• 제목/요약/키워드: product inhibition

검색결과 644건 처리시간 0.022초

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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    • 제25권1호
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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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    • 제1권1호
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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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    • 제18권2호
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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.

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

  • 박관혁;서범석;손동주;박영현;장성근
    • 한국산학기술학회논문지
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    • 제4권4호
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    • pp.357-360
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    • 2003
  • 작약의 methanol 추출물은 혈소판 활성 실험에서 혈소판 응집에 대해 강한 억제를 보였다. 활성성분은 chromatography방법을 사용하여 정제하였고 NMR과 기존의 Data로 분석하였다. Compound 1b는 benzoyloxypaeoniflorin과 동일한 구조임을 확인하였으며. compound 2e는 작약의 주성분인 paeoniflorin과 동일한 화학구조를 가졌으며 , compound 3a의 분석결과 구조적 유사성은 있으나 동일한 구조식은 확인 할 수 없었지만 collagen에서 응집억제활성이 90%이상의 뛰어난 활성을 나타내어 benzoyloxypaeoniflorin과 유사하게 benzoyl 기가 다른 작용기로 치환되었거나 Rl group이 다른 작용기로 치환된 형태로 추측하였다. Paeoniflorin이 collagen보다 thrombin에서 강한 억제를 보이는 것은 Ca/sup 2+/ chelate를 형성함으로 인해 calcium 대사산물이 파괴된 것으로 추측했다. Compound 3a는 paeoniflorin의 benzoyl 기에 있는 OH기나 paeoniflorin의 glycoside 5-carbon위치의 OH기 대신에 다른 작용기가 대사산물로의 역할을 수행했을 것으로 추정했다.

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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
    • 한국축산식품학회지
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    • 제34권1호
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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.

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

  • Hong, Yong-Ki;Seu, Jung-Hwn
    • 한국미생물·생명공학회지
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    • 제9권4호
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    • pp.179-183
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    • 1981
  • 진균류의 세포벽제거 및 이에 따른 protoplast생성 등에 많이 이용되어지고 있는 chitinase를 Streptomyces sp. 115-5 균주로부터 생산하여 순수 정제한 다음, 이 chitinase의 작용을 저해하는 포도당의 저해양상을 조사하였다. 포도당 외에 D-glucuronic acid, D-sorbitol및 D-xylose등도 chitinase의 활성을 저해하였다. 그런고로, 포도당 분자에 의한chitinase의 활성 저해 효과에는 위의 분자들의 공통부분인 2번, 3번 및 4번 탄소의 hydroxyl group들의 구조위치가 중요한 영향을 가진다는 것을 알 수 있다. 그리고 포도당에 의한 chitinase의 저해양상은 competitive inhibition 과 non-competitive inhibition 과의 혼합 저해형으로 나타났다.

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

  • 최승만;김창덕;이민호;최영호;랑문정;안호정;윤여표
    • 약학회지
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    • 제43권3호
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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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    • 제35권2호
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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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    • 제27권1호
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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.