• Title/Summary/Keyword: Elastase inhibitory effect

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Inhibitory Effect on Melanin Formation, Collagenase and Elastase Activity by synthesized Coenzyme $Q_{10}$ Derivatives (세포내 멜라닌 생성 및 Collagenase와 Elastase에 대한 Coenzyme $Q_{10}$ 유도체들의 억제활성)

  • Choi, Won-Sik;Jang, Do-Yoen;Nam, Seok-Woo;Eo, Jin-Yong;Lee, Kyoung-Ju
    • Applied Biological Chemistry
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    • v.51 no.3
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    • pp.164-170
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    • 2008
  • Coenzyme $Q_{10}$ and six derivatives of coenzyme Qn were synthesized and tested for their inhibitory effects on melanogenesis occurred in murine melanoma (B16/F1) cells and on collagenase/elastase activities as well. As the result, synthetic coenzyme Qn showed a potent inhibitory effect on melanin formation, collagenase and elastase activities in all tested concentrations. Among these synthetic compounds, coenzyme $Q_1$ and coenzyme $Q_2$ potentially inhibited melanin formation and elastase activity when compared to other coenzyme Qn derivatives. For the collagenase activities, all coenzyme Qn derivatives inhibited 80-85% of controls. As compared, coenzyme Qn derivatives exhibited strong inhibitory activities with the decrease of isoprenoid unit number of coenzyme Qn derivatives except for collagenase activity. For the inhibition of collagenase activity, moiety of benzoquinone might be considered as the active functional group. Taken together, coenzyme $Q_1$ and coenzyme $Q_2$ might be used for functional cosmetics.

Effects of Paeoniae radix alba(PRA) on Skin whitening and Elasticity using Melanoma cells (백작약(白芍藥)이 피부 미백 및 주름에 미치는 영향)

  • Lee, Jong-Cheol;Park, Soo-Yeon;Choi, Jeong-Hwa;Kim, Jong-Han
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.25 no.1
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    • pp.1-11
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    • 2012
  • Objective : Paeoniae radix alba(PRA) can enrich the blood and regulate menstruation, astringe yin and arrest sweating, calm the liver and arrest pain. This study was designed to investigate effects of PRA on skin whitening and elasticity using melanoma cells. Methods : In this experiment, effect of PRA on cell viability, inhibition of melanin synthesis and inhibitory effect on tyrosinase and elastase. Results : 1. More than $1,000\;{\mu}g/ml$ of PRA treated group showed lowered proliferation rates significantly compared to non-treated control group. 2. All of treated groups were lower levels of melanin synthesis respectively. 3. PRA did not show inhibitory effect on tyrosinase activities in vitro. But, PRA suppressed tyrosinase activities in B16F10 cells significantly. 4. PRA suppressed elastse type 1 activities in dose-dependent manner in vitro. But, PRA slightly suppressed elastase type 4 activities in vitro, and PRA also slightly suppressed elastase activities in vivo. Conclusion : These results suggest that PRA can inhibit melanin synthesis through ihhibitory action on tyrosinase activity and inhibt elastase activity, and also suggest that these results can be used for the study on maintaining skin whitening or elasticity.

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.

Effects of Albizziae Cortex Extracts on the Elastase Activity and DPPH and NO Scavenging Activities

  • Leem, Kang-Hyun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.25 no.2
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    • pp.306-310
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    • 2011
  • Elastic fibers are found in the skin, lungs, arteries, veins and other structures. Elastases destroy the elastic fibers and cause the emphysema and pulmonary hypertension. Oxidative stress is needed for these pathologic changes. Accordingly, present study was designed to investigate the effect of Albizziae Cortex extracts (ACE) on elastase activity and anti-oxidative effects of ACE. The in vitro inhibitory effects on elastase and di(phenyl)-(2,4,6-trinitrophenyl)iminoazanium (DPPH) and nitric oxide (NO) free radical scavenging activities of ACE were measured. The elastase activity was significantly inhibited by ACE. DPPH and NO free radicals were significantly scavenged as well. ACE showed the elastase-inhibiting effects and anti-oxidative activities in vitro. These results suggest that ACE may have potential roles in the treatment of pulmonary emphysema and pulmonary hypertension.

Antioxidant and Antibacterial Activities, and Tyrosinase and Elastase Inhibitory Effect of Fermented Omija (Schizandra chinensis Baillon.) Beverage (오미자 발효액의 항산화 및 항균 활성과 미용효과)

  • Cho, Eun-Kyung;Cho, Hea-Eun;Choi, Young-Ju
    • Journal of Applied Biological Chemistry
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    • v.53 no.4
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    • pp.212-218
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    • 2010
  • This study was aimed to investigate the contents of chemical components and the biological activity of fermented Omija (Schizandra chinensis Baillon.) beverage (FOB), which have not been well known up to now. General compositions and the contents of mineral and vitamin of FOB were lower than Omija before fermentation (OBF). In addition, most sucrose was digested into glucose and fructose in FOB. This suggests that the beneficial contents may be made from general compositions by fermentation, though more evidences are needed. Antioxidant activity of FOB was measured by using 2,2-diphenyl-l-picryl-hydrazyl (DPPH) free radical scavenging activity and superoxide dismutase-like activity (SODA). DPPH radical scavenging activity and SODA were increased in a dose-dependent manner, and were about 79.7% and 60.8% at four times diluted FOB (25% of FOB), respectively. The FOB also showed strong antibacterial activity on Escherichia coli. Beauty effect of FOB was demonstrated by the analysis of tyrosinase and elastase inhibitory activities, and they were remarkably increased in a dose-dependent manner. Tyrosinase inhibitory activity was about 82% at two times diluted FOB (50% of FOB) and elastase inhibitory activity was 78.2% at five times diluted FOB (20% of FOB). These results suggest that FOB has a strong antioxidant activity, and tyrosinase and elastase inhibitory effects.

Inhibitory Effects of Saposhnikoviae Radix Extracts on the Melanin Production and Elastase Activity in B16F10 cells (흑색종 세포주에서 멜라닌 생성과 엘라스타제 활성 억제에 미치는 방풍의 효과)

  • Choi, Chan Hun;Wang, Kung The;Cho, Hye Rin;Jeong, Jong Gil;Jeong, Hyun Woo
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.28 no.3
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    • pp.296-302
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    • 2014
  • Saposhmikoviae Radix can treat various skin disease by anti-pruitus and anti-inflammatory effects. This study was designed to investigate effects of Saposhmikoviae Radix Extracts(SRE) on skin elasticity and whitening using B16F10 cell lines. In this experiment, We observed effect of SRE on cell viability, inhibition of melanin synthesis and inhibitory effect on tyrosinase and elastase. In results, SRE treated group showed lowered proliferation rates significantly compared to non-treated group. More than SRE $125{\mu}g/m{\ell}$ of treated groups were lower levels of melanin synthesis respectively. SRE did not show inhibitory effect on tyrosinase activities in vitro and in B16F10 cells. Finally, SRE suppressed elastse type I and IV activities in dose-dependent manner in vitro. And SRE also slightly suppressed elastase activities in B16F10 cells. In conclusion, these results suggest that SRE can inhibit melanin synthesis and inhibt elastase activity. So, We suggest that SRE can be maintained skin elasticity or whitening.

The effect of Elastase inhibition and Tyrosinase by Rheum undulatum Stokes extracts (대황(大黃)의 Elastase 활성 억제와 Tyrosinase 억제연구)

  • Lee, Jong-Chul;Kim, Kyung-Jun
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.22 no.3
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    • pp.36-46
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    • 2009
  • Objective : Recently, the demands for the effective and safe depigmentating and anti-aging agents of the skin have increased due to the medical, pharmaceutical and cosmetic reasons. The aim of this study is to search new materials from the traditional herbal medicines which inhibit the aging process of skin in vitro. Methods : herbal medicines(80% ethanol or water extracts) were screened for their inhibitory activities against elastase. Results : Rheum undulatum (final concentrstion 1 mg/ml) appeared over 30% of inhibition of elastase activity. so we are investigated anti wrinkle effects of Rheum undulatum look through MMP-1 inhibition activity. also Extracts of Rheum undulatum showed higher anti tyrosinase activity than arbutin (final concentration 1 mg/ml). Conclusion : These results suggest that herbal medicines could be strong potential sources of inhibition of anti-aging and whitening effects for the skin.

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Effects of Astragali Radix Extracts on the Elastase Activity and DPPH and NO Scavenging Activities (황기(黃芪)의 elastase 활성과 DPPH, NO 소거능에 미치는 영향)

  • Mou, Jong-Cheng;Lee, Se-Na;Kim, Myung-Gyou;Kim, Myoung-Hee;Kim, Hyung-Jun;Jo, Hak-Jun;Leem, Kang-Hyun
    • The Korea Journal of Herbology
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    • v.26 no.1
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    • pp.59-63
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    • 2011
  • Objectives : Elastic fibers are found in the skin, lungs, arteries, veins and other structures. The defects of elastic matrix aggravate hypertension which is associated with alteration in the great arteries, arteries, and arterioles. The elastase inhibitors were undergoing in clinical studies about emphysema and pulmonary hypertension. This study was designed to investigate the effect of Astragali Radix extracts (AR) on elastase activity and anti-oxidative effects. Methods : The elastase inhibitory activity and DPPH (1,1-diphenyl-2-picrylhydrazyl) and NO free radical scavenging activities of AR were measured. Results : The elastase activity was significantly inhibited by AR. The significant DPPH and NO free radical scavenging activities were observed in AR as well. Conclusion : AR showed the anti-elastase effects and anti-oxidative activities in vitro. These results suggest that AR may be a possible drug for the treatment of pulmonary emphysema and pulmonary hypertension.

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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The effects of Ohbaesangami (OBSGM) on the mucosa and skin diseases (오배산가미(五倍散加味)가 점막(粘膜) 및 피부질환(皮膚疾患)에 미치는 영향)

  • Roh, Seok-Sun;Hong, Seok-Hoon
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.20 no.2 s.33
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    • pp.10-35
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    • 2007
  • Objectives : To investigate the effects of Ohbaesangami (OBSGM) on mucosa and skin diseases, anti-microbial and anti-inflammatory tests were performed using several in vitro test models. Results : In anti-microbial test, OBSGM showed the slight inhibitory effect against Propionibacterium acnes (P. acnes) and Staphylococcus aureus (S. aureus). In anti-oxidant test, OBSGM showed the potent radical scavenging activity. In anti-inflammatory test, OBSGM weakly inhibited the lipopolysaccharide (LPS)-induced nitric oxide(NO) release from the RAW 264.7 macrophage cells. OBSGM also inhibited the LPS-induced $interleukin-1{\beta}(IL-1{\beta})$ and cyclooxygenase-2 (COX-2) expressions. The inhibitory effects of OBSGM on macrophage activation was via the inhibition of $NF-{\kappa}B$, evidenced by transient transfection assay. Furthermore, OBSGM markedly inhibited the activation of Jun-N-terminal kinase (JNK) and p38 MAP kinase in RAW 264.7 cells. In skin wrinkle formation assay, OBSGM strongly inhibited collagnease and elastase, whose activities are tightly related with the wrinkle formation. In addition, OBSGM inhibited the activities of MMP-1, MMP-2 on the mRNA levels in RAW 264.7 cells. However, OBSGM did not show an inhibitory potential on tyrosinase activity and melanin synthesis, indicating that it could not be applicable for skin whitening. Conclusion : These results suggest that the anti-inflammatory effect of OBSGM may be due to its inhibitory potentials on the macrophage activation. And, the anti-wrinkle effects of OBSGM may be due to its inhibitory potential on the collagnease and elastase activities. Therefore, OBSGM could be applicable for the treatment of mucosa and skin diseases.

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