• Title/Summary/Keyword: Elastase inhibition

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Inhibition of Experimental Systemic Inflammation (Septic Inflammation) and Chronic Bronchitis by New Phytoformula BL Containing Broussonetia papyrifera and Lonicera japonica

  • Ko, Hyun Jeong;Kwon, Oh Song;Jin, Jeong Ho;Son, Kun Ho;Kim, Hyun Pyo
    • Biomolecules & Therapeutics
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    • v.21 no.1
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    • pp.66-71
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    • 2013
  • Broussonetia papyrifera and Lonicera japonica have long been used in the treatment of inflammatory disorders in Chinese medicine, especially respiratory inflammation. Previously, a new phytoformula (BL) containing B. papyrifera and L. japonica was found to exert strong anti-inflammatory activity against several animal models of inflammation, especially against an animal model of acute bronchitis. In the present investigation, the effects of BL on animal models of septic inflammation and chronic bronchitis are examined. Against lipopolysaccharide (LPS)-induced septic inflammation in mice, BL (200-400 mg/kg) reduced the induction of some important proinflammatory cytokines. At 1 h after LPS treatment, BL was found to considerably inhibit TNF-${\alpha}$ production when measured by cytokine array. At 3 h after LPS treatment, BL inhibited the induction of several proinflammatory cytokines, including IFN-${\gamma}$ and IL-$1{\beta}$, although dexamethasone, which was used as a reference, showed a higher inhibitory action on these biomarkers. Against chronic bronchitis induced by LPS/elastase instillation in rats for 4 weeks, BL (200-400 mg/kg/day) significantly inhibited cell recruitment in bronchoalveolar lavage fluid. Furthermore, BL considerably reduced lung injury, as revealed by histological observation. Taken together, these results indicate that BL may have a potential to treat systemic septic inflammation as well as chronic bronchitis.

Studies on Skin Permeation with Polymer Micelles and the Cell Penetrating Peptide of Pyrus Serotina Var Stem Extracts

  • An, Gyu Min;Park, Su In;Kim, Min Gi;Heo, Soo Hyeon;Shin, Moon Sam
    • Korean Chemical Engineering Research
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    • v.58 no.1
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    • pp.21-28
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    • 2020
  • The stem extract from Pyrus serotina var has natural antioxidant ability, but the extraction method does not result in a soluble compound in cosmetic formulations. This study investigated the cosmetic efficacy of the Pyrus serotina var stem extract and its epidermis permeation ability when combined with polymer micelles and a cell penetrating peptide. The total concentration of polyphenol compounds was determined to be 103.1644 ± 1.38 mg/g in the ethanol extract and 78.97 ± 1.45 mg/g in the hydrothermal extract. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging effects were 55.94 ± 0.22% in the ethanol extract at 1,000 mg/L. Superoxide dismutase (SOD) activity rates were 104.05 ± 3.28% in the ethanol extract at 62.5 mg/L. The elastase inhibition rate was 67.21 ± 2.72% in the ethanol extract at 1,000 mg/L. An antimicrobial effect was observed in the Propionibacterium acnes strain. In the epidermal permeability experiment, it was confirmed that formulation of the polymer micelle containing the Pyrus serotina var stem extract and cell penetrating peptide (R6, hexa-D-arginine) showed small particle size and much better skin permeability. The cumulative amount of total Pyrus serotina var stem extract that penetrated to the skin over time increased over 24 hours in three formulations. The three formulations showed 51.61 ㎍/㎠ (Formulation 0), 75.97 ㎍/㎠ (Formulation 1) and 95.23 ㎍/㎠ (Formulation 2) skin penetration, respectively. Therefore, it was confirmed that the ethanol extracts of Pyrus serotina var stem showed good cosmetic efficacy and excellent epidermis permeation ability when combined with a polymer micelle and cell penetrating peptide. Thus, this extract has the potential to be used as a safe and natural cosmetic material in the future.

Enhancement of Anti-wrinkle Activities of Abeliophyllum distichum Nakai through Low Temperature Extraction Process (미선나무의 저온 추출 공정에 의한 항주름 활성 증진)

  • Kim, Nam Young;Lee, Hyeon Yong
    • Korean Journal of Medicinal Crop Science
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    • v.23 no.3
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    • pp.231-236
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    • 2015
  • Skin anti-wrinkle activities of the stems and leaves of Abeliophyllum distichum Nakai were evaluated by the extracts obtained from various extraction processes such as using hot water at $100^{\circ}C$, 70% ethanol at $85^{\circ}C$, and 70% ethanol with ultrasonication at $60^{\circ}C$ The ultrasonicated extract showed 95.62% of the highest cell viability in addition of $0.3mg/m{\ell}$ of the extracts into the normal human fibroblast cell, CCD-986sk. For antioxidant activities, the extracts using ultrasonicated extract showed the highest DPPH free radical scavenging as 80.27%, followed by 75.88% and 62.44% for the extracts using ethanol extract and water extract. The ultrasonicated extract also showed the highest elastase inhibition activity as 25.32%, compared to ethanol extract and water extract based method at 22.01% and 12.88%, respectively. MMP-1 production was most effectively decreased down to $2908.1pg/m{\ell}$ with ultrasonicated extract while $6640.8pg/m{\ell}$ with water extract and $3609.3pg/m{\ell}$ with ethanol extract, in addition of $0.3mg/m{\ell}$. Collagen production was increased up to $154.7ng/m{\ell}$ in addition of ultrasonicated extract, and followed by $121.4ng/m{\ell}$ and $31.2ng/m{\ell}$ for ethanol extract and water extract, respectively. These results indicate that the ethanol extract should have skin anti-wrinkling activities and can be improved by the ultrasonication process that high energy input elute more amounts of bioactive substances eluting more amounts of bioactive substances from the high energy input of ultrasonication.

Effect of Anti-Skin Wrinkle and Antioxidant of Agastache rugosa Kentz through Fermentation Process of the lactic acid (유산균 발효 배초향 추출물의 항산화 활성과 주름개선 효능)

  • Kim, Nam Young;Park, Dae Su;Lee, Hyeon Yong
    • Korean Journal of Medicinal Crop Science
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    • v.23 no.1
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    • pp.37-42
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    • 2015
  • This study was to investigate anti-skin wrinkle effect of Agastache rugosa Kentz extracts by extraction processes. In the comparison of the effect of the solvent extraction, the extracts by 70% ethanol (EE) showed better biological activities that those by hot water. Therefore, further fermented Agastache rugosa was applied to 70% ethanol extraction process (FEE). FEE showed higher DPPH scavenging activity of 62.98% than EE's 62.71% at $1.0mg/m{\ell}$, but there was no significant. Elastase inhibition was measured 23.0% from FEE at $1.0mg/m{\ell}$. Cytotoxicity showed the highest 16.26% from FEE, this value is safe in the cell experiment. Collagen production showed $113.1ng/m{\ell}$ from FEE, on the other hand EE was measured $77.4ng/m{\ell}$ in adding $1.0mg/m{\ell}$. MMP-1 production was observed $1398pg/m{\ell}$ from FEE and EE was measured $1632pg/m{\ell}$. These results were found the highest antioxidant and anti-wrinkle effect. As a result, it was also confirmed that anti-skin wrinkle activities of the Agastache rugosa Kentz extract was correlated with anti-oxidant activities.

Screening of Functional Materials from Solvent Fractions of Apple Flower Leaf Extract (사과꽃잎 추출물의 용매 분획으로부터 기능성 소재의 탐색)

  • Choi, Sun-Ju;Cho, Eun-Ah;Cho, Eun-Hye;Jeong, Yoon-Joo;Ku, Chang-Sub;Ha, Byung-Jhip;Chae, Hee-Jeong
    • KSBB Journal
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    • v.26 no.2
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    • pp.165-171
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    • 2011
  • Fractional solvent extraction by organic solvents such as hexane, chloroform, ethylacetate, and butanol was carried out using 70% ethanol extract of apple flower leaves. Biological activities including antioxidant, whitening, antimicrobial and anti-wrinkle activities were investigated and bio-active materials of the extracts were identified using GC/MSD. Among the tested solvent fractions, ethylacetate fraction showed the highest total polyphenol content (1218.94 ${\mu}g/mL$), and flavonoid (140 ${\mu}g/mL$). The DPPH radical scavenging activities was over 80% at a dry matterbased concentration of 200 ${\mu}g/{\mu}L$ and SOD-like activity was over 90% at 50 ${\mu}g/mL$ concentration in ethylacetate fraction that was slightly lower than of ascorbic aicd. Tyrosinase inhibition activity related to skin-whitening was over 60% by ethylacetate fraction of 100 ${\mu}g/mL$. As an anti-aging effect, elastase inhibitory activity was about 45% in ethylacetate fraction. Also, it showed a significantly antimicrobial activity against P. acenes. From GC/MSD analysis, a characteristic peak of high content in ethylacetate fraction was identified as kaempferol, which has been reported as a bioactive compound.

Biological Activities of Cosmetic Material from Ten Kinds of Flower Ethanol Extracts (화장품 소재로서의 꽃 10 종 에탄올추출물 생리활성 특성연구)

  • Lee, Tae Bum;So, Yang Kang;Kim, Se Yul;Hwang, Ji Young
    • Korean Journal of Medicinal Crop Science
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    • v.28 no.4
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    • pp.260-275
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    • 2020
  • Background: We investigated the antioxidant, anti-wrinkles, whitening, and moisturizing properties and amounts of phenolic compounds of ethanol extracts from flowers of 10 resource plants from Namwon and Mt. Jiri., Korea. Methods and Results: We measured antioxidant efficacy based on the total polyphenol, and total flavonoid content, and the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. We evaluated the inhibitory effect on melanin synthesis and tyrosinase activity for the whitening effect. Furthermore, we analyzed the elastase and matrix metalloproteinase-1 (MMP-1) inhibition activity for anti-wrinkle capacity. To evaluate the moisturizing effect, we examined hyaluronan synthase (HAS) mRNA expression. In addition, the 19 phenolic compounds were detected using high performace liquid chromatography (HPLC). Among the 10 flowers, the antioxidant effect was high in the order of Rosa multiflora, Nelumbo nucifera, and Elsholtzia splendens. Whitening effect was high in the order of N. nucifera, R. multiflora, and Dendranthema zawadskii. As for the anti-wrinkle property, N. nucifera was the most effective followed by R. multiflora. Taraxacum coreanum was the best for moisturizing effect, followed by D. zawadskii, and E. splendens. Seven phenolic compounds were detected in the extracts of the 10 flowers. Conclusions: Overall, the extracts of five flowers extracts showed strong potential as antioxidant, whitening, anti-wrinkle, and moisturizing functional cosmetic agents.

Inhibitory Effects of Flavonoids Isolated from Leaves of Petasites japonicus on $\beta$-Secretase (BACE1)

  • Song, Kyung-Sik;Choi, Sun-Ha;Hur, Jong-Moon;Park, Hyo-Jun;Yang, Eun-Ju;MookJung, In-Hee;Yi, Jung-Hyun;Jun, Mi-Ra
    • Food Science and Biotechnology
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    • v.17 no.6
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    • pp.1165-1170
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    • 2008
  • The deposition of the amyloid $\beta}$ ($A{\beta}$)-peptide following proteolytic processing of amyloid precursor protein (APP) by $\beta$-secretase (BACE1) and $\gamma$-secretase is critical feature in the progress of Alzheimer's disease (AD). Consequently, BACE1, a key enzyme in the production of $A{\beta}$, is a prime target for therapeutic intervention in AD. In the course of searching for BACE1 inhibitors from natural sources, the ethyl acetate fraction of Petasites japonicus showed potent inhibitory activity. Two BACE1 inhibitors quercetin (QC) and kaempferol 3-O-(6"-acetyl)-$\beta$-glucopyranoside (KAG) were isolated from P. japonicus by activity-guided purification. QC, in particular, non-competitively attenuated BACE1 activity with $IC_{50}$ value of $2.1{\times}10^{-6}\;M$ and $K_i$ value of $3.7{\times}10^{-6}\;M$. Both compounds exhibited less inhibition of $\alpha$-secreatase (TACE) and other serine proteases including chymotrypsin, trypsin, and elastase, suggesting that they ere relatively specific and selective inhibitors to BACE1. Furthermore, both compounds significantly reduced the extracellular $A{\beta}$ secretion in $APP_{695}$-transfected B103 cells.

Comparison of Functional Properties of Blood Plasma Collected from Black Goat and Hanwoo Cattle

  • Shine Htet Aung;Edirisinghe Dewage Nalaka Sandun Abeyrathne;Mahabbat Ali;Dong Uk Ahn;Young-Sun Choi;Ki-Chang Nam
    • Food Science of Animal Resources
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    • v.43 no.1
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    • pp.46-60
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    • 2023
  • Slaughterhouse blood is a by-product of animal slaughter that can be a good source of animal protein. This research purposed to examine the functional qualities of the blood plasma from Hanwoo cattle, black goat, and their hydrolysates. Part of the plasma was hydrolyzed with proteolytic enzymes (Bacillus protease, papain, thermolysin, elastase, and α-chymotrypsin) to yield bioactive peptides under optimum conditions. The levels of hydrolysates were evaluated by 15% sodium dodecyl sulfate polyacrylamide gel electrophoresis. The antioxidant, metal-chelating, and angiotensin I-converting enzyme (ACE) inhibitory properties of intact blood plasma and selected hydrolysates were investigated. Accordingly, two plasma hydrolysates by protease (pH 6.5/55℃/3 h) and thermolysin (pH 7.5/37℃/3-6 h) were selected for analysis of their functional properties. In the oil model system, only goat blood plasma had lower levels of thiobarbituric acid reactive substances than the control. The diphenyl picrylhydrazyl radical scavenging activity was higher in cattle and goat plasma than in proteolytic hydrolysates. Ironchelating activities increased after proteolytic degradation except for protease-treated cattle blood. Copper-chelating activity was excellent in all test samples except for the original bovine plasma. As for ACE inhibition, only non-hydrolyzed goat plasma and its hydrolysates by thermolysin showed ACE inhibitory activity (9.86±5.03% and 21.77±3.74%). In conclusion, goat plasma without hydrolyzation and its hydrolysates can be a good source of bioactive compounds with functional characteristics, whereas cattle plasma has a relatively low value. Further studies on the molecular structure of these compounds are needed with more suitable enzyme combinations.

Antioxidant, Anti-wrinkle and Antimicrobial Effects of Coffee Grounds Extract from Dutch Coffee (더치 Coffee Grounds 추출물의 항산화, 주름개선, 항균 효과)

  • Park, Su In;Kim, Ah Reum;Kim, Seon Hwa;An, Gyu Min;Kim, Min Gi;Shin, Moon Sam
    • Journal of the Korean Applied Science and Technology
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    • v.35 no.4
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    • pp.1038-1047
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    • 2018
  • This study confirmed possibility of cosmetic material for Espresso coffee grounds extracted at high temperature, high pressure, short time and Dutch coffee grounds extracted at low temperature, atmospheric pressure, long time. For this purpose, we evaluated the biological activities of antioxidant, anti-wrinkles and antimicrobial effects using ethanol extracts of Esproso and Dutch coffee grounds. The results of total polyphenolic compound contents was $90.39{\pm}0.04mg/g$ for Dutch coffee grounds extract, which was higher than $64.96{\pm}0.38mg/g$ for Espresso coffee grounds extract, based on $113.63{\pm}0.22mg/g$ for coffee beans extract as the reference one. DPPH radical scavenging activity and SOD-like activity of Dutch coffee grounds extract were found to be better than those of Espresso coffee grounds extracts, referenced on coffee bean extract. As a result of inhibition effect of Elastase activity, Dutch coffee grounds extract showed higher inhibition effect than Espresso coffee grounds extract, based on coffee bean extract. In addition, Dutch coffee grounds extract showed good anti-microbial effects at Escherichia coli, Bacillus, Propionibacterium acnes and there was little difference in the clear zone size between Dutch coffee grounds extract and coffee bean extract as a reference one. From the results of the experiments, it was confirmed that Dutch coffee grounds extract had excellent antioxidant, anti-wrinkle and antimicrobial effects and could be used as safe natural cosmetic material in the future.

A Study of Anti-wrinkle Activities as a Functional Cosmetic Ingredient of Rhododendron brachycarpum Extracts (만병초(Rhododendron brachycarpum) 추출물의 기능성 화장품 소재로써의 주름개선 활성에 관한 연구)

  • Yeom, Hyeon-Ji;Oh, Min-Jeong;Chae, Jung-Woo;Lee, Jin-Young
    • Journal of Life Science
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    • v.32 no.8
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    • pp.622-632
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    • 2022
  • The purpose of this study was to investigate activities as functional cosmetic materials, focusing on Rhododendron brachycarpum (RB) and Rhododendron fortunei (RF). The tyrosinase inhibitory effect, related to skin-whitening, was 32.6% and 39.3% respectively at the concentration of 1,000 ㎍/ml. The elastase inhibitory effect, related to skin anti-wrinkling activity, was 30% and 36.2% at 1,000 ㎍/ml concentration. Collagenase inhibitory activity showed 77.7%, and 80.2% respectively at 1,000 ㎍/ml concentration, which demonstrated excellent inhibitory activity. For a cell viability test, that measured on fibroblast cells by RB and RF extracts. Furthermore, the cell viability test showed 100.9% and 98.9% with cell viability at 100 ㎍/ml concentration in CCD-986Sk. The protein expression inhibitory effect of RB and RF extracts was measured by western blot at 25, 50, and 100 ㎍/ml concentrations, and the β-actin was used as a positive control. As a result, western blot of RB and RF extracts was measured by the expression inhibition rate of the MMP-1, MMP-2, MMP-3 protein, and was decreased by 67.2%, 65.5%, 13.6%, and 89.1%, 85.0%, and 62.7% at 100 ㎍/ml concentration. The mRNA expression inhibitory effect of RB and RF extracts was measured by RT-PCR at 25, 50, and 100 ㎍/ml concentrations, and the GAPDH was used as a positive control. According to the results of RT-PCR of RB and RF extracts, the expression inhibition rate of the MMP-1, MMP-2, and MMP-3 mRNA was decreased by 70.1%, 9.1%, 37.9%, and 38.2%, 8.3%, 57.3% at 100 ㎍/ml concentrations. So, RB and RF extracts showed the anti-wrinkle effectiveness as a functional cosmetic material.