Effect of quercetin on traits of the metabolic syndrome, endothelial function and inflammation in men with different APOE isoforms.

BACKGROUND AND AIMS: The polyphenol quercetin may prevent cardiovascular diseases due to its vasorelaxant and anti-oxidative properties. We investigated the effects of quercetin on risk factors of atherosclerosis, biomarkers of inflammation and oxidative stress, depending on the apolipoprotein E (APOE) genotype. METHODS AND RESULTS: In a double-blind crossover study 49 healthy male subjects with APOE genotype 3/3 (n = 19), 3/4 (n = 22) and 4/4 (n = 8) consumed 150 mg/d quercetin or placebo for 8 weeks each, intermitted by a three-week washout phase. After each intervention, endothelial function, anthropometry, metabolic and inflammatory parameters were measured in the fasting and postprandial state following a standardized lipid-rich meal. Endothelial function was not changed. In all subjects combined, quercetin significantly decreased waist circumference (P = 0.004) and postprandial systolic blood pressure (P = 0.044). Postprandial triacylglycerol concentrations were significantly decreased and HDL-cholesterol concentrations increased after quercetin as compared to placebo consumption (P = 0.025). Quercetin also moderately increased levels of TNFα (P = 0.024). There was a significant gene-diet interaction for waist circumference and for body mass index (BMI). CONCLUSIONS: Quercetin supplementation improved some risk factors of cardiovascular disease, yet exerted slightly pro-inflammatory effects. Genotype-dependent effects were seen only on waist circumference and BMI.

Non-steroidal anti-inflammatories--XII. Mode of action of anti-inflammatory methane sulfonanilides.

The influence of anti-inflammatory methane sulfonanilides on the arachidonic acid metabolism in ram seminal vesicle homogenate depends on the pK3 of the individual substance: more acidic compounds suppress, less acidic compounds stimulate PG synthesis and enhance the PGH2/PGG2 ratio. As oxygen radicals are liberated during the conversion of PGG2 to PGH2 it is suggested that the less acidic methane sulfonanilides are scavengers of the (pro-inflammatory) oxygen radicals.

Blood glucose lowering sulfonamides with asymmetric carbon atoms. 3. Related N-substituted carbamoylbenzoic acids.

Both enantiomers of 4-N-[1-(5-Fluoro-2-methoxyphenyl)ethyl]carbamoylmethylbenzoic acid display hypoglycemic activity. The more potent (S) enantiomer is approximately equipotent with the acylaminoethylbenzoic acids of the type HB 699 (Figure 1; Table I). Observations are given that suggest that these benzoic acids act at the same receptor as the hypoglycemic sulfonylureas and sulfonylaminopyrimidines and further that this receptor includes important binding sites.

[On the surface-anesthetic activity of some ether alcohols (author's transl)]. / Uber die oberflächenanästhetische Wirkung einiger Atheralkohole.

An account of the preparation and surface anesthetic potency of 12 ether alcohols of the type X-O-Y-OH is given in this paper. The anaesthetic intensity and effective duration of a chloronaphthalene derivative of this type lie within the range of action of cocain.

Chemotherapeutic nitroheterocycles. 18. 2-(5-Nitro-2-imidazolylmethylene)-1-indanones, -1-tetralones, and -acetophenones substituted by aminoalkoxy groups.

2-(5-Nitro-2-imidazolylmethylene)-1-indanones, -1-tetralones, and -acetophenones substituted by aminoalkoxy groups and related compounds (41-69, table ii) were synthesized and their antimicrobial activities were evaluated (table iii). Some of these compounds (e.g. 47, 52, and 59) suprisingly exhibited a broad antibacterial spectrum including Proteus species and Pseudomonas aeruginosa. Extraordinary antitrichomonal activities could also be observed in vitro (MIC of compound 59, 0.0004 pg/ml) and six of the title compounds (48, 49, 52, 58, 64, 66) displayed in vivo activity in mice against Trichomonas vaginalis comparable to that of metronidazole (70).