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1. The gastroprotective activity of two azomethine prodrugs of (R)-alpha-methylhistamine was examined in lesions induced by absolute ethanol (1 ml/rat intragastrically for 1 h). 2. Pretreatment with (R)-alpha-methylhistamine as well as with the prodrugs (30 and 100 mg/kg intragastrically [IG]) significantly reduced macroscopically visible lesions caused by ethanol, with protection being almost complete at 100 mg/kg. 3. Histologically, in rats pretreated with the three compounds at a dose of 100 mg/kg, the evidence of damage was rare, with the appearance of gastric mucosa being similar in the different groups. 4. Present results are suggestive of a local component in the protective activity of (R)-alpha-methylhistamine.

AbstractThe efficacy of thyroid (FNAB) processed by liquid‐based cytology (LBC) in Hashimoto's Thyroiditis (HT) in two reference periods, is evaluated. The morphologic features of 820 cases with both methods and the cyto‐histological comparison are analyzed. The diagnosis of hyperplastic nodules (HN) in HT, its mimickers especially in presence of oxyphilic cells and the role of immunocytochemistry (IHC) are studied.150 cases of HT processed by conventional smear (CS) in 1996–98 and 670 with LBC in 2005–2007,were included. The majority of FNAB were carried out under USguidance and fixed with ethyl alcohol for the CS. LBC material was rinsed in the Cytolit solution, processed according to the manufacturer's recommendations. Among the 150 CS, 83 were HT while 67 were HN in HT; in the second triennium 245 LBC were HT and 425 were HN in HT. In the first period a follow‐up (including a second FNA or surgery) was done in 92 cases, in the second period in 116.In the surgical group 97.1% in the first period were benign (all HT and 34/36 HN) and 2.8% malignant(all HN). In 2005–2007, 94% were benign (15 HT and 45/49 HN) and 6%malignant. Thirty HN from the second triennium had ICC for HBME‐1 and Galectin‐3 resulting negative in 93.5%. Among these cases, 10 had a benign histology and a concordant negative ICC.LBC can be used as a valid method for HT, especially for the possible application of ICC to HN, and it allows a correct preoperative selection of lesions Diagn. Cytopathol. 2011; © 2011 Wiley‐Liss, Inc.

We report the effect of ethanol on monooxygenase activities in primary hamster hepatocyte cultures maintained on collagen-coated dishes. The addition of 50mM ethanol to cell cultures both from control and ethanol pretreated animals almost completely maintained, at least for 72hr, the P4502E1-dependent aniline hydroxylase (AnH) activity and the 2E1 immunodetectable apoprotein content at the levels of the corresponding 4-hr plated hepatocytes. On the contrary, other P450-dependent monooxygenase activities, as assayed by testosterone hydroxylases, kept decreasing falling-after 72hr of culture-to the levels of the 4-hr plated hepatocytes. In both cases, in the absence of ethanol, a rapid decline of AnH activities and 2E1 apoprotein contents were also observed, attaining undetectable levels at 72hr. The hybridizable 2E1 mRNA also rapidly declined in both cultures, but such decline was not significantly altered by the presence of 50mM ethanol in the culture medium. Furthermore, we show that P4502E1 in the liver possesses a rapid degradation phase with a half-life of about 6hr. Thus, in the hamster, P4502E1 appears regulated at post-translational level, as in rat, probably by a protein stabilization mechanism.

Thirty four crude extracts of Panamanian plants, from nine species of Celastraceae and Lamiaceae, were assayed for xanthine oxidase (XO) inhibitory activity. The enzymatic activity was estimated by measuring the increase in absorbance at 290 nm due to uric acid formation. Eighty five percent of the crude extracts were found to possess XO inhibitory activity at 50 micrograms/ml and all the extracts of the species from Lamiaceae were active even at 1 micrograms/ml. The ethanol extracts of Hyptis obtusiflora Presl ex Benth. (Lamiaceae) and H. lantanaefolia Poit. (Lamiaceae) exhibited the highest activity with an inhibition of approximately 40% at 1 micrograms/ml.

The main system of central ethanol (EtOH) oxidation is mediated by the enzyme catalase. By reacting with H2 O2 , brain catalase forms compound I (the catalase-H2 O2 system), which is able to oxidize EtOH to acetaldehyde (ACD) in the brain. We have previously shown that ACD regulates EtOH motivational properties and possesses reinforcing effects by itself. In this study, we investigate the effects of alpha-lipoic acid (ALA), a scavenging agent for H2 O2 , on oral EtOH self-administration.To this end, we trained Wistar rats to orally self-administer EtOH (10%) by nose poking. The effect of intraperitoneal pretreatment with ALA was evaluated during (i) maintenance of EtOH self-administration, (ii) EtOH self-administration under a progressive ratio (PR) schedule of reinforcement, and (iii) oral EtOH priming to induce reinstatement of EtOH seeking behavior. Moreover, we tested the effect of ALA on saccharin (0.05%) reinforcement, as assessed by oral self-administration.The results indicate that ALA dose-dependently reduced the maintenance, the break point of EtOH self-administration under a PR and the reinstatement of EtOH seeking behavior without suppressing saccharin self-administration.These results support that ALA may have a potential use in alcoholism treatment.

Acute oral administration of ethanol (3.2g/kg) to rats increased (DOPAC) levels in the caudate nucleus, but had no effect on DOPAC levels in the substantia nigra and frontal cortex and failed to modify dopamine content in any of the above areas. On the other hand, the administration of the same dose of ethanol to rats which had been chronically treated with ethanol (3.2g/kg daily for 60 days), produced a decrease of DA content and a parallel increase of DOPAC levels in all areas studied. In chronically treated rats, 24 hrs after last ethanol administration dopamine levels in the frontal cortex were 60% higher than in controls. The results suggest that ethanol administration causes dopamine release in different brain areas.

The interaction between quercetin and lipoxygenase was investigated by fluorescence spectroscopy. The analysis of the emission quenching at different temperatures revealed that the quenching mechanism correspond to a static process and, as consequence, a complex quercetin-lipoxygenase is formed. The thermodynamic parameters ΔG, ΔH and ΔS were calculated to be-32.57 kJ mol(-1),-3.21 kJ mol(-1) and 87.14 J mol(-1) K(-1) respectively, which suggest that hydrophobic forces plays a major role in the stabilization of the complex quercetin-lipoxygenase. The distance, r, between donor (lipoxygenase) and acceptor (quercetin) was calculated to be 3.84 nm based on Förster's non-radiative energy transfer theory. The results obtained from the evaluation of three dimensional florescence spectra suggest a conformational modification of the protein in the region of the coupling with quercetin.