Anti-Helicobacter pylori agents endowed with H2-antagonist properties

New anti-Helicobacter pylori (H. pylori) agents endowed with H2-antagonists properties were obtained by combining the lamtidine derived pharmacophoric group with the antibiotic calvatic acid. All the compounds were tested for their irreversible H2-antagonist properties and for their ability to inhibit 20 H. pylori strains, two of them metronidazole resistant. The most active derivative (compound 4) displayed antimicrobial activity similar to metronidazole.     

A description of ammonium content of output waters from trout farms in relation to stocking density and flow rates

Daily levels of ammonium content in the outflow water of an intensive trout farm and of a mountain pond stocked with rainbow trout were monitored. Output water was sampled for 30 days and analysed every 30 min by an automatic ion selective electrode system (Applikon ADI 2013); input water was also monitored. The ammonium output level was influenced more by atmospheric events than nitrogen excretion by fish. Observed data confirmed an overall ammonium excretion model previously estimated in both laboratory and field conditions. The high water flow, that characterises the intensive trout farm where the observations were made induced a high dilution of metabolites. Consequently, if the peaks of ammonium output did not reach values of 0.35–0.40 mg l⁻¹ the environmental impact was limited and not easily detected. Our results allow us to affirm that the optimal level of water flow rate for effective zeolite-operated filtration is around 10.3 l t⁻¹ s⁻¹.     

PCR–RFLP analysis of mitochondrial DNA in tench Tinca tinca

Polymorphism was detected at ND1, ND6, D‐loop and cyt b segments of mtDNA in 105 tench (Tinca tinca L.), using the polymerase chain reaction–restriction fragment length polymorphism (PCR–RFLP) technique and five composite haplotypes were identified. The diversity indices and the results of the population comparisons revealed that the identified markers provide a powerful tool for further studies on this species.     

Furoxan analogues of the histamine H3-receptor antagonist imoproxifan and related furazan derivatives

Synthesis and pharmacological characterisation of a series of compounds in which the oxime substructure present in imoproxifan was constrained in the pentatomic NO-donor furoxan ring, as well as their structurally related furazan analogues devoid of NO-donating properties, are described. The whole series of products displayed reversible histamine H3-antagonistic activity on guinea-pig ileum. 4-(4-(3-(1H-Imidazol-4-yl)propoxy)phenyl)furoxan-3-carbonitrile 16 was also able to induce partial relaxation when added to the bath after electrical contraction of the guinea-pig ileum during the study of its H3-antagonistic properties. This phenomenon seems to be dependent on NO-mediated sGC activation. The lipophilic-hydrophilic balance of all the products was investigated.     

How Different Dietary Methionine Sources Could Modulate the Hepatic Metabolism in Rainbow Trout?

In aquafeeds in which plant proteins are used to replace fishmeal, exogenous methionine (Met) sources are demanded to balance the amino acid composition of diets and meet the metabolic fish requirements. Nonetheless, since different synthetic Met sources are commercially available, it is important to determine their bioavailability and efficacy. To address this issue, we conducted a two-month feeding trial with rainbow trout (Oncorhynchus mykiss), which were fed diets supplemented with five different forms of Met: Met-Met, L-Met, HMTBa, DL-Met, and Co DL-Met. No differences in growth performance were found in trout fed with different Met forms, but changes in the whole-body composition were found. In particular, Met-Met and L-Met promoted a significant body lipid reduction, whereas the protein retention was significantly increased in fish fed with HMTBa and Co DL-Met. The latter affected the hepatic Met metabolism promoting the trans-sulfuration pathway through the upregulation of CBS gene expression. Similarly, the L-Met enhanced the remethylation pathway through an increase in BHMT gene expression to maintain the cellular demand for Met. Altogether, our findings suggest an optimal dietary intake of all tested Met sources with similar promoting effects on fish growth and hepatic Met metabolism. Nevertheless, the mechanisms underlying these effects warrant further investigation.     

In vitro effect of caffeine on some aspects of nitrogen metabolism in isolated rat hepatocytes

Long-term exposure to high doses of caffeine affects several aspects of nitrogen metabolism, such as purine, pyrimidine and urea synthesis. However, little is known about the mechanisms of these changes and if they occur at shorter term. We have studied in isolated hepatocytes: 1) the in vitro effect of high doses of caffeine on amino acid levels, 2) the main destination of ammonia and carbon chains from amino acid catabolism, and 3) the cytosolic and mitochondrial redox states. We have found that, whereas it has a small effect on urea synthesis and on the levels of the cofactors and intermediates, it decreases the levels of several amino acids, the gluconeogenesis and the redox state. Our results suggest that a longer exposure to caffeine is necessary to affect the normal functions of some metabolic pathways.