The influence of prolonged clofibrate treatment on the plasma drug concentration and liver NADP-linked enzymes activity

The clofibric acid (CPIB) concentration in the rat blood plasma during 14 days of treatment with clofibrate and after cessation of the treatment, was measured and compared with the changes of some NADP-linked dehydrogenases activity. CPIB rapidly accumulates in the plasma during the first two days of clofibrate administration reaching a maximum concentration of about 0.6 mM. Then a linear decrease of the drug concentration was observed. The second day after clofibrate treatment had been completed, CPIB could no longer be detected in the plasma. Liver malic enzyme activity increased constantly up to the third day after cessation of the treatment. There was a decrease of activity which reached its control level on the 32nd day of the experiment. The variation patterns of hexose monophosphate shunt dehydrogenases activity and liver weight were similar to the changes of malic enzyme activity.     

Microbial transformation of azacarbazoles. I. N-methylation of alpha-, beta-, and gamma-carbolines by Kitasatosporia setae strain

Microbial transformation of selected azacarbazoles, compounds noted for their activity as antitumor agents, conducted with Kitasatosporia setae strain resulted in N-methylation of pyridine nucleus of alpha-, beta- and gamma-carboline molecule. Formed quaternized intermediates were converted in alkaline conditions into corresponding iso-carbolines. The structure of the final products, alpha-, beta- and gamma-iso-carbolines have been established on the basis of spectral data and confirmed by chemical synthesis.     

Mechanisms of enhanced carbohydrate and lipid metabolism in adipose tissue in uremia.

OBJECTIVE: Hyperlipidemia is a permanent finding in advanced renal failure. It is supposed to be responsible for the accelerated arteriosclerosis and cardiovascular complications observed in patients with that disease. The background is partially determined, however, our knowledge in this matter is not yet satisfactory. METHODS: This study is based on the experimental rat model of chronic renal failure (CRF). Considering white adipose tissue (WAT) lipogenesis upregulation in CRF, along with the determination of acetyl coenzyme A carboxylase (ACC) and fatty acid synthase (FAS) genes expression, we have measured WAT gene expression for sterol regulatory binding protein 1 (SREBP-1) at the level of protein mass and mRNA abundance. Furthermore, we have determined glucose uptake, glucose-to-CO 2 conversion rate, and glucose translocator (GLUT-4) gene expression in WAT. RESULTS: Upregulation of both FAS and ACC gene expression was found in WAT of CRF rats. It was accompanied by WAT SREBP-1 gene overexpression. Moreover, we have observed the increased glucose uptake, glucose to CO 2 conversion rate, and GLUT-4 gene expression in WAT of CRF rats in comparison with controls. CONCLUSION: SREBP-1 gene overexpression may contribute to enhanced lipogenesis upregulation in WAT of CRF rats. It is not excluded that the increased WAT glucose metabolism activity is also induced by this mechanism, although there is no evidence currently to that end. We hypothesize that the increased WAT lipogenesis capacity could be a part of mechanism(s) leading to CRF-induced hyperlipidemia.     

Applying the posterior fasciocutaneous thigh flap in bed sores treatment]

The paper presents the possibilities of applying the posterior thigh flap in the treatment of ischial pressure sores. Between 2000 and 2004 the flap was used in three cases treated in the Orthopaedics and Traumatology Department of the Medical Universtity in Bialystok. The indications, contraindications, operative technique and advantages of the posterior thigh flap are described. In all three cases the ischial bed sores healed well without recurrences. The posterior fasciocutaneous pedicled flap is a good method of treatment for not too extensive bed sores in the ischial region.This flap can be applied in recurrences found after primary bed sore treatment with another method. However the fasciocutaneous flap has a limited range of transposition as compared with cutaneous flaps.     

Effect of polyacid aqueous solutions on photocuring of polymerizable components of resin-modified glass ionomer cements.

OBJECTIVES: Resin-modified glass ionomer cements (RMGI) are hybrid materials prepared by incorporation of polymerizable components (typically 2-hydroxyethyl methacrylate (HEMA) with possible addition of multifunctional methacrylates) into a conventional acid-base mixture (a polymeric acid with powdered calcium fluoro-aluminosilicate glasses). During setting, the photopolymerization process and the acid-base reaction affect each other. The aim of this work was to examine the effect of a 45% aqueous solution of poly(acrylic acid) (PAA) and the liquid component of a commercial glass ionomer cement on HEMA and triethyleneglycol dimethacrylate (TEGDMA) photopolymerization. METHODS: The polymerization was initiated by 2,2-dimethoxy-2-phenylacetophenone (DMPA) and camphorquinone (CQ)/coinitiator system. The reaction course was monitored under Ar and air by isothermal differential scanning calorimetry. RESULTS: The main effect of addition of polyacid solution (PAA and commercial) up to 10wt% to HEMA on the polymerization initiated with DMPA was earlier onset of autoacceleration. For the process initiated by the CQ-based system, the addition of 5wt% of PAA solution strongly accelerated the polymerization and increased the conversion, both in Ar atmosphere as well as in air. TEGDMA photopolymerization was not influenced or slightly retarded by the presence of 3wt% of PAA solution (the upper limit of solubility), depending on the initiating system used. SIGNIFICANCE: Under initiation conditions used in curing of commercial dental products (CQ-based two component initiating system), the presence of polyacid-aqueous solution in HEMA-based photocurable component increases markedly the polymerization rate and the conversion both in Ar atmosphere as well as in air. This result contributes to a characterization of the setting process of RMGIs.     

Synthesis and anticonvulsant properties of some arylsuccinate methylpyridylimides

In reaction of alpha-phenyl, alpha-p-chlorophenyl and alpha-m-chlorophenylsuccinic acid with various aminopyridines, N-pyridyl-substituted succinimides (compounds 1-14) were obtained. These compounds were investigated for their CNS activity. Compounds 1, 2, 5, 6 and 7 displayed anticonvulsant properties in the maximum electroshock test. Compounds 5 and 6 were also active in the pentetrazole test.