• Title/Summary/Keyword: tyrosinase inhibitor

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The skin protective effects of compound K, a metabolite of ginsenoside Rb1 from Panax ginseng

  • Kim, Eunji;Kim, Donghyun;Yoo, Sulgi;Hong, Yo Han;Han, Sang Yun;Jeong, Seonggu;Jeong, Deok;Kim, Jong-Hoon;Cho, Jae Youl;Park, Junseong
    • Journal of Ginseng Research
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    • v.42 no.2
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    • pp.218-224
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    • 2018
  • Background: Compound K (CK) is a ginsenoside, a metabolite of Panax ginseng. There is interest both in increasing skin health and antiaging using natural skin care products. In this study, we explored the possibility of using CK as a cosmetic ingredient. Methods: To assess the antiaging effect of CK, RT-PCR was performed, and expression levels of matrix metalloproteinase-1, cyclooxygenase-2, and type I collagen were measured under UVB irradiation conditions. The skin hydrating effect of CK was tested by RT-PCR, and its regulation was explored through immunoblotting. Melanin content, melanin secretion, and tyrosinase activity assays were performed. Results: CK treatment reduced the production of matrix metalloproteinase-1 and cyclooxygenase-2 in UVB irradiated NIH3T3 cells and recovered type I collagen expression level. Expression of skin hydrating factors-filaggrin, transglutaminase, and hyaluronic acid synthases-1 and -2-were augmented by CK and were modulated through the inhibitor of ${\kappa}B{\alpha}$, c-Jun N-terminal kinase, or extracellular signal-regulated kinases pathway. In the melanogenic response, CK did not regulate tyrosinase activity and melanin secretion, but increased melanin content in B16F10 cells was observed. Conclusion: Our data showed that CK has antiaging and hydrating effects. We suggest that CK could be used in cosmetic products to protect the skin from UVB rays and increase skin moisture level.

Statistically Designed Enzymatic Hydrolysis for Optimized Production of Icariside II as a Novel Melanogenesis Inhibitor

  • Park, Jun-Seong;Park, Hye-Yoon;Rho, Ho-Sik;Ahn, Soo-Mi;Kim, Duck-Hee;Chang, Ih-Seop
    • Journal of Microbiology and Biotechnology
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    • v.18 no.1
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    • pp.110-117
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    • 2008
  • Three kinds of prenylated flavonols, icariside I, icariside II, and icaritin, were isolated from an icariin hydrolysate and their effects on melanogenesis evaluated based on mushroom tyrosinase inhibition and quantifying the melanin contents in melanocytes. Although none of the compounds had an effect on tyrosinase activity, icariside II and icaritin both effectively inhibited the melanin contents with an $IC_{50}$ of 10.53 and $11.13{\mu}M$, respectively. Whereas icariside II was obtained from a reaction with ${\beta}$-glucosidase and cellulase, the icariin was not completely converted into icariside II. Thus, for the high-purity production of icariside II, the reaction was optimized using the response surface methodology, where an enzyme concentration of 5.0mg/ml, pH 7, $37.5^{\circ}C$, and 8 h reaction time were selected as the central conditions for the central composite design (CCD) for the enzymatic hydrolysis of icariin into icariside II using cellulase. Empirical models were developed to describe the relationships between the operating factors and the response (icariside II yield). A statistical analysis indicated that all four factors had a significant effect (p<0.01) on the icariside II production. The coefficient of determination $(R^2)$ was good for the model (0.9853), and the optimum production conditions for icariside II was an enzyme concentration of 7.5mg/ml, pH 5, $50^{\circ}C$, and 12 h reaction time. A good agreement between the predicted and experimental data under the designed optimal conditions confirmed the usefulness of the model. A laboratory pilot scale was also successful.

Whitening Efficacy Study of Natural Compounds-Peptide Derivatives via cAMP Signaling Pathway (cAMP 신호전달과정을 통한 신규 천연유래물질 펩타이드 유도체의 미백 효능 연구)

  • Lee, Hye-Suk;Shin, Kyong-Hoon;Ryu, Geun-Seok;Jee, Kyung-Yup;Cho, In-Shik;Kim, Han-Young
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.37 no.3
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    • pp.275-282
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    • 2011
  • Novel whitening agents were prepared using peptide-Natural origin compound derivatives. The peptide could be an antagonist of MC1R and Natural origin compound were well-known material as a Tyrosinase inhibitor. We also suggest the new assay method which could evaluate the Antagonistic effectiveness to MC1R using cAMP signaling pathway. 24 candidates were synthesized and 11 peptide derivatives were selected by cAMP assay method. To evaluate cAMP assay, the selected peptide derivatives were assayed to evaluate their melanogensis inhibitory activity. At this work, we could know that the sequences which include -RW- have a melanogensis inhibitory activity, and cAMP assy could use as a evaluating method of MC1R antagonist. But, to evaluate the whitening activity of some material, cross-checking with melanin inhibitory assay method was recommended.

Melanogenesis inhibition activity of floralginsenoside A from Panax ginseng berry

  • Lee, Dae Young;Lee, Jongsung;Jeong, Yong Tae;Byun, Geon Hee;Kim, Jin Hee
    • Journal of Ginseng Research
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    • v.41 no.4
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    • pp.602-607
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    • 2017
  • Background: Panax ginseng is a traditional herb used for medicinal purposes in eastern Asia. P. ginseng contains various ginsenosides with pharmacological effects. In this study, floralginsenoside A (FGA), ginsenoside Rd (GRD), and ginsenoside Re (GRE) were purified from P. ginseng berry. Methods: Chemical structures of FGA, GRD, and GRE were determined based on spectroscopic methods, including fast atom bombardment mass spectroscopy, ID-nuclear magnetic resonance, and infrared spectroscopy. Inhibitory activities of these compounds on melanogenesis were studied by measuring the expression of protein and melanin content in the melan-a cell line. This inhibitory activity was confirmed by observing pigmentation and tyrosinase activities of zebrafish. Results: GRD, GRE, and FGA were not cytotoxic at concentrations less than $20{\mu}M$, $80{\mu}M$, and $160{\mu}M$ in melan-a cells, respectively. GRD, GRE, and FGA inhibited melanin biosynthesis in melan-a cells by 15.2%, 22.9%, and 23.9% at $20{\mu}M$, $80{\mu}M$, and $160{\mu}M$, respectively. FGA was observed to display the most potent inhibitory effect. In addition, FGA decreased microphthalmia-associated transcription factor protein expression in a dose-dependent manner. Moreover, FGA induced extracellular signal-regulated kinase phosphorylation level in melan-a cells. In addition, melanin pigment content and tyrosinase activity in zebrafish treated with FGA at $160{\mu}M$ were reduced. Conclusion: FGA showed the most potent inhibition of melanogenesis in both in vitro and in vivo studies. This study suggests that FGA purified from P. ginseng may be an effective melanogenesis inhibitor.

Anthocyanins from Hibiscus Syriacus Inhibit Melanogenesis by Activating the ERK Signaling Pathway

  • Karunarathne, Wisurumuni Arachchilage Hasitha Maduranga;Molagoda, Ilandarage Menu Neelaka;Park, Sang Rul;Kim, Jeong Woon;Lee, Oh-Kyu;Kwon, Hae Yun;Oren, Matan;Choi, Yung Hyun;Ryu, Hyung Won;Oh, Sei-Ryang;Jo, Wol Soon;Lee, Kyoung Tae;Kim, Gi-Young
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2019.10a
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    • pp.90-90
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    • 2019
  • Hibiscus syriacus exhibited promising potential as a new source of food and colorants containing various anthocyanins. However, the function of anthocyanins from H. syriacus has not been investigated. In the current study, we evaluated whether anthocyanins from the H. syriacus varieties Pulsae and Paektanshim (PS and PTS) inhibit melanin biogenesis. B16F10 cells and zebrafish larvae were exposed to PS and PTS in the presence or absence of ${\alpha}$-melanocyte-stimulating hormone (${\alpha}$-MSH), and melanin contents accompanied by its regulating genes and proteins were analyzed. PS and PTS moderately downregulated mushroom tyrosinase activity in vitro, but significantly decreased extracellular and intracellular melanin production in B16F10 cells, and inhibited ${\alpha}$-MSH-induced expression of microphthalmia-associated transcription factor (MITF) and tyrosinase. PS and PTS also attenuated pigmentation in ${\alpha}$-MSH-stimulated zebrafish larvae. Furthermore, PS and PTS activated the phosphorylation of extracellular signal-regulated kinase (ERK), whereas PD98059, a specific ERK inhibitor, completely reversed PS- and PTS-mediated anti-melanogenic activity in B16F10 cells and zebrafish larvae, which indicates that PS- and PTS-mediated anti-melanogenic activity is due to ERK activation. Moreover, chromatography data showed that PS and PTS possessed 17 identical anthocyanins as a negative regulator of ERK. These findings suggested that anthocyanins from PS and PTS inhibited melanogenesis in vitro and in vivo by activating the ERK signaling pathway.

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Changes of Microorganisms, Enzyme activity and Physiological functionality in the traditional Deonjang with various concentrations of Lentinus edodes during fermentation (표고버섯 첨가에 따른 재래식 된장 발효 과정중의 미생물, 효소 활성 및 기능성의 변화)

  • Rhee, Chang-Ho;Lee, Joo-Baek;Jang, Sang-Moon
    • Applied Biological Chemistry
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    • v.43 no.4
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    • pp.277-284
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    • 2000
  • In order to investigate the changes of microorganisms, enzyme activity and physiological functionality of five types of traditional Deonjang prepared with various concentrations of Lentinus edodes. The pH of traditional Deonjang was decreased but total acidity was increased during fermentation. NaCl concentrations was increased up to $15.67{\sim}16.02%$ until $30{\sim}45$ days of fermentation but decreased after that. Amino acidity was increased on the traditional Deonjang with increasing the mixture ratio of Lentinus edodes. Reducing sugar content was increased up to $30{\sim}45$ days of fermentation. Total sugar content was increased up to $18.21{\sim}20.57%$ until 30 days of fermentation. As the mixing ratio of Lentinus edodes increased, total sugar also increased. The number of bacteria was highest in all sample after 45 days fermentation, while that of mold was decreased during fermentation. Amylase activity was decreased but protease activity, tyrosinase inhibitor and ACE inhibitor were increased on the traditional Doenjang with increasing the mixture ratio of Lentinus edodes. Antimutagenic activities of traditional Deonjang (10% Cortinellus edodes) were 83.15%, 65.88% against MNNG, NPD on S. typhimutium TA100 and 54.59%, 55.00% against NQO, NPD on S. typhimutium TA98

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Screening of Bioactive Compounds from Mushroom Pholiota sp. (비늘버섯으로부터 생리기능성 물질의 탐색)

  • Yu, Hyung-Eun;Cho, Soo-Muk;Seo, Geon-Sik;Lee, Byeong-Seok;Lee, Dae-Hyoung;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.34 no.1
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    • pp.15-21
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    • 2006
  • Extracts from 63 kinds of Pholiota sp. fruiting bodies were prepared using water and methanol, and then their physiological functionalities were investigated. The methanol extracts from Pholiota adiposa PAD030 showed high fibrinolytic activity and those of P. adiposa ASI PAD-022 showed potential inhibitory activity of 76.8% against ${\beta}-hydroxy-{\beta}-methylglutaryl(HMG)-CoA$ reductase. The highest antioxidant and tyrosinase inhibitory activities were found in the water extracts of Pholiota sp. PSP-015 (72.7%) and methanol extracts of P. nameko PNA-024 (69.5%), respectively. However, superoxide dismutase(SOD)-like activity and elastase inhibitory activity were low in almost of the extracts. The HMG-CoA reductase inhibitor from the fruiting body of P. adiposa PAD-022 which showed the highest functionality was extracted maximally when powder of the fruiting body was shaked at $30^{\circ}C$ for 12 h by methanol and its HMG-CoA reductase inhibitory activity was 80.2%.

Melanogenesis Promotion by 3-Deazaneplanocin A, a Specific Inhibitor of S-Adenosylhomocysteine Hydrolase, in B16/F10 Melanoma Cells (B16/F10 흑색종 세포에서 S-Adenosylhomocysteine Hydrolase 의 선택적 저해제 3-Deazaneplanocin A 에 의한)

  • Hwang, Yun Jeong;Boo, Yong Chool
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.47 no.2
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    • pp.107-121
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    • 2021
  • Skin hypopigmentation, which is observed in albinism or vitiligo, occurs when melanin synthesis is decreased by genetic, epigenetic, and other factors. To identify drug candidates that can promote melanin synthesis in cells, we screened an epigenetic modulator library consisting of 141 cell-permeable, small molecule drugs. B16/F10 murine melanoma cells were treated with each drug at 0.1 𝜇M and melanin synthesis and cell viability were subsequently monitored. As a result, (-)-neplanocin A, 3-deazaneplanocin A (DZNep), and DZNep hydrochloride were found to increase cellular melanin synthesis without causing cytotoxicity. Because these three structurally related drugs exhibited similar dose-dependent effects on melanin synthesis and cell viability, DZNep was selected as a representative drug for additional experiments. DZNep increased intracellular melanin content and tyrosinase (TYR) activity. DZNep also induced the expression of TYR, tyrosinase-related protein 1 (TYRP1), and dopachrome tautomerase (DCT) at the mRNA and protein levels. DZNep also induced the mRNA and protein expression of microphthalmia-associated transcription factor (MITF), a key regulator of melanin synthesis. DZNep is a specific inhibitor of S-adenosylhomocysteine hydrolase and it caused the accumulation of S-adenosylhomocysteine that inhibits histone methyltransferases in cells. This study suggests that melanogenesis can be modulated by targeting S-adenosylhomocysteine hydrolase in certain cellular contexts.

Anti-melanogenesis effect of 4-hydroxy-5-methyl-3[2H]-furanone, an antioxidant isolated from pine needles (솔잎에서 분리된 항산화 물질인 4-hydroxy-5methyl-3[2H]-furanone의 멜라닌 생성 억제작용)

  • 부용출;전체옥
    • 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.

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New Whitening Agent : Selina-4(14), 7(11)-dien-8-one (신규 미백제 : Selina-4(14), 7(11)-dien-8-one)

  • Kim, Cheong-Taek;Chang, Yun-Hee;Lee, Sang-Hwa;Kang, Sang-Jin;Cho, Wan-Goo
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.31 no.1 s.49
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    • pp.17-23
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    • 2005
  • We had previously reported that Selina (selina-4(14), 7(11)-dien-8-one) was isolated from methanol extract of Afractylodes rhizome and has strong whitening activity in B16 melanoma cells. In this report, we demonstrated its action mechanism in melan-a cells, non-tumorigenic melanocytes. We also investigated the clinical efficacy of cosmetic preparation containing Selina. Selina reduced the melanin synthesis of Melan-a cells by $50\%$ at a concentration of $10 {\mu}g/mL$ without any apparent cytotoxicity. We also found that the treatment of cells with Selina decreased tyrosinase activity by $60\%$ at a concentration of $10 {\mu}g/mL$ but Selina was not a direct inhibitor of tyrosinase activities. To elucidate the action mechanism of Selina, we investigated the changes in mRNA and protein level of tyrosinase, TRP-1 and TRP-2 using RT-PCR and western blotting, respectively. As a result, the mRNA and protein level of tyrosinase were markedly reduced at $10 {\mu}g/mL$ of Selina without any effect on TRP-1 and TRP-2. These results suggest that Selina exerts its whitening effect mainly through regulating expression of tyrosinase. A 7 week-clinical trial using formulation containing $0.2\%$ selina-4(14), 7(11)-dien-8-one with 20 volunteers resulted in statistically significant whitening effect (p < 0.05), without any adverse effect. Based on these results, Selina (selina-4(14), 7(11)-dien-8-one) can be s useful and safe ingredient for the cleanness and brightness of skin.