• 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.

• Natural Product Sciences
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• v.23 no.3
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• pp.192-200
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• 2017

Skin aging is a complex biological process due to intrinsic and extrinsic factors. Free radical oxidative is one of extrinsic factors that induce activation of collagenase, elastase and hyaluronidase. Natural product from plants has been used as antioxidant and antiaging. This study aimed to evaluate antioxidant and antiaging properties of Hibiscus sabdariffa extract (HSE) and its compounds including myricetin, ascorbic acid, and ${\beta}$ carotene. The phytochemical of H. sabdariffa was determined using modified Farnsworth method and presence of phenols, flavonoids and tannins were in moderate content, whereas triterpenoids and alkaloids were in low content. Total phenolic content performed using Folin-Ciocalteu method, was $23.85{\mu}gGAE/mg$. Quantitative analysis of myricetin, ${\beta}-carotene$, and ascorbic acid of HSE was performed with Ultra-High Performance Liquid Chromatography (UHPLC) that shows $78.23{\mu}g/mg$ myricetin, $0.034{\mu}g/mg$ ${\beta}-carotene$, whilst ascorbic acid was not detected. HSE has lower activity on DPPH ($IC_{50}=195.73{\mu}g/mL$) compared to ${\beta}-carotene$, the lowest in ABTS assay ($IC_{50}=74.58{\mu}g/mL$) and low activity in FRAP assay ($46.24{\mu}MFe(II)/{\mu}g\;$) compared to myricetin, ${\beta}-carotene$. Antiaging was measured through inhibitory activity of collagenase, elastase, and hyaluronidase. HSE had weakest collagenase inhibitory activity ($IC_{50}=750.33{\mu}g/mL$), elastase inhibitory activity ($103.83{\mu}g/mL$), hyaluronidase inhibitory activity ($IC_{50}=619.43{\mu}g/mL$) compared to myricetin, ${\beta}-carotene$, and ascorbic acid. HSE contain higher myricetin compared to ${\beta}-carotene$. HSE has moderate antioxidants and lowest antiaging activities. Myricetin is the most active both antioxidant and antiaging activities.

• Applied Chemistry for Engineering
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• v.33 no.2
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• pp.195-201
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• 2022

The main objective of this work is to prepare Rehmannia glutinosa extract (RE) incorporated functional chitosan (CH) based biomaterials and evaluate their physical properties, RE release properties, inhibitory effect of melanogenesis, and antioxidant and elastase inhibitory activities. RE incorporated CH based biomaterials were synthesized by a casting method and UV curing process. The surface and cross sections of prepared biomaterials were characterized by a field emission scanning electron microscope (FE-SEM). The physical properties such as tensile strength and elongation at break were also investigated. To apply the transdermal drug delivery system, RE release properties were examined with pH 4.5, 5.5, and 6.5 buffer solutions and artificial skin test at 36.5 ℃. Results indicated that RE release of RE incorporated biomaterials with/without the addition of plasticizers [glycerol (GL) and citric acid (CA)] at pH 6.5 was about 1.10 times higher than that of at pH 4.5. In addition, results of the artificial skin test verified that RE was released constantly for 6 h. To verify the applicability of the prepared biomaterials, tyrosinase, 2,2-diphenyl-1-picrylhydrazyl (DPPH), and elastase assays were investigated. Results indicated that RE incorporated biomaterials added CA exhibited tyrosinase activation, DPPH radical scavenging activity rate, and elastase activation of 45.12, 89.40, and 59.94%, respectively.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2019.10a
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• pp.63-63
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• 2019

The thinning Green ball apple was extracted using water and ethanol and a phenolic concentration of thinning Green ball apple was $50-200{\mu}g/mL$. The water and ethanol extracts of thinning Green ball apple showed 94.69% and 92.24% 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity and 100.30% and 99.16% 2,2'-Azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging activity at phenolic concentration of $200{\mu}g/mL$, respectively. The water and ethanol extracts of thinning Green ball apple showed antioxidant protection factor of 1.76 antioxidant protection factor and 1.76 antioxidant protection factor, respectively. The water and ethanol extracts showed 101.46% and 99.64% anti-oxidative effect on thiobarbituric acid reactive substances at phenolic concentration of $200{\mu}g/mL$. Hence, the water and ethanol extracts of thinning Green ball apple can be considered a potential anti-oxidant. The water and ethanol extracts showed 33.28% and 32.14% hyaluronidase inhibition, respectively, at phenolic concentration of $150{\mu}g/mL$. The water and ethanol extracts showed 47.33% and 40.92% elastase inhibition and 46.19% and 65.58% collagenase inhibition at phenolic concentration of $200{\mu}g/mL$, respectively. About these experiments, thinning Green ball apple was found to exhibit anti-oxidation activity as well as hyaluronidase, elastase and collagenase inhibitory activities. Therefore, thinning Green ball apple can be considered a potential source for functional food.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.34 no.4
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• pp.275-286
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• 2008

In this study, we investigated the anti-oxidative, anti-wrinkle and whitening effects of Platycarya strobilacea bark extracts. The free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activity ($FSC_{50}$) of extract / fractions of Platycarya strobilacea was in the order: 50% ethanol extract ($6.75{\mu}g/mL$) < deglycosylated aglycone fraction ($6.62{\mu}g/mL$) < ethyl acetate fraction ($4.15{\mu}g/mL$). Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of some Platycarya strobilacea extracts on ROS generated in $Fe^{3+}$-EDTA/$H_2O_2$ system were investigated using the luminol-dependent chemiluminescence assay. The order of ROS scavenging activity was ethyl acetate fraction (OSC50, $0.56{\mu}g/mL$) < 50% ethanol extract ($0.02{\mu}g/mL$) < deglycosylated aglycone fraction ($0.01{\mu}g/mL$). The deglycosylated aglycone fraction showed the most prominent scavenging activity. The protective effects of extract / fractions of Platycarya strobilacea on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The ethanol extract (50%) suppressed photohemolysis in a concentration dependent manner, particularly ethyl acetate fraction exhibited the most prominent cellular protective effect (${\tau}_{50}$, 717.27 min at $10{\mu}g/mL$). The inhibitory effect of Platycarya strobilacea extracts on tyrosinase were investigated to assess their whitening efficacy. Finally, their anti-elastase activities were measured to predict the anti-wrinkle efficacy in the human skin. The inhibitory effect ($IC_{50}$) on tyrosinase of some Platycarya strobilacea extracts was 50% ethanol extract ($243.98{\mu}g/mL$) < ethyl acetate fraction ($153.87{\mu}g/mL$) < deglycosylated aglycone fraction ($137.53{\mu}g/mL$). Also, The inhibitory effect of elastase ($IC_{50}$) of some Platycarya strobilacea extracts was 50% ethanol extract ($31.01{\mu}g/mL$) < ethyl acetate fraction ($14.42{\mu}g/mL$) < deglycosylated aglycone fraction ($1.48{\mu}g/mL$). The cream containing the ethyl acetate fraction of Platycarya strobilacea extracts was formulated. The skin hydration, transepidermal water loss, and the whitening effects were investigated after topical application of the cream. The skin hydration of cream containing extract was increased by $2{\sim}8%$ than the placebo cream, transepidermal water loss was decreased. The cream containing extract suppressed the melanogenesis of skin by 9.55% than the placebo cream. These results indicate that extract / fractions of Platycarya strobilacea can function as antioxidants in biological systems, particularly skin exposed to UV radiation by anti-oxidative activity and protect cellular membranes against ROS. The inhibitory effect on elastase and tyrosinase, and the increase of skin hydration and the whitening effect of the cream containing extract could be applicable to new functional cosmetics for antiaging.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.35 no.3
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• pp.235-241
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• 2009

In this study, the antioxidative effects, inhibitory effects on tyrosinase, elastase of Persicaria perfoliata extracts were investigated. The deglycosylated fraction of extract ($12.38{\mu}g$/mL) showed the most prominent free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activity ($FSC_{50}$). Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of P. perfoliata extracts on ROS generated in $Fe^{3+}$-EDTA/$H_2O_2$ system were investigated using the luminol-dependent chemiluminescence assay. The ethyl acetate fraction of extract ($0.35{\mu}g$/mL) showed the most prominent ROS scavenging activity. The protective effects of P. perfoliata extract/fractions on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The P. perfoliata extracts suppressed photohemolysis in a concentration dependent manner ($1{\sim}50{\mu}g$/mL) except the deglycosylated fraction of extract. The inhibitory effect of P. perfoliata extracts on tyrosinase was investigated to assess their whitening efficacy. Inhibitory effects ($IC_{50}$) on tyrosinase were determined with ethyl acetate fraction of P. perfoliata extract ($136.00{\mu}g$/mL) and deglycosylated fraction of extract ($68.10{\mu}g$/mL). Finally, their anti-elastase activities were measured to predict the anti-wrinkle efficacy in the human skin. Inhibitory effects ($IC_{50}$) on elastase were determined with ethyl acetate fraction of P. perfoliata extract ($67.20{\mu}g$/mL) and deglycosylated fraction of extract ($43.50{\mu}g$/mL). These results indicate that extract/fractions of P. perfoliata can function as antioxidants in biological systems, particularly skin exposed to UV radiation by scavenging $^1O_2$ and other ROS, and protect cellular membranes against ROS. Extract/fractions of P. perfoliata can be applicable to new functional cosmetics for antioxidant, antiaging.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.34 no.3
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• pp.233-244
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• 2008

In this study, the antioxidative effects, inhibitory effects on elastase and tyrosinase, and component analysis of Psidium guajava leaf extracts were investigated. The free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activities $(FSC_{50})$ of extract/fractions of Psidium guajava leaf were in the order: 50% ethanol extract $(7.05{\mu}g/mL)$ < ethyl acetate fraction $(3.36{\mu}g/mL)$ < deglycosylated flavonoid aglycone fraction $(3.24{\mu}g/mL)$. Reactive oxygen species (ROS) scavenging activities $(OSC_{50})$ of some Psidium guajava leaf extracts on ROS generated in $Fe^{3+}-EDTA/H_2O_2$ system were investigated using the luminol-dependent chemiluminescence assay. The order of ROS scavenging activities were 50% ethanol extract $(OSC_{50},\;2.17{\mu}g/mL)$ < ethyl acetate fraction $(0.64{\mu}g/mL)$ < deglycosylated flavonoid aglycone fraction $(3.39{\mu}g/mL)$. Aglycone fraction showed the most prominent ROS scavenging activity. The protective effects of extract/fractions of Psidium guajava leaf on the rose-bengal sensitized photohemolysis of human erythrocytes were investigated. The Psidium guajava leaf extracts suppressed photohemolysis in a concentration dependent manner $(1{\sim}10{\mu}g/mL)$, particularly deglycosylated flavonoid aglycone fraction exhibited the most prominent celluar protective effect ${\tau}_{50}\;107.5min\;at\;1{\mu}g/mL)$. Aglycone fraction obtained from the deglycosylation reaction of ethyl acetate fraction among the Psidium guajava leaf extracts, showed 1 band in TLC and 1 peak in HPLC experiments (360 nm). One component was identified as quercetin. TLC chromatogram of ethyl acetate fraction of Psidium guajava leaf extract revealed 5 bands and HPLC chromatogram showed 5 peaks, which were identified as quercetin 3-O-gentobioside (10.32%) , quercetin 3-O-${\beta}$-D-glucoside (isoquercitin, 13.30%), quercetin 3-O-${\beta}$-D-galactoside (hyperin, 11.34%), quercetin 3-O-${\alpha}$-L-arabinoside (guajavarin, 19.70%), quercetin 3-O-${\beta}$-L-rhamnoside (quercitrin, 45.33%) in the order of elution time. The inhibitory effect of Psidium guajava leaf extracts on tyrosinase were investigated to assess their whitening efficacy. Finally, their anti-elastase activities were measured to predict the anti-wrinkle efficacy in the human skin. Inhibitory effects $(IC_{50})$ on tyrosinase of some Psidium guajava leaf extracts was 50% ethanol extract $(149.67{\mu}g/mL)$ < ethylacetate fraction $(30.67{\mu}g/mL)$ < deglycosylated aglycone fraction $(17.10{\mu}g/mL)$. Inhibitory effects $(IC_{50})$ on elastase of some Psidium guajava leaf extracts was 50% ethanol extract $(6.60{\mu}g/mL)$ < deglycosylated aglycone fraction $(5.66{\mu}g/mL)$ < ethylacetate fraction $(3.44{\mu}g/mL)$. These results indicate that extract/fractions of Psidium guajava leaf can function as antioxidants in bioloigcal systems, particularly skin exposed to UV radiation by scavenging $^1O_2$ and other ROS, and protect cellular membranes against ROS. And component analysis of Psidium guajava leaf extract and inhibitory activity on elastase of the aglycone fraction could be applicable to new functional cosmetics for smoothing wrinkles.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.25 no.1
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• pp.69-88
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• 1999

Several solvent extracts from Alpinia katsumudai were prepared and their various anti-inflammatory activities were evaluated. Alpinia katsumadai extract showed high various anti-inflammatory effects among the 8 medicinal plant extracts, Butanol extract from Alpinia katsumndai showed a potent anti-oxidative and free radical scavenging activities, Free radical scavenging effect of butanol fraction of Alpinia katsumadai($IC_{50}$/ : 50$\mu$g/m$\ell$) was higher than butylated hydroxytoluene($IC_{50}$/ : 50$\mu$g/m$\ell$) and ascorbic acid($IC_{50}$/ : 22$\mu$g/m$\ell$). Alpinia katsumadai butanol fraction exhibited relatively high antioxidative activity($IC_{50}$/ : 335$\mu$g/m$\ell$) compared to ascorbic acid. The inhibitory effect of Alpinia katsumadal ethanol extract on elastase exhibited 10 to 78% at 100 to 1000$\mu$g/m$\ell$ concentration , tile $IC_{50}$/ values with 465.7$\mu$g/m$\ell$ for porcine pancreatic elastase(PPE) and 481.9$\mu$g/m$\ell$ for human leukocyte elastase(HLE), respectively The Alpinta katsumadai extract inhibited effectively hyaluronidase activity($IC_{50}$/ 335$\mu$g/m$\ell$), and showed inhibition in vitro on delayed hypersensitivity when it was topically applied. These results suggest that Alpinia katsumadai extract may reduce inflammatory skin trouble. The Alpinia katsumadai extract also showed higher Inhibitory effect of melanin biosynthesis on cultured melanoma cell compared to arbutin and kojic acid.

• The Korea Journal of Herbology
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• v.31 no.4
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• pp.53-60
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• 2016

Objective : The purpose of this study was to investigate anti-aging and antioxidant effects of extracts of Nelumbo nucifera leaves (NN-L) using ethanol on skin .Methods : Each part of leaves(NN-L), flowers(NN-F) and stem(NN-S) was extracted with 70% ethanol. We performed radical scavenging assay(DPPH, ABTS+, Superoxide anion radical), elastase inhibition assay, collagenase inhibition assay. NN-L extracts were tested for cell viability(MTT assay), MMP-1 inhibition and MMP-1 protein expression on CCD-986sk cells (human fibroblast line).Results : Recently, many studies have reported that elastin is also involved in inhibiting or repairing wrinkle formation, although collagen is a major factor in the skin wrinkle formation. We measured its free radical scavenging activity, elastase inhibitory activity and expression of MMP-1 (matrix metalloprotease-1) in human fibroblast cells. Among the parts of Nelumbo nucifera, NN-L showed the highest antioxidant activities and in radical scavenging. DPPH, ABTS+ and Superoxide anion radical scavenging activity of NN-L at concentration of 1,000 μg/mL were 91.43%, 99.31% and 73.7% respectively. In vitro elastase and collagenase inhibition effects of NN-L at concentration of 1,000 μg/mL was 42.8% and 55.3% respectively. The ethanol extract of NN-L showed cell viability of 95.4% in 50 μg/mL concentration. In addition, The results from Western blot assay showed that NN-L decreased the expression of MMP-1 protein in a dose-dependent manner (by up to 35.0% at 50 μM).Conclusion : The findings suggest that the NN-L great potential as a cosmeceutical ingredient with antioxidant and anti-wrinkling effects.

• Journal of the Korean Applied Science and Technology
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• v.39 no.1
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• pp.27-33
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• 2022

The purpose of this study was to investigate the functionality of Lycium chinense Miller. as a functional cosmetic material. The total polyphenol content in the extract was 17.3 mg/mL, and as a result of confirming cytotoxicity through MTT assay before the enzyme experiment, it was confirmed that it did not affect cell growth at all concentrations below 1000 ㎍/mL. As a result of conducting DPPH radical scavenging tests as an antioxidant efficacy test, it showed 84.97% scavenging ability at a concentration of 1000 ㎍/mL, and showed very excellent antioxidant efficacy in SOD-like activity test with a result of 80.54% at 1000 ㎍/mL. The measured elastase inhibitory activity, the inhibition rate of 50.93% was observed at 1000 ㎍/mL, indicating that the extract of Lycium chinense Miller. was effective in inhibiting elastase. All these findings suggested that 70% ethanol extract of Lycium chinense Miller. was confirmed as a functional cosmetic material by confirming its antioxidant and anti-wrinkle efficacy.