• 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.

• Korean Chemical Engineering Research
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• v.50 no.4
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• pp.604-609
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• 2012

Properties of fucoidan used for functional cosmetic ingredients and the effect of fucoidan molecular weight on the cosmetic functions were studied. Fucoidan was extracted from Undaria pinnatifida sporophylls and molecular weight (35~160 kDa) of fucoidan was controlled by contact glow discharge electrolysis (CGDE). To test possibility of fucoidan as a cosmetics material, tyrosinase inhibition property, water-holding property, elastase activity inhibition property and DPPH free radical scavenging property were measured. Water-holding property of fucoidan was higher than that of hyaruronic acid, which is known as the one of the best water-holding material. The water-holding strength of fucoidan slightly increase as molecular weight of fucoidan decrease. Elastase activity inhibition (anti wrinkle effect) of fucoidan was higher than that of adenosine using standard material for anti wrinkle test. Optimum molecular weight of fucoidan to obtain highest tyrosin inhibition effect, elastase inhibition effect and radical scavenger effect is 100 kDa.

• Journal of Microbiology and Biotechnology
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• v.16 no.8
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• pp.1320-1324
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• 2006

The pancreatic and neutrophil elastases are associated with several illnesses including lung and vascular diseases, various cancers, and pancreatitis. The development of a potent and specific inhibitor to the elastases could lead to new therapies. In this study, an agar diffusion method was modified to include a substrate-dye conjugate (Elastin-Congo red) as a substrate of elastase and an indicator of elastase inhibitory activity. The Elastin-Congo red agar plates consisted of 0.1 % Elastin-Congo red and 2.5% agar. The elastase and elastase inhibitors were simultaneously loaded into wells, ultimately resulting in halo formations in which the halo diameter decreased as the concentration of elastase inhibitor increased. The concentration of elastase inhibitor in the samples, therefore, was inversely proportional to the halo diameters. This simplified method provided an excellent correlation with the standard microplate technique, which uses a chromogenic substrate. The concentration of elastase inhibitor obtained from the culture supernatant of a recombinant elastase inhibitor produced by the yeast Pichia pastoris was easily determined. This study has established a simple modified and inexpensive agar diffusion method that is potentially useful for the identification, quantification, and screening of new elastase inhibitors.

• Korean Journal of Pharmacognosy
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• v.37 no.2 s.145
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• pp.92-96
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• 2006

Six phlorotannins were isolated from Ecklonia cava, a brown alga belonging to Alariaceae, collected offshore Jeju Island. Among the phlorotannins, dieckol showed strong elastase inhibition and hyaluronidase ingibition.

• The Korean Journal of Pharmacology
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• v.32 no.3
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• pp.425-431
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• 1996

Human neutrophil elastases (HNElastase, EC 3.4.21.37), a causative factor of inflammatory diseases, are regulated by plasma proteinase inhibitors, alpha-proteinase inhibitor and ${\alpha}_2-macroglobulin$. Under certain pathological conditions, however, released enzymes or abnormal function of inhibitors may cause various inflammatory disease. NSAIDs have been clinically applied for treatment of inflammatory diseases. Inhibition of cyclooxygenase is a known mechanism of action of NSAIDs in the treatment of inflammatory disease. In in vitro experiments, HNElastase was inhibited by naproxen, phenylbutazone, and oxyphenbutazone, but ibuprofen, ketoprofen, aspirin, salicylic acid, and tolmetin did not inhibit elastase. HNElastase was also inhibited by chelating agents, EDTA & EGTA, and tetracyclines. Removal of divalent metal ions by EDTA caused inhibition of elastase, and reconstitution of the metal ions recovered the enzyme activity to a certain level. Frequencies and contours in the Raman spectra of various conditions of human neutrophil elastase undergo drastic changes upon partial removal and/or reconstitution of calcium and zinc ions. The metal ion content dependent activities and change of the contour of the Raman spectrogram suggest us that the mechanism of action of a chelator or chelator-like agents on neutrophil elastase may be related to the conformational change at/or near the active site, especially -C=O radical or -COOH radical.

• The Korean Journal of Food And Nutrition
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• v.36 no.2
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• pp.114-121
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• 2023

The objective of this study is to evaluate the antioxidant components, elastase inhibition activities, and melanin synthesis rates of Korean traditional Actinidia (Actinidia arguta) fruits and leaves depending on the ethanol extraction concentrations. The total polyphenol content was the highest in the 50% ethanol extract of both fruits and leaves, with values of 634.1 mg GAE/100 g and 3,985.2 mg GAE/100 g, respectively. The total flavonoid content was the highest in the fruit 90% extract and leaf 50% extract at 191.9 mg/100 g and 2655.6 mg/100 g, respectively. The vitamin C content was the highest in the 50% extract of leaves at 2990.3 mg/100 g. Elastase inhibition was the highest at 56.9% in the leaf 50% extract at a concentration of 1,000 ㎍/mL. Melanin synthesis inhibition showed the highest melanin synthesis inhibitory effect among the extracts, as the leaf 50% extract showed an inhibitory rate of 65% or more. Therefore, the antioxidant components, elastase inhibition activities, and melanin synthesis inhibitory rate were better in leaves than in fruits. The leaf 50% extract was particularly the best among the extracts. Korean traditional Actinidia leaves can be considered as potential sources for new functional materials.

• The Korean Journal of Pharmacology
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• v.29 no.1
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• pp.131-137
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• 1993

Human neutrophil elastase (HNE, EC 3,4,21, 11), a mediator of tissue breakdown, was inhibited by tetracycline, oxytetracycline and demeclocycline. Among them, oxytetracycline showed the most potent inhibitory effect on the activity of HNE. IC50 of this drug at our specific condition was less than 1 mM. Tetracycline inhibited human neutrophil elastase non-competitively, and oxytetracycline inhibited competitively. Ki values of tetracycline and oxytetracycline were 4.9 mM and 0.39 mM, respectively. Structural modified tetracycline, de-dimethylaminotetracycline, which showed no antibiotic activity since the active dimethylamino radical was removed from the position #4 of the tetracycline, showed similar inhibition effect on the activity of human neutrophil elastase to that of tetracycline. Thus, we speculated that inhibition of human neutrophil elastase by tetracyclines was not depended on the dimethylamino radical which is a critical active site for antibiotic effect, rather it was depended on the hydoxyl radical of tetracyclines. Therefore, the property of inhibiting elastase may be an additional molecular biochemical mechanism of action of these drugs at the inflammatory sites.

• Journal of the Korean Society of Food Science and Nutrition
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• v.41 no.1
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• pp.110-115
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• 2012

Various unripe peach (Prunus persica L. Batsch) seeds, which were picked on late May, were subjected to 80% methanol extracts to investigate the antioxidant activities, whitening effects, and anti-wrinkle activities. The yield of 6 cultivars (Takinosawa Gold, Kawanakawase Hakuto, Madoka, Yumefuji, Nagasawa Hakuho, and Hong Bak) from unripe peaches were the highest on Yumefuji, followed by Madoka, Kawanakawase Hakuto, Takinosawa Gold, Hong Bak, and Nagasawa Hakuho (6.16%, 6.08%, 5.65%, 5.25%, 5.23%, and 5.20%). The content of the total polyphenol of seed extracts ranged from 18.33 to 27.08 mg/g. The antioxidant in vitro assays including the DPPH and ABTS radical scavenging activities were the highest with Hong Bak and Kawanakawase Hakuto. The tyrosinase inhibition activity greatly affected the Takinosawa Gold and Kawanakawase Hakuto. Compared to the elastase inhibition activity of 6 cultivars, Madoka was higher than others, while the lowest was Hong Bak. The significant correlation coefficient values were determined (more than p=0.05) between the yield, total polyphenol content, antioxidant activities, tyrosinase inhibition, and elastase inhibition activities. The results suggested that the total polyphenol content has a high positive value on the DPPH, ABTS radical scavenging activity, and tyrosinase inhibition activity. Also, the tyrosinase inhibition activity and elastase inhibition activity showed a significant correlation (r=+0.594). The ABTS inhibition activity and tyrosinase inhibition activity that is the most suitable character represented significant positive correlation (r=+0.846). This data suggested that the methanol extracts from these unripe peaches could be potential candidates for natural cosmetics.

• Journal of Microbiology and Biotechnology
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• v.10 no.1
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• pp.81-85
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• 2000

An elastase inhibitor, SMFEI02, was isolated from culture broth of Streptomyces lavendulae SMF11. The inhibitor was purified by ultrafiltration followed by XAD-7 column and Dowex-1 anion-exchange chromatographies, and preparative HPLC. The molecular formula was determined to be $C_{14}H_{16}N_2O_2$ (MW244) by HRFAB-MS analysis. The inhibitor was identified to be a diketopiperazine cyclo(S-Phe-S-Pro) by the optical rotation value and MNR spectral data, and showed inhibitory activities for trypsin, chymotrypsin, cathepsin B, and papain as well as elastase with the Ki values ranging from 1.78mM to $2.86{\;}\mu\textrm{m}$. The inhibition showed a competitive mode for elastase, chymotrypsin, and cathepsin B, whereas it showed a noncompetitive mode for trypsin and papain.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.23 no.1
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• pp.135-148
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• 2010

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 Galla Rhois (GR) inhibitory activity against aging process of skin in vitro. GR was screened for their inhibitory activity against elastase. GR (final concentration 1 mg/ml) appeared over 40% of inhibition of elastase activity. So we investigated anti wrinkle effects of GR look through MMP-1 inhibition activity. Also Extracts of GR showed higher anti-tyrosinase activity than arbutin (final concentration 1 mg/ml). These results suggest that GR could be potential sources of anti-aging and whitening effects for the skin. Objective : Galla Rhois extracts, Elastase (pancreatic from porcine pancreas), N-Succinyl-(Ala)3-p-nitroanilide, Ursolic acid, mushroom tyrosinase, L-tyrosine, arbutin, Amicon Ultra, Hand Hold UV lamp, MMP-1 primary antibody, MMP-1 secondary antibody Result : 1. GR appeared over 40% of elastase inhibitory activity. 2. GR had MMP-1 inhibition activity. 3. GR showed higher anti-tyrosinase activity than arbutin. Conclusion : According to above results, it is supposed that Galla Rhois could be strong potential sources of anti-aging and whitening effects for the skin.