coumarins

..The coumarin analogue and scopoletin inhibited monoamine oxidase with moderate IC(50) values. The new coumarino-lignan and cleomiscosin C showed lipid peroxidation inhibitory activity comparable to vitamin E...

..Their chemical structures were determined by MS, NMR spectroscopy and chemical analysis. Complete assignments of the 1H and 13C NMR spectroscopic data were achieved by 1D and 2D NMR experiments including DEPT, HSQC, HMBC and ROESY...

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...

..This is a novel mechanism for a gyrase inhibitor and presents new possibilities for antibacterial drug development...

..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...

..5% and 68.3% inhibition, respectively). In summary, the compounds predominantly displayed suppressive and antiinflammatory activities in the investigated models...

..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 ..

..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...

..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...

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..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...

..Then, the CmF extract was subjected to silica gel column chromatography and recrystallization to give five coumarins: osthol, imperatorin, bergapten, isopimpinellin, and xanthotoxin...

..Feeding of the mutant with the aminocoumarin moiety of novobiocin led to a new, artificial simocyclinone derivative...

..Our results should facilitate the design of drug molecules that target these unexploited binding pockets...

b>Coumarins are of many different structures...

..From these results, FCE and one of its components, esculetin, were predicted to be potentially useful as ingredients in cosmetics for protecting against photoaging...

..We demonstrate that wedelolactone is an inhibitor of IKK, a kinase critical for activation of NF-kappaB by mediating phosphorylation and degradation of IkappaBalpha...

..Its use in the study of DNA manipulations involving ssDNA intermediates is demonstrated in assays for DNA unwinding, catalyzed by DNA helicases...

..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...

Treatment with vitamin K antagonists (coumarins) is associated with an increased risk of bleeding...

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..The significant results in vitro and in vivo showed that CBSA-NP was a promising brain drug delivery carrier with low toxicity...

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Six furoquinolines and five coumarins have been isolated from the roots of Esenbeckia grandiflora subsp. brevipetiolata. The leaves yielded two dihydrochalcones and two flavonol rhamnosides...

..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...

Two new coumarins, murrmeranzin (1) and murralonginal (2), together with four known compounds minumicrolin (3), murrangatin (4), meranzin hydrate (5) and hainanmurpanin (6) have been isolated from the aerial parts of Murraya paniculata...

..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...

..The results indicated that the developed method could be considered to be a simple, rapid and reliable method for the quality evaluation of Cortex Fraxini...

b>Coumarins comprise a group of natural phenolic compounds found in a variety of plant sources...

..Their structures and configurations were elucidated by spectroscopic methods including 2D-NMR techniques. Sikokianin A, chamaechromone, and quercetin showed in vitro antiviral activity against HBsAg secretion...

..Repeated column chromatography for the EtOAc and n-BuOH fractions led to the isolation of two new coumarins, oxypeucedanin hydrate-3''-butyl ether and isopraeroside IV along with six known coumarins, isoimperatorin, ..

..Under the best SFE conditions tested for the three coumarins, which involved extraction at 50 degrees C and 27...

..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...

The antioxidant activity of eight coumarins and two flavonols isolated from Haplopappus multifolius was studied with the DPPH radical method...

..DC afforded six known coumarins as well as (+)-meranzin hydrate (7), not previously reported as a natural product...

A series of coumarins incorporating hydroxy-, chloro- and/or chloromethyl-moieties in positions 3-, 4-, 6- and 7- of the heterocyclic ring were investigated for the inhibition of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1)...

..antiviral, P-glycoprotein (P-gp) inhibitory and antiinflammatory activity have been attributed to sesquiterpene coumarins; structures containing a common coumarin group and a sesquiterpene moiety...

Two series of disubstituted coumarins incorporating ether and acetyl/propionyl moieties in positions 6,7- and 7,8- of the heterocyclic ring were synthesized investigated for the inhibition of the zinc enzyme carbonic anhydrase (CA, EC 4...

..By using this HPLC-ESI-MS/MS method, all 11 coumarins were separated and determined within 10min...

..43 times higher than that of LIP, and 3.10 times higher than that of CLP. Both pharmacokinetics and distribution in mice were also investigated to show that this novel brain targeting drug delivery system was promising...

..named surangin D), was isolated from the bark of Mammea siamensis collected in Vietnam, along with four known coumarins, surangins B and C, and theraphins B and C, and seven xanthones, 1,7-dihydroxyxanthone, 7-hydroxy-1-..

..The methodology involves the three-component Biginelli reaction. On the other hand, substituted salicylaldehyde and beta-oxodithioesters reacted under the same condition to afford the substituted 2H-chromene-2-thiones in high yields...

..fraction of the roots of Angelica purpuraefolia, along with one ferulate (2) and three other known coumarins (3-5) including khellactone (3)...

..The structure elucidation was done by one and two dimensional NMR experiments, and other spectroscopic methods in combination with incorporation experiments using 13C labelled precursors...

..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...

..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...

..Thus, a novel anti-cancer drug, GUT-70 isolated from the stem bark of C. brasiliense induces caspase-mediated and p53-independent apoptosis to overcome multidrug resistance and may become a potent leukemia therapeutics...

..We set up a robust synthetic procedure tunable on the substitution patterns to achieve. These coumarins possess excellent fluorescence quantum yields (up to 0...

..identification of the most important interactions driving the binding and clearly indicated the allowed and disallowed regions for appropriate structural modifications of coumarins and closely related heterocyclic molecular scaffolds.

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...

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..sabulosa that produced marked antinociception against the acetic acid-induced visceral nociceptive response, supporting the ethnomedical use of P. sabulosa...

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b>Coumarins, also referred as benzopyran-2-ones, and their corresponding nitrogen counterpart, 1-azacoumarins also referred to as carbostyrils, are a family of nature-occurring lactones and lactams respectively...

..19+/-0.01 microM and a high selectivity for AChE/BuChE, and compound 6b acted as non-competitive AChE inhibitor with IC50 value of 0.43+/-0.02 microM. Structure-activity relationships (SARs) of prepared compounds were discussed...

b>Coumarins, 4-hydroxycoumarins, and 4-hydroxyquinolin-2(1H)-ones can be conveniently prepared by treatment of alpha-halocarboxylic acid esters of salicylaldehyde, o-hydroxyacetophenone, methyl salicylate, and methyl N-methyl- or N-..

..A difference has to be made between those patients taking paracetamol (acetaminophen) for pain relief or as an antipyretic during infectious diseases...

b>Coumarins, also known as benzopyrones, are present in remarkable amounts in plants, although their presence has also been detected in microorganisms and animal sources...

..When L-proline is used as an additional promoter to obtain coumarins from o-hydroxybenzaldehydes, the reaction also proceeds in high yields...

..Its efficacy, however, in pregnant women with prosthetic heart valves is questioned, therefore coumarins are preferred for this indication...

..2 mg/mouse, i.v.)-induced hepatitis were studied. At the dose of 200 mg/kg (i.p.), these coumarins inhibited more than 90% of the Con A-induced elevation of plasma alanine aminotransferase activity, but ..

..HPLC-DAD-MS) method has been developed for the simultaneous identification and quantification of its main coumarins, oxypeucedanin hydrate, oxypeucedanin, ostruthol, imperatorin, osthole, isoimperatorin, and ostruthin...

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)...

..Results obtained from these studies have produced novobiocin analogues that manifest low micromolar activity against several cancer cell lines...

..The docking scores are compared with the inhibition of hCA II and show good correlation with biological activity...

Complexes of lanthanum (III) with bis-coumarins: bis(4-hydroxy-2-oxo-2H-chromen-3-yl)-piridin-2-yl-methane; bis(4-hydroxy-2-oxo-2H-chromen-3-yl)-piridin-3-yl-methane and bis(4-hydroxy-2-oxo-2H-chromen-3-yl)-piridin-4-yl-methane were ..

In order to identify antitumor-promoting agents, we performed primary in vitro screening of 31 coumarins isolated from 11 plants of the Citrus species (Rutaceae), examining their possible inhibitory effects on Epstein-Barr virus early ..

The Benzopyrones are a group of compounds whose members include coumarins and flavonoids. Dietary exposure to benzopyrones is quite significant, as these compounds are found in vegetables, fruit, seeds, nuts, coffee, tea and wine...

..The development of potent STS inhibitors will allow investigation of the role of this enzyme in physiological and pathological processes...

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..pressure chemical ionisation MS detection has been developed for the separation and identification of coumarins in plants of Peucedanum palustre L. (Moench) and Angelica archangelica (L.) var. archangelica...

..In this study, we demonstrate that osthole is a promising agent for treating osteoporosis...

..These results demonstrate that AUR exposure in post-initiation period suppresses the occurrence of HCCs with beta-catenin mutation, presumably by negative selection for neoplastic cells harboring the mutation...

..Unlike PDX, these peptides inhibit furin via a different mechanistic pathway. The study provides an alternate strategy for development of efficient peptide-based inhibitors of Proprotein Convertases including furin...

..In addition, turnover of the probes on the target strand occurs and yields substantial signal amplification...

..Our results suggest that AUR, which bears a geranyloxyl side chain, has a longer life span than ETC, and this property may be associated with its previously reported chemopreventive and xenobiotics metabolizing activities...

..Although the promoters of omlA and fur overlapped, Fur did not play any regulatory role in the expression of omlA due to the fact that inactivation of Fur did not affect the expression of omlA either in the presence or absence of iron...

..p. were attenuated by pretreatment with COUMATE. The results suggest that the arylsulfamate based steroid sulfatase inhibitors such as COUMATE interfere with the influx of the DHEAS anion into the brain...

..In conclusion, these compounds, particularly nobiletin, may be valuable for prostate cancer prevention...

..Thus, our goal was to determine the anticarcinogenic effects of auraptene against breast cancer...

..Chinese mangrove Rhizophora mucronata, yielded 11 new compounds including cytosporones J-N (1-3, 5-6), five new coumarins pestalasins A-E (8-12), and a new alkaloid named pestalotiopsoid A (14), along with the known compounds ..

..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...

Naturally occurring coumarins possess anti-carcinogenic activities in part by inducing carcinogen-detoxifying enzymes glutathione S-transferase (GST) and/or NAD(P)H quinone oxidoreductase (NQO1)...

Naturally occurring coumarins (NOCs) are anti-carcinogenic in the mouse skin model...

Complexes of cerium (III) with bis-coumarins: 3,3'-benzylidene-bis(4-hydroxy-2H-1-benzopyran-2-one) and bis(4-hydroxy-2-oxo-2H-chromen-3-yl)-(1H-pyrazol-3-yl)-methane were synthesized by reaction of cerium (III) salt and the ligands, in ..

..The purpose of the present study was to compare a broader range of naturally occurring coumarins (simple coumarins, and furanocoumarins of the linear and angular type) for their abilities to modulate hepatic ..

..In contrast, the hydroxycinnamic acids and hydroxycinnamyl alcohols possessed little antimicrobial activity, with the exception of the hydroxycinnamic acids, which were antibacterial...

..Second generation inhibitors, such as 2-MeOE2bisMATE, which also inhibit the growth of ER- tumours should be active against a wide range of cancers...

Twenty-one coumarins were examined for their antiproliferative activity towards several cancer cell lines, namely lung carcinoma (A549), melanin pigment producing mouse melanoma (B16 melanoma 4A5), human T-cell leukemia (CCRF-HSB-2), and ..

..Whether coumarins can prevent these complications is unclear...

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..The rate constant for the ester cleavage and liberation of cAMP is about 10(9) s(-1), estimated for the axial isomer of 6 by analysis of the fluorescence increase of the alcohol 12 formed upon laser pulse photolysis...

..furanocoumarin, that showed antifungal activity, was considered as a lead structure for a group of synthetic coumarins. Antifungal activities of the synthesized coumarins and angelicin derivatives were reported against Candida ..

Systematic fractionation of Angelica gigas roots led to the isolation of linear furano(pyrano)coumarins such as bergapten (1), decursinol angelate (2), decursin (3), nodakenetin (4) and nodakenin (5)...

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..The stability of aurapten in the aurapten-enriched preparation was higher than that of purified aurapten. These results suggest that aurapten is readily recovered from hassaku peel oil using SP70, and thus may be used as a food additive...

b>Coumarins (e.g., warfarin) are used for the treatment and prophylaxis of venous and arterial thromboembolism. Unfortunately, their use is limited by bleeding...

..of the free acids of the cyclic nucleotides with the corresponding 7(dialkylamino)-substituted 4(diazomethyl)coumarins. Irradiation of the DMACM- and DEACM-caged cyclic nucleotides with UV light stimulates the release of the cyclic ..

..The benzopyran ring displays aromatic character. The packing of the molecules in the lattice is mainly due to C-H...O hydrogen bonds...

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..CONCLUSION: Compound I, V and VI were isolated from Gerbera genus for the first time...

..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...

..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, ..

..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...

..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, ..

..Anticoagulants, including heparins and coumarins, are the mainstay of treatment and prevention of thromboembolic disorders...

..Anticoagulants, including heparins and coumarins, are the mainstay of treatment and prevention of thromboembolic disorders...

..and heteroatom analogues, furans, thiophenes, pyrroles, oxazoles, isoxazoles, pyrazoles, pyridines, quinolines, coumarins, indenes, indenones, naphthols, and phenols...

..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 ..

..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)...

..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)...

..The antioxidant effect of flavonoids, coumarins, and catechins will be studied in terms of hydroxyl substitution, conjugation of rings, and o-methylation of ..

..The antioxidant effect of flavonoids, coumarins, and catechins will be studied in terms hydroxyl substitution, conjugation of rings, and o- methylation of ..

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..Also of key importance, is that the inactivation of P450 2A enzymes will impact the metabolism of the tobacco specific carcinogens, NNK and NNN. ..

..Also of key importance, is that the inactivation of P450 2A enzymes will impact the metabolism of the tobacco specific carcinogens, NNK and NNN. ..

..Overall, these studies will help to achieve a better understanding of Gt signaling mechanisms as well as other G protein signaling systems and will provide information relevant to retinal diseases. ..

..If successful, we anticipate that our technology will be of use in understanding and developing treatments for the conditions listed above. ..

..In summary, the proposed research will be sharply aimed at the discovery and very rapid development of new anticancer drugs for the NCI programs directed at improving human cancer treatments. ..

..This research would develop a new level of understanding of structure, function, and regulation of PDE6 necessary to uncover the mechanisms of PDE6 mutations in diseased retina. ..

..Malaria and African sleeping sickness kill about 2 million and 200,000 people, respectively, each year. New drugs are needed because existing drugs are either ineffective or resistance has developed. ..

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..Once such features are identified, the design of new and possibly more effective antitumor drugs should be feasible...

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..The areas of public health research include, among others, cancer, infectious diseases, neurodegenerative diseases such as Alzheimer's disease, and heart and cardiovascular disease. ..

..The design of new and possibly more effective agents should then be feasible. ..

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