The pharmacological properties of native N-methyl-D-aspartate (NMDA) receptors were determined in rat brain sections with quantitative autoradiography of [(3)H](E)-2-amino-4-propyl-5-phosphono-3-pentenoic acid (CGP39653) binding. With five competitive antagonists as displacers, two subpopulations of binding sites were observed in the horizontal plane of section examined. These two populations c...

It is known that His-48 is part of the active center in pancreatic phospholipase. To further elucidate the role of histidine-48 in the active center of pancreatic phospholipase A2, we have modified the enzyme with a number of bromo ketones and methyl benzenesulfonates. Rapid methylation occurred with methyl p-nitrobenzenesulfonate. Methylated phospholipase shows total loss of enzymatic activity...

The reaction of readily available 1 -methyl-4-nitropyrrole-2- carboxylic acid (1) with thionyl chloride afforded the corresponding acyl chloride 2. The reaction of compound 2 with thiosemicarbazides yielded 1-(1 -methyl-4-nitrop yrrole-2-carbony1)- thiosemicarbazides (3) which cyclized in basic medium to 5-(1-methyl-4-nitropyrrole- 2-y1)-2,4-dihydro-3H- l,2,4-triazole-3- thione 4. Alkylatio...

Alkylresorcinols (AR) could be good biomarkers of consumption of fiber-rich cereal products. The aim of this study was to examine the relationship between plasma ARs or urinary AR metabolites and cereal fiber intake in women consuming their habitual diet. Twenty-five postmenopausal and 31 premenopausal women were recruited. The subjects included also vegetarians (n = 20) to obtain a broad range...

Transcription of two unfolded protein response genes, hacA and bipA, was examined in Aspergillus niger strains overproducing membrane proteins. Despite elevated bipA mRNA levels, no 5'-truncated hacA transcript was detected, raising the possibility of a hacA-independent induction of bipA mRNA under the stress of membrane protein overproduction in A. niger.

Four oxidized flavonoid derivatives generated from reacting quercetin (a pentahydroxylated flavone) with the peroxyl radical generator 2,2'-azobis-isobutyronitrile (AIBN) were isolated by chromatographic methods and identified by NMR and MS analyses. Compounds included 2-(3,4-dihydroxybenzoyl)-2,4,6-trihydroxy-3(2H)-benzofuranone (2); 1,3,11a-trihydroxy-9-(3,5,7-trihydroxy-4H-1-benzopyran-4-on-...

reaction of aryl methyl ketone with isatin in the presence of a base afforded 2- arylquinoline-4-carboxylic acid (3). reaction of diazomethane with compound 3 yielded the ester 4. compound 5 was prepared from the reaction of n, n'-dialkylethyl (or propyl) arnine with 4. addition of hydrazine hydrate to compound 4a gave 2- (2- pyridyl) quinoline-4-carboxylic acid hydrazide (6). reaction of ...

The biogenesis of rosmarinic acid (alpha-O-caffeoyl-3,4-dihydroxyphenyl-lactic acid), the second most common ester of caffeic acid in the plant kingdom, was studied in Mentha arvense and Mentha piperita. Administration of (14)C-labelled compounds showed that, whereas the caffeoyl moiety was formed from phenylalanine via cinnamic acid and p-coumaric acid, the 3,4-dihydroxyphenyl-lactic acid moie...

The new methyl orthoformate of the powerful antioxidant hydroxytyrosol (or 2-(3,4-dihydroxyphenyl)ethanol) has been synthesized by a two-step high yielding procedure. The protection stabilizes hydroxytyrosol against fast oxidation and allows both easy chromatographic purification and long term storage. The protective group is hydrolyzed over pH = 10 and below pH = 5, thus allowing the release o...