A series of novel benzo[b]thiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1-one derivatives 6a-f, 7a-f and their corresponding alcohols 8a-f were synthesized and evaluated for their affinity towards 5-HT(1A) receptors. The influence of arylpiperazine moiety and benzo[b]thiophene ring substitutions on binding affinity was studied. The most promising analogue, 1-(benzo[b]thiophen-2-yl)-3-(4-(pyridi...

As test substances we selected naphthalene, benzo[a]pyrene and anthracene. Benzo[a]pyrene was selected, as the most common PAH required for the determination, as it is a component of most PAH mixtures and a procarcinogen, and is usually determined as an individual target PAH substance (http://water.epa.gov/drink/contaminants/basicinformation/benzo-a-pyrene.cfm). Naphthalene and anthracene are s...

The rote of prostaglandin endoperoxide synthetase in thà ̈ in vìvo activation of benzo(a)py rene to reactive metabolites capable of interacting irreversibly with cellular macromolecules was stud ied in guinea pig liver, lung, kidney, spleen, small intestine, colon, and brain. DNA and protein covalent binding experiments were made after systemic administration of acetylsalicylic acid (200 mg/kg)...

The metabolism of benzo(a)pyrene by human liver microsomes and human lymphocytes has been analyzed by high-pressure liquid chromatography. Human liver forms seven known metabolites and at least five additional unidentified metabolites that migrate as distinct peaks. Lymphocytes incubated with benzo(a)pyrene for 30 min do not form dihydrodiols. Lymphocytes incubated for 24 hr with benzo(a)pyrene...

Soil microorganisms play an important role in the degradation of PAHs and use various metabolic pathways for this process. The effect soil pH, different amendments co-cultivation fungi on activity ligninolytic enzymes was evaluated. For that purpose, three were studied: Trichoderma viride, Penicillium chrysogenum Agrocybe aegerita. Biodegradation assays with a mixture 200 ppm (fluorene, pyrene,...

The interactions of regular DNA and abasic site-containing DNA (AP-DNA) with quinolizinium (1a), the linearly fused benzo[b]quinolizinium (2a), the angularly fused benzo[a]quinolizinium (3a), benzo[c]quinolizinium (4a), and dibenzo[a,f]quinolizinium (5a) as well as derivatives thereof were studied with photometric and viscosimetric titrations (regular DNA), fluorimetric titrations and thermal D...

The hamster embryo cell bioassay has been used to study the effect of metal salts on morphological transformation. A synergistic enhancement of the transformation frequency was found for the combined treatment with organic carcinogens [benzo(a)pyrene, N-hydroxy-2-acetylaminofluorene, and 4-nitroquinoline 1-oxide] and nickel sulfate, cadmium acetate, or potassium chromate. Chromic chloride and z...

Human placenta is a readily available organ that responds to maternal environmental insult and has been previously used to investigate metabolism and bioactivation of procarcinogens, for example, benzo[a]pyrene. HPLC in combination with synchronous fluorescence spectroscopy was used to examine 28 placentas for the presence of benzo[a]pyrene diol epoxide-DNA adducts, and 10 of these were found t...

The in vitro oxidation of the two polycyclic aromatic hydrocarbons anthracene and benzo[a]pyrene, which have ionization potentials of <=7.45 eV, is catalyzed by laccases from Trametes versicolor. Crude laccase preparations were able to oxidize both anthracene and the potent carcinogen benzo[a]pyrene. Oxidation of benzo[a]pyrene was enhanced by the addition of the cooxidant 2,2(prm1)-azinobis(3-...

The present study was designed to determine the systemic influence of ultraviolet (UVB) irradiation upon subsequent carcinogenesis induced by benzo(a)pyrene. The source of UV irradiation consisted of six Westinghouse FS-40 fluorescent sunlamps. Female BALB/c mice received five 30-min dorsal UVB radiation treatments per week for 13 wk. At the end of 13 wk, irradiated and unirradiated mice receiv...