• Title/Summary/Keyword: Inhibitory Activity

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Effect of Buthus on $Na^+-K^+-ATPase$ activity in cerebral synaptosomes (전갈(全蝎)이 뇌조직(腦組織)의 $Na^+-K^+-ATPase$ 활성(活性)에 미치는 영향(影響))

  • Yoon, Jong-Yeong;Shin, Hyeon-Chul;Yoon, Chul-Ho;Seo, Un-Kyo;Kim, Jong-Dae;Jeong, Ji-Cheon
    • The Journal of Internal Korean Medicine
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    • v.19 no.1
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    • pp.431-441
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    • 1998
  • This study was undertaken to determine whether Buthus exract(BTE) affects Na^+-K^+-ATPase$ activity of nervous tissues. The enzym activity was measured in synaptosomal fraction prepared from rabbit brain cortex. Na^+-K^+-ATPase$ activity was inhibited by BTE over concentration range of 0.05-0.5% in a dose-dependent manner. The enzyme activity was increased by an increase in $Na^+$ concentration from 5 to 100mM, $K^+$ concentration from 0.5 to 10mM, and $Mg^{2+}$ concentration from 0.2 to 5mM. These changes in ion concentrations did not produce any effect on the inhibitory effect of BTE on $Na^+-K^+-ATPase$ activity. An increase in ATP concentration from 0.1 to 3mM caused an increase in the enzyme activity. The inhibition of the enzyme activity by BTE were not different between two ATP concentrations. A sulfhydryl group protector DTT prevented PCMB-induced inhibition of $Na^+-K^+-ATPase$ activity, but the BTE-induced inhibition was not altered by DTT. The inhibition of enzyme activity by combination of ouabain and BTE was not different from that by Buthus alone. These results suggest that Buthus exerts inhibitory effect on $Na^+-K^+-ATPase$ activity in cerebral synaptosomes, and the action mechansim is similar to that of ouabain.

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Inhibitory Effects of Angiotensin Converting Enzyme and α-Glucosidase, and Alcohol Metabolizing Activity of Fermented Omija (Schizandra chinensis Baillon) Beverage (오미자 발효음료의 알코올 분해능과 Angiotensin Converting Enzyme 및 α-Glucosidase 저해효과)

  • Cho, Eun-Kyung;Cho, Hea-Eun;Choi, Young-Ju
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.39 no.5
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    • pp.655-661
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    • 2010
  • The nutraceutical role of fermented omija (Schizandra chinensis) beverage (FOB) was determined through the analysis of fibrinolytic and alcohol metabolizing activities, nitrite scavenging activity, and angiotensin converting enzyme and $\alpha$-glucosidase inhibitory effects. Firstly, FOB increased fibrinolytic activity in a dose-dependent manner and indicated angiotensin converting enzyme inhibitory activity of 94.8% at 20% FOB (0.6 mg/mL). In addition, the inhibitory activities of FOB on $\alpha$-amylase and $\alpha$-glucosidase were determined to be 100% at 100% FOB (3 mg/mL) and 49% at 60% FOB (1.8 mg/mL), respectively. Nitrite scavenging activity of FOB was about 96.1%, 72.3%, and 68.3% on pH 1.2, 3.0, and 6.0 at 100% FOB, respectively. To determine influence of FOB on alcohol metabolism, the generating activities of reduced-nicotinamide adenine dinucleotide (NADH) by alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH) were measured. Facilitating rate of ADH activity was 70.3% at 50% FOB, but ALDH activity was not affected. These results revealed that FOB has a strong alcohol metabolizing activity, and fibrinolytic and nitrite scavenging activities and exhibits the angiotensin converting enzyme, $\alpha$-amylase, and $\alpha$-glucosidase inhibitory activities.

Component Analysis and Study on Anti-elastase Activity of Equisetum arvense Extracts(II) (쇠뜨기 추출물의 성분 분석과 엘라스타제 활성 저해 효과 연구(II))

  • Park, Soo-Nam;Yang, Hee-Jung
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.33 no.3
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    • pp.139-144
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    • 2007
  • In the previous study, we reported the antioxidative activity of Equisetum arvense extracts. In this study, its inhibitory effect on elastase and components were investigated. Aglycone fractions obtained from the deglycosylation reaction of ethylacetate fraction among the Equisetum arvense extracts, showed 4 bands and 4 peaks in TLC and HPLC experiments, respectively. Four components were identified as luteolin(composition ratio, 19.12%), quercetin(12.87), apigenin(15.81) and kaempferol(52.20). TLC chromatogram of ethylacetate fraction of Equisetum arvense extract revealed 7 bands and HPLC chromatogram showed 8 peaks, which were identified as kaempferol-3,7-O-diglucoside(composition ratio, 15.74%), luteolin-5-O-glucoside(galuteolin, 11.91), apigenin-5-O-glucoside(12.91), kaempferol-3-O-glucoside(astragalin, 27.94), quercetin-glycoside(10.81, structure was not determined), kaempferol-glycoside (12.33, structure was not determined), luteolin(3.72) and apigenin(4.62) in the order of elution time. The inhibitory effect of aglycone fraction on elastase($IC_{50}$, $9.8{\mu}g/mL$) was very high. But ethylacetate fraction(flavonoid glycosides) rarely exhibited the inhibitory activity on elastase. Combined with the previous results of the antioxidative activity of Equisetum arvense extracts, it is concluded that the inhibitory activity on elastase of the aglycone fraction could be applicable to new functional cosmetics for smoothing wrinkles.

Screening of Bioactive Compounds from Edible Mushroom and Production of Anti-osteoporosis Osteoclast Differentiation Inhibitor (몇 가지 주요 식용버섯의 생리기능성 물질 탐색과 파골세포 분화 저해물질의 생산)

  • Jang, In-Taek;Kim, Young-Hun;Kim, Jeong-Han;Lee, Yun-Hae;Ju, Young-Cheoul;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.40 no.2
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    • pp.114-117
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    • 2012
  • For development of new bioactive compounds from main edible mushrooms, we determined some physiological functionalities of water extracts from mushrooms. Among water extracts from some mushroom fruiting bodies, water extracts from Pleurotus ostreatus showed 73.2% of anti-hypertensive angiotensin I-converting enzyme inhibitory activity and 73.3% of anti-gout xanthine oxidase inhibitory activity, respectively. Fibrinolytic activity was also showed 21.5 mm of clear zone in water extract of Lyophyllum cinerascens. However, the other physiological functionalities were very weaked except 40.3% of antioxidant activity in Lentinus lepideus. Furthermore, the water extracts of Pleurotus eryngii and Lyophyllum cinerascens showed high anti-osteoporosis osteoclast differentiation inhibitory activity. However, the water extract from Lentinus lepideus and Pleurotus ostreatus were not detected any osteoclast differentiation inhibitory activity.

Antioxidant and Antiaging Assays of Hibiscus sabdariffa Extract and Its Compounds

  • Widowati, Wahyu;Rani, Andani Puspita;Hamzah, R. Amir;Arumwardana, Seila;Afifah, Ervi;Kusuma, Hanna Sari W.;Rihibiha, Dwi Davidson;Nufus, Hayatun;Amalia, Annisa
    • 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.

Quantitative structure-activity relationships and molecular shape similarity of the herbicidal N-substituted phenyl-3,4-dimethylmaleimide Derivatives (제초성 N-치환 phenyl-3,4-dimethylmaleimide 유도체의 정량적인 구조-활성관계와 분자 유사성)

  • Sung, Nack-Do;Ock, Hwan-Suk;Chung, Hun-Jun;Song, Jong-Hwan
    • The Korean Journal of Pesticide Science
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    • v.7 no.2
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    • pp.100-107
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    • 2003
  • To improve the growth inhibitory activity against the shoot and root of rice plant (Oryza sativa L) and barnyard grass (Echinochloa crus-galli), a series of N-substituted phenyl-3,4-dimethylmaleimdes derivatives as substrates were synthesized and then their the inhibitory activities of protoporphyrinogen oxidase (1.3.3.4), protox were measured. The quantitative structure-activity relationships (QSAR) between structures and the inhibitory activities were studied quantitatively using the 2D-QSAR method. And also, molecular sharp similarity between the substrate derivatives and protogen, substrare of protox enzyme were studied. The activities of the two plants indicated that barnyard grass had a higher activity than the rice plant and their correlation relationships have shown in proportion for each. Accordingly, the results of SARs suggest that the electron donating groups as $R_2=Sub.X$ group will bind to phenyl ring because the bigger surface area of negative charged atoms in the substrate molecule derivatives may increase to the higher the activity against barnyard grass. Based on the molecular shape similarity, when the derivatives and protogen, subsbrate of protox enzyme were superimposed by atom fitting, the similarity indices (S) were above 0.8 level but the correlation coefficients (r) between S values and the activities showed not good.

Hyaluronidase Inhibitory Activity of Extracts from Doenjang, Chungkookjang and Miso (된장, 청국장 및 미소추출물의 Hyaluronidase 저해활성)

  • Ahn, Sun-Kyung;Hong, Kwang-Won
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.34 no.8
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    • pp.1119-1123
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    • 2005
  • The inhibitory effects of water and methanol extracts of Doenjang, Chungkookjang and Miso on bovine hyaluronidase were examined. The extracts were vacuum-dried and the resulting pellets were dissolved with 0.1 M acetate buffer with 1$\%$ DMSO to a final concentration of 50 mg/mL. The water extracts of Doenjang, Chungkookjang and Miso inhibited 62$\%$, 70$\% $, 56$\%$ of hyaluronidase activity, respectively, while the extract of crushed soybean inhibited 24$\%$ of the activity. Under the same condition, disodiumcromoglycate known as an anti-allergic drug inhibited 46$\%$ of hyaluronidase activity at the concentration of 0.35 mg/mL as a positive control. Also the methanol extracts of Doenjang, Chungkookjang and Miso inhibited 48$\%$, 52$\%$, 70$\%$ of hvaluronidase activity, respectively, while the extract of crushed soybean inhibited 46$\%$ of the activity. After heat treatment of the water extracts of Doenjang, Chungkookjang and Miso at 100"C for 10 min, hyaluronidase inhibitory effects of them were reduced approximately to half. However, hyaluronidase inhibitory effects of methanol extracts were maintained well even after heat treatment.

Whitening Effect of Dayflower (Commelina communis L.) Extract by Inhibition of N-Linked Glycosylation Process and Melanogenesis (N-Linked Glycosylation 저해에 의한 닭의장풀 추출물의 미백효능)

  • Park, Sun-Hee;Lee, Bang-Yong;Lee, Seung-Hyun;Han, Chang-Sung;Kim, Jin-Guk;Kim, Kyoung-Tae;Kim, Ki-Ho;Kim, Young-Heui
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.35 no.1
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    • pp.73-78
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    • 2009
  • In order to investigate the potential of a Dayflower (Commelina communis L.) extract as an active in gredient for whitening cosmetics, we prepared aqueous Commelina communis L. extract We measured its mushroom tyrosinase inhibitory activity, cellular tyrosinase activity, and melanin synthesis inhibitory activity in B16 melanoma cells. It did not show inhibitory activity against mushroom tyrosinase but showed melanin synthesis inhibitory activity. In a melanin synthesis inhibition assay using mouse B16-F10 melanoma cell, it suppressed melanin production up to 32% at a concentration of $1,000{\mu}/mL$ without cytotoxicity, and also reduced cellular tyrosinase activity to above 50 % above the concentration of $250{\mu}g/mL$. In study on the melanogenic protein expressions, it had especially influence on expression of tyrosinase protein, which is a well-known key protein on melanogenesis, and tyrosinase expression was gradually decreased in a dose-dependent. Dayflower also blocked N-glycosylation of TRP-2, but affected on the expression of TRP-1 rather than on blocking of N-glycosylation processing. Therefore, this result suggests that aqueous Commelina communis L. extract could be used as an active ingredient for whitening cosmetics.