• 제목/요약/키워드: purine compounds

검색결과 25건 처리시간 0.018초

Effects of 1,7-Substituted Methylxanthine Derivatives on LPS-Stimulated Expression of Cytokines and Chemokines in Raw 264.7 and HK-2 Cells

  • Kang, Joo-Yeon;Shin, Hea-Soon
    • Journal of Microbiology and Biotechnology
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    • 제25권2호
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    • pp.296-301
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    • 2015
  • Chronic kidney diseases are based on uncontrolled immunological and inflammatory responses to pathophysiological renal circumstances such as glomerulonephritis, which is caused by immunological mechanisms of glomerular inflammation with increased production of renal pro-inflammatory cytokines. Pentoxifylline (PTX) exhibits anti-inflammatory properties by inhibiting cytokine and chemokine production through aggregation of erythrocytes and thrombocytes. We synthesized a series of 1,7-substituted methylxanthine derivatives by the Traube purine reaction, and the formation of purine ring was completed through nitrosation, a reduction of the nitroso to the amine by catalytic hydrogenation as derivatives of PTX. Then we studied biological activities such as renal anti-inflammatory effects of the synthesized compounds in the production of cytokines such as nitric oxide (NO), interleukin (IL)-1β, IL-6, and tumor necrosis factor-α (TNF-α) and of chemokines such as monocyte chemoattractant protein-1 and IL-8 in Raw 264.7 and HK-2 cells. Renal antiinflammatory activities of this novel series of N-1 and N-7-substituted methylxanthine showed that the N-7 methyl-group-substituted analogs (S7b) showed selective 61% and 77% inhibition of the production of NO and IL-8. The other replacement of the N-1-(CH2)4COCH3 roup, as in the case of compound S6c, also showed an effective 50% and 77% inhibition of TNF-α and IL-8 production in LPS-stimulated Raw 264.7 and HK-2 cells.

인산감수성(燐酸感受性)이 다른 대두품종간(大豆品種間) 유기산(有機酸) 및 당(糖)에 대(對)한 질소원(窒素源)의 영향(影響) (Effects of Nitrogen Sources on Sugars and Organic Acids of Soybean Cultivars Different in Phosphorus Sensitivity)

  • 박훈;찰스 에이 스뚜디
    • 한국토양비료학회지
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    • 제10권2호
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    • pp.85-92
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    • 1977
  • 인산감수성(燐酸感受性)이 다른 9개대두재배종(個大豆栽培種) Lee, Hill, Harosoy, Clark-63, Chippewa 및 R56-49을 서로 다른 질소원(窒素源)으로 수경재배(水耕栽培)하여 엽중유리당(葉中遊離糖)과 유기산(有機酸)을 gas chronatograph로 조사(調査)하여 미동정(未同定)의 X, Y peak와 Sucrose peak가 주(主) peak로 나타났다. X 화합물(化合物)은 NO3-N 급여(給與)경우 흔적으로 나타난데 반하여 NH4-N나 urea 급여(給與)경우에 다량(多量)나타났다. Y 화합물(化合物)을 Urea 급여(給與)경우 감소하는 경향이었다. Sucrose는 NH4-N 급여(給與)에서 흔적으로 나타나고 Urea에서 NO3-N에서보다 높았다. X 화합물(化合物)은 erythrose에서 유래(由來)한 4 탄소(炭素) 산성당(酸性糖)이거나 Purine이나 Pyrimidine에서 유래(由來)한 환상화합물(環狀化合物)로 Y 화합물(化合物)은 glycolysis path에서 유래(由來)한 6 탄당(炭糖)으로 추정(推定)되었다. Y/X 치(値)는 인산감수성(燐酸感受性)의 좋은 지표(指標)가 되므로(역관계(逆關係)) 이 두 화합물(化合物)은 ammonia 독작용(毒作用) 및 인산감수성(燐酸感受性) 기작(機作)에 관여(關與)하는 요인화합물(要因化合物)로 보였다.

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Metabolomic profiling of postmortem aged muscle in Japanese Brown beef cattle revealed an interbreed difference from Japanese Black beef

  • Susumu Muroya;Riko Nomura;Hirotaka Nagai;Koichi Ojima;Kazutsugu Matsukawa
    • Animal Bioscience
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    • 제36권3호
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    • pp.506-520
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    • 2023
  • Objective: Japanese Brown (JBR) cattle, especially the Kochi (Tosa) pedigree (JBRT), is a local breed of moderately marbled beef. Despite the increasing demand, the interbreed differences in muscle metabolites from the highly marbled Japanese Black (JBL) beef remain poorly understood. We aimed to determine flavor-related metabolites and postmortem metabolisms characteristic to JBRT beef in comparison with JBL beef. Methods: Lean portions of the longissimus thoracis (loin) muscle from four JBRT cattle were collected at 0, 1, and 14 d postmortem. The muscle metabolomic profiles were analyzed using capillary electrophoresis time-of-flight mass spectrometry. The difference in post-mortem metabolisms and aged muscle metabolites were analyzed by statistical and bioinformatic analyses between JBRT (n = 12) and JBL cattle (n = 6). Results: A total of 240 metabolite annotations were obtained from the detected signals of the JBRT muscle samples. Principal component analysis separated the beef samples into three different aging point groups. According to metabolite set enrichment analysis, post-mortem metabolic changes were associated with the metabolism of pyrimidine, nicotinate and nicotinamide, purine, pyruvate, thiamine, amino sugar, and fatty acid; citric acid cycle; and pentose phosphate pathway as well as various amino acids and mitochondrial fatty acid metabolism. The aged JBRT beef showed higher ultimate pH and lower lactate content than aged JBL beef, suggesting the lower glycolytic activity in postmortem JBRT muscle. JBRT beef was distinguished from JBL beef by significantly different compounds, including choline, amino acids, uridine monophosphate, inosine 5'-monophosphate, fructose 1,6-diphosphate, and betaine, suggesting interbreed differences in the accumulation of nucleotide monophosphate, glutathione metabolism, and phospholipid metabolism. Conclusion: Glycolysis, purine metabolism, fatty acid catabolism, and protein degradation were the most common pathways in beef during postmortem aging. The differentially expressed metabolites and the relevant metabolisms in JBRT beef may contribute to the development of a characteristic flavor.

Chemical Constituents of the Fruiting Bodies of Clitocybe nebularis and Their Antifungal Activity

  • Kim, Young-Sook;Lee, In-Kyoung;Seok, Soon-Ja;Yun, Bong-Sik
    • Mycobiology
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    • 제36권2호
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    • pp.110-113
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    • 2008
  • During a continuing search for antimicrobial substances from Korean native wild mushroom extracts, we found that the methanolic extract of the fruiting body of Clitocybe nebularis exhibited mild antifungal activity against pathogenic fungi. Therefore we evaluated the antifungal substances and other chemical components of the fruiting body of Clitocybe nebularis, which led to the isolation of nebularine, phenylacetic acid, purine, uridine, adenine, uracil, benzoic acid, and mannitol. Nebularine showed mild antifungal activity against Magnaphorthe grisea and Trichophyton mentagrophytes, and phenylacetic acid potently inhibited the growth of Pythium ultium and displayed moderate antifungal activity against Magnaphorthe grisea, Botrytis cinerea, and Trichophyton mentagrophytes. The other isolated compounds showed no antimicrobial activity.

새로운 사이클로프로필 뉴크레오사이드 유도체의 합성과 생리활성 (Synthesis of Novel Cyclopropyl Nucleoside Derivatives as Potential Antiherpetic Agent)

  • 강진아;천부순;문형룡
    • 약학회지
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    • 제56권4호
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    • pp.230-235
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    • 2012
  • Synthesis of novel cyclopropyl pyrimidine and purine nucleoside derivatives 2~8 with ${\alpha}$-configuration was successfully accomplished using an epoxide-ring opening reaction, lactonization, a hydroboration-oxidation reaction and a Mitsunobu reaction as the key steps. Antiviral activities against HSV-1 and -2, HIV-1 and -2, coxsackie B1and B3 viruses and poliovirus were assayed. Three compounds 4, 7 and 8 exhibit cytotoxicity-derived antiviral activity only in HIV-1 and -2.

Pleiotropic Effects of Caffeine Leading to Chromosome Instability and Cytotoxicity in Eukaryotic Microorganisms

  • Chung, Woo-Hyun
    • Journal of Microbiology and Biotechnology
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    • 제31권2호
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    • pp.171-180
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    • 2021
  • Caffeine, a methylxanthine analog of purine bases, is a compound that is largely consumed in beverages and medications for psychoactive and diuretic effects and plays many beneficial roles in neuronal stimulation and enhancement of anti-tumor immune responses by blocking adenosine receptors in higher organisms. In single-cell eukaryotes, however, caffeine somehow impairs cellular fitness by compromising cell wall integrity, inhibiting target of rapamycin (TOR) signaling and growth, and overriding cell cycle arrest caused by DNA damage. Among its multiple inhibitory targets, caffeine specifically interacts with phosphatidylinositol 3-kinase (PI3K)-related kinases causing radiosensitization and cytotoxicity via specialized intermediate molecules. Caffeine potentiates the lethality of cells in conjunction with several other stressors such as oxidants, irradiation, and various toxic compounds through largely unknown mechanisms. In this review, recent findings on caffeine effects and cellular detoxification schemes are highlighted and discussed with an emphasis on the inhibitory interactions between caffeine and its multiple targets in eukaryotic microorganisms such as budding and fission yeasts.

Phenanthrene Derivatives, 3,5-Dimethoxyphenanthrene-2,7-diol and Batatasin-I, as Non-Polar Standard Marker Compounds for Dioscorea Rhizoma

  • Yoon, Kee-Dong;Yang, Min-Hye;Nam, Sang-Il;Park, Ju-Hyun;Kim, Young-Choong;Kim, Jin-Woong
    • Natural Product Sciences
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    • 제13권4호
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    • pp.378-383
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    • 2007
  • Phenathrene derivatives, such as batatasins, are well-known constituents in Dioscorea Rhizoma. Although phenanthrenes have been reported as representative compounds in this plant, standard markers for quality control have been focused on the polar constituents (saponins and purine derivatives). Herein, simple, rapid and reliable HPLC method was developed to determine 3,5-dimethoxyphenanthrene-2,7-diol (DMP) and batatasin-I (BA-I) as non-polar standard maker compounds of Dioscorea Rhizoma. DMP and BA-I were analyzed under optimized HPLC conditions [column: Columbus $5{\mu}$ C18 100A ($30{\times}4.6mm$ i.d., $5{\mu}m$; mobile phase: $H_2O$ with 0.025% $CH_3COOH$ (v/v) for solvent A and $CH_3CN$ with 0.025% $CH_3COOH$ (v/v) for solvent B, gradient elution; flow rate: 2 mL/min; detection: 260 nm), and each experiment was finished within 13 min. Good linearity was achieved in the range from 0.5 to $10.0{\mu}g/mL$ for each compound, and intra- and inter-day precision were in the acceptable levels. The recovery test were performed with three different Dioscorea Rhizoma samples (D. opposita, D. batatas and D. japonica), and showed its accuracy values in the range of 97.2 - 102.8% for three different concentrations of DMP and BA-I. The content levels of DMP and BA-I were ranged under 0.0020%. These results demonstrated that amounts of DMP and BA-I are easily determined with conventional HPLC-UV-DAD method although the content levels were lower than those of saponins and allantoin in Dioscorea Rhizoma. This HPLC method could be used for quality control of various Dioscorea preparations.

알데히드 옥시다제의 활성에 미치는 리도카인 및 프로카인아미드의 영향 (The Effect of Lidocaine and Procainamide on the Hepatic Aldehyde Oxidase Activity)

  • 허근;김진숙;김대경;하은필;이상일;용철순
    • 약학회지
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    • 제43권6호
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    • pp.756-761
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    • 1999
  • Lipid peroxidation mediated by hydroxyl radicals which are generated during myocardial ischermia has suggested as a possible mechanism of ischemic myocardial damage. Recently, it has been reported that anti-arrhythmic action of lidocaine, a local anesthetic, is attributed to its "membrane-stabilizing" properties through scavenging free radicals, thus, inhibiting lipid peroxidation. Aldehyde oxidase and xanthine oxidase which catalyze the oxidation of many purine, pyrimidine and pteridine derivatives are known as free radical generating systems. In this experiment, we studied the effect of lidocaine and procainamide on the hepatic aldehyde and xanthine oxidase activity and antioxidative activities. It was found that lidocaine and procainamide inhibited both NADPH-dependent and independent lipid peroxidation. Both of tested compounds were found to be ineffective in inhibiting xanthine oxidase. Lidocaine and procainamide, however, inhibited aldehyde oxidase activity in vitro as well as in vivo. Based on the above results, lidocaine and procainamide could be employed as a therapeutic agent for aldehyde oxidaserelated disease.d disease.

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Dendropanax morbifera and Rubus coreanus Miq. Extracts Inhibits the Formation of Uric Acid Crystal by Reducing Xanthine Oxidase Activity

  • Hurh, Joon;Simu, Shakina Yesmin;Han, Yaxi;Ahn, Jong-Chan;Yang, Deok-Chun
    • 한국자원식물학회:학술대회논문집
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    • 한국자원식물학회 2018년도 춘계학술발표회
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    • pp.95-95
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    • 2018
  • Uric acid is the end product of purine metabolism in human body, originating from hypoxanthine after enzyme catalysis by Xanthine oxidase (XOD). Hyperuricemia results as a result of either over-generation of uric acid or a reduction in its excretion. In silico modelling methods such as Absorption, Distribution, Metabolism, Excretion and Toxicity (ADMET) prediction, Autodock 4.2.6 program were used to study the potential inhibitory compounds of XOD. Also we investigated the inhibition of XOD activity by using the extracts of Dendropanax morbifera and Rubus coreanus Miq spectrophotometrically. According to ADMET data, several compounds from D. morbifera and R. coreanus plants, were found to be more potent in inhibiting the XOD activity than allopurinol. XOD inhibitory activity is evaluated by quantifying the formation of uric acid by measuring the absorbance at 290 m ($A_{290}$).D. morbifera extract inhibited XOD activity at $250{\mu}g/ml$, however the extracts from R. coreanus has inhibited XOD activity at $25{\mu}g/ml$. The major compound of R. coreanus, ellagic acid significantly increased the inhibition rate from $9{\mu}g/ml$ and showed a 71% suppression rate at $15{\mu}g/ml$. Finally, these results suggested a potential inhibitory activities of the extracts from D. morbifera and R. coreanus Miq, but further research is needed to validate to ensure their safe usage as drug.

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미생물에 의한 5′-이노신산의 생산에 관한 연구 (제1보) 5′-이노신산 생산균주의 분리 (Studies on the Fermentative Production of Inosine-5′-monophosphate by Microorganisms (Part 1) Derivation of 5′-IMP Producing Mutants from Brevibacterium ammoniagenes)

  • 배종찬;공운영;손충홍;장욱;유주현
    • 한국미생물·생명공학회지
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    • 제7권3호
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    • pp.119-125
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    • 1979
  • (l) 핵산관련물질 생산균주의 분리를 위한 변이 유기제와 최적 처리조건은 UV; 30 cm, 1 min, NTG; 200 $\mu\textrm{g}$/ml, 20min, DES; 0.32 %, 90 min, EMS; 5%, 60 min 이었으며 이때 변이솔는 각각 0.083 %, 0.67%, 1.1 %, 및 0.45%로 DES가 가장 양호하였다. (2) Purine 영양요구변이주 239 strain 중 5'-IMP 생산균주는 모두 6 strain이었으며 이중 adenine-guanine 동시요구주 D-2150이 4.8mg/ml로 가장 우수하였다. (3) D-21530 strain의 배양액에서 얻은 결정을 paper chromatogram의 Rf치, 자외선 및 적외선 흡수 spectum 비교, 가수분해에 의한 hypoxanthine 생성량 및 orcinol 반응에 의한 D-ribose의 생성량을 검토한 결과 5'-IMP로 동정되었다. 이 연구을 할때 협력하여 주신 제일제당주식회사 김홍집 상무, 그리고 핵산의 정량분석을 하여준 문화식 씨에게 감사드립니다.

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