Viguilenin,a germacranolide from Viguiera linearis

The new germacranolide, viguilenin, was isolated from Viguiera linearis and its structure was established by chemical and spectroscopic means.     

Effects of lipoxin B on colony-forming capacity of human peripheral blood mononuclear cells in diffusion chambers

The lipoxin B (5, 14, 15-trihydroxy-6, 8, 10, 12-eicosatetraenoate) obtained by the enzymatic peroxidation of 5, 15-dihydroxy-6, 8, 11, 13-eicosatetraenoate (5, 15-DHETE) with the homogenous rabbit reticulocytes lipoxygenase and purified by HPLC stimulates the proliferation and differentiation of granulocyte-monocyte colony formation units (CFU-GMdc) of human peripheral blood at 3.6 X 10(-9) 3.6 X 10(-8)M in diffusion chamber placed in mouse abdominal cavity. The lipoxin B precursors namely 5,15-DHETE and arachidonic acid had stimulating influence at about 10(-6) and 10(-3)M respectively. The formation of polynuclear cells under the action of the studied lipoxygenase metabolites of the arachidonic acid was shown.     

Glutathione and ascorbic acid metabolism and antioxidant enzyme activity in the tissues of vitamin E-deficient rats

In has been shown in the experiments on male rats that alimentary vitamin E deficit causes the decrease of reduced glutathione and ascorbic acid concentration in the liver and lungs and that of glutathione-S-transferase, glutathione reductase in the liver and lungs, catalase in the liver and glutathione peroxidase in the heart activity, but increases the amount of glutathione disulfide in the liver and lungs and superoxide dismutase and gamma-glutamyltransferase activity in the liver. The data obtained show the selective character of reaction participants of the antioxidant system of rats' organism to the deficit of one of the antioxidant factors--vitamin E and also testify to complex interrelation between separate members of this system.     

Enzymatic antioxidant system of endotheliocytes

It is shown that endothelial cells from human umbilical vein have a reduced activity and gene expression of the “classic” antioxidant enzymes (Cu,Zn-superoxide dismutase, catalase, and Se-containing glutathione peroxidase). At the same time, a high expression level of peroxiredoxin genes was identified in the same endothelial cells, which obviously indicates the predominant involvement of these enzymes in protecting the endothelium from the damaging effect of free radical peroxidation.     

Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification

We previously reported the initial discovery of a novel class of stabilized benzylidene ketal M(2) receptor antagonists. This paper discusses new analogues consisting of benzamide modifications which not only improved M(2) receptor affinity and selectivity, but also enhanced the pharmacokinetic properties of the series. These changes led to the discovery of a highly potent and selective M(2) antagonist, which demonstrated in vivo efficacy and had good bioavailability in multiple species.