• Title/Summary/Keyword: Tyrosinase inhibition activity

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The Study on the Whitening Effect of Ephedra sinica Extract (마황추출물의 미백효과에 관한 연구)

  • Yoo Yung-Geun;Joung Min-Seok;Choi Song-Wan;Kim Joong-Hoi
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.31 no.2 s.51
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    • pp.153-159
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    • 2005
  • In this study, we investigated the application of an extract from Ephedra sinica which has been composed of traditional Korean medicine as a whitening ingredient. The extract of Ephedra sinica which was obtained from the mixture of methanol and water (1:1) the inhibitory effect of tyrosinase. Then, Ephedra sinica was extracted by two different solvents. One was water and the other was methylene chloride. Only, the water extract of Ephedra sinica showed the inhibitory effort of tyrosinase; the anti-tyrosinase activity with $0.2\%$ of the water extract was $60.6\%$. But the extract of Ephedra sinica in methylene chloride fraction showed little inhibitory effect on tyrosinase. The inhibitory effect of the concentrated water extract of Ephedra sinica was tested on L-DOPA auto-oxidation and melanin synthesis in B-16 melanoma. In L-DOPA auto-oxidation, $0.5\%$ of the concentrated water extract showed $87\%$ of inhibition of L-DOPA auto-oxidation and the $0.75\%$ concentrated Ephedra sinica extract in wafer fraction inhibited $98.8\%$ of that. In melanin synthesis of B-16 melanoma, the concentrated water effect of Ephedra sinica inhibited $70.2\%$ or $79.9\%$ of inhibitory effect on that at the concentration of $0.05\%$ or $0.075\%$, respectively. For verifying the skin whitening effect of the concentrated water extract of Ephedra sinica in vivo, we performed the clinical test of that. The research showed the significant skin whitening effect of a cream containing $0.5\%$ Ephedra sinica extract and the statistical analysis showed a significant difference (p < 0.05) between sample (containing $0.5\%$ Ephedra sinica extract) and placebo after 10 weeks.

Physiological Activity of Methanol Extracts from Sambucus sieboldiana var. miquelii (Nakai) Hara (지렁쿠나무 메탄올 추출물의 생리활성 연구)

  • Oh, Yu Jin;Cho, Hae Jin;Woo, Hyun Sim;Byeon, Jun-Gi;Kim, Yeong-Su;Kim, Dae Wook
    • Journal of Life Science
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    • v.30 no.11
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    • pp.965-972
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    • 2020
  • Sambucus sieboldiana var. miquelii (Nakai) Hara is distributed in Korea, China, and Japan, and has been used as an anti-rheumatic in folk medicine in oriental countries. The present study aims to investigate the potential use of this species in health functional foods, cosmetics, and food preservatives. Methanol extracts of leaves and branches from this plant were prepared to quantitatively analyze the total phenol and flavonoid contents, and to investigate the antioxidative and enzyme inhibitory activities, and the inhibition of nitric oxide (NO) production activity. The results showed that the total polyphenol and flavonoid contents of the crude extract were 1.52±0.1 mg/g and 1.73±0.1 mg/g, respectively. S. sieboldiana polyphenols exhibited potent scavenging activity shown by 2, 2'-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and 2, 2-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation assay. The crude extract also exhibited significant α-glucosidase and tyrosinase inhibitory activity with IC50 values of 183.5 ㎍/ml and 323.9 ㎍/ ml, respectively. Additionally, the crude extract exhibited strong anti-inflammatory activity determined through the nitric oxide inhibition assay in a dose-dependent manner with an IC50 value of 36.7 ㎍/ml and no cytotoxic effect on the macrophages. Therefore, we demonstrated that the leaves and branches of S. sieboldiana extract possess antioxidant, anti-diabetic, depigmentation potential, and NO production inhibitory activities. According to recent research, S. sieboldiana has great potential as a source of the bioactive compound which could be used as food, cosmetics, and pharmaceutical agents.

The Anti-Wrinkle and Whitening Effect of Extracts of Castanea crenata Inner Shell (밤부산물(율피)의 주름개선 및 미백 효과)

  • Jang, Min-Jung;Cheon, Soon-Ju;Kim, Hui-Yeong;Kwoen, Dae-Jun;Kim, Hak-Yoon;Kim, Sea-Hyun;Lee, Jin-Tae
    • Journal of Life Science
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    • v.21 no.5
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    • pp.734-738
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    • 2011
  • Aging in humans is inexorable and inescapable. The progressive decrease of physiological capacity and the reduction of the ability to cope with environmental stresses lead to increased susceptibility and vulnerability to human disease. Recently, in the cosmetic industry, many researchers have paid considerable attention to delaying or improving the symptoms of skin aging. Since the early 1990`s, there have been various challenges in developing cosmeceutical products which have strong anti-aging effects, and this has been an important issue in the cosmetic industry. Meanwhile, development of anti-aging cosmetics supported by biochemical activities in the skin has been researched. Castanea crenata inner Shell solvent extracts were investigated for anti-wrinkle and whitening effects, in order to apply it as a functional ingredient for cosmetic products. For anti-wrinkle effect, elastase inhibition activity of Castanea crenata inner shell acetone extract (CA) was 51.0% at a concentration of 100 ug/ml. The collagenase inhibition activity of CA and Castanea crenata inner shell ethanol extract (CE) was 96.4%, 94.3% at a concentration of 50 ug/ml. The tyrosinase inhibitory effect, which is related to skin-whitening, was 47.2% and 45.8% in CA and CE at a concentration of 500 ug/ml. All these results suggest that Castanea crenata inner shell can be effectively used as a cosmeceutical ingredient for the prevention of wrinkles.

Physiological Activities of Leaf and Root Extracts from Liriope platyphylla (맥문동(Liriope platyphylla) 잎과 뿌리 추출물의 생리활성)

  • Seo, Soo-Jung;Kim, Nam-Woo
    • Food Science and Preservation
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    • v.17 no.1
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    • pp.123-130
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    • 2010
  • We compared physiological activities in reflux extracts from Liriope platyphylla leaves and roots. The water extract of roots had the highest solid extraction yield of 53.96%. The greatest level of total polyphenols was 186.88 mg/g in methanol extracts from leaves, whereas water extract from leaves showed the highest concentration of flavonoid compounds, at 159.29 mg/g. The leaf extract had 97.42% of the electron-donating ability (EDA) of the positive control, at 0.5 mg/mL. The superoxide dismutase (SOD)-like activity of water extract of leaves was 9.75% of the positive control value, at 1.0 mg/mL. The nitrite scavenging ability of methanolic extract from leaves was highest, at 40.56% of the positive control level at pH 1.2 and a concentration of 1.0 mg/mL, whereas root extracts were ineffective in this regard. Inhibition of xanthine oxidase by leaf extracts was more than 99% of the positive control value at 1.0 mg/mL, whereas water and methanolic root extracts had activities of 93.75% and 68.47%, respectively. When tyrosinase inhibition was examined, the water extract of leaves had 22.80% of positive control activity but methanolic extracts were inactive. These results indicate that leaves of L. platyphylla will be more useful for development of functional products than the roots, which are used to make medicinal preparations.

Citrus Peel Wastes as Functional Materials for Cosmeceuticals

  • Kim, Sang-Suk;Lee, Jung-A;Kim, Ji-Young;Lee, Nam-Ho;Hyun, Chang-Gu
    • Journal of Applied Biological Chemistry
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    • v.51 no.1
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    • pp.7-12
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    • 2008
  • The suitability of CPWs, by-products of the juice industry, was investigated as a source for the production of cosmeceuticals. Four kinds of CPWs, CW, CWE, CWER, and CWEA, were examined for their antioxidant potentials in terms of DPPH radical-scavenging ability for anti-wrinkle applications, inhibition of tyrosinase or melanin production for whitening products, and anti-inflammatory effects to treat various skin diseases such as atopic dermatitis and acne as well as for anti-bacterial activity against acne-inducing pathogens. Of the four extracts, CWER was the most potent tyrosinase inhibitor ($IC_{50}$ value: $109\;{\mu}g/mL$), and CWEA ($IC_{50}:\;167\;{\mu}g/mL$) showed good antioxidative effects. CWE and CWEA samples had dose-dependent inhibitory effects on the melanin production. The cytotoxic effects of the four CPWs were determined by colorimetric MTT assays using human keratinocyte HaCaT cells. Most extracts exhibited low cytotoxicity at $100\;{\mu}g/mL$. These results suggest CPWs are attractive candidates for topical applications on the human skin.

MR304-1, A Melanin Synthesis Inhibitor Produced by Trichoderma harzianum (Trichoderma harzianum이 생산하는 melanin 생성 저해물질 MR304-1)

  • Lee, Choong-Hwan;Chung, Myung-Chul;Lee, Ho-Jae;Lee, Ke-Ho;Kho, Yung-Hee
    • Microbiology and Biotechnology Letters
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    • v.23 no.6
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    • pp.641-646
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    • 1995
  • During the screening of inhibitors of melanin biosynthesis from microbial secondary metabolites, a fungal strain MR304 which was capable of producing high level of an inhibitor was selected. Based on taxonomic studies, this fungus could be classified as Trichoderma harzianum. The active compound (MR304-1) was purified from culture broth by Diaion HP-20 column chromatography, ethylacetate extraction, Sephadex LH-20 column chromatographv and HPLC. The inhibitor was identified as 3-(1,5-dihvdroxy-3-isocyanocyclopent-(E)-3-envl)prop-2-enoate by spectroscopic methods of UV, ESIMS, $^{1}$H-NMR, $^{13}$C-NMR, NOE, HMQC and HMBC. MR304-1 showed strong mushroom tyrosinase inhibitory activity with IC$_{50}$ value of 0.25 $\mu $g/ml. It inhibited melanin biosynthesis with 15 mm inhibition zone at 30 $\mu $g/paper disc in Streptomyces bikiniensis, a bacterium used as an indicator organism in this work. It also inhibited melanin biosynthesis in B16 melanoma cells with a niinimum inhibitory concentration of 0.05 $\mu $g/ml.

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Physiological Activities of Roots Extracts from Calystegia japonica

  • Lee, Yang-Suk;Choi, Bok-Dong;Joo, Eun-Young;Kim, Nam-Woo
    • Biomedical Science Letters
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    • v.15 no.4
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    • pp.335-342
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    • 2009
  • This study was investigated to evaluate the contents of polyphenols and flavonoids, and physiological activities of various extracts from Calystegia japonica roots for making good use of their functional materials. The roots of C. japonica were extracted with water (WE), ethanol (EE) and hot water (HWE) by different methods. Among these extracts, the highest extracting yield was 30.30% of HWE, while the highest contents of total polyphenols and flavonoids were 40.85% and 6.40% of WE, respectively. The nitrite scavenging abilities were ranged from 31.31% (HWE) to 37.46% (EE) at pH 1.2 and 1.0 mg/ml concentration. In the measurements of electron donating abilities, EE showed the highest effect as 91.83% at 0.3 mg/ml assay concentration, and the electron donating ability was decreased as the extract concentration was increased. In the results of superoxide dismutase (SOD)-like activity, HWE showed the highest effect as 7.15% at 1.0 mg/ml. The tyrosinase inhibition activities of WE and EE were 15.28% and 14.97%, respectively. The xanthine oxidase inhibitory effects were ranged from 97.50 to 99.28% at 1.0 mg/ml. These results indicate that C. japonica extract has a good antioxidant effects and could be useful for developing functional products.

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Improved Bioactivity of 3-O-β-ᴅ-Glucopyranosyl Platycosides in Biotransformed Platycodon grandiflorum Root Extract by Pectinase from Aspergillus aculeatus

  • Ju, Jung-Hun;Lee, Tae-Eui;Lee, Jin;Kim, Tae-Hun;Shin, Kyung-Chul;Oh, Deok-Kun
    • Journal of Microbiology and Biotechnology
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    • v.31 no.6
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    • pp.847-854
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    • 2021
  • Platycodon grandiflorum (balloon flower) root (Platycodi radix, PR) is used as a health supplement owing to its beneficial bioactive properties. In the present study, the anti-inflammatory, antioxidant, and whitening effects of deglycosylated platycosides (saponins) from PR biotransformed by pectinase from Aspergillus aculeatus were investigated. The bioactivities of the platycosides improved when the number of sugar moieties attached to the aglycone platycosides was decreased. The deglycosylated saponins exhibited higher lipoxygenase inhibitory activities (anti-inflammatory activities) than the precursor platycosides and the anti-inflammatory compound baicalein. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity of the pectinasetreated PR extract was higher than that of the non-treated PR extract. The trolox-equivalent antioxidant capacity (TEAC) assay showed improved values as the saponins were hydrolyzed. The tyrosinase inhibitory activities (whitening effects) of deglycosylated platycosides were higher than those of the precursor platycosides. Furthermore, 3-O-β-ᴅ-glucopyranosyl platycosides showed higher anti-inflammatory, antioxidant, and whitening activities than their precursor glycosylated platycosides. Therefore, 3-O-β-ᴅ-glucopyranosyl platycosides may improve the beneficial effects of nutritional supplements and cosmetic products.

The Inhibitory Effects of Poria cocos Bark Extract on Melanogenesis (복령피 추출물의 멜라닌 생성 저해 효과)

  • Lee, Eung-Ji;Bae, Seong-Yun;Son, Rak-Ho;Lee, Yong-Hwa
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.35 no.3
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    • pp.243-250
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    • 2009
  • To develop a new natural whitening agent for cosmetics, we investigated the inhibitory effects of Poria cocos Bark extracts (PCBE) and its active compound on melanogenesis. PCBE showed ROS scavenging activities in 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and xanthine/xanthine oxidase system with the $IC_{50}$ values of $19.4{\pm}2.21{\mu}g$/mL and $IC_{50}=103{\pm}3.33{\mu}g$/mL, respectively. PCBE reduced intracellular tyrosinase activity about 34 % at concentration of $50{\mu}g$/mL. And PCBE reduced melanin contents of B16 melanoma cells about 51 % at concentration of $50{\mu}g$/mL without cell cytotoxicity (below $100{\mu}g$/mL). We purified one active compound from PCBE and identified its structure. It was identified as 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid, triterpene family, by $^1H$-NMR, $^{13}C$-NMR and Mass analysis. 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid showed ROS scavenging activities in DPPH radical and xanthine/xanthine oxidase system with the $IC_{50}$ values of $4.3{\pm}0.15{\mu}g$/mL and $54{\pm}1.67{\mu}g$/mL, respectively. Also, it was shown that 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid reduced intracellular tyrosinase activity about 43 % at concentration of $10{\mu}g$/mL. And it inhibited melanin synthesis in a dose dependent manner ($IC_{50}=3.6{\mu}g$/mL) without cell cytotoxicity (below $100{\mu}g$/mL). 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid inhibited tyrosinase, TRP-1 and TRP-2 expression at protein level. These results suggest that PCBE and 3-$\beta$-hydroxylanosta-7,9(11),24-trien-4-oic acid reduced melanin formation by the inhibition of tyrosinase activity and expression in B16 melanoma cells. Therefore, we suggest that PCBE could be used as a useful whitening agent.

A Novel Synthesized Tyrosinase Inhibitor, (E)-3-(4-hydroxybenzylidene) chroman-4-one (MHY1294) Inhibits α-MSH-induced Melanogenesis in B16F10 Melanoma Cells (신규 합성물질 (E)-3-(4-하이드록시벤질리딘)크로마논 유도체의 티로시나아제 효소활성 저해 및 멜라닌 생성 억제 효과)

  • Jeon, Hyeyoung;Lee, Seulah;Yang, Seonguk;Bang, EunJin;Ryu, Il Young;Park, Yujin;Jung, Hee Jin;Chung, Hae Young;Moon, Hyung Ryong;Lee, Jaewon
    • Journal of Life Science
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    • v.31 no.8
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    • pp.719-728
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    • 2021
  • Melanin pigments are abundantly distributed in mammalian skin, hair, eyes, and nervous system. Under normal physiological conditions, melanin protects the skin against various environmental stresses and acts as a physiological redox buffer to maintain homeostasis. However, abnormal melanin accumulation results in various hyperpigmentation conditions, such as chloasma, freckles, senile lentigo, and inflammatory pigmentation. Tyrosinase, a copper-containing enzyme, plays an important role in the regulation of the melanin pigment biosynthetic pathway. Although several whitening agents based on tyrosinase inhibition have been developed, their side effects, such as allergies, DNA damage, mutagenesis, and cytotoxicity of melanocytes, limit their applications. In this study, we synthesized 4-chromanone derivatives (MHY compounds) and investigated their ability to inhibit tyrosinase activity. Of these compounds, (E)-3-(4-hydroxybenzylidene)chroman-4-one (MHY1294) more potently inhibited the enzymatic activity of tyrosinase (IC50 = 5.1±0.86 μM) than kojic acid (14.3±1.43 μM), a representative tyrosinase inhibitor. In addition, MHY1294 showed competitive inhibitory action at the catalytic site of tyrosinase and had greater binding affinity at this site than kojic acid. Furthermore, MHY1294 effectively inhibited α-melanocyte stimulating hormone (α-MSH)-induced melanin synthesis and intracellular tyrosinase activity in B16F10 melanoma cells. The results of the present study indicate that MHY1294 may be considered as a candidate pharmacological agent and cosmetic whitening ingredient.