The pharmacological effect of BGC20-1531, a novel prostanoid EP4 receptor antagonist, in the Prostaglandin E2 human model of headache

Using a human Prostaglandin E2 (PGE2) model of headache, we examined whether a novel potent and selective EP4 receptor antagonist, BGC20-1531, may prevent headache and dilatation of the middle cerebral (MCA) and superficial temporal artery (STA). In a three-way cross-over trial, eight healthy volunteers were randomly allocated to receive 200 and 400 mg BGC20-1531 and placebo, followed by a 25-min infusion of PGE2. We recorded headache intensity on a verbal rating scale, MCA blood flow velocity and STA diameter. There was no difference in headache response or prevention of the dilation of the MCA or the STA (P > 0.05) with either dose of BGC20-1531 relative to placebo, although putative therapeutic exposures were not reached in all volunteers. In conclusion, these data suggest that the other EP receptors may be involved in PGE2 induced headache and dilatation in normal subjects

Regioselective synthesis of plant (iso)flavone glycosides in Escherichia coli

The flavonoids genistein, biochanin A, luteolin, quercetin, and kaempferol are plant natural products with potentially useful pharmacological and nutraceutical activities. These natural products usually exist in plants as glycosides, and their glycosylation has a remarkable influence on their pharmacokinetic properties. The glycosyltransferases UGT71G1 and UGT73C8 from Medicago truncatula are excellent reagents for the regioselective glycosylation of (iso)flavonoids in Escherichia coli grown in Terrific broth. Ten to 20 mg/L of either genistein or biochanin A 7-O-glucoside was produced after feeding genistein or biochanin A to E. coli expressing UGT71G1, and similar levels of luteolin 4’-O- and 7-O-glucosides were produced after feeding luteolin to cultures expressing UGT73C8. For the production of kaempferol 3-O-glucoside or quercetin 3-O-glucoside, the Phe148Val or Tyr202Ala mutants of UGT71G1 were employed. Ten to 16 mg/L of either kaempferol 3-O- or quercetin 3-O-glucosides were produced on feeding kaempferol or quercetin to E. coli expressing these enzymes. More than 90% of the glucoside products were released to the medium, facilitating their isolation

[Nutritional status of vitamin A in preschoolers with ocular diseases]

The purpose was to evaluate the nutritional status of vitamin A in preschool children with ocular diseases attending to the Hospital Civil of Guadalajara. In a cross sectional design 100 preschool children between 24 and 71 mo of age with ocular diseases were included. Vitamin A intake was evaluated by 24 h dietetic recall, plasma Retinol concentration by high pressure liquid chromatography (HPLC); and, conjunctiva impression cytology (CIC) was carried out by a trained pathologist. ANOVA and U Mann Whitney tests, and also Spearman correlations were estimated. There were 44.1% females and 55,9% males. Strabismus was the most common disease (41,9%), conjunctivitis (19,4%), and congenital diseases (17,2%). The mean intake of Vitamin A was 374 microg/d +/- 706 and the serum concentration of retinol was of 30 microg/dL +/- 7,6; CIC was normal in 75,6%. The percentage of vitamin A deficiency was 3,2% according to the serum concentration of Retinol and 3,5% to the CIC criteria. It was not association between the nutritional status of vitamin A and ocular diseases. A positive correlation between vitamin A intake and weight/height index (r = 0,244) was found. In conclusion, most preschool children covered the dietary reference intake recommendation of vitamin A; deficiency of this vitamin was lower and, it was not associated to ocular diseases

Nutritional status of vitamin A in preschoolers with ocular diseases [Estado nutricio de vitamina A en preescolares con padecimientos oculares]

The purpose was to evaluate the nutritional status of vitamin A in preschool children with ocular diseases attending to the Hospital Civil of Guadalajara. In a cross sectional design 100 preschool children between 24 and 71 mo of age with ocular diseases were included. Vitamin A intake was evaluated by 24 h dietetic recall, plasma Retinol concentration by high pressure liquid chromatography (HPLC); and, conjunctiva impression cytology (CIC) was carried out by a trained pathologist. ANOVA and U Mann Whitney tests, and also Spearman correlations were estimated. There were 44.1% females and 55,9% males. Strabismus was the most common disease (41,9%), conjunctivitis (19,4%), and congenital diseases (17,2%). The mean intake of Vitamin A was 374 ug/d ± 706 and the serum concentration of retinol was of 30 ug/dL ± 7,6; CIC was normal in 75,6%. The percentage of vitamin A deficiency was 3,2% according to the serum concentration of Retinol and 3,5% to the CIC criteria. It was not association between the nutritional status of vitamin A and ocular diseases. A positive correlation between vitamin A intake and weight/height index (r = 0,244) was found. In conclusion, most preschool children covered the dietary reference intake recommendation of vitamin A; deficiency of this vitamin was lower and, it was not associated to ocular diseases