• Title/Summary/Keyword: Human tyrosinase

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Identification of ML106 Phase 1 Metabolites in Human Liver Microsomes Using High-Resolution Quadrupole-Orbitrap Mass Spectrometry

  • Jo, Jun Hyeon;Nam, WoongShik;Kim, Sunjoo;Lee, Doohyun;Min, Kyung Hoon;Lee, Taeho;Lee, Sangkyu
    • Mass Spectrometry Letters
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    • v.7 no.3
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    • pp.69-73
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    • 2016
  • High-resolution quadrupole-Orbitrap mass spectrometry (HRMS), with high-resolution (> 10,000 at full-width at half-maximum) and accurate mass (< 5 ppm deviation) capabilities, plays an important role in the structural elucidation of drug metabolites in the pharmaceutical industry. ML106, a derivative of imidazobenzimidazole, decreased melanin content and tyrosinase activity in a dose-dependent manner. Here, we investigated the phase 1 metabolic pathway of ML106 using HRMS in human liver microsomes (HLMs) and recombinant cDNA-expressed cytochrome P450 (CYP). After the incubation of ML106 with pooled HLMs and recombinant cDNA-expressed CYP in the presence of NADPH, five phase 1 metabolites, including three mono-hydroxylated metabolites (M1-3) and two di-hydroxylated metabolites (M4 and M5), were investigated. The metabolite structures were postulated by the elucidation of protonated mass spectra using HRMS. The CYP isoforms related to the hydroxylation of ML106 were studied after incubation with recombinant cDNA-expressed CYP. Here, we identified the phase 1 metabolic pathway of ML106 induced by CYP in HLMs.

Antioxidant and Anticancer Activities of Lotus (Nelumbo nucifera) Leaf and Root (연(蓮) 잎과 뿌리의 항산화 및 항암활성)

  • Jeong, Chang-Ho;Son, Ki-Bong;Kim, Jin-Hee;Kang, Sun-Kyung;Park, Eun-Young;Seo, Kwon-Il;Shim, Ki-Hwan
    • Food Science and Preservation
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    • v.17 no.1
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    • pp.131-138
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    • 2010
  • To obtain basic data on the use of lotus as a raw material in functional food, antioxidant and anticancer activities of the leaf and root were investigated. Total flavonoid and total phenolic contents, at 12.84 mg/g and 24.33 mg/g respectively, were higher in white lotus leaf (WLL) than in any other part of the plant. The radical-scavenging activity of different tissues of lotus, measured in the DPPH radical-scavenging assay, increased with higher concentrations of solvent fractions. The butanol fraction of white lotus leaf showed the highest DPPH radical-scavenging activity. The reducing power of fractions increased in a dose-dependent manner. The butanol fraction of WLL had the greatest reducing power, and showed strong antioxidant activity in the linoleic acid system, and high-level inhibition of tyrosinase. Fractions from lotus were also capable of scavenging nitrite, depending on the concentration of the fractions. Butanol fractions of the leaf of white and red lotus scavenged 95.61% and 92.15% of available nitrite, respectively, when used at 1 mg/mL concentrations. Butanol fractions from leaf of white and red lotus exhibited the strongest inhibitory effects on human lung and colon cancer cells.

Anti-skin Aging Potential of Alcoholic Extract of Phragmites communis Rhizome

  • Ha, Chang Woo;Kim, Sung Hyeok;Lee, Sung Ryul;Jang, Sohee;Namkoong, Seung;Hong, Sungsil;Lim, Hyosun;Kim, Youn Kyu;Sohn, Eun-Hwa
    • Korean Journal of Plant Resources
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    • v.33 no.6
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    • pp.604-614
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    • 2020
  • Chronological aging and photoaging affect appearance, causing wrinkles, pigmentation, texture changes, and loss of elasticity in the skin. Phragmites communis is a tall perennial herb used for its high nutritional value and for medicinal purposes, such as relief from fever and vomiting and facilitation of diuresis. In this study, we investigated the effects of ethanol extract of P. communis rhizome (PCE) on skin aging. The total flavonoid and total phenolic content in PCE were 2.92 ± 0.007 ㎍ of quercetin equivalents (QE) and 231.8 ± 0.001 ㎍ of gallic acid equivalents (GAE) per 100 mg of dried extract (n = 3). The half-maximal inhibitory concentration (IC50) values of PCE for 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) and hydrogen peroxide scavenging activities were 0.96 and 0.97 mg/mL, respectively. PCE showed inhibitory effects on tyrosinase when L-tyrosine (IC50 = 1.25 mg/mL) and L-3,4-dihydroxyphenylalanine (IC50 = 0.92 mg/mL) were used as substrates. PCE treatment up to 200 ㎍/mL for 24 h did not cause any significant cytotoxicity in B16F10 melanocytes, human dermal fibroblasts (HDFs), and HaCaT keratinocytes. In B16F10 melanocytes, PCE (25 and 50 ㎍ /mL) inhibited melanin production and cellular tyrosinase activity after challenge with α-melanocyte-stimulating hormone (α-MSH; p < 0.05). In HDFs, PCE suppressed the mRNA expression of matrix metalloproteinase-1 (MMP-1) and reduced the activity of elastase (p < 0.05). In addition, ultraviolet B (UVB)-mediated downregulation of hyaluronic acid synthase-2 gene expression in HaCaT keratinocytes was also effectively suppressed by PCE treatment. Overall, our results showed that PCE has potential anti-skin aging activity associated with the suppression of hyperpigmentation, wrinkle formation, and reduction in dryness. PCE is a promising candidate for the development of an anti-skin aging cosmetic ingredient.

산삼의 배양 및 그 응용에 관한 연구

  • 신미희
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.27 no.2
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    • pp.45-56
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    • 2001
  • Korea mountain ginseng known as oriental miracle drug is an important medicinal plant. The effect of mountain ginseng adventitious roots extract has been described. The valuable root of mountain ginseng contained several kinds of ginsenosides that have been confirmed to have many active functions for the human body. However, the study of mountain ginseng has a limit because the price of wild ginseng is very expensive and rare. The mountain ginseng adventitious roots were derived from mountain ginseng callus that were induced from mountain ginseng roots. Adventitious roots were separated from callus and grown in solid media(Murachige and stoog media). It was cultured in a 20L bioreactor. After culturing for 40days, adventitious roots were harvested. Afterwards the harvested mountain ginseng adventitious roots were dryed and extracted. We examined the effect on melanogenesis of mountain ginseng adventitious roots extract. Here, we report the inhibitory effect of melanin biosynthesis on the adventitious roots extract of In vitro test. Also, we assessed the safety of adventitious roots extract. In vitro, cytotoxicity of adventitious roots extract was assessed in mouse fibroblast using two method: The neutral red uptake assay and the MTT assay. In vivo, the allergic and irritant were Patch teated in 30 patients. Consequently, extract of mountain ginseng adventitious roots have inhibitory effect on melanin biosynthesis in B-16 melanoma cell test, tyrosinase inhibitory test and DOPA auto-oxidation test. There were decreased 86%(0.5% concentration), 45%(1% concentration) and 61%(1% concentration), respectively.

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Vinegar Produced from Chrysanthemum zawadskii and Pearl Shell (구절초진주식초)

  • Ann, Yong-Geun;Oh, Moon-Hun;Lee, Byung-Yup
    • The Korean Journal of Food And Nutrition
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    • v.25 no.1
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    • pp.90-98
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    • 2012
  • With the addition of ethanol to wax gourd extract and by acetic fermentation, 5.0% acidity vinegar was produced. After putting 10% extract(10% concentration) of Chrysanthemum zawadskii in this, and by dissolving shell, Chrysanthemum zawadskii-pearl vinegar was produced. When a 1% of ark shell, oyster shell, or ear shell was added to wax gourd vinegar, 95.6~98.4% of the shell dissolved, and when a 2% content of shell was added, 97.2~98.4% was dissolved. The acidity of vinegar which dissolved 1% shell was pH 3.0~3.17, and the acidity of vinegar which dissolved 2% shell was pH 1.11~ 1.20. The pH values of vinegar which dissolved 1%, and 2% shell contents were 4.54~4.55, and 4.86~4.95, respectively. When 1% shell was dissolved, the acidity was higher than that of commercial vinegar, with a high pH value and low level of free acid. This shows that when Chrysanthemum zawadskii 1% is added during acetic acid fermentation, the inhibition was 44.4%, and 22.2% respectively. In this regard, Chrysanthemum zawadskii should be added after the fermentation of acetic acid. The calcium content of 1% shell vinegar is 0.4%, and that of 2% vinegar is 0.78%. Non-heated native wax gourd shows an angiotensin converting enzyme inhibition rate of 21.7%, an antioxidant activity of 5.23%, and a tyrosinase inhibition rate of 5.5%. In the case of heated-extracted wax gourd, the angiotensin converting enzyme inhibition rate was 16.1%, superoxide dismutase activity was 20.5%, antioxidant activity was 23.2%, and the tyrosinase inhibition rate was 7.1%. Also, in the case of Chrysanthemum zawadskii, the angiotensin converting enzyme inhibition rate was 28.8%, the xanthine oxidase inhibition rate was 28.2%, the superoxide dismutase activity was 14.5%, the antioxidant activity was 3.2%, and the tyrosinase inhibition rate was 9.2% Data also revealed that when a 10% sample of the heated-wax gourd extract was added to A549 human lung cancer epithelial cells of, the number of cancer cells declined by 80% in 72 hours, When a 10% native extract was added, the number of cells declined by, 74% in 48 hours, and when a heated-extract of Chrysanthemum zawadskii was added, 100% of the cells died after 72 hours.

Biotransformation of Pueraria lobata Extract with Lactobacillus rhamnosus vitaP1 Enhances Anti-Melanogenic Activity

  • Kwon, Jeong Eun;Lee, Jin Woo;Park, Yuna;Sohn, Eun-Hwa;Choung, Eui Su;Jang, Seon-A;Kim, Inhye;Lee, Da Eun;Koo, Hyun Jung;Bak, Jong Phil;Lee, Sung Ryul;Kang, Se Chan
    • Journal of Microbiology and Biotechnology
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    • v.28 no.1
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    • pp.22-31
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    • 2018
  • Isoflavone itself is less available in the body without the aid of intestinal bacteria. In this study, we searched for isoflavone-transforming bacteria from human fecal specimens (n = 14) using differential selection media. Isoflavone-transforming activity as the production of dihydrogenistein and dihydrodaidzein was assessed by high-performance liquid chromatography and we found Lactobacillus rhamnosus, named L. rhamnosus vitaP1, through 16S rDNA sequence analysis. Extract from Pueraria lobata (EPL) and soy hypocotyl extract were fermented with L. rhamnosus vitaP1 for 24 and 48 h at $37^{\circ}C$. Fermented EPL (FEPL) showed enhanced anti-tyrosinase activity and antioxidant capacities, important suppressors of the pigmentation process, compared with that of EPL (p < 0.05). At up to $500{\mu}g/ml$ of FEPL, there were no significant cell cytotoxicity and proliferation on B16-F10 melanoma cells. FEPL ($100{\mu}g/ml$) could highly suppress the content of melanin and melanosome formation in B16-F10 cells. In summary, Lactobacillus rhamnosus vitaP1 was found to be able to biotransform isoflavones in EPL. FEPL showed augmented anti-melanogenic potential.

Evaluation of Cosmeceutical Properties of Fish Skin By-product Hydrolysates Collected During Surimi Manufacturing Process (연육 제조과정에서 발생하는 어피 부산물의 활용을 위한 Cosmeceutical 활성 평가)

  • Oh, Jae-Young;Lee, Hyo-Geun;Je, Jun-Geon;Wang, Lei;Kim, Hyun-Soo;Jeon, You-Jin
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.53 no.3
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    • pp.297-307
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    • 2020
  • This study investigated the cosmetic effects of enzymatic hydrolytes of an aquatic by-product, fish skin. The skins of olive flounder Paralichthys olivaceus (PO) and Alaska pollock Gadus chalcogrammus (AP) were hydrolyzed using pepsin, Alcalase, and Protemax. Three enzymatic hydrolytes were obtained and the inhibitory effects of these hydrolytes on the aging-related enzymes tyrosinase, elastase, and collagenase were determined. The results indicated that the pepsin hydrolytes of PO and PA had stronger activities than the other hydrolytes. PO and PA also significantly reduced the intracellular reactive oxygen species levels in and improved the viability of H2O2-treated Vero cells; decreased nitric oxide production by and increased the cell viability of lipopolysaccharide-treated RAW 264.7 cells; and reduced intracellular reactive oxygen species levels and improved the viability of ultraviolet B irradiated HaCaT cells and human dermal fibroblasts. Furthermore, PO and PA remarkably reduced the intra- and extracellular melanin contents of alpha-melanocyte-stimulating hormone-stimulated B16F10 cells. These results demonstrate that PO and PA have potential for use in the cosmetic industry.

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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Enhancement of Skin-Whitening and UV-Protective Effects of Centella asiatica L. Urban by Utrasonification Process (초음파 병행을 통한 병풀의 미백 및 자외선 차단 활성 증진 효과)

  • Ha, Ji-Hye;Kwon, Min-Chul;Kim, Seung-Seop;Jeong, Myoung-Hoon;Hwang, Baik;Lee, Hyeon-Yong
    • Korean Journal of Medicinal Crop Science
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    • v.18 no.2
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    • pp.79-85
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    • 2010
  • Enhancement effect of ultrasonification process on UV-protection and skin-whitening activities using Centella asiatica L. Urban extract was investigated. Cytotoxicity of the extracts measured on human skin fibroblast cells, CCD-986sk, and then, ultrasonification associated extracts showed 5~9% lower cytotoxicity then normal crude extracts on 1.0 mg/$m{\ell}$ of highest sample concentration. The associated extrats showed highest inhibition activity of hyaluronidase on 1.0 mg/$m{\ell}$ of concentration as 54.2%. Also, the associated extract reduced expression of MMP-1 on UV-irradiated CCD-986sk cells down to 100.2% from 136.1%, and revealed high inhibitory potency on tyrosinase as 74.6% by adding 1.0 mg/$m{\ell}$ of concentration. Ultrasonification associated extract showed strong inhibition effect of melanin production on Clone M-3 cells as 84.2% by adding 1.0 mg/$m{\ell}$ of concentration. From the preliminary observations, we considered that the extracts from C. asiatica could be potent natural materials for skin-whitening and anti-aging agent, and could enhance the activities by ultrasonification process.

Enhancement of Antioxidant Activities and Whitening Effect of Acer mono Sap Through Nano Encapsulation Processes (고로쇠 수액 나노입자의 항산화 활성 및 미백 효과의 증진)

  • Kim, Ji-Seon;Seo, Yong-Chang;Choi, Woon-Yong;Kim, Hack-Soo;Kim, Bo-Hyeon;Shin, Dae-Hyeon;Yoon, Chang-Soon;Lim, Hye-Won;Ahn, Ju-Hee;Lee, Hyeon-Yong
    • Korean Journal of Medicinal Crop Science
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    • v.19 no.3
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    • pp.191-197
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    • 2011
  • In this study, we investigated antioxidant activities and whitening effects of Acer mono sap by encapsulation of nanoparticles. Acer mono sap was through ultra high pressure process and then encapsulated by lecithin. Nano-encapsulated The nanoparticles of Acer mono sap showed highest free radical scavengering effect as 89.7% in adding sample (1.0 mg/ml), compared to sap of non-encapsulation. It was showed strong inhibition effect on melanin production test by Clone M-3 cells as 47.8%. High inhibitory of tyrosinase was also measured as 85.8% by adding lecithin nano-particle of 1.0 mg/ml. The nano-particles also showed 14.8% of low cytotoxicity against human normal fibroblast cells in adding 1.0 mg/ml of the highest concentration. These results indicate that Acer mono sap may be a source of cosmetic agents capable of improving whitening effect and antioxidant activites.