A series of novel 10-(4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)-3-methyl-1H,10H-pyrano[4,3-b]chromen-1-ones were synthesized by a pseudo-three-component reaction of 4-hydroxy-6-methyl-2-oxo-2H-pyran-2-one (TAL) with 2-hydroxyarylaldehydes using different acids as catalysts and solvents. The approa...

Recently, we have shown that the therapeutically-used progestin and antiandrogen cyproterone acetate (CPA) causes the formation of high levels of DNA adducts in rat hepatocytes and rat liver [J. Topinka, U. Andrae, L.R. Schwarz, T. Wolff, Cyproterone acetate generates DNA adducts in rat liver an...

Four new precise accurate and selective methods have been developed for the determination of gestodene (I) and cyproterone acetate (II). The first method (A) depends on reaction of (I) and (II) with isoniazide in an acid medium and the colored products were measured at 378 and 400 nm, respective...

The synthesis and vascular 5-HT1B receptor activity of a novel series of substituted 3-amido phenylpiperazine and 4-(4-methyl-1-piperazinyl)-1-benzo[b]thiophene derivatives is described. Modifications to the amido linked sidechains of the 3-amidophenyl-piperazine derivatives and to the 2-sidecha...

We report the synthesis of a new ligand, 4,4′-bis(3,5-dimethoxyphenyl)-6,6′-dimethyl-2,2′-bipyridine, optimised for binding to copper(I) and with pendant functionality that can eventually be developed into metallodendritic structures. The synthesis and photophysical properties of complexes wi...

A hierarchically porous polypyrrole-coated nanostructured composite of reduced graphene oxide and magnetite nanoparticles (PPy-rGOx-Fe3O4) incorporated into alginate hydrogel microspheres was synthesized and applied as a magnetic solid phase extraction adsorbent. The double network porous nanost...

The present work reports an experimental and theoretical study of molecular structure of 4-Amino-2-chloropyrimidine-5-carbonitrile (ACPC) in solid phase. Raman and infrared (IR) spectra of ACPC have been recorded in the region of 3600–100 cm−1 and 4000–200 cm−1, respectively. Calculations with...

Naphthalene (NA) is a ubiquitous pollutant to which humans are widely exposed. 1,2-Dihydro-1,2-dihydroxynaphthalene (NA-dihydrodiol) is a major metabolite of NA generated by microsomal epoxide hydrolase (mEH). To investigate the role of the NA-dihydrodiol and subsequent metabolites (i.e. 1,2-nap...

Streptomyces avermitilis contains 33 cytochrome P450 genes in its genome, many of which play important roles in the biosynthesis process of antimicrobial agents. Here, we characterized the biochemical function and structure of CYP107W1 from S. avermitilis, which is responsible for the 12-hydroxy...

Platensimycin (PTM), produced by several strains of Streptomyces platensis, is a promising drug lead for infectious diseases and diabetes. The recent pilot-scale production of PTM from S. platensis SB12026 has set the stage for the facile semi-synthesis of a focused library of PTM analogues. In ...

In alkaline pulping wood pulp is reacted with concentrated aqueous alkali at elevated temperatures. In addition to producing cellulose for the manufacture of paper, alkaline pulping also generates large amounts of isosaccharinic acids as waste products. Isosaccharinic acids are potentially usefu...

Mixtures of dissimilar surfactants can have superior properties compared to those of the individual surfactant components involved, which provide impetus for research on interactions between surfactants. It was also demonstrated that a change in the composition of external phase promotes remarka...

Fatty acid binding proteins (FABPs) serve as critical modulators of endocannabinoid signaling by facilitating the intracellular transport of anandamide and whose inhibition potentiates anandamide signaling. Our previous work has identified a novel small-molecule FABP inhibitor, α-truxillic acid...

Ethnopharmacological relevanceStichopus japonicus (sea cucumber), edible traditional food in Asia, and its extracts are renowned for their wound healing, pain relieving, and cosmetic effects in traditional medicine. Holothurins, toxins isolated from sea cucumber, are thought to be active compone...

SummaryThe oligosaccharide antibiotic avilamycin A is composed of a polyketide-derived dichloroisoeverninic acid moiety attached to a heptasaccharide chain consisting of six hexoses and one unusual pentose moiety. We describe the generation of mutant strains of the avilamycin producer defective ...

Background: Streptomyces viridochromogenes Tü57 is the producer of avilamycin A. The antibiotic consists of a heptasaccharide side chain and a polyketide-derived dichloroisoeverninic acid as aglycone. Molecular cloning and characterization of the genes governing the avilamycin A biosynthesis is...

A HPLC method is described for the simultaneous determination of avilamycin A and B in pig faeces, following extraction using acetonitrile and normal-phase solid phase extraction. The HPLC stationary phase was Kromosil 5 μ C-18 with a mobile phase of 48% acetonitrile and 52% 0.01N ammonium acet...

The oligosaccharide antibiotics avilamycin A and C are produced by Streptomyces viridochromogenes Tü57. Both consist of a heptasaccharide chain, which is attached to a polyketide-derived dichloroisoeverninic acid moiety. They show excellent antibiotic activity against Gram-positive bacteria. Bo...

We assessed the putative link between avilamycin-resistant Enterococcus faecium carriage and avilamycin consumption in broilers. As part of the French programme of monitoring for antimicrobial resistance, broilers sampled at slaughterhouse in 1999 and 2000 and carrying avilamycin-resistant E. fa...

A sensitive and reliable method for determining the total avilamycin residues was developed using LC–MS/MS. Avilamycin (consisting of avilamycin A and 15 other minor factors) and its metabolites in porcine muscle, fat, and liver were analysed as the marker residue dichloroisoeverninic acid (DIA...