coumarins

Summary

Summary: Synthetic or naturally occurring substances related to coumarin, the delta-lactone of coumarinic acid. The various coumarins have a wide range of proposed actions and uses including as ANTICOAGULANTS, pharmaceutical aids, indicators and reagents, photoreactive substances, and ANTINEOPLASTIC AGENTS.

Top Publications

  1. ncbi The structure and pharmacological functions of coumarins and their derivatives
    Longhuo Wu
    Engineering Research Center of Molecular Medicine, Ministry of Education, Huaqiao University Main Campus, Quanzhou, China 362021
    Curr Med Chem 16:4236-60. 2009
  2. ncbi Antioxidant activities of coumarins from Korean medicinal plants and their structure-activity relationships
    Phuong Thien Thuong
    College of Pharmacy, Chungnam National University, Daejeon 305 764, Korea
    Phytother Res 24:101-6. 2010
  3. ncbi Anti-oxidative and photo-protective effects of coumarins isolated from Fraxinus chinensis
    Bum Chun Lee
    College of Pharmacy, Chungbuk National University, Cheongju 361 763, Korea
    Arch Pharm Res 30:1293-301. 2007
  4. ncbi Neuroprotective effects of osthole pretreatment against traumatic brain injury in rats
    Yalong He
    Department of Neurosurgery, Xijing Institute of Clinical Neuroscience, Xijing Hospital, Fourth Military Medical University, No 127, ChangLe Western Road, Xi an, Shanxi 710032, China
    Brain Res 1433:127-36. 2012
  5. pmc Novobiocin and coumermycin inhibit DNA supercoiling catalyzed by DNA gyrase
    M Gellert
    Proc Natl Acad Sci U S A 73:4474-8. 1976
  6. ncbi Coumarins: old compounds with novel promising therapeutic perspectives
    M E Riveiro
    Laboratorio de Patología y Farmacología Molecular, Instituto de Biologia y Medicina Experimental, Vuelta de Obligado 2490 C1428DN, Buenos Aires, Argentina
    Curr Med Chem 17:1325-38. 2010
  7. ncbi Metabolism of coumarin by human P450s: a molecular modelling study
    David F V Lewis
    School of Biomedical and Molecular Sciences, University of Surrey, Stag Hill, Guildford, Surrey GU2 7XH, UK
    Toxicol In Vitro 20:256-64. 2006
  8. ncbi Enhanced electrostatic interaction between chitosan-modified PLGA nanoparticle and tumor
    Rui Yang
    Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151 742, Republic of Korea
    Int J Pharm 371:142-7. 2009
  9. ncbi Liposomal formulations of Etoposide and Docetaxel for p53 mediated enhanced cytotoxicity in lung cancer cell lines
    Kaustubh A Jinturkar
    Pharmacy Department, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Post Box No 51, Kalabhavan, Vadodara 390 001, Gujarat State, India
    Biomaterials 33:2492-507. 2012
  10. ncbi Effects of (-) mammea A/BB isolated from Calophyllum brasiliense leaves and derivatives on mitochondrial membrane of Leishmania amazonensis
    M A Brenzan
    Pós doutoranda em Ciências Farmacêuticas, Departamento de Farmácia e Farmacologia, Universidade Estadual de Maringa, Av Colombo 5790, 87020 900 Maringa, PR, Brazil
    Phytomedicine 19:223-30. 2012

Detail Information

Publications385 found, 100 shown here

  1. ncbi The structure and pharmacological functions of coumarins and their derivatives
    Longhuo Wu
    Engineering Research Center of Molecular Medicine, Ministry of Education, Huaqiao University Main Campus, Quanzhou, China 362021
    Curr Med Chem 16:4236-60. 2009
    b>Coumarins are of many different structures...
  2. ncbi Antioxidant activities of coumarins from Korean medicinal plants and their structure-activity relationships
    Phuong Thien Thuong
    College of Pharmacy, Chungnam National University, Daejeon 305 764, Korea
    Phytother Res 24:101-6. 2010
    The aim of this work was to study the structure-activity relationships of the antioxidant activity of natural coumarins isolated from four Korean medicinal plants (1-17) and four purchased coumarins (18-21)...
  3. ncbi Anti-oxidative and photo-protective effects of coumarins isolated from Fraxinus chinensis
    Bum Chun Lee
    College of Pharmacy, Chungbuk National University, Cheongju 361 763, Korea
    Arch Pharm Res 30:1293-301. 2007
    ..From these results, FCE and one of its components, esculetin, were predicted to be potentially useful as ingredients in cosmetics for protecting against photoaging...
  4. ncbi Neuroprotective effects of osthole pretreatment against traumatic brain injury in rats
    Yalong He
    Department of Neurosurgery, Xijing Institute of Clinical Neuroscience, Xijing Hospital, Fourth Military Medical University, No 127, ChangLe Western Road, Xi an, Shanxi 710032, China
    Brain Res 1433:127-36. 2012
    ..In summary, these results suggested that osthole had a neuroprotective effect against TBI, and the protection may be associated with its antioxidative and antiapoptotic functions...
  5. pmc Novobiocin and coumermycin inhibit DNA supercoiling catalyzed by DNA gyrase
    M Gellert
    Proc Natl Acad Sci U S A 73:4474-8. 1976
    ..We conclude that DNA gyrase controls the supercoiling of DNA in E. coli...
  6. ncbi Coumarins: old compounds with novel promising therapeutic perspectives
    M E Riveiro
    Laboratorio de Patología y Farmacología Molecular, Instituto de Biologia y Medicina Experimental, Vuelta de Obligado 2490 C1428DN, Buenos Aires, Argentina
    Curr Med Chem 17:1325-38. 2010
    Natural as well as synthetic coumarins have recently drawn much attention due to its broad pharmacological activities...
  7. ncbi Metabolism of coumarin by human P450s: a molecular modelling study
    David F V Lewis
    School of Biomedical and Molecular Sciences, University of Surrey, Stag Hill, Guildford, Surrey GU2 7XH, UK
    Toxicol In Vitro 20:256-64. 2006
    ....
  8. ncbi Enhanced electrostatic interaction between chitosan-modified PLGA nanoparticle and tumor
    Rui Yang
    Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151 742, Republic of Korea
    Int J Pharm 371:142-7. 2009
    ....
  9. ncbi Liposomal formulations of Etoposide and Docetaxel for p53 mediated enhanced cytotoxicity in lung cancer cell lines
    Kaustubh A Jinturkar
    Pharmacy Department, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Post Box No 51, Kalabhavan, Vadodara 390 001, Gujarat State, India
    Biomaterials 33:2492-507. 2012
    ..The study opens up a new strategy to treat lung cancer especially in cases of drug resistance. Moreover direct delivery to lung may provide an important role in complete remission of the disease due to target specificity...
  10. ncbi Effects of (-) mammea A/BB isolated from Calophyllum brasiliense leaves and derivatives on mitochondrial membrane of Leishmania amazonensis
    M A Brenzan
    Pós doutoranda em Ciências Farmacêuticas, Departamento de Farmácia e Farmacologia, Universidade Estadual de Maringa, Av Colombo 5790, 87020 900 Maringa, PR, Brazil
    Phytomedicine 19:223-30. 2012
    ..In addition, the compound (3) may be acting to depolarize the mitochondrial membrane potential of the cells, leading to death of the parasite...
  11. pmc The plant coumarins auraptene and lacinartin as potential multifunctional therapeutic agents for treating periodontal disease
    Annie Marquis
    Groupe de Recherche en Ecologie Buccale, Faculte de Medecine Dentaire, Universite Laval, 2420 Rue de la Terrasse, Quebec City, QC, Canada
    BMC Complement Altern Med 12:80. 2012
    ..In the present study, we evaluated the effect of auraptene and lacinartin, two natural oxyprenylated coumarins, on the growth, adherence properties, and collagenase activity of Porphyromonas gingivalis...
  12. ncbi The 43-kilodalton N-terminal fragment of the DNA gyrase B protein hydrolyzes ATP and binds coumarin drugs
    J A Ali
    Department of Biochemistry, University of Leicester, U K
    Biochemistry 32:2717-24. 1993
    ..The implications of these results with respect to the mechanism of supercoiling by DNA gyrase and the inhibition of gyrase by coumarin drugs are discussed...
  13. ncbi Toxicology and risk assessment of coumarin: focus on human data
    Klaus Abraham
    Federal Institute for Risk Assessment BfR, 14195 Berlin, Germany
    Mol Nutr Food Res 54:228-39. 2010
    ..Heavy consumers of cassia cinnamon may reach a daily coumarin intake corresponding to the TDI...
  14. ncbi A crystal structure of the bifunctional antibiotic simocyclinone D8, bound to DNA gyrase
    Marcus J Edwards
    Department of Biological Chemistry, John Innes Centre, Colney, Norwich NR4 7UH, UK
    Science 326:1415-8. 2009
    ..Our results should facilitate the design of drug molecules that target these unexploited binding pockets...
  15. ncbi Praeruptorin D and E attenuate lipopolysaccharide/hydrochloric acid induced acute lung injury in mice
    Peng Jiu Yu
    School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China
    Eur J Pharmacol 710:39-48. 2013
    ..Taken together, these results suggested that PD and PE might be useful in the therapy of lung injury...
  16. ncbi Poly(lactide)-vitamin E derivative/montmorillonite nanoparticle formulations for the oral delivery of Docetaxel
    Si Shen Feng
    Department of Chemical and Biomolecular Engineering, National University of Singapore, Block E5, 02 11, 4 Engineering Drive 4, Singapore 117576, Singapore
    Biomaterials 30:3297-306. 2009
    ..59% for Taxotere((R)) to 78% for the PLA-TPGS/MMT NP formulation and 91% for the PLA-TPGS NP formulation respectively. Oral chemotherapy by nanoparticles of biodegradable polymers is feasible...
  17. ncbi Lactoferrin-conjugated PEG-PLA nanoparticles with improved brain delivery: in vitro and in vivo evaluations
    Kaili Hu
    Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, 200032, People s Republic of China
    J Control Release 134:55-61. 2009
    ..Cell viability experiment results confirmed good safety of the biodegradable Lf-NP. The significant in vitro and in vivo results suggest that Lf-NP is a promising brain drug delivery system with low toxicity...
  18. ncbi Accumulation of coumarins in Arabidopsis thaliana
    Kosuke Kai
    Institute for Chemical Research, Kyoto University, Gokasho, Uji, Kyoto 611 0011, Japan
    Phytochemistry 67:379-86. 2006
    The biosynthesis of coumarins in plants is not well understood, although these metabolic pathways are often found in the plant kingdom. We report here the occurrence of coumarins in Arabidopsis thaliana ecotype Columbia...
  19. ncbi Lung-specific delivery of paclitaxel by chitosan-modified PLGA nanoparticles via transient formation of microaggregates
    Rui Yang
    National Research Laboratory for Transporters Targeted Drug Design, College of Pharmacy, Seoul National University, Seoul 151 742, Korea
    J Pharm Sci 98:970-84. 2009
    ....
  20. ncbi Cationic albumin-conjugated pegylated nanoparticles as novel drug carrier for brain delivery
    Wei Lu
    Department of Pharmaceutics, School of Pharmacy, Fudan University Fenglin Campus, Shanghai 200032, People s Republic of China
    J Control Release 107:428-48. 2005
    ..The significant results in vitro and in vivo showed that CBSA-NP was a promising brain drug delivery carrier with low toxicity...
  21. ncbi Antitumor effects of Osthol from Cnidium monnieri: an in vitro and in vivo study
    Szu Yuan Chou
    Department of Obstetrics and Gynecology, Taipei Medical University Wan Fang Medical Center, Taipei, Taiwan
    Phytother Res 21:226-30. 2007
    ..formosanum Yabe of Taiwan's endemic plants contained little osthol, with no imperatorin, and its major components were different from that of C. monnieri. Therefore, it is suggested that C. formosanum also may possess economic worth...
  22. ncbi Structural insights into hydroxycoumarin-induced apoptosis in U-937 cells
    Maria E Riveiro
    Laboratorio de Radioisotopos, Facultad de Farmacia y Bioquimica, Argentina
    Bioorg Med Chem 16:2665-75. 2008
    ..The dihydroxylated coumarins, 7,8-dihydroxy-coumarin and esculetin, induced DNA fragmentation as well as characteristic morphological changes ..
  23. ncbi Antiproliferative effect of isopentenylated coumarins on several cancer cell lines
    S Kawaii
    Laboratory of Bio-organic Chemistry, Tokyo Denki University, Hatoyama, Saitama, Japan
    Anticancer Res 21:1905-11. 2001
    33 coumarins, mainly the simple isopentenylated coumarins and derived pyrano- and furanocoumarins, were examined for their antiproliferative activity towards several cancer and normal human cell lines...
  24. ncbi Hair growth promoting activity of Eclipta alba in male albino rats
    R K Roy
    Department of Pharmaceutical Sciences, Dr HS Gour University, Sagar, MP, India
    Arch Dermatol Res 300:357-64. 2008
    ..The result of treatment with 2 and 5% petroleum ether extracts were better than the positive control minoxidil 2% treatment...
  25. ncbi Cytotoxic effects of mammea type coumarins from Calophyllum brasiliense
    Ricardo Reyes-Chilpa
    Instituto de Quimica, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria, Delagación Coyoacan México D F 04510, Mexico
    Life Sci 75:1635-47. 2004
    ..The organic extracts from the leaves yielded coumarins of the mammea type: mammea A/BA, A/BB, B/BA, B/BB, C/OA, C/OB, B/BA cyclo F, B/BB cyclo F, and isomammeigin...
  26. ncbi Biflavanones, diterpenes, and coumarins from the roots of Stellera chamaejasme L
    Zhi Hong Jiang
    School of Pharmaceutical Sciences, Nagasaki University, Japan
    Chem Pharm Bull (Tokyo) 50:137-9. 2002
    ..coumarin glycoside (3), along with six lignans, two phenylpropanoids, five flavonoids, two diterpenes, and three coumarins were isolated from the roots of Stellera chamaejasme L. (Thymelaeaceae)...
  27. ncbi Synthetic and natural coumarins as cytotoxic agents
    Irena Kostova
    Department of Chemistry, Faculty of Pharmacy, Medical University, 2 Dunav St, Sofia 1000, Bulgaria
    Curr Med Chem Anticancer Agents 5:29-46. 2005
    b>Coumarins, an old class of compounds, are naturally occurring benzopyrene derivatives. A lot of coumarins have been identified from natural sources, especially green plants...
  28. ncbi Praeruptorin A inhibits lipopolysaccharide-induced inflammatory response in murine macrophages through inhibition of NF-κB pathway activation
    Peng Jiu Yu
    School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China
    Phytother Res 25:550-6. 2011
    ..Taken together, the results suggest that PA may exert antiinflammatory effects in vitro in LPS-stimulated RAW 264.7 macrophages through inhibition of NF-κB signal pathway activation...
  29. pmc Anticonvulsant activity of a nonpeptide galanin receptor agonist
    Külliki Saar
    Department of Neurochemistry and Neurotoxicology, Stockholm University, SE 10691 Stockholm, Sweden
    Proc Natl Acad Sci U S A 99:7136-41. 2002
    ..These findings introduce a systemically active nonpeptide galanin agonist anticonvulsant...
  30. ncbi Osthole improves aspects of spatial performance in ovariectomized rats
    Ming Tsuen Hsieh
    Institute of Chinese Pharmaceutical Sciences, China Medical University, Taichung, 404, Taiwan, R O C
    Am J Chin Med 32:11-20. 2004
    ..The action mechanism of the effects of osthole on performance deficits was related to the estrogen-like properties and activating the central cholinergic neuronal system...
  31. ncbi Effect of oral antiplatelet agents on major bleeding in users of coumarins
    Tom Schalekamp
    Division of Pharmacoepidemiology and Pharmacotherapy, Utrecht Institute for Pharmaceutical Sciences, Faculty of Science, Utrecht University, Utrecht, The Netherlands
    Thromb Haemost 100:1076-83. 2008
    Treatment with vitamin K antagonists (coumarins) is associated with an increased risk of bleeding...
  32. ncbi Coumarin-derived Cu(2+)-selective fluorescence sensor: synthesis, mechanisms, and applications in living cells
    Hyo Sung Jung
    Department of Chemistry, Korea University, Seoul 136 701, Korea
    J Am Chem Soc 131:2008-12. 2009
    ..The results indicate that 1 should be useful for the fluorescence microscopic imaging and the study on the biological functions of Cu(2+)...
  33. ncbi Chromones and coumarins from the dried fructus of Cnidium monnieri
    Jianyu Zhao
    Center for Natural Products Research, Chengdu Institute of Biology of the Chinese Academy of Sciences, P R China
    Fitoterapia 82:767-71. 2011
    ..on the ethanolic extract of the dried fructus of Cnidium monnieri offered three chromones and eight coumarins. Among them, a new chromone and a new coumarin were identified and elucidated as 5,7-dihydroxy-6-[(2Z)-4-(β-d-..
  34. ncbi [Comparative studies on pharmacological effects of the main chemical constituents of Peucedanum praeruptorum from He'nan and Jiangxi]
    Cun Zhang
    Institute of Chinese Materia Medica, China Academy of Traditional Chinese Medicine, Beijing 100700, China
    Zhongguo Zhong Yao Za Zhi 30:1356-8. 2005
    ..To compare the pharmacological effect of the main coumarin constituents of Peucedanum praeruptorum from Jiangxi and He'nan...
  35. ncbi A review on coumarins as acetylcholinesterase inhibitors for Alzheimer's disease
    Preet Anand
    Department of Chemistry, Punjabi University, Patiala 147002, Punjab, India
    Bioorg Med Chem 20:1175-80. 2012
    ..b>Coumarins are the phytochemicals with wide range of biological activities including AChE inhibition...
  36. ncbi Single-dose methoxsalen effects on human cytochrome P-450 2A6 activity
    E D Kharasch
    Department of Anesthesiology, University of Washington, Seattle 98195, USA
    Drug Metab Dispos 28:28-33. 2000
    ..Alternative doses, timing, and/or routes of methoxsalen administration are required for greater, longer, and more reproducible CYP2A6 inhibition than that provided by single-dose methoxsalen...
  37. ncbi Wedelolactone inhibits adipogenesis through the ERK pathway in human adipose tissue-derived mesenchymal stem cells
    Seyoung Lim
    School of Nano Bioscience and Chemical Engineering, Ulsan National Institute of Science and Technology, Ulsan, Republic of Korea
    J Cell Biochem 113:3436-45. 2012
    ..Taken together, these results indicate that wedelolactone inhibits adipogenic differentiation through ERK pathway and suggest a novel inhibitory effect of wedelolactone on adipogenic differentiation in hAMSCs...
  38. ncbi Osthole attenuates focal inflammatory reaction following permanent middle cerebral artery occlusion in rats
    Fei Li
    School of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
    Biol Pharm Bull 35:1686-90. 2012
    ..The present study demonstrated that osthole may be a novel neuroprotective therapy in the treatment of focal ischemic stroke...
  39. ncbi Stereoselective metabolism of (±)-praeruptorin A, a calcium channel blocker from Peucedani Radix, in pooled liver microsomes of rats and humans
    Y L Song
    State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macao SAR, China
    Xenobiotica 42:231-7. 2012
    ..Both enantiomers were eliminated faster in RLMs than in HLMs, while lPA showed greater species difference. PA enantiomers exhibited stereoselective metabolism in RLMs and HLMs, implying chiral discrimination in their actions...
  40. ncbi Alkaloid and coumarins from the green fruits of Aegle marmelos
    Suda Chakthong
    Department of Chemistry, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla 90112, Thailand
    Phytochemistry 75:108-13. 2012
    ..Antifungal and antibacterial activities of selected compounds were also evaluated...
  41. ncbi (+/-)-3'-O, 4'-O-dicynnamoyl-cis-khellactone, a derivative of (+/-)-praeruptorin A, reverses P-glycoprotein mediated multidrug resistance in cancer cells
    XiaoLing Shen
    Bioactive Products Research Group, Department of Biology and Chemistry, City University of Hong Kong, Hong Kong SAR, China
    Bioorg Med Chem 14:7138-45. 2006
    ..These results suggest that DCK could bind simultaneously with substrates to Pgp but perhaps at an allosteric site and thus affect Pgp-substrate interactions...
  42. ncbi The neuroprotective effect of praeruptorin C against NMDA-induced apoptosis through down-regulating of GluN2B-containing NMDA receptors
    Le Yang
    Department of Pharmacology, School of Pharmacy, The Fourth Military Medical University, Xi an, Shaanxi Province 710032, PR China
    Toxicol In Vitro 27:908-14. 2013
    ..These findings suggest that Pra-C partially protects cortical neurons by inhibiting the expression of GluN2B-containing NMDA receptors and regulating the Bcl-2 family...
  43. ncbi Osthole protects lipopolysaccharide-induced acute lung injury in mice by preventing down-regulation of angiotensin-converting enzyme 2
    Yun Shi
    Department of Pathology and Pathophysiology, Fourth Military Medical University, Xi an 710032, PR China
    Eur J Pharm Sci 48:819-24. 2013
    ..ACE2 inhibitor blocked the protective effect of osthole in NR 8383 cell lines. Taken together, our study showed that osthole improved survival rate and attenuated LPS-induced ALI and ACE2 may play a role in it...
  44. ncbi Osthol, a coumarin isolated from common cnidium fruit, enhances the differentiation and maturation of osteoblasts in vitro
    Lei Guo Ming
    Institute of Orthopaedics, Lanzhou General Hospital, Lanzhou Command of CPLA, Lanzhou, China
    Pharmacology 88:33-43. 2011
    ....
  45. ncbi Xenobiotic reductase A in the degradation of quinoline by Pseudomonas putida 86: physiological function, structure and mechanism of 8-hydroxycoumarin reduction
    Julia J Griese
    Laboratorium Proteinkristallographie, Universitat Bayreuth, Germany
    J Mol Biol 361:140-52. 2006
    ..putida strains unable to degrade quinoline, it appears to have more than one physiological function and is an example of how enzymes with low substrate specificity can help to explain the variety of degradation pathways possible...
  46. ncbi Compounds from Wedelia chinensis synergistically suppress androgen activity and growth in prostate cancer cells
    Feng Min Lin
    Agricultural Biotechnology Research Center, Academia Sinica, 128 Academia Road, Sec 2, Nan Kang, Taipei 11529, Taiwan
    Carcinogenesis 28:2521-9. 2007
    ..The paradigm of multiple activities and synergism is a useful framework to investigate the therapeutic effects of whole extracts from assorted medicinal plant species...
  47. pmc A multifunctional bioconjugate module for versatile photoaffinity labeling and click chemistry of RNA
    Stefanie Kellner
    Institute of Pharmacy and Biochemistry, Johannes Gutenberg University Mainz, Staudinger Weg 5, D 55128 Mainz, Germany
    Nucleic Acids Res 39:7348-60. 2011
    ..Alternatively, the azide function can be used for further derivatization by click-chemistry. This allows e.g. the introduction of an additional fluorophore for excitation with visible light...
  48. ncbi VKORC1: molecular target of coumarins
    J Oldenburg
    Institute for Experimental Haematology and Transfusion Medicine, University Clinic Bonn, Bonn, Germany
    J Thromb Haemost 5:1-6. 2007
    ..VKORC1 is the key enzyme of the vitamin K cycle and the molecular target of coumarins, which represent the most commonly prescribed drugs for therapy and prevention of thromboembolic conditions...
  49. ncbi The use of coumarins as environmentally-sensitive fluorescent probes of heterogeneous inclusion systems
    Brian D Wagner
    Department of Chemistry, University of Prince Edward Island, Charlottetown, PE, Canada
    Molecules 14:210-37. 2009
    b>Coumarins, as a family of molecules, exhibit a wide range of fluorescence emission properties...
  50. ncbi Inhibitory effect of oxycoumarins isolated from the Thai medicinal plant Clausena guillauminii on the inflammation mediators, iNOS, TNF-alpha, and COX-2 expression in mouse macrophage RAW 264.7
    Tomonori Nakamura
    Department of Molecular Pharmacology and Pharmacotherapeutics, Graduate School of Pharmaceutical Sciences, Chiba University, Chiba, 260 8675, Japan
    J Nat Med 63:21-7. 2009
    ..It was expected that these compounds show anti-inflammatory activities...
  51. pmc Converging pharmacological and genetic evidence indicates a role for steroid sulfatase in attention
    William Davies
    Behavioural Genetics Group, School of Psychology and Department of Psychological Medicine, School of Medicine, University of Cardiff, London, United Kingdom
    Biol Psychiatry 66:360-7. 2009
    ..Preliminary work in mice and humans has suggested the X-linked gene STS (which encodes the enzyme steroid sulfatase) as a mediator of attentional functioning and as a candidate gene for ADHD...
  52. ncbi Anticonvulsant and acute neurotoxic effects of imperatorin, osthole and valproate in the maximal electroshock seizure and chimney tests in mice: a comparative study
    Jarogniew J Luszczki
    Department of Pathophysiology, Medical University of Lublin, Jaczewskiego 8, PL 20 090 Lublin, Poland
    Epilepsy Res 85:293-9. 2009
    ....
  53. ncbi Osthole suppresses fatty acid synthase expression in HER2-overexpressing breast cancer cells through modulating Akt/mTOR pathway
    Victor Chia Hsiang Lin
    Department of Urology, E Da Hospital, Department of Nursing, I Shou University, Kaohsiung, Taiwan
    J Agric Food Chem 58:4786-93. 2010
    ..These results suggested that osthole has the potential to advance as chemopreventive or chemotherapeutic agent for cancers that overexpress HER2...
  54. ncbi Inhibitory effects of coumarins from the stem barks of Fraxinus rhynchophylla on adipocyte differentiation in 3T3-L1 cells
    Eunjin Shin
    College of Pharmacy, Chungbuk National University, Cheongju, Korea
    Biol Pharm Bull 33:1610-4. 2010
    ..Activity-guided fractionation led to the isolation of six coumarins such as esculetin (1), scopoletin (2), fraxetin (3), fraxidin (4) esculin (5) and fraxin (6)...
  55. ncbi Evaluation of auraptene content in citrus fruits and their products
    K Ogawa
    Department of Citriculture, National Institute of Fruit Tree Science, Ministry of Agriculture, Forestry and Fisheries, Okitsu, Shimizu, Shizuoka 424 0292, Japan
    J Agric Food Chem 48:1763-9. 2000
    ..49 mg/g) and in the juice sac (1.73 mg/g). Citrus fruit products, for example, brand-named grapefruit juice and marmalade, retain about 0. 1 mg and 0.3 mg/100 g of auraptene, respectively...
  56. ncbi Coumarins and carbazoles from Clausena excavata exhibited antimycobacterial and antifungal activities
    Arunrat Sunthitikawinsakul
    Planta Med 69:155-7. 2003
    Four known coumarins, dentatin (1), nor-dentatin (2), clausenidin (3) and xanthoxyletin (5), and six known carbazole derivatives, 3-formylcarbazole (6), mukonal (7), 3-methoxycarbonylcarbazole (8), murrayanine (9), 2-hydroxy-3-formyl-7-..
  57. ncbi Antimicrobial and antioxidant activities of coumarins from the roots of Ferulago campestris (Apiaceae)
    Adriana Basile
    Dipartimento delle Scienze Biologiche, Sezione di Biologia Vegetale, Universita Federico II, Via Foria 223, 80139 Napoli, Italy
    Molecules 14:939-52. 2009
    We report the isolation of several coumarins and the stereochemical assessment of some pyranocoumarins, as well as the antibacterial and antioxidant activities of the three most abundant ones (grandivittin, agasyllin and aegelinol ..
  58. ncbi Inhibition of topoisomerase IIα: novel function of wedelolactone
    Petr Benes
    Department of Experimental Biology, Faculty of Science, Masaryk University, Czech Republic
    Cancer Lett 303:29-38. 2011
    ..Wedelolactone interacted with dsDNA and inhibited the activity of DNA topoisomerase IIα. We conclude that wedelolactone can act as growth suppressor independently of NFκB and androgen receptors...
  59. ncbi Auraptene: a natural biologically active compound with multiple targets
    Salvatore Genovese
    Dipartimento di Scienze del Farmaco, Università G d Annunzio di Chieti Pescara, Via dei Vestini 31, Chieti Scalo CH, Italy
    Curr Drug Targets 12:381-6. 2011
    ....
  60. ncbi Brain delivery property and accelerated blood clearance of cationic albumin conjugated pegylated nanoparticle
    Wei Lu
    Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, 200032, People s Republic of China
    J Control Release 118:38-53. 2007
    ..Understanding these issues is important for the future development of CBSA-NP as a brain delivery carrier and for the attenuation of toxicity or immunological responses to the nanodevice following a consequence of nanomedication...
  61. pmc Simocyclinone D8, an inhibitor of DNA gyrase with a novel mode of action
    Ruth H Flatman
    Department of Biological Chemistry, John Innes Centre, Norwich Research Park, Colney, Norwich NR4 7UH, UK
    Antimicrob Agents Chemother 49:1093-100. 2005
    ..This is a novel mechanism for a gyrase inhibitor and presents new possibilities for antibacterial drug development...
  62. ncbi Osthole and imperatorin, the active constituents of Cnidium monnieri (L.) Cusson, facilitate glutamate release from rat hippocampal nerve terminals
    Su Jane Wang
    School of Medicine, Fu Jen Catholic University, Hsin Chuang, Taipei Hsien 24205, Taiwan
    Neurochem Int 53:416-23. 2008
    ..Together, these results suggest that osthole or imperatorin effects a facilitation of glutamate release from nerve terminals by positively modulating N-and P/Q-type Ca(2+) channel activation through a signaling cascade involving PKC...
  63. ncbi Inhibition of snake venoms and phospholipases A(2) by extracts from native and genetically modified Eclipta alba: isolation of active coumestans
    Luciana C Diogo
    Department of Biotechnology, University of Ribeirao Preto, Ribeirao Preto, Sao Paulo, Brazil
    Basic Clin Pharmacol Toxicol 104:293-9. 2009
    ..The search for antivenom is justified by the need of finding active principles that are more efficient in neutralizing snake venoms and also as an attempt to complement serum therapy...
  64. ncbi The cytotoxic properties of natural coumarins isolated from roots of Ferulago campestris (Apiaceae) and of synthetic ester derivatives of aegelinol
    Sergio Rosselli
    Dipartimento Chimica Organica E Paternò, Universita di Palermo, Viale delle Scienze, Parco d Orleasn II, 90128 Palermo, Italy
    Nat Prod Commun 4:1701-6. 2009
    Grandivittin (1), agasyllin (2), aegelinol benzoate (3) and felamidin (20), four natural coumarins isolated from Ferulago campestris, and several synthetic ester derivatives of aegelinol (4) were tested against four tumor cell lines...
  65. ncbi A safety assessment of coumarin taking into account species-specificity of toxicokinetics
    S P Felter
    The Procter and Gamble Company, Miami Valley Innovation Center, 11810 E Miami River Road, Cincinnati, OH 45252, USA
    Food Chem Toxicol 44:462-75. 2006
    ....
  66. ncbi Inhibition of gastric H+,K+-ATPase activity by flavonoids, coumarins and xanthones isolated from Mexican medicinal plants
    Ricardo Reyes-Chilpa
    Instituto de Quimica, Universidad Nacional Autonoma de Mexico, D F Mexico, Mexico
    J Ethnopharmacol 105:167-72. 2006
    ..the properties of some of their chemical constituents, four natural xanthones, an acetylated derivative, two coumarins (mammea A/BA and mammea C/OA) isolated from Calophyllum brasiliense Cambess and two flavonoids (minimiflorin and ..
  67. ncbi Isolation of 8'-phosphate ester derivatives of amicoumacins: structure-activity relationship of hydroxy amino acid moiety
    Makoto Hashimoto
    Reseach Institute of Pharmaceutical Sciences, Musashino University, Shinmachi, Nishitokyo, Tokyo, Japan
    J Antibiot (Tokyo) 60:752-6. 2007
    ..Comparison of the antibacterial activities against methicillin-resistant Staphylococcus aureus (MRSA) of these compounds suggested that C-8' hydroxyl and C-12' amide group of amicoumacin A played a critical role for anti-MRSA activity...
  68. ncbi Cytotoxic activity of coumarins from the fruits of Cnidium monnieri on leukemia cell lines
    Ling Ling Yang
    School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan, ROC
    Planta Med 69:1091-5. 2003
    ..Then, the CmF extract was subjected to silica gel column chromatography and recrystallization to give five coumarins: osthol, imperatorin, bergapten, isopimpinellin, and xanthotoxin...
  69. ncbi Cloning and analysis of the simocyclinone biosynthetic gene cluster of Streptomyces antibioticus Tü 6040
    Ute Galm
    Pharmazeutische Biologie, Pharmazeutisches Institut, Auf der Morgenstelle 8, 72076 Tubingen, Germany
    Arch Microbiol 178:102-14. 2002
    ..Feeding of the mutant with the aminocoumarin moiety of novobiocin led to a new, artificial simocyclinone derivative...
  70. ncbi Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK complex
    M Kobori
    Department of Cell Biology, Harvard Medical School, Boston, MA, USA
    Cell Death Differ 11:123-30. 2004
    ..We demonstrate that wedelolactone is an inhibitor of IKK, a kinase critical for activation of NF-kappaB by mediating phosphorylation and degradation of IkappaBalpha...
  71. ncbi Mass spectrometry reveals that the antibiotic simocyclinone D8 binds to DNA gyrase in a "bent-over" conformation: evidence of positive cooperativity in binding
    Marcus J Edwards
    Department of Biological Chemistry, John Innes Centre, Norwich Research Park, Colney, United Kingdom
    Biochemistry 50:3432-40. 2011
    ..This general approach will be applicable to other systems with multiple binding sites and highlights mass spectrometry's role as a powerful emerging tool for unraveling the complexities of biomolecular interactions...
  72. ncbi Preparation and brain delivery property of biodegradable polymersomes conjugated with OX26
    Zhiqing Pang
    Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 200032, PR China
    J Control Release 128:120-7. 2008
    ..v. administration. These results indicated that OX26(34)-PO is a promising carrier for peptide brain delivery...
  73. ncbi Increased bleeding risk with concurrent use of selective serotonin reuptake inhibitors and coumarins
    Tom Schalekamp
    Division of Pharmacoepidemiology and Pharmacotherapy, Utrecht Institute for Pharmaceutical Sciences, Faculty of Science, Utrecht University, Utrecht, The Netherlands
    Arch Intern Med 168:180-5. 2008
    Treatment with vitamin K antagonists (coumarins) is associated with an increased risk of bleeding...
  74. ncbi Osthole, a potential antidiabetic agent, alleviates hyperglycemia in db/db mice
    Hong Jen Liang
    Department of Food Science, Yuanpei University, Hsinchu, Taiwan
    Chem Biol Interact 181:309-15. 2009
    ..These results suggest that osthole can alleviate hyperglycemia and could be potentially developed into a novel drug for treatment of diabetes mellitus...
  75. ncbi Transferrin-conjugated nanoparticles of poly(lactide)-D-alpha-tocopheryl polyethylene glycol succinate diblock copolymer for targeted drug delivery across the blood-brain barrier
    Chee Wee Gan
    Department of Chemical and Biomolecular Engineering, National University of Singapore, Singapore
    Biomaterials 31:7748-57. 2010
    ..Moreover, our preliminary ex vivo biodistribution investigation demonstrated that although not as satisfactory, the Tf-conjugated PLA-TPGS NPs formulation could be able to deliver imaging/therapeutic agents across the BBB...
  76. ncbi Dietary administration with prenyloxycoumarins, auraptene and collinin, inhibits colitis-related colon carcinogenesis in mice
    Hiroyuki Kohno
    Department of Oncologic Pathology, Kanazawa Medical University, Uchinada, Ishikawa, Japan
    Int J Cancer 118:2936-42. 2006
    ..Our findings may suggest that certain prenyloxycoumarins, such as auraptene and collinin, could serve as an effective agent against colitis-related colon cancer development in rodents...
  77. ncbi Apoptogenic effect of 7,8-diacetoxy-4-methylcoumarin and 7,8-diacetoxy-4-methylthiocoumarin in human lung adenocarcinoma cell line: role of NF-kappaB, Akt, ROS and MAP kinase pathway
    Anita Goel
    Molecular Immunogenetics Laboratory, Institute of Genomics and Integrative Biology, Mall Road, Delhi 110007, India
    Chem Biol Interact 179:363-74. 2009
    Coumarin (1,2-benzopyrone) is a naturally occurring fragrant compound found in a variety of plants and spices. Coumarins have attracted intense interest in recent years because of their diverse pharmacological activities...
  78. ncbi Chemoprevention of 4-nitroquinoline 1-oxide-induced oral carcinogenesis by citrus auraptene in rats
    T Tanaka
    First Department of Pathology, Kanazawa Medical University, Uchinada, Ishikawa, Japan
    Carcinogenesis 19:425-31. 1998
    ....
  79. ncbi 7,8-Dihydroxy-4-methylcoumarin induces apoptosis of human lung adenocarcinoma cells by ROS-independent mitochondrial pathway through partial inhibition of ERK/MAPK signaling
    Anita Goel
    Molecular Immunogenetics Laboratory, Institute of Genomics and Integrative Biology, Mall Road, Delhi 110 007, India
    FEBS Lett 581:2447-54. 2007
    b>Coumarins have attracted intense interest in recent years because they have been identified from natural sources, especially green plants and have diverse pharmacological properties...
  80. ncbi Aggressive behavior induced by the steroid sulfatase inhibitor COUMATE and by DHEAS in CBA/H mice
    L B Nicolas
    , , Comportement, , , , France
    Brain Res 922:216-22. 2001
    ..These results confirm the correlation between aggressive behavior and STS concentration in mice. In addition, we confirm that the steroid metabolism can modulate the behavior in rodents...
  81. pmc Fluorescent single-stranded DNA binding protein as a probe for sensitive, real-time assays of helicase activity
    Mark S Dillingham
    DNA Protein Interactions Unit, Department of Biochemistry, School of Medical Sciences, University of Bristol, Bristol, United Kingdom
    Biophys J 95:3330-9. 2008
    ..Its use in the study of DNA manipulations involving ssDNA intermediates is demonstrated in assays for DNA unwinding, catalyzed by DNA helicases...
  82. pmc Biosynthetic gene cluster of simocyclinone, a natural multihybrid antibiotic
    A Trefzer
    Pharmazeutische Biologie, Albert Ludwigs Universitat Freiburg, 79104 Freiburg, Germany
    Antimicrob Agents Chemother 46:1174-82. 2002
    ..Production of simocyclinone D8 was clearly detectable in the wild-type strain but was not detectable in the mutant strains. This indicated that indeed the sim gene cluster had been cloned...
  83. ncbi Antibacterial activity of crude extracts from Mexican medicinal plants and purified coumarins and xanthones
    Kakuko Yasunaka
    Department of Microbiology and Immunology, School of Medicine, Fukuoka University, Nanakuma, Jonan ku, Fukuoka 814 0180, Japan
    J Ethnopharmacol 97:293-9. 2005
    ..Clusiaceae), and Mammea americana L. (Clusiaceae) were highly active against Staphylococcus aureus. Coumarins (mammea A/BA and mammea A/AA) and xanthones, namely jacareubin and 1,3,5,6-tetrahydroxy-2-(3,3-dimethylallyl) ..
  84. ncbi Antiproliferative effects of isopentenylated coumarins isolated from Phellolophium madagascariense Baker
    C Riviere
    Institut de Chimie Pharmaceutique Albert Lespagnol, EA2692, rue J Laguesse, BP 83, F 59006 Lille, France
    Nat Prod Res 20:909-16. 2006
    From the leaves of Phellolophium madagascariense Baker (Apiaceae), an endemic herb to Madagascar, three known coumarins (osthol, murraol and meranzin hydrate) have been isolated and identified...
  85. pmc In vitro anti-Helicobacter pylori activity of the probiotic strain Bacillus subtilis 3 is due to secretion of antibiotics
    I V Pinchuk
    , ENITA de Bordeaux, 33175 Gradignan Cedex, France
    Antimicrob Agents Chemother 45:3156-61. 2001
    ..An additive effect between amicoumacin A and the nonamicoumacin antibiotic against H. pylori was demonstrated...
  86. ncbi Calibrated automated thrombin generation measurement in clotting plasma
    H Coenraad Hemker
    Synapse BV, Cardiovascular Research Institute, University of Maastricht, Maastricht, The Netherlands
    Pathophysiol Haemost Thromb 33:4-15. 2003
    ....
  87. ncbi Structures of the TetR-like simocyclinone efflux pump repressor, SimR, and the mechanism of ligand-mediated derepression
    Tung B K Le
    Department of Molecular Microbiology, John Innes Centre, Norwich Research Park, Norwich NR4 7UH, UK
    J Mol Biol 408:40-56. 2011
    ....
  88. ncbi Attenuation of experimental autoimmune encephalomyelitis in C57 BL/6 mice by osthole, a natural coumarin
    Xiaohong Chen
    Department of Neurology, The Third Affiliated Hospital, Sun Yat Sen University, 600 Tianhe Road, Guangzhou, Guangdong 510630, China
    Eur J Pharmacol 629:40-6. 2010
    ..In addition, osthole blocked the reduction of NGF and suppressed IFN-gamma increase in EAE mice. These results suggested that osthole might be a new pharmacological approach to treat multiple sclerosis...
  89. ncbi Osthole-mediated cell differentiation through bone morphogenetic protein-2/p38 and extracellular signal-regulated kinase 1/2 pathway in human osteoblast cells
    Po Lin Kuo
    Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan, Taiwan
    J Pharmacol Exp Ther 314:1290-9. 2005
    ..In this study, we demonstrate that osthole is a promising agent for treating osteoporosis...
  90. ncbi Effects of osthole on migration and invasion in breast cancer cells
    Dapeng Yang
    Department of Developmental Genetics, Nanjing Medical University, China
    Biosci Biotechnol Biochem 74:1430-4. 2010
    ..This is the first report on the inhibitory function of Osthole in migration and invasion in breast cancer cells. Our findings indicate a need for further evaluation of Osthole in breast cancer chemotherapy and chemoprevention...
  91. ncbi Immunomodulatory and anti-inflammatory activity of selected osthole derivatives
    Michał Zimecki
    Department of Experimental Therapy, Institute of Immunology and Experimental Therapy, R Weigla str 12, 53 114, Wroclaw, Poland
    Z Naturforsch C 64:361-8. 2009
    ..5% and 68.3% inhibition, respectively). In summary, the compounds predominantly displayed suppressive and antiinflammatory activities in the investigated models...
  92. ncbi Platelet anti-aggregatory effects of coumarins from the roots of Angelica genuflexa and A. gigas
    Yong Yook Lee
    Natural Products Research Institute, Seoul National University, Seoul 110 460, Korea
    Arch Pharm Res 26:723-6. 2003
    Five coumarins, isoimperatorin (1), pabulenol (2), isooxypeucedanin (3), oxypeucedanin hydrate (4) and osthol (5) were isolated from the MeOH extract of Angelica genuflexa in the course of searching for anti-platelet and anti-coagulant ..
  93. ncbi Coupling of the biosynthesis and export of the DNA gyrase inhibitor simocyclinone in Streptomyces antibioticus
    Tung B K Le
    Department of Molecular Microbiology, John Innes Centre, Colney Lane, Norwich NR4 7UH, UK
    Mol Microbiol 72:1462-74. 2009
    ..In addition, an intermediate in the biosynthetic pathway, simocyclinone C4, which is essentially inactive as a DNA gyrase inhibitor, also induces simX expression in vivo and relieves simX repression by SimR in vitro...
  94. ncbi Citrus auraptene suppresses azoxymethane-induced colonic preneoplastic lesions in C57BL/KsJ-db/db mice
    Kei Hayashi
    Department of Surgical Oncology, Oncologic Pathology, Kanazawa Medical University, 1 1 Daigaku, Uchinada, Oshikawaa 020 0903, Japan
    Nutr Cancer 58:75-84. 2007
    ....
  95. pmc In vivo and in vitro patterns of the activity of simocyclinone D8, an angucyclinone antibiotic from Streptomyces antibioticus
    Lisa M Oppegard
    Department of Pharmacology, University of Minnesota Medical School Twin Cities, 6 120 Jackson Hall, 321 Church Street SE, Minneapolis, MN 55455, USA
    Antimicrob Agents Chemother 53:2110-9. 2009
    ....
  96. ncbi Antimicrobial coumarins from the stem bark of Afraegle paniculata
    Valerie Beatrice Tsassi
    Department of Organic Chemistry, Faculty of Science, University of Yaounde I, Yaounde, Cameroon
    Nat Prod Commun 5:559-61. 2010
    ..Preliminary studies indicated that compounds 2, 3, 5, and 7 showed potent antibacterial, fungicidal, and algicidal properties, while 6 showed only moderate algicidal property...
  97. ncbi Antiamoebic coumarins from the root bark of Adina cordifolia and their new thiosemicarbazone derivatives
    Prince Firdoos Iqbal
    Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India
    Eur J Med Chem 44:2252-9. 2009
    ..The compounds exhibit >80% viability at 3.125-200 microg/ml. It is apparent from these results that umbelliferone and skimmin may be a useful lead for the development of new antiamoebic drugs...
  98. ncbi Transport and metabolism of (±)-praeruptorin A in Caco-2 cell monolayers
    W H Jing
    Institute of Chinese Medical Sciences, University of Macau, Taipa, Macau, China
    Xenobiotica 41:71-81. 2011
    ..In summary, PA enantiomers were rapidly transported across Caco-2 cells and partially hydrolyzed by carboxylesterases during permeation. These findings provide mechanistic understanding of in vivo pharmacokinetic properties of dl-PA...
  99. ncbi [Studies on chemical constituents of Peucedanum delavayi]
    Qian shun Yan
    Ningxia Medicinal College, Yinchuan, China
    Zhong Yao Cai 31:1157-9. 2008
    ..To study the chemical constituents of the radix and rhizome of Peucedanum delavayi...
  100. ncbi Synthesis and evaluation of anticancer activity of some imidazothiazolyl, imidazobenzothiazolyl and dihydroimidazothiazolyl coumarins
    Kagne Srimanth
    Department of Chemistry, Regional Engineering College, Warangal, A P, India
    Arzneimittelforschung 52:388-92. 2002
    ..The compounds showed very good activity against different tumor cell lines...
  101. ncbi Armenin and isoarmenin--two prenylated coumarins from the aerial parts of Artemisia armeniaca
    Mahdi Mojarrab
    Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran
    Chem Biodivers 8:2097-103. 2011
    ..preparative HPLC analyses of the MeOH extract of the aerial parts of Artemisia armeniaca yielded four prenylated coumarins, 7-hydroxy-8-(4-hydroxy-3-methylbutoxy)coumarin (named armenin), 8-hydroxy-7-(4-hydroxy-3-methylbutoxy)coumarin (..

Research Grants60

  1. NATURAL & SYNTHETIC COUMARINS AS ANTICARCINOGENIC AGENTS
    John DiGiovanni; Fiscal Year: 2002
    ..We have recently found that several natural, as well as novel synthetic coumarins, have the potential to be effective inhibitors of mouse skin carcinogenesis by PAHs...
  2. Analysis of Phenolic Phytochemical by ESI-MS
    Jennifer Brodbelt; Fiscal Year: 2003
    ..quantitation of flavonoids in kale, soy, and urine, the second involving the identification and quantitation of coumarins in urine and tissue, the third involving the quantitation and identification of tocopherol compounds in tissue, ..
  3. Anticarcinogenic effects of naturally occurring coumarins on mammary carcinogenes
    HEATHER KLEINER HANCOCK; Fiscal Year: 2007
    ..Award will enable me to study the extent and mechanisms of the inhibitory effects of naturally occurring coumarins (NOCs) and 1'-acetoxychavicol acetate (ACA) in human and rodent models of mammary carcinogenesis...
  4. Dual Direct Inhibitors of Thrombin and Factor Xa
    UMESH RAMANLAL DESAI; Fiscal Year: 2012
    ..Anticoagulants, including heparins and coumarins, are the mainstay of treatment and prevention of thromboembolic disorders...
  5. Pilot-Scale Heterocyclic and Carbocyclic Libraries for High Throughout Screening
    RICHARD LAROCK; Fiscal Year: 2009
    ..alkenes and arynes will be employed to prepare specially diverse libraries of indoles, benzofurans, benzopyrans, coumarins, isocoumarins, phthalides, pyrones, 2-quinolones, pyridines, isoquinolin-1-ones, isoindolin-1-ones, ..
  6. Synthesis of Medicinally Important Heterocycles
    RICHARD LAROCK; Fiscal Year: 2007
    ..and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, naphthols, and phenols...
  7. Novel Extended Red-Shifted Rhodamine Dyes
    NICHOLAS CAIRNS; Fiscal Year: 2004
    ..In existing applications of commonly used short and medium wavelength dyes such as coumarins, fluoresceins and rhodamines, assay or tissue components can severely interfere with the fluorescence properties ..
  8. ENDOCRINE DISRUPTING CHEMICALS AND AROMATASE
    Shiuan Chen; Fiscal Year: 2009
    ..The proposed studies will focus on 1014 phytochemicals (including chalcones, chromones, coumarins, flavanones, flavones and isoflavones) that would be purchased from Indofine Co (Somerville, New Jersey)...
  9. NATURAL PRODUCT DERIVATIVES THAT POTENTLY INHIBIT HIV1
    Graham Allaway; Fiscal Year: 1999
    ..proposal will characterize the six most potent drug candidates discovered in the collaboration: A) Three related coumarins: Di-Camphanoyl-Khallactone (DCK), 4-methyl DCK and thiolactone DCK; B) Three related triterpenes: ..
  10. Modulators of Nicotine-Mediated Dopamine Release
    Simon Efange; Fiscal Year: 2003
    ..Specifically, we propose to synthesize 8 related substituted chromans and coumarins. These compounds will be screened for 1) binding to alpha3beta2, alpha6/alpha3beta2, alpha4beta2, alpha7, ..
  11. Antioxidants and oxidative damage in mitochondria
    Cecilia Giulivi; Fiscal Year: 2004
    ..The antioxidant effect of flavonoids, coumarins, and catechins will be studied in terms of hydroxyl substitution, conjugation of rings, and o-methylation of ..
  12. Antioxidants and oxidative damage in mitochondria
    Cecilia Giulivi; Fiscal Year: 2002
    ..The antioxidant effect of flavonoids, coumarins, and catechins will be studied in terms hydroxyl substitution, conjugation of rings, and o- methylation of ..
  13. Pharmacogenetics and Antithrombotic Therapy
    Brian Gage; Fiscal Year: 2003
    ..Using high performance liquid chromatography, we will measure the levels of the 2 enantiomers of warfarin and test Hypothesis 4: Clearance of S-warfarin will be significantly decreased in the presence of 2C9 SNPs. ..
  14. Improving gene therapy-mediated radiosensitization
    Theodore Lawrence; Fiscal Year: 2006
    ..abstract_text> ..
  15. Molecular Modulators of HCV Replication
    Neerja Kaushik Basu; Fiscal Year: 2007
    ..This will enable us to understand, at the molecular level, the replication process of hepatitis C virus and will further facilitate the development of effective drugs/inhibitors against HCV. ..
  16. MOLECULAR TOXICOLOGY IN HUMAN KIDNEY CELLS
    Lawrence Lash; Fiscal Year: 2007
    ..Achievement of these aims should build on our previous work in human kidney cells and extend it to provide a much more complete understanding of the various and complex ways in which DCVC affects the human kidney [unreadable] [unreadable]..
  17. Methyl selenium regulation of Angiogenic switch Mech
    Junxuan Lu; Fiscal Year: 2006
    ..unreadable] [unreadable]..
  18. BIOCHEMICAL STUDIES OF 14 KDA PHOSPHOLIPASES A2
    Michael Gelb; Fiscal Year: 2006
    ..These studies will contribute to our fundamental understanding of how mammalian cells initiate the eicosanoid cascade. ..
  19. Exploring Symptom Control in Chronic Critical Illness
    Judith Nelson; Fiscal Year: 2008
    ..Not applicable. [unreadable] [unreadable] [unreadable]..
  20. Molecular Target Focused Discovery of Anticancer Drugs
    GEORGE PETTIT; Fiscal Year: 2007
    ..In summary, the proposed research will be sharply aimed at the discovery and very rapid development of new anticancer drugs for the NCI programs direct at improving human cancer treatments. ..
  21. Improving Palliative Care in Chronic Critical Illness
    Judith Nelson; Fiscal Year: 2008
    ..The environment is a renowned center for research in geriatric palliative care and chronic critical illness and for clinical research training; the institution offers enthusiastic support. [unreadable] [unreadable]..
  22. Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.
    BARRY TROST; Fiscal Year: 2009
    ..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
  23. Fluorescence Zinc BioSensing and Imaging Technology
    RICHARD BLAIR THOMPSON; Fiscal Year: 2010
    ..This novel technology will provide the basis for new diagnostics and treatments. ..
  24. Gemcitabine-Radiation for Advanced Pancreatic Cancer
    Theodore S Lawrence; Fiscal Year: 2010
    ..We feel our preclinical and clinical team with a track record of 10 years of carrying out leading clinical trials in this area makes it likely that these studies will improve patient outcome. ..
  25. Molecular Target Focused Discovery of Anticancer Drugs
    George R Pettit; Fiscal Year: 2010
    ....
  26. New statistical tools for single molecule experiments
    David S Talaga; Fiscal Year: 2010
    ..Aim 3 provides useable tools for experimental design and analysis to allow other investigators to exploit these methods for their own research. ..
  27. ASYMMETRIC SYNTHESIS OF NOVEL NATURAL PRODUCTS
    MICHAEL CRIMMINS; Fiscal Year: 2006
    ..Synthesis of the biologically active agents guanacastepene, and SCH 351448 will also be pursued. ..
  28. FLOW SHEAR INDUCED NF-KB MEDIATED REGULATION
    Sumathy Mohan; Fiscal Year: 2003
    ..Understanding of NF- kappaB signaling mechanisms in VCAM-1 regulation can also be applied to other inflammatory conditions. ..
  29. Developmental Exposure to Nicotine
    RUSSELL POLAND; Fiscal Year: 2003
    ....
  30. Beta-Cell Mass And Function In Implants and Pancreas
    Wen Hong Li; Fiscal Year: 2003
    ..abstract_text> ..
  31. BIOCHEMISTRY OF PROTEIN PRENYLATION
    Michael Gelb; Fiscal Year: 2002
    ....
  32. Micromass LCT Mass Spectrometer
    MICHAEL CRIMMINS; Fiscal Year: 2004
    ..The major users group is highly dependent on rapid turn around mass spectral data. Since there is currently no Departmental mass spectrometry facility, the research programs of the major users have been seriously hampered for some time. ..
  33. MULTIPLEX ANALYSIS OF INBORN ERRORS OF METABOLISM
    Michael Gelb; Fiscal Year: 2001
    ..abstract_text> ..
  34. QUANTITATIVE IMAGING OF ZINC METABOLISM IN THE BRAIN
    Richard Thompson; Fiscal Year: 2002
    ..abstract_text> ..
  35. RISK FACTORS FOR UTI IN POST MENOPAUSAL WOMEN
    Stephan Fihn; Fiscal Year: 2001
    ..Diabetic patients will be followed with glycosylated hemoglobin at least annually. Patients will monitor their urine monthly at home with leukocyte esterase/nitrite dipsticks and make a clinic visit if they test positive. ..
  36. Exploring Measurement of Palliative Care Quality in ICUs
    Judith Nelson; Fiscal Year: 2008
    ..N/A [unreadable] [unreadable] [unreadable]..
  37. BIOCHEMISTRY OF HEPATITIS C VIRUS REPLICASE
    Neerja Kaushik Basu; Fiscal Year: 2003
    ..Aim 2: To elucidate the catalytic roles of specific amino acid residues in the polymerase function. Aim 3: To determine protein-protein interactions between HCV replicase and other nonstructural viral proteins. ..
  38. SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORS
    AMOS SMITH; Fiscal Year: 2001
    ..abstract_text> ..
  39. Basal Ig Signaling and Receptor Editing
    Michael Farrar; Fiscal Year: 2009
    ..abstract_text> ..
  40. QUANTITATIVE IMAGING OF ZINC METABOLISM IN THE BRAIN
    Richard Thompson; Fiscal Year: 2003
    ..abstract_text> ..
  41. Treatment of Depression with Massage in End of Life AIDS
    RUSSELL POLAND; Fiscal Year: 2002
    ....
  42. Conference on Drug Against Tropical Protozoan Parasites
    Michael Gelb; Fiscal Year: 2002
    ..We consider the poster sessions that occur throughout our meeting to be just as important as the collection of lecture presentations. ..
  43. PRICE: Pivotal Research in Cardiology in the Elderly
    Michael Rich; Fiscal Year: 2008
    ....
  44. GLUTATHIONE AND MITOCHONDRIA IN TOXIC RENAL INJURY
    Lawrence Lash; Fiscal Year: 2003
    ..This information may have therapeutic applications for prevention of renal cellular injury or for understanding mitochondrial diseases or age-related decreases that occur in mitochondrial function. ..
  45. RADIATION DOSE ESCALATION FOR FOCAL LIVER CANCER
    Theodore Lawrence; Fiscal Year: 2005
    ....
  46. SLEEP DEPRIVATION AND 5-HT AUTOREGULATORY PROCESSES
    RUSSELL POLAND; Fiscal Year: 2005
    ..A better understanding of these sleep deprivation-related changes has the potential to advance our knowledge, both in sleep physiology and antidepressant mechanisms of action. ..
  47. Synthetic Studies of Chiral Organometallics
    ROBERT GAWLEY; Fiscal Year: 2004
    ..4. To pursue our recent findings relating to possible stereoelectronic effects on transmetalation and the nature of heteroatom participation in tin-lithium exchanges using rapid injection NMR. ..
  48. Interactive Effects of Flaxseed and Tamoxifen in Breast*
    Lilian Thompson; Fiscal Year: 2004
    ..abstract_text> ..
  49. EFFECTORS AND IINHIBITORS OF SARS VIRUS POLYMERASE
    Neerja Kaushik Basu; Fiscal Year: 2006
    ..Further, analysis of the sensitivity of the SARS-CoV RdRp towards a panel of known and novel inhibitors of polymerases will provide new leads in the quest for specific antiviral agents against the SARS-CoV RdRp. ..
  50. Topomer selection by chemists from All structures
    Richard Cramer; Fiscal Year: 2006
    ..abstract_text> ..
  51. ASYMMETRIC SYNTHESIS OF ANTITUMOR AGENTS
    MICHAEL CRIMMINS; Fiscal Year: 2005
    ..Laulimalide stimulates tubulin polymerization more effectively than paclitaxel. Laulimalide is a representative of a new class of microtubule stabilizing agents with promise for therapeutic potential. ..
  52. Sensor for Paralytic Shellfish Poisons
    ROBERT GAWLEY; Fiscal Year: 2006
    ..The most toxic PSP, saxitoxin, is also 1 of only 3 "small molecules" on the government's list of "Select Agents". Fast, inexpensive means of detection PSPs is desirable. [unreadable] [unreadable] [unreadable]..
  53. Liver Radioprotection by Systemic of Regional Amifostine
    Theodore Lawrence; Fiscal Year: 2007
    ..Our preliminary data, research team, and record for translating preclinical findings to the clinic suggest that this proposal is likely to improve the outcome of treatment of patients with diffuse intrahepatic cancer. ..
  54. Selenium and prostate cancer apoptosis pathways
    Junxuan Lu; Fiscal Year: 2007
    ..The mechanistic insights will help to guide the design of novel Se agents with better efficacy and tolerance and to interpret the results of PCa prevention trials with Se. ..
  55. Light activated bioactive substrate release
    RICHARD GIVENS; Fiscal Year: 2008
    ..abstract_text> ..
  56. Design and Synthesis of HIV-1 Protease Inhibitors
    AMOS SMITH; Fiscal Year: 2004
    ....
  57. SYNTHESIS OF SPONGISTATIN ANTITUMOR AGENTS
    AMOS SMITH; Fiscal Year: 2007
    ..abstract_text> ..
  58. NMR systems : 2 Bruker Avance 500 Consoles
    AMOS SMITH; Fiscal Year: 2006
    ..The areas of public health research include, among others, cancer, infectious diseases, neurodegenerative diseases such as Alzheimer's disease, and heart and cardiovascular disease. [unreadable] [unreadable] [unreadable]..