Showing papers in "Biochemical Pharmacology in 1995"

TL;DR: Upon intravenous administration to mice, 2-Ara-Gl caused the typical tetrad of effects produced by THC: antinociception, immobility, reduction of spontaneous activity, and lowering of the rectal temperature.

TL;DR: Information on NOS has increased to such an extent that this new commentary had to be restricted to some important biochemical aspects of the NOS enzymes, namely their protein and cDNA structure, their cellular distribution, and the mechanism controlling their expression.

TL;DR: The present data suggest that HIV-1 integrase inhibition may contribute to the antiviral activity of curcumin, and suggest new strategies for antiviral drug development that could be based uponCurcumin as a lead compound for the development of inhibitors of HIV- 1 integrase.

TL;DR: In vitro, curcumin inhibited lipopolysaccharide (LPS)-induced production of TNF and IL-1 by a human monocytic macrophage cell line, Mono Mac 6, and it was demonstrated thatCurcumin, at the corresponding concentration, inhibited LPS-induced activation of nuclear factor kappa B and reduced the biological activity of T NF in L929 fibroblast lytic assay.

TL;DR: The results suggest that gentamicin acts as an iron chelator, and that the iron-gentamicin complex is a potent catalyst of free radical formation.

TL;DR: Increased levels of ROIs, referred to as oxidative stress, are linked to pathophysiological phenomena because many adverse conditions, including ionizing and UV irradiation, heat shock, viral and bacterial infections, as well as environmental pollutants cause oxidative stress.

TL;DR: It is likely that cytochrome P450 is involved in the metabolism of CY, and the metabolite(s) that is generated may be more toxic and/or potent in inhibiting GSH synthesis.

TL;DR: It is found that prior intracellular reduction of TA to dihydrolipoic acid is not an obligatory mechanism for an antioxidant effect of the drug, which may also operate via Cu(2+)-chelation.

TL;DR: EGb 761 afforded protection against oxidative damage in all the systems the authors analyzed and is an efficient scavenger of peroxyl radicals, which supports the hypothesis of an antioxidant therapeutic action of EGb 7 61.

TL;DR: Results suggest that the molecular target of leflunomide action is DHODH, and the immunomodulating activity may be related to the inhibition of UMP synthesis in proliferating lymphocytes.

TL;DR: Examination of hepatic levels of mRNA for CYPs 1A2, 2C9, 2E1 and 3A4 by solution hybridization indicates that the disease-specific alterations of xenobiotic-metabolizing CYP enzymes among patients with cirrhosis is due, at least in part, to pre-translational mechanisms.

TL;DR: It is demonstrated that continuous exposure of human colon cancer cells to 5-FU leads to TS gene amplification and overexpression of TS protein with resultant development of fluoropyrimidine resistance.

TL;DR: Results indicate that oxygen radicals may have a central role to play in the induction of apoptosis and that dithiocarbamates can serve as potent inhibitors of apoptotic bodies induced by a wide variety of stimuli.

TL;DR: The allosteric properties of plasma membrane-bound NO synthase inhibited by Mn2+ (as reflected by changes in the Hill coefficient) were changed by cholesterol, consistent with modulations of the fluidity of the lipid microenvironment of the enzyme.

TL;DR: Data indicate that different pathways affecting cell proliferation and cell death are induced depending on whether selenium undergoes metabolism predominantly to hydrogen selenide or to methylselenol.

TL;DR: The results indicate that the three dihydrodiol dehydrogenases, as well as the two reductases, are implicated in the reduction of ketone-containing drugs in human liver cytosol.

TL;DR: The hybrid oligonucleotide was absorbed intact through the gastrointestinal tract, indicating the possibility of oral administration of olig onucleotides, a finding that may be important in the development of antisense oligon nucleotides as therapeutic agents.

TL;DR: It is concluded that age but not gender is a constitutional factor that influences the hepatic content of cytochrome P450 and selected CYP proteins.

TL;DR: In vitro studies confirmed that naringenin is a weak estrogen that also exhibits partial antiestrogenic activity in the female rat uterus and MCF-7 human breast cancer cells.

TL;DR: The pharmacokinetic parameters for GEM 91 in each tissue and biological fluids were calculated using computer-based two-compartmental i.v. bolus or absorption models to understand the pharmacology and toxicology of antisense oligodeoxynucleotide phosphorothioates, in general.

TL;DR: Evidence for the ATP-dependent transport of doxorubicin (DOX) obtained from the present in vivo and in vitro studies strongly indicates that P-gp in the brain capillaries functions actively as an efflux pump in the physiological state, providing a major mechanism to restrict the transfer of DOX into the brain.

TL;DR: The authors showed that glycolysis slowed down between the 60th and 120th minute of hypoxia, while EGb and bilobalide delayed the onset of glycoleysis activation.

TL;DR: MMP is a potent, tight-binding competitive inhibitor that does not discriminate between the two IMPDH isozymes.

TL;DR: Correlations of rates of theophylline 8-hydroxylation to 1,3-DU with other P450 form-specific activities, in a series of ten human liver microsomal preparations, revealed that at low concentrations the metabolism was catalyzed primarily by P4501A2, while at high substrate concentrations P4502E1 was primarily responsible for catalysis.

TL;DR: It is discovered that the putative EP1 receptor antagonist 6-isopropoxy-9-oxoxanthene-2-carboxylic acid (AH 6809) also has affinity for the human EP2 receptor, and behaved as an EP2 receptors antagonist and inhibited prostaglandin E2-stimulated increases in cyclic AMP.