Search results for "DISCOVERY"
showing 10 items of 4119 documents
Effect of Flavonol Derivatives on the Carrageenin-Induced Paw Edema in the Rat and Inhibition of Cyclooxygenase-1 and 5-Lipoxygenase in Vitro
2000
Alkoxyflavonols were synthesized by the Algar-Flynn-Oyamada (AFO) cyclization of chalcones. Hydroxyflavonols were prepared by dealkylation of methoxyflavonols by refluxing in hydroiodic acid. The alkoxyflavonols 3-hydroxy-2-(2,3,4-trimethoxyphenyl)-4H-chromen-4-one (6), 2-(4-ethoxyphenyl)-3-hydroxy-4H-chromen-4-one (7), 2-(4-butoxyphenyl)-3-hydroxy-4H-chromen-4-one (10), and 2-(3-n-butoxyphenyl)-3-hydroxy-4H-chromen-4-one (11) as well as the trihydroxy derivative 3-hydroxy-2-(3,4,5-trihydroxyphenyl)-4H-chromen-4-one (18) displayed high anti-inflammatory activity in carrageenin-induced rat paw edema. Additionally, the inhibition of enzymes of the arachidonic acid cascade by the derivatives w…
Foetidissimosides C–F, Novel Glycosides from the Roots ofCucurbita foetidissima
2004
Two novel echinocystic acid (=(3β,16α)-3,16-dihydroxyolean-12-en-28-oic acid) glycosides, foetidissimosides C (1), and D (2), along with new cucurbitane glycosides, i.e., foetidissimosides E/F (3/4) as an 1 : 1 mixture of the (24R)/(24S) epimers, were obtained from the roots of Cucurbita foetidissima. Their structures were elucidated by means of a combination of homo- and heteronuclear 2D-NMR techniques (COSY, TOCSY, NOESY, ROESY, HSQC, and HMBC), and by FAB-MS. The new compounds were characterized as (3β,16α)-28-{[O-β-D-glucopyranosyl-(13)-O-β-D-xylopyranosyl-(14)-O-6-deoxy-α-L-mannopyranosyl-(12)-α-L-arabinopyranosyl]oxy}-16-hydroxy-28-oxoolean -12-en-3-yl β-D-glucopyranosiduronic acid (1…
A New Steroidal Saponin from Dioscorea cayenensis
2004
The new 26-O-beta-D-glucopyranosyl-3beta,26-dihydroxy-20,22-seco-25(R)-furost-5-en-20,22-dione-3-O-alpha-L-rhamnopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->4)-[alpha-L-rhamnopyranosyl-(1-->2)]-beta-D-glucopyranoside (1), along with the known methyl protodioscin (2), asperoside (3) and prosapogenin A of dioscin (4) were isolated from the rhizomes of Dioscorea cayenensis LAM.-HOLL (Dioscoreaceae). Their structures were established mainly on the basis of 600 MHz 2D-NMR spectral data. 4 exhibited antifungal activity against the human pathogenic yeasts Candida albicans, C. glabrata and C. tropicalis (MICs of 20.8, 6.25, 25 microg/ml, respectively), whereas saponins 1-3 were inactive.
Fermentbestimmungen in Erythrocyten von Kranken mit Porphyria cutanea tarda
1969
In Erythrocyten von 12 Kranken mit Porphyria cutanea tarda konnte eine Aktivitatssteigerung der Enzyme G-6-PDH, 6-PGDH sowie der NADH- und der NADPH-abhangigen Glutathionreduktion festgestellt werden, deren Ursache diskutiert wird.
Enzyme-mediated enantioselective acylation of secondary amines in organic solvents
1991
Abstract Porcine pancreatic lipase (PPL) and lipase Amano P catalyze the enantioselective acylation of cyclic 1,2- and 1,3-amino alcohol derivatives in organic solvents. The enatiomeric excesses (ee′s) were shown to depend on the enzyme, reaction time, temperature and type of substrate.
Ursane-Type Triterpene Saponins fromZygophyllum geslini
2007
Four new ursane-based triterpene glycosides, compounds 1–4, as well as the known glycosides zygophylosides E, G, and H, and 3-O-(β-D-quinovopyranosyl)quinovic acid 28-(O-β-D-glucopyranosyl) ester, were isolated from the BuOH-soluble fraction of the MeOH/H2O 7 : 3 extracts of Zygophyllum geslini (roots or aerial parts). Their structures were established mainly by 1D- and 2D-NMR techniques, in combination with HR-MS analysis and acid hydrolysis.
Non-steroidal Anti-inflammatory Agents, Part 24[1] Pyrrolidino Enaminones as Models to Mimic Arachidonic Acid
1997
The pyrrolidino enaminones, with the carboxylic acid chain fixed at the nitrogen, inhibit cyclooxygenase more potently or selectively than 5-lipoxygenase. According to the structure-activity relationships discussed the potency depends significantly on the chain length of the carboxylic acid, the substitution pattern of the heterocyclic moiety and of the phenyl group. Compound 4c is the most efficient inhibitor of cyclooxygenase. For the binding profile the unfolded conformation of arachidonic acid and the energy-minimized conformations of flurbiprofen, diclofenac, ML 3000, and lead compound 4a were compared. In addition to known structural features, similar distances of the carboxylic acid …
Dysidotronic acid, a new and selective human phospholipase A2 inhibitor from the sponge Dysidea sp.
2000
Abstract A new bioactive sesquiterpenoid, named dysidotronic acid 1, with a rearranged drimane skeleton has been isolated from the sponge Dysidea sp. from Vanuatu islands, along with bolinaquinone 2. The chemical structure of 1 was determined on the basis of spectroscopic data. Dysidotronic acid significantly inhibited human synovial phospholipase A2 (PLA2) at 10 μM, with an IC50 value of 2.6 μM and a higher selectivity and potency towards this enzyme than the reference inhibitor manoalide.
Metabolism of stilbene phytoalexins by Botrytis cinerea: 1. Characterization of a resveratrol dehydrodimer
1998
Abstract Resveratrol, a grapevine phytoalexin, is metabolized by a laccase-like stilbene-oxidase of Botrytis cinerea, the causal organism for grey mould. Characterization of one major metabolite formed during this degradation process as a resveratrol dehydrodimer allowed us to precize the reaction mechanism of this enzyme on stilbenes.
New sesquiterpene lactones and acetylenes from chrysanthemum lavandulifolium
1990
Abstract The aerial parts of Chrysanthemum lavandulifolium Mak. (Asteraceae) yielded three new acetylenes of the spiroacetal type 1-3, as well as two new germacranolides 4-5 and several known lactones.