pp.104-117
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• 2009

Objective : Melanin is one of the most important facor in skin color. Melanin protects human skin from ultraviolet radiation otherwise it causes melanin pigmentation. So this experiment is carried out for test whether Scutellaria baicalensis Georgi(SBG) inhibits melanin synthesis and tyrosinase activity in mouse B16 melanoma cells. Method : The melanin synthesis inhibition effects of SBG were examined by in vitro melanin production assay. We assessed inhibitory effects of SBG on melanin contents from B16F1 melanoma cell, on tyrosinase activity(cell and cell free system), effect of SBG on the expression tyrosinase, Microphthalmia-associated Transcription Factor(MITF), Extracellular signal-regulated Kinase(ERK). Result : SBG inhibited melanin synthesis induced $\alpha$-MSH($\alpha$-Melanin Stimulating Hormone) in B16F1. SBG inhibited tyrosinase activity and expression. And SBG down-regulates MITF and stimulated ERK activation in B16F1. Conclusion : According to above results, SBG was improved its suppression effect to the inhibition of melanin synthesis, tyrosinase activation, and tyrosinase promotor activation. So SBG is considered to be used for an strong source of skin whitening effect.

• Journal of Life Science
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• v.16 no.5
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• pp.870-875
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• 2006

This study was carried out to investigate the whitening effect of mycelial culture broth of P. japonica in the mixture of cucumber and grape extracts. In the inhibition test of melanin biosynthesis of melanoma cell, B16BL6, the culture broth of P. japonica more then $50\;{\mu}l/ml$ (5%) concentration inhibited the melanin biosynthesis of the cell entirely without cytotoxicity. More then 10 days incubation of P. japonica in the mixture was required to have the inhibition activity. In vitro inhibition test of melanin biosynthesis of the culture broth of P. japonica was investigated in the concentration dependent manner of 10% to 50%. 30% concentration of the culture broth inhibited completely tyrosinase activity. In the cytotoxicity test, cucumber and grape extract itself has a strong cytotoxicity to the melanoma cell, B16Bl6. The value of $IC_{50}$ of the cucumber and grape extracts against the melanoma cells was 5% concentration. However, the culture broth of P. japonica incubated in the cucumber and grape extracts did not show the cytotoxcity up to 20% against melanoma cell, B16BL6. Therefore, we concluded that the culture broth of P. japonica in the mixture of cucumber and grape extracts can be used as a whitening cosmetic resource.

• Biomedical Science Letters
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• v.29 no.3
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• pp.201-205
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• 2023

Free adenine is mainly made during the polyamine synthesis in proliferating cells. Adenine molecule itself acts biological modulator in inflammation and cell death. In the previous report, we showed that adenine induces apoptotic cell death of B16-F10 mouse melanoma cells by eliciting of PARP and caspase 3 cleavages. In this study, we examined the adenine effect on other apoptotic molecules affecting caspase activation in B16-F10 melanoma cells. Adenine treatment make pro-apoptotic molecules active states. Bax/Bcl-2 ratio was increased and phosphorylation of mTOR and Akt was decreased in a dose dependent manner. These results showed the possibility that Bax/Bcl-2, Akt and mTOR are engaged in adenine induced apoptosis of melanoma cells.

• Fashion & Textile Research Journal
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• v.8 no.3
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• pp.326-330
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• 2006

The results of the research for the whitening effect and functional machanism of 1-(2-cyclohexylmethoxy-6-hydroxyphenyl)-3-(4-hydroxymethylphenyl)-propenone are as follow : 1. Propenone inhibited concentration-dependently the generation of melanin increased by the stimulation of ${\alpha}$-MSH and protoporphyrin IX, and $IC_{50}$ value was six to eight ${\mu}M$. This was five to seven times superior in the inhibiting effect, compared with kojic acid used as positive control group. 2. Propenone did not have a decolorizing effect on melanin already generated. 3. Propenone was observed to have toxicity of over $100{\mu}M$ for the mouse melanoma B16 cells.

• Natural Product Sciences
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• v.4 no.3
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• pp.161-169
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• 1998

The analogues of lichen components showing anti-tyrosinase activities were synthesized. 4-Alkylresorcinol derivatives showed both the inhibitory activity and cytotoxicity in B-16 melanoma cells at the doses of 10 mM to 1.2 mM. Resorcinol and 4-methylresorcinol showed the inhibitory effect with a low cytotoxicity at the doses of 2.5 mM and $600\;{\mu}M$ among 4-alkylresorcinols, respectively. Some diphenylmethane derivatives (Type A, B, and C) had strong activities with a low cytotoxicity. While xanthine derivatives had no effect. Glucosides of 4,5-alkylresorcinol and the diphenylmethane derivative (Type B) were prepared to decrease the cytotoxicity. As a result, no effect were observed. Liposome of the diphenylmethane derivative (Type B) was prepared for the same purpose, and the latter showed a remarkable effect at the dose of $15\;{\mu}M$ with a low cytotoxicity.

• Journal of Life Science
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• v.23 no.12
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• pp.1516-1524
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• 2013

To find a novel skin whitening agent, the effect of cordycepin-enriched Cordyceps militaris (CM${\alpha}$) extract fermented by fungi on anti-melanogenesis in B16F0 mouse melanoma cells was investigated. Fermented CM${\alpha}$ was prepared with fungi, including Monascus purpureus (Mp), Aspergillus oryzae (Ao), Aspergillus kawachii (Ak), and Rhizopus oryzae (Ro), respectively. When the content of the phenolics and the flavonoids and the activities of the antioxidant and the mushroom tyrosinase inhibition were measured in the CM fermented by Ak (AkF-CM), the highest content of the phenolics was 46 mg/g dry weight and the highest content of the flavonoids was 0.93 mg/g; the highest activity of the DPPH radical scavenging was 62.74% and the highest activity of the mushroom tyrosinase inhibition was 79.97% CM${\alpha}$CM${\alpha}$. From this result, AkF-CM${\alpha}$ exhibited the highest mushroom tyrosinase inhibitory activity and so it was used in subsequent anti-melanogenesis. B16F0 melanoma cells were treated with 1-10 mg/ml concentrations of AkF-CM${\alpha}$ and 200 ${\mu}M$ arbutin as the positive control. The melanin content and cell viability of the melanoma cells by arbutin treatment decreased to 43% and 92% of the control, respectively. AkF-CM${\alpha}$ treatment at 1, 3, and 5 mg/ml concentrations decreased the extracellular melanin release induced by IBMX treatment by 35%, 45%, and 53%, respectively. AkF-CM${\alpha}$ showed inhibitory activity against both intracellular tyrosinase in melanoma cells and mushroom tyrosinase. AkF-CM${\alpha}$ reduced the protein level of tyrosinase in the IBMX-stimulated cells. These results indicate that AkF-CM${\alpha}$ suppressed the activity and protein content of cellular tyrosinase and decreased the total melanin content in cultured B16F0 melanoma cells.

• The Journal of Korean Obstetrics and Gynecology
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• v.22 no.1
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• pp.95-109
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• 2009

Purpose: This study was performed to determine the inhibitory effect of Sihosogansangagambang (SS) on melanin synthesis in B16F10 melanoma cells (B16F10). Methods: The inhibitory effects of Sihosogansangagambang on melanin synthesis were used by in vitro assay. To elucidate inhibitory effects of SS on melanin synthesis, we determined the melanin release in B16F10. And to investigate the mechanism of inhibitory effect of SS, we assessed the gene expression of tyrosinase, TRP-1, TRP-2 and ERK-1 in B16F10. Results: 1. SS decreased the release of melanin in B16F10 melanoma cells. 2. SS inhibited mushroom tyrosinase activity in vitro. 3. SS decreased the expression of tyrosinase, TRP-2 in B16F10 melanoma cells, but did not decreased the expression of TRP-1 in B16F10 melanoma cells. 4. SS decreased the expression of ERK-1 in B16F10 melanoma cells. Conclusion: From these results, it may be suggested that SS is possesed of the antimelanogenetic effects.

• Journal of Life Science
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• v.23 no.12
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• pp.1495-1500
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• 2013

The objective of this study was to evaluate the anti-melanogenic effects of Hizikia fusiforme (HF) fractions in ${\alpha}$-melanocyte stimulating hormone-induced B16F10 mouse melanoma cells. Ethanol extractions of Hizikia fusiforme (EEHF) were subjected to fraction by using dichloromethane (CFHF), ethyl acetate (EAFHF), butanol (BFHF), and water (WFHF). EEHF, CFHF, and EAFHF inhibited tyrosinase activity and melanin synthesis in B16F10 mouse melanoma cells in a dose-dependent manner. The melanin contents were inhibited by 40.5% and 33.2% in response to treatment with 50 ${\mu}g/ml$ of EEHF and CFHF, respectively. In addition, tyrosinase activities showed a 53.3% and 54.1% reduction in treatment with 50 ${\mu}g/ml$ of EEHF and CFHF. Western blotting analysis showed that EEHF, CFHF, and EAFHF inhibited tyrosinase, TRP-1, TRP-2, and MITF expression in a dose-dependent manner. In conclusion, these findings indicate that ethanol and dichloromethane fractions of Hizikia fusiforme, which inhibit melanin synthesis and tyrosinase activity, are effective skin-whitening agents.