• Title/Summary/Keyword: Elastase inhibition

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Experimental studies about the inhibitory effect on tyrosinase and elastase activities by various herb medicines (수종(數種)의 한약재의 Tyrosinase와 Elastase 활성 억제 효과에 대한 실험적 연구)

  • Jung, Jae-Hoon;Kim, Kyung-Jun
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.22 no.2
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    • pp.82-91
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    • 2009
  • Objectives : The purpose of this study is to investigate whitening effects and anti-wrinkle effects of a few 80% ethanol extracted herbal medicines. Methods : In the first study, a few 80% ethanol extracted herbal medicines were screened for their inhibitory activities against the tyrosinase. In the second study, a few 80% ethanol extracted herbal medicines were screened for their inhibitory activities against elastase. Results : 1. We showed 28%, 27% and 19% inhibitions of mushroom tyrosinase at 500 $\mu$g/ml concentration of ASR, AIF and ABR extracts and they were showed higher anti-tyrosinase activity than arbutin's. We also could observe that the decreased mushroom tyrosinase activities in RR, CML, LR, AGR and TH extracts. 2. RR, AF and ABR (final concentrstion 1 mg/ml) were appeared 60%, 98%, 83% of inhibitions of elastase activity, and they were showed higher anti-elastase activity than that of ursolic acid. We also could observe that the decreased elastase activities in AIF, AR, LR and CML extracts. Conclusions : These results suggest that ASR, AIF and ABR extracts contribute to the anti-melanin activities and represent potential sources of whitening agent, and RR, AF and ABR extracts contribute to the anti-elastase activities and represent potential sources of anti-wrinkle agent. These results suggest that some herbal medicines could be strong potential sources of inhibition about anti-aging and whitening effects for the skin.

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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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Inhibition of Porcine Pancreatic Elastase (PPE) by Korean Mistletoe (Viscum album var.coloratum) Fractions

  • Lyu, Su-Yun;Moon, You-Sun;Kwon, Young-Ju;Joo, Hye-Jin;Park, Won-Bong
    • Natural Product Sciences
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    • v.9 no.4
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    • pp.278-285
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    • 2003
  • The serine proteases such as human leukocyte elastase (HLE) and porcine pancreatic elastase (PPE) are classified in the chymotrypsin family, and possibly the most destructive enzymes having the ability to degrade virtually all of the connective components in the body. In the present study, the extracts of water and methanol of Korean mistletoe (Viscum album var. coloratum) inhibited significantly the PPE activity. The fractions eluated on Amberlite XAD-2 from methanol extract were further purified on the repeated $SiO_2$ column chromatography and the fractions A, B and C were eluated. The fractions A, B and C at 3 mg/ml inhibited significantly the PPE activity up to 66%, 95% and 85%, respectively. In conclusion, the fraction A assumed as lignans or phenylpropanes, and fraction B and C assumed as triterpenoids showed the PPE inhibitory effects on the PPE and that these compounds in mistletoe may be used for treatment of pathological processes such as age-dependent tissue loss or inflammation.

Inhibition of Human Neutrophil Elastase by Sesquiterpene Lactone Dimers from the Flowers of Inula britannica

  • Kim, Kwan-Chul;Kim, Dae-Jung;Lee, Myung Sun;Seo, Ji Yun;Yoo, Ick-Dong;Lee, Ik-Soo
    • Journal of Microbiology and Biotechnology
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    • v.28 no.11
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    • pp.1806-1813
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    • 2018
  • A new sesquiterpene lactone dimer [1], together with five known compounds (2-6), was isolated from the flowers of Inula britannica. The structures of these compounds were established by extensive spectroscopic studies and chemical evidence. The inhibitory activities of these isolated compounds (1-6) against human neutrophil elastase (HNE) were also evaluated in vitro; compounds 1 and 6 exhibited significant inhibitory effects against HNE activity, with $IC_{50}$ values of 8.2 and $10.4{\mu}m$, respectively, comparable to that of epigallocatechin gallate (EGCG; $IC_{50}=10.9{\mu}M$). In addition, compounds 3 and 5 exhibited moderate HNE inhibitory effects, with $IC_{50}$ values of 21.9 and $42.5{\mu}M$, respectively. In contrast, compounds 2 and 4 exhibited no such activity ($IC_{50}$ > $100{\mu}M$). The mechanism by which 1 and 3 inhibited HNE was noncompetitive inhibition, with inhibition constant ($K_i$) values of 8.0 and $22.8{\mu}M$, respectively.

The Effect of Cosmetic on Anti-Wrinkle of Acer mono Sap (우산고로쇠의 향장효과)

  • Sohn, Sang Hyun;Lee, Sang Won;Shin, Yu Su;Kim, Hyung Don;Yang, Seung Ok;Kim, Seung Yu;Kim, Young Ock
    • Korean Journal of Medicinal Crop Science
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    • v.21 no.4
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    • pp.262-267
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    • 2013
  • The purpose of this study was to research for anti-oxidation and anti-wrinkle effects of Acar mono Sap (AM). To cosmetic effect of AM, safety effect (MTT assay), anti-wrinkle effect (elastase, MMP-1 inhibition assay) and anti-oxidant effect (DPPH assay) were measured. When water extract of AM was used for cell viability, it was over 100% at 6% (6 ml/100 ml in phosphate buffer) concentration. AM showed 45.7% elastase inhibition and 23.7% MMP-1 inhibition at 50% (50 ml/100 ml in phosphate buffer) concentration so that it had good anti-wrinkle characteristic. And AM showed 68.9% antioxidation capacity at 50% concentration by using a DPPH assay. Consequently, AM can be used as natural materials or additives for human skin owing to their beneficial biologic functions, including the anti-wrinkle effect, for cosmetic compositions.

Antibiotics; Methicillin, Cefamandole and Oxytetracycline, Can Modulate the Activity of Human Neutrophil Elastases (Methicillin, Cefamandole, Oxytetracycline에 의한 사람 호중구 Elastase의 변화)

  • Ghim, Sa-Youl;Jeong, Hye-Young;Bae, Sung-Jun;Kang, Koo-Il
    • The Korean Journal of Pharmacology
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    • v.25 no.1
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    • pp.109-113
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    • 1989
  • Human neutrophil elastase (HNE, EC 3, 4 21, 11), a major causative factor in the induction of pulmonary emphysema, were purified by two steps of liquid chromatography. Purified elastases were cross-reacted with antibody to human neutrophil elastases. Methicillin and cefamandole, which are known as inhibitors of cell wall synthesis of microorganisms, could inhibit the activity of human neutrophil elastase up to 50% with 10mM of both agents and $IC_{50}$ of methicillin was 9.8 mM. Gentamicin, one of the aminoglycosides, also inhibits human neutrophil elastases up to 60% of original activity with 10 mM of this agent and $IC_{50}$ was 9.0 mM. We could demonstrate similar effects in oxytetracycline. 10 mM of oxytetracycline inhibited 95% of human neutrophil elastase and $IC_{50}$ was 0.3 mM. Overall, oxytetracycline, cefamandole and methicillin are strong inhibitors of human neutrophil elastase, and they could be a drug of cholice for the diseases which were known as pathogenesis related to elastase. We also suggest that the mechanism of action of these antibitics are different from the mechanism of antimicrobial effects like inhibition of both cell wall synthesis and protein synthesis.

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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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Melanin synthesis and skin wrinkle inhibitory effects of the medicinal mushroom Ganoderma applanatum

  • Yoon, Ki Nam;Lee, Tae Soo
    • Journal of Mushroom
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    • v.19 no.3
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    • pp.150-159
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    • 2021
  • Anti-melanogenesis and skin anti-wrinkle effects of methanol (ME) and hot water (HE) extracts from the fruiting bodies of Ganoderma applanatum were investigated in this study. The total phenolic contents of the ME and HE of the mushroom were 11.68 and 3.15 ㎍ GAEs/mg, respectively, whereas the total flavonoid contents of the ME and HE were 21.82 and 2.69 ㎍ QEs/mg, respectively. The survival rate of B16-F10 murine melanoma cells treated with 750 ㎍ ME and HE were 83.46% and 85.54%, respectively, thereby suggesting that mushroom extracts were slightly cytotoxic at the tested concentration. The in vitro tyrosinase inhibition by ME (83.15%) and HE (83.44%) was significantly lower than that of kojic acid (99.61%), the positive control, at 2.0 mg/mL. Although the inhibition of cellular melanin synthesis in B16-F10 melanoma cells by 2.0 mg/mL of ME (50.24%) and HE (51.24%) was lower than that of arbutin (64.84%), the inhibition by both ME and HE was higher than 50%. Collagenase inhibition by HE was comparable to 2.0 mg/mL epigallocatechin (EGCG), the positive control; however, elastase inhibition by ME and HE was lower than that of EGCG at the concentration tested. The results showed that the fruiting bodies of G. applanatum had good anti-tyrosinase, good anti-collagenase, and moderate anti-elastase activities, which might be useful for developing novel skin-whitening and anti-wrinkle agents.

Antioxidant and Elastase Inhibitory Effects of Equisetum hyemale Extract (속새(Equisetum hyemale) 추출물의 항산화 및 Elastase 저해 효과)

  • Song, Jin Hwa;Song, Hyun Sook;Lee, Geo Lyong
    • Journal of Naturopathy
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    • v.10 no.2
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    • pp.86-92
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    • 2021
  • Background: The presence of antioxidants was not confirmed in the medicinal plant Equisetum hyamale grass. Purposes: This study was to determine the antioxidant and elastase inhibition effects of extracts of E. hyemale. Methods: Antioxidant functions of E. hyemale stems and roots were measured and extracted with hot water (HW) and ethyl alcohol (70EOH, 100EOH). Results: The extraction yield of stems was higher in HW extraction than in ethyl alcohol extraction. The polyphenol content was significantly higher in the root extract than in the stem. Total flavonoid content of 70EOH extract was significantly higher in root extract than in stem. The elastase inhibitory function of the extract was 46% in the root and 49% in the stem at 100 ppm of the extract. The ABTS free radical scavenging function was in the order of HW<70EOH<100EOH

A Study on Skin Care Effects of Rapeseed Meal Extract (유채박 추출물의 피부미용 효과에 관한 연구)

  • Kim, Sun Mi;Na, Myung Soon
    • KSBB Journal
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    • v.28 no.3
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    • pp.177-184
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    • 2013
  • This research was to investigate the inhibitory effects of tyrosinase, elastase and collagenase using rapeseed meal extract for the functional cosmetics. Gamma-tocopherol and alpha-tocopherol contents were 304.9 and 212.2 mg/kg, respectively. In the case of delta-tocopherol and plastochromanol-8, they were 12.1 and 35.7 mg/kg, respectively. The total phenol content of methanol extract was the highest (49.6 mg/g) which was about 4.96 fold higher than that of water extract. The maximum nitrite scavenging activities of methanol and acetone extract at pH 1.2 were 85.2 and 80.1%, respectively, at 8.0 mg/mL. When the extract concentration of rapeseed meal increased upto 2.0 mg/mL, cell viabilities did not appear to have any significant cytotoxic effect, irrespective of extracts. Tyrosinase and elastase inhibition activities increased from 25.2 to 42.5% and 25.3 to 48.0%, respectively, as methanol extract concentration increased from 0.5 to 1.0 mg/mL. The collagenase inhibition activities of methanol and acetone extracts at 1.0 mg/mL were 67.2 and 68.0%, respectively. These results showed that the methanol and acetone extract of rapeseed meal can be used as a new source of functional cosmetic agent.