• Title/Summary/Keyword: product inhibition

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Isolation of Constituents with Nitric Oxide Synthase Inhibition Activity from Phryma leptostachya var. asiatica

  • Kim, Donghwa;Lee, Sang Kook;Park, Kyoung-Sik;Kwon, Na-Yun;Park, Hee-Juhn
    • Natural Product Sciences
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    • v.25 no.1
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    • pp.34-37
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    • 2019
  • Phytochemical studies were performed to identify the active principles of Phryma leptostachya var. asiatica (Phyrymaceae) for anti-inflammation. The anti-inflammatory activity was assessed by measuring the inhibition rate on nitric oxide (NO) formation in lipopolysaccharide (LPS)-activated macrophage 264.7 cells. Of the five compounds including ursolic acid, phrymarolin I, harpagide, haedoxancoside A, and acteoside isolated from this plant, ursolic acid showed the most prominent inhibition of NO formation. Therefore, ursolic acid may be the anti-inflammatory principle of Phryma leptostachya var. asiatica.

THE PHOTOCHEMICAL REACTION OF 1-HALO-2-(PHENYLAKYL)BENZENES

  • Park, Yong-Tae;Kim, Young-Hee;Lee, Ick-Heung
    • Journal of Photoscience
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    • v.1 no.1
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    • pp.39-45
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    • 1994
  • Haloarene in which the phenyl group and halophenyl group are connected by alkyl groups were synthesized to study the photochemical behavior. The photochemical reactions of 1-halo-2-(phenylalkyl)enzenes (1 and 2) were studied in several aerated or unaerated solvents. In the case of 2-benzyl-1-halobenzene photoreduced product (biphenyl) is major in acetonitrile or benzene. In cyclohexane or acetonitrile with triethylamine, photoreduced product is obtained exclusively, while in acetonitrile with toluene, xylene, or sodium hydroxide photocyclized product (fluorene) is mainly obtained. In the case of 1-halo-2-phenethylbenzenes (5 and 6), photocyclized product (9,10-dihydrophenanthrene and phenanthrene) are major in acetonitrile or benzene. While the haloarenes 1 or 2 connecting the two arene rings by methylene is photoreduced, the other haloarene 5 or 6 connecting by ethylene is photocyclized. In cyclohexane or acetonitrile with a small amount of triethylamine, photoreduced reactions of 5 or 6 mainly occur. In acetonitrile with sodium hydroxide, toluene, or xylene, photocyclization of 5, 6 occur exclusively. The triplet state is mainly involved in the photocyclization of 5 or 6, because of the inhibition of oxygen.

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Antioxidant Activity of Some Yogurt Starter Cultures

  • Kim, H.S.;Chae, H.S.;Jeong, S.G.;Ham, J.S.;Im, S.K.;Ahn, C.N.;Lee, J.M.
    • Asian-Australasian Journal of Animal Sciences
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    • v.18 no.2
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    • pp.255-258
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    • 2005
  • Several commercial yogurt starter cultures (L. acidophilus LA5, L. casei 01, L. acidophilus LA100, L. bulgaricus LB207 and L. rhamnosus GG744) were investigated for antioxidant activity by using in vitro assays. From the results of the present work, all strains tested showed varying degrees of antioxidant activity. L. bulgaricus LB207 showed the highest antioxidant activity, with a linoleic acid peroxidation inhibition of 81.3%. Hydroxy radical scavenging activity, ferrous iron chelating activity, reducing power and superoxide dismutase (SOD) activity were also studied. L. bulgaricus LB207 showed the highest hydroxy radical scavenging activity and L. casei 01 showed the highest chelating activity. L. bulgaricus LB207 and L. acidophilus LA100 showed good reducing power. All the strains in this study showed low SOD activity. The results of the present work suggest that antioxidant activity of L. bulgaricus LB207 due to its strong hydroxy radical scavenging activity and reducing power.

Study on Inhibition of Platelet Aggregation of Bioactive Constituents from Paeonia lactiflora (작약의 혈소판 응집억제작용에 관한 연구)

  • 박관혁;서범석;손동주;박영현;장성근
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.4 no.4
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    • pp.357-360
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    • 2003
  • Methanol extracts from Paeonia lactiflora showed a strong inhibition against platelet aggregation on platelet activation test. Therefore, the bioactive constituents from Paeonia lactiflora were prepared using chromatography methods and were analyzed by NMR and reference data. Compound 1b was confirmed a same structure with henzoyloxypaeoniflorin, compound 2e was a same structure with paeoniflorin; main product of Paeonia lactiflora. Analytical data of compound 3a were not consistent with any known paeoniflorin soucture, but showed the souctural similarity with it. And also the aggregation inhibition activity of compound 3a showed a strong inhibition($\geq$ 90%) induced by collagen. Therefore it suggested that the structure of compound 3a may be the similar structure of benzoyloxypaeoflorin with a functional group in place of benzoyl group and/or a different functional group in stead of Rl. We suggested that benzoyl group of benzoyloxypaeoniflorin substitued instead of 5-carbon OH group on glycoside moiety paeoniflorin played role of the metabolite in case of a platelet aggregation inhibition activity. Paeoniflorin showed more strong inhibition by thrombin than collagen. Therefore, it may be destructed a calcium metabolite as a forming $Ca^2+$ chelate. Compound 3a may be that other functional group instead of OH group of 5-carbon on glycoside moiety of paeoniflorin and/or OH group of benzoyl moiety of paeoniflorin played role of the metabolite in a platelet aggregation inhibition.

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Optimizing Carnosine Containing Extract Preparation from Chicken Breast for Anti-glycating agents

  • Kim, Seung-Ki;Kwon, Dodan;Kwon, Da-Ae;Paik, In Kee;Auh, Joong-Hyuck
    • Food Science of Animal Resources
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    • v.34 no.1
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    • pp.127-132
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    • 2014
  • Optimization of carnosine and anserine extraction from chicken breast was performed using response surface methodology (RSM) to obtain the maximized physiological activities for anti-glycation and anti-oxidation. The optimum extraction conditions were water extraction for 1.6 h in the case of the 20-wk laying hen muscle and water extraction for 2.12 h in the case of 90-wk laying hen muscle. Higher carnosine and anserine contents were measured in the 20-wk laying hen muscle, along with higher physiological activities, which increased in direct proportion with the dipeptide contents. The extracts prepared from the 20-wk laying hen under optimum conditions showed 57% inhibition of advanced glycated end-product formation, 64% inhibition of lipid peroxidation, and 61% of DPPH radical scavenging effects. On the other hand, 52% inhibition of AGE formation, 62% inhibition of lipid peroxidation, and 53% of DPPH radical scavenging effect were demonstrated within the 90-wk laying hen. In addition, the ratio of carnosine was a key indicator for the physiological activities of the extracts.

Some Kinetic Properties of an Extracellular Chitinase from Streptomyces sp, 115-5 (Streptomyces속 115-5 균주로부터 생성된 Chitinase의 저해작용기작)

  • Hong, Yong-Ki;Seu, Jung-Hwn
    • Microbiology and Biotechnology Letters
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    • v.9 no.4
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    • pp.179-183
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    • 1981
  • An extracellular chitinase was purified from the culture fluid of Streptomyces sp. 115-5, and its inhibition mechanism by end product was studied. The activity of chitinase was suppressed by the reducing sugar as the reaction proceeded, and the activity was inhibited by the addition of D-glucose. Besides D-glucose, the rate of chitin hydrolysis was inhibited by D-glucuronic acid, D-sorbitol and D-xylose in the reaction system of the enzyme. it was found that the hydroxyl groups at the C-2, C-3 and C-4 position of D-glucose molecule play an important role in the inhibition of the chitinase activity. D-glucose was found to inhibit the enzyme activity by mixed type of competitive and non-competitive mode.

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Screening of $5{\alpha}-Reductase$ Inhibition and Comedolytic Effects from Natural Products (천연물로부터 $5{\alpha}-Reductase$ 활성억제 및 면포용해효과의 검색)

  • 최승만;김창덕;이민호;최영호;랑문정;안호정;윤여표
    • YAKHAK HOEJI
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    • v.43 no.3
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    • pp.342-350
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    • 1999
  • The antibacterial activity against Propionibacterium acnes (P. acnes), $5{\alpha}-reductase$ inhibition and comedolytic effects are the important pharmacological target sites of antiacne drughs. We previously reported on the antibacterial activities against P. acnes by natural products. In the present study the screening of $5{\alpha}-reductase$ inhibition and comedolytic effects from natural products were performed. Seven natural products such as Angelica koreana, Sophora flavescens, Prunus persica, Bombyx mori, Areca catechu, Galla rhois and Gleditschia koraiensis perfectly inhibited the activity of $5{\alpha}-reductase$ at the concentration of 0.01% (w/v). Sixteen natural products which were shown to have the potent antibacterial activities against P.acnes or $5{\alpha}-reductase$ inhibition activities were assayed for the comedolytic test. In the results of comedolytic effects on experimentally-induced comedones (EIC), Sophora flavescens showed the strongest comedolytic effect on EIC, and Polygonum cuspidatum and Angelica koreana showed stronger comedolytic effects on EIC than azelaic acid used for a positive control at the concentration of 3% (w/v). These results suggest that several natural products including Sophora flavescens can be developed as noble antiacne agents.

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Characterization of Aspartate Aminotransferase Isoenzymes from Leaves of Lupinus albus L. cv Estoril

  • Martins, Maria Luisa Louro;De Freitas Barbosa, Miguel Pedro;De Varennes E Mendonca, Amarilis Paula Alberti
    • BMB Reports
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    • v.35 no.2
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    • pp.220-227
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    • 2002
  • Two aspartate aminoransferase (EC 2.6.1.1) isoenzymes (AAT-1 and AAT-2) from Lupinus albus L. cv Estoril were separated, purified, and characterized. The molecular weight, pI value, optimum pH, optimum temperature, and thermodynamic parameters for thermal inactivation of both isoenzymes were obtained. Studies of the kinetic mechanism, and the kinetics of product inhibition and high substrate concentration inhibition, were performed. The effect of some divalent ions and irreversible inhibitors on both AAT isoenzymes was also studied. Native PAGE showed a higher molecular weight for AAT-2 compared with AAT-1. AAT-1 appears to be more anionic than AAT-2, which was suggested by the anion exchange chromatography. SDS-PAGE showed a similar sub-unit molecular weight for both isoenzymes. The optimum pH (between 8,0 and 9.0) and temperature ($60-65^{\circ}C$) were similar for both isoenzymes. In the temperature range of $45-65^{\circ}C$, AAT-2 has higher thermostability than AAT-1. Both isoenzymes showed a high affinity for keto-acid substrates, as well as a higher affinity to aspartate than glutamate. Manganese ions induced an increase in both AAT isoenzymes activities, but no cooperative effect was detected. Among the inhibitors tested, hydroxylamine affected both isoenzymes activity by an irreversible inhibition mechanism.

Anti-inflammatory, Anti-glycation, Anti-tyrosinase and CDK4 Inhibitory Activities of Alaternin (=7-Hydroxyemodin)

  • Bhatarrai, Grishma;Choi, Jeong-Wook;Seong, Su Hui;Nam, Taek-Jeong;Jung, Hyun Ah;Choi, Jae Sue
    • Natural Product Sciences
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    • v.27 no.1
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    • pp.28-35
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    • 2021
  • The aim of this study was to anatomize the therapeutic potential of alaternin (=7-hydroxyemodin) against inflammation, advanced glycation end products (AGEs) formation, tyrosinase, and two cyclin-dependent kinases (CDKs), CDK2 and CDK4, and compare its potency with emodin. Alaternin showed lower cytotoxicity and higher dose-dependent inhibition against lipopolysaccharide (LPS) induced nitric oxide (NO) production with half maximal inhibitory concentration (IC50) of 18.68 µM. Similarly, alaternin efficaciously inhibited biotransformation of fluorescent AGEs and amyloid cross-β structure on the bovine serum albumin (BSA)-glucose-fructose system, five times more than emodin. Interestingly, alaternin also showed selective activity against CDK4 at 170 µM, whereas emodin inhibited both CDK2 and CDK4 at a concentration of 17 and 380 µM respectively. In addition, alaternin showed dose-dependent inhibitory activity against mushroom tyrosinase with inhibition percentage of 35.84 % at 400 µM. Altogether, alaternin with pronounced inhibition against inflammatory mediator (NO), glycated products formation, and targeted inhibition towards CDK4 receptor can be taken as an important candidate to target multiple diseases.