• Title/Summary/Keyword: Elastase Inhibitory Activity

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Molecular Pharmacological Interaction of Phenylbutazone to Human Neutrophil Elastase

  • Kang, Koo-Il
    • The Korean Journal of Physiology and Pharmacology
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    • v.2 no.3
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    • pp.385-393
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    • 1998
  • Human neutrophil elastase (HNElastase, EC 3.4.21.37), a causative factor of inflammatory diseases, was purified by Ultrogel AcA54 gel filtration and CM-Sephadex ion exchange chromatography. HNElastase was inhibited by phenylbutazone in a concentration dependent manner up to 0.4 mM, but as the concentration increased, the inhibitory effect gradually diminished. Binding of phenylbutazone to the human neutrophil elastase caused strong Raman shifts at 200, 440, and 1194 $cm^{-1}$. The peak at 1194 $cm^{-1}$ might be evidence of the presence $of\;-N=N-{\Phi}$ radical. The core area of the elastase, according to the visual molecular model of human neutrophil elastase, was structurally stable. A deeply situated active center was at the core area surrounded by hydrophobic amino acids. Directly neighboring the active site was one positively charged atom and two atoms carrying a negative charge, which enabled the enzyme and the drug to form a strong interaction. Phenylbutazone may form a binding, similar to a key & lock system to the atoms carrying opposite charges near the active site of the enzyme molecule. Furthermore, the hydrophobicity of the surrounding amino acid near the active site seemed to enhance the binding strength of phenylbutazone. Binding of phenylbutazone near the active site may cause masking of the active site, preventing the substrate from approaching the active site and inhibiting elastase activity.

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Functional Biological Activity of Hot Water and Ethanol Extracts from Taraxaci Herba (포공영의 열수 및 에탄올 추출물의 기능적 생리활성)

  • Lim, Ae-Kyung;Kim, Jung-Ok;Jung, Mee-Jung;Jung, Hee-Kyoung;Hong, Joo-Heon;Kim, Dae-Ik
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.37 no.10
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    • pp.1231-1237
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    • 2008
  • This study was conducted to investigate the functional biological effects of hot water and ethanol extracts from Taraxacum mongolicum (TM). Then, the hot water and ethanol extracts of TM were measured for total flavonoids content, total phenolics content, electron donating ability, nitrite-scavenging ability, SOD-like activity, tyrosinase inhibitory effect, and elastase inhibitory effect. Total flavonoids contents of hot water and ethanol extracts from TM were 7.80$\pm$0.97 mg/g and 9.12$\pm$0.51 mg/g, respectively, and total phenolics contents were estimated as 54.20$\pm$1.95 mg/g for water extract and 79.43$\pm$4.44 mg/g for ethanol extract. The $RC_{50}$ values for electron donating ability of hot water and ethanol extracts were 943.98 $\mu$g/mL and 309.41 $\mu$g/mL. SOD-like activity and nitrite-scavenging ability were dependent on concentration of hot water and ethanol extracts, and the activity of ethanol extract was higher than that of hot water extract. However, hot water and ethanol extracts from TM showed no inhibitory activities on the elastase and tyrosinase inhibitory activities. Based on the above results, the ethanol extract of TM seems to be the most pertinent for use as functional food and cosmetic.

Isolation and Characterization of Elastase Inhibitor from Areca catechu (빈랑으로부터 Elastase 저해물질의 분리 및 특성조사)

  • 조중제;이건국;조병기;최정도
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.26 no.1
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    • pp.163-186
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    • 2000
  • We have previously screened 150 medicinal plants on the inhibition of elastase and found a significant inhibitory effects of the extracts of Areca catechu L. on the aging and inflammation against the skin tissues. To isolate and identify the compounds having biological activity, we was further purified by each of the solvent fractions, silica gel column chromatography, preparative TLC and reversed-Phase HPLC. Peak in HPLC, which coincided with the inhibitory activity against elastase, was identified as Phenolic substance using various colorimetric methods, UV, and IR. $IC_{50}$/ values of phenolic substance purified from Areca catechu were 26.9 $\mu\textrm{g}$/$m\ell$ for porcine pancreatic elastase (PPE) and 60.8 $\mu\textrm{g}$/$m\ell$ for human neutrophil elastase (HNE). This Phenolic substance showed more potent activity than those of reference compounds, oleanolic acid (76.5 $\mu\textrm{g}$/$m\ell$ for PPE, 219.2 $\mu\textrm{g}$/$m\ell$ for HNE) and ursolic acid (31.0 $\mu\textrm{g}$/$m\ell$ for PPE, 118.6 $\mu\textrm{g}$/$m\ell$ for HNE). According to the Lineweaver-Burk Plots, the inhibition against both PPE and HNE by this phenolic substance was competitive with substrate. Phenolic substance from Areca catechu exhibited high free radical scavenging effect ($SC_{50}$/ : 6 $\mu\textrm{g}$/$m\ell$) and inhibited effectively hyaluronidase activity ($IC_{50}$/: 210 $\mu\textrm{g}$/$m\ell$). These results suggest that the Phenolic substance Purified from Areca catechu showed anti-aging effect by protecting connective tissue proteins.

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Physicochemical Characteristics of Fermented Phragmites communis Extract and Its Biological Activity (갈대 발효추출물의 이화학적 특성 및 생리활성 연구)

  • Kang, Chang-Hee;Kim, Sang-Cheol;Jeong, Sang-Chul;Han, Woong;Lee, Seung-Young;Yu, Sang-Mi;Jin, Hyun-Mi;Kim, Yeong-Su
    • Korean Journal of Pharmacognosy
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    • v.47 no.3
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    • pp.273-279
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    • 2016
  • This study evaluates the tyrosinase, elastase inhibitory and antioxidant activities of isolated Lactobacillus rhamnosus fermented extracts of Phragmites communis Trinius. After culture for 4 days at $30^{\circ}C$ using 1% P. communis extract, the cell mass of L. rhamnosus reached $1.4{\times}10^{10}CFU/mL$. The number of cells on P. communis extract and MRS medium was similar. This results indicated that P. communis extract can be used as an economical medium for industrial lactic acid bacteria production. The fermented P. communis extract exhibited 4 fold higher tyrosinase inhibitory effect than non fermented P. communis extract. The non fermented P. communis extract has no inhibitory effect on elastase. However the fermented P. communis extract show high inhibitory effect on elastase ($IC_{50}$; $249{\mu}g/mL$). These results indicated that the fermented P. communis extract can potentially be used for developing new cosmetic or health food ingredients.

Study on Anti-Skin Aging Effect of Sanguisorba officinalis L. (지유(地楡)의 피부 노화(老化)에 대한 연구(硏究))

  • Kim, Kyoung-Shin;Tak, Dong-Yul;Kim, Byoung-Soo;Kang, Jung Soo
    • Journal of Haehwa Medicine
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    • v.21 no.2
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    • pp.63-72
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    • 2013
  • To develop a new anti-skin aging cosmetics or functional foods by using antioxidative activity and collagenase inhibitor, a potent collagenase or elastase inhibitor was screened from various extracts of medicinal plants and its optimal extraction condition was investigated. And antioxidative activity, antimicrobial activity and inhibitory of effect against collagenase activity were investigated. In the these results, we selected the Sanguisorba (Sanguisorba officinalis L.) that presents a potential biological activities. Sanguisorba which is very rich in triterpenoid saponin and tannins was recently reported its anti-oxidant activities and phytoestogenic activities in vivo test and many clinical studies. The experiments were carried out in vitro to determine anti-oxidant activities of Sanguisorba extracts on DPPH radical scavenging activity assay, Superoxidase scavenging activity assay, Elastase and collagenase activity assay. It show that the Sanguisorba extracts have the most significant anti-oxidant on free radical scavenging activity assay, and also inhibited significantly activities of elastase, collagenase. Further, Sanguisorba extracts are activated Type I collagen protein expression in CCD-986sk cells. These result suggest that the Sanguisorba extracts on DPPH radical scavenging activity assay, Superoxidase scavenging activity assay, elastase and collagenase activity assay, Type I collagen protein expression in CCD-986sk cells effected could be developed cosmetic ingredients for anti-aging.

Inhibitory activities of phenolic compounds isolated from Chionanthus retusa flower on biological enzymes (이팝나무 꽃에서 분리한 페놀 화합물의 생리활성 효소 억제효과)

  • Lee, Eun-Ho;Cho, Young-Je
    • Food Science and Preservation
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    • v.25 no.1
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    • pp.117-123
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    • 2018
  • This study was designed to determine the biological activities of Chionanthus retusus flower extracts. Water and 90% ethanol extracts of C. retusus flower were prepared. The inhibitory activities of water and ethanol extracts with a phenolic content of $200{\mu}g/mL$ against xanthine oxidase were 25.60% and 15.92%, respectively. Further, the water extract did not show any inhibitory activity against ${\alpha}$-glucosidase whereas the ethanol extract showed 100.00% inhibition of ${\alpha}$-glucosidase. The inhibitory activities of the extracts against tyrosinase were 17.27% (water extract) and 36.13% (ethanol extract), which suggest that the extracts may have a whitening effect. The water extract did not inhibit elastase activity but showed a collagenase-inhibitory activity of 20.21%. On the contrary, the ethanol extract showed 96.26% and 35.93% inhibition of collagenase and elastase, respectively. These findings suggest that the extracts may have an anti-wrinkle effect. Lastly, the extracts showed a hyaluronidase inhibitory activity of 36.96% (water extract) and 88.70% (ethanol extract), suggesting that they may have an anti-inflammatory effect. The results indicate that C. retusus flower extracts containing phenolic compounds can be used as functional resources because they have anti-gout, carbohydrate degradation-inhibitory, whitening, anti-wrinkle, and anti-inflammatory effects.

α-Glucosidase Inhibitory Effects for Solvent Fractions from Methanol Extracts of Sargassum fulvellum and Its Antioxidant and Alcohol-Metabolizing Activities (참모자반 메탄올 추출 분획물의 항산화 및 숙취해소능과 α-glucosidase 활성저해효과)

  • Kang, Su Hee;Cho, Eun Kyung;Choi, Young Ju
    • Journal of Life Science
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    • v.22 no.10
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    • pp.1420-1427
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    • 2012
  • We investigated the physiological activity and solvent-partitioned fractions of methanol extracts from the green seaweed Sargassum fulvellum. The methanol extract from S. fulvellum was sequentially fractionated with n-hexane (SFMH), methanol (SFMM), buthanol (SFMB), and water (SFMA). We investigated the antioxidant activities of solvent fractions from S. fulvellum by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging capacity and an SOD activity assay. DPPH radical scavenging capacity of SFMM was 79.5% at 10 mg/ml. SOD activity of SFMM was 79.9% at 10 mg/ml. Nitrite scavenging activities of solvent fractions from S. fulvellum were investigated under different pH conditions and showed the most remarkable effect at pH 1.2. In particular, the activity of SFMB was higher than the other fractions. ADH activity and ALDH activity of SFMM were 177.0% and 167.4% at 10 mg/ml, respectively. ${\alpha}$-Glucosidase inhibitory activity of SFMH increased in a dose-dependent manner and was about 94.1% at 2 mg/ml. Elastase inhibitory activity was 93.2% at 2 mg/ml. These results revealed that S. fulvellum extracts have strong antioxidant and alcohol dehydrogenase activities and ${\alpha}$-glucosidase inhibitory activity, suggesting that S. fulvellum extracts have potential as a source of natural products for health and beauty.

Verification of the Physiological Activity of Geranium thunbergii Extract and Anti-inflammatory Activity in Raw 264.7 Cells (현지초(Geranium thunbergii) 추출물의 생리활성 및 Raw 264.7 cells에서의 항염활성 검증)

  • Seung-Mi Park;Min-Jeong Oh;Jin-Young Lee
    • Journal of Life Science
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    • v.34 no.1
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    • pp.28-36
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    • 2024
  • We evaluated the efficacy of Geranium thunbergii (GT), which has so far been understudied as a cosmetic material, and conducted anti-inflammatory-related activity studies. We measured the electron donation ability and ABTS+ radical scavenging ability to confirm the antioxidant ability of GT and found values of 91% and 94% at a concentration of 50 ㎍/ml, respectively, confirming that GT had excellent antioxidant ability. Tyrosinase inhibitory activity was measured to evaluate whitening activity, and it was found that inhibitory activity was 24.8% at the highest concentration of 1,000 ㎍/ml. Elastase and collagenase inhibitory activity were measured to determine the wrinkle improvement activity of the GT; 30.6% and 90% inhibitory activity were shown at the highest concentration of 1,000 ㎍/ml, respectively. Excellent inhibitory activity was confirmed through the measurement of collagenase inhibitory activity. Before the cell experiments were conducted, the survival rate of the macrophages Raw 264.7 according to GT treatment was determined based on the MTT assay, and the cell survival rate was greater than 83.6% at a concentration of 100 ㎍/ml. Subsequent cell-related experiments were conducted at concentrations of 100 ㎍/ml or less. The NO production inhibitory activity according to the GT treatment by NO assay was measured, and a 74.9% inhibitory rate was confirmed at a concentration of 100 ㎍/ml. Western blotting was performed to determine protein expression inhibition, and both COX-2 and iNOS factors were concentration-dependently inhibited in GT. Based on these results, GT is considered to have potential as an anti-inflammatory functional cosmetic material.

Screening of Biological Activity of Caragana sinica Extracts (골담초(Caragana sinica) 추출물의 생리활성 탐색)

  • Jeon, Young-Suk;Jo, Bun-Sung;Park, Hye-Jin;Kang, Sun-Ae;Cho, Young-Je
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.9
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    • pp.1211-1219
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    • 2012
  • In this study, extracts from Caragana sinica flowers and leaves were tested for antioxidant and angiotensin converting enzyme inhibitory activities, along with xanthine oxidase, tyrosinase, elastase, and astringent effects. Total phenolic compounds of acetone extracts from Caragana sinica flowers and leaves were the highest at 3.42 and 2.98 mg/g, respectively, when various extraction solvents were used. Optimal conditions for extraction of phenolic compounds from Caragana sinica leaves and flowers were 70% ethanol for 18 hr. DPPH scavenging activities were the highest in 70% ethanol extracts of Caragana sinica. ABTS radical cation decolorization values of 70% ethanol extracts were higher than those 60% ethanol extracts at 74%. Antioxidant protection factor was 1.2 PF in 70% ethanol extracts from Caragana sinica flowers and leaves. TBARS was lower than that of control (0.54 ${\mu}M$) in all sections. Angiotensin converting enzyme inhibitory activity of Caragana sinica flower extract was 80~90% at a phenolic concentration of 0.2~1.0 mg/mL, whereas xanthin oxidase inhibitory activity of Caragana sinica leaf extract was higher than that of flower extract. Tyrosinase inhibitory activity, which is related to skin-whitening, was above 20%, whereas elastase inhibitory activity related to anti-wrinkle effect was above 50% at a phenolic concentration of 0.8 mg/mL. Astringent effects of Caragana sinica flower and leaf extracts were higher than tannic acid as a control at an equivalent concentration. This result suggests that extracts from Caragana sinica flowers and leaves are suitable as functional foods having anti-hypertension, anti-gout, and medicinal cosmetic activities, including whitening and anti-wrinkle effects.

Inhibitory Effects of Maesaengi (Capsosiphon fulvescens) Extracts on Angiotensin Converting Enzyme and α-Glucosidase (매생이 추출물의 angiotensin converting enzyme 및 α-glucosidase 활성 저해 효과)

  • Cho, Eun-Kyung;Yoo, Seul-Ki;Choi, Young-Ju
    • Journal of Life Science
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    • v.21 no.6
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    • pp.811-818
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    • 2011
  • Physiological activities of hot water (MHW) and 80% ethanol (MEH) extracts from Maesaengi (Capsosiphon fulvescens) were investigated in this study. For the evaluation of antioxidant activities for MHW and MEH, 2,2-diphenyl-1-pic-rylhydrazyl (DPPH) radical scavenging activity and superoxide dismutase (SOD)-like activity were measured. DPPH radical scavenging activity and SOD-like activity of MHW, and MEH were increased weekly in a dose-dependent manner, and were about 10.8, 13.8, 62.4, and 27.1% at 10 mg/ml, respectively. The angiotensin converting enzyme (ACE) inhibitory activities of MHW and MEH were about 5.9% and 49.7% at 1 mg/ml, respectively. The ${\alpha}$-glucosidase inhibitory effect of MHW and MEH were about 1.4% and 67.3% at 1 mg/ml, respectively. To determine the influence of MHW and MEH on alcohol metabolizing activity, the generating activities of reduced-nicotinamide adenine dinucleotide (NADH) by alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH) were measured. Facilitating rates of ADH activity by MHW and MEH were increased weekly in a dose-dependent manner and ALDH activities were not detected. Elastase inhibitory activities of MHW and MEH were 75.9% and 51.2% at 10 mg/ml, respectively.