Synthesis and biological evaluation of 4,5-dihydro-1H-pyrazole derivatives as potential nNOS/iNOS selective inhibitors. Part 2: Influence of diverse substituents in both the phenyl moiety and the acyl group

In a preliminary article, we reported a series of 4,5-dihydro-1H-pyrazole derivatives as neuronal nitric oxide synthase (nNOS) inhibitors. Here we present the data about the inhibition of inducible nitric oxide synthase (iNOS) of these compounds. In general, we can confirm that these pyrazoles are nNOS selective inhibitors. In addition, taking these compounds as a reference, we have designed and synthesized a series of new derivatives by modification of the heterocycle in 1-position, and by introduction of electron-donating or electron-withdrawing substituents in the aromatic ring. These derivatives have been evaluated as nNOS and iNOS inhibitors in order to identify new compounds with improved activity and selectivity. Compound 3r, with three methoxy electron-donating groups in the phenyl moiety, is the most potent nNOS inhibitor, showing good selectivity nNOS/iNOS.     

Synthesis,antiproliferative and mitochondrial impairment activities of bis-alkyl-amino transplatinum complexes

A convenient synthetic route and the characterization of complexes trans-[PtCl₂(L)(PPh₃)] (L = Et₂NH (2), (PhCH₂)₂NH (3), (HOCH₂CH₂)₂NH) (4) are reported. The antiproliferative activity was evaluated on three human tumor cell lines. The investigation on the mechanism of action highlighted for the most active complex 4 the capacity to affect mitochondrial functions. In particular, both the induction of the mitochondrial permeability transition phenomenon and an aspecific membrane damage occurred, depending on concentration.     

Reservoir to river passage of age‐0+ year fishes,indication of a dispersion pathway for a non‐native species

This study demonstrates passage of age‐0+ year individuals of pikeperch Sander lucioperca, common bream Abramis brama and non‐native tubenose goby Proterorhinus semilunaris from the Nové Mlýny Reservoir into the River Dyje (Danube River basin, Czech Republic) through the turbine of a hydropower facility. Most fishes had standard length (L_S) in the range 12–33 mm. Seasonal patterns corresponded with spawning activity, i.e. an early single spawning event for S. lucioperca, multiple spawning events for A. brama and continuous spawning with a later start and prolonged duration for P. semilunaris. Sander lucioperca, P. semilunaris and larger A. brama (>22 mm) drifted almost exclusively during the dark; smaller A. brama displayed no preference for light or dark. Proterorhinus semilunaris displayed significantly lower mortality than other species when passing through the turbine (3% compared to 18%). The passage of high numbers of P. semilunaris from the reservoir (estimated at 473 000 individuals per year), and their subsequent mass downstream drift, may have contributed to rapid population establishment along the River Dyje and the quick downstream expansion.     

Description of the larvae of Dicronocephalus wallichi bourgoini Coleoptera: Scarabaeidae: Cetoniinae) with observations on nesting behavior and life cycle of two Dicronocephalus species under laboratory conditions

Larva of the fruit beetle Dicronocephalus wallichi bourgoini Pouillaude 1914 is described and illustrated. The following unique morphological characters within Cetoniinae are discussed: shape of claw, spindle-shaped last antennomera, general body shape. The presence of metathoracic egg-bursters in the first instar larva has been found. Its significance for distinguishing the first instar larvae of Cetoniinae is discussed. The nesting behaviours of D. wallichi bourgoini and D. adamsi(Pascoe 1863) are described. The course of the life cycle of both species under laboratory condition is presented and discussed.     

Disruption of Cell-to-Cell Signaling Does Not Abolish the Antagonism of Phaeobacter gallaeciensis toward the Fish Pathogen Vibrio anguillarum in Algal Systems

Quorum sensing (QS) regulates Phaeobacter gallaeciensis antagonism in broth systems; however, we demonstrate here that QS is not important for antagonism in algal cultures. QS mutants reduced Vibrio anguillarum to the same extent as the wild type. Consequently, a combination of probiotic Phaeobacter and QS inhibitors is a feasible strategy for aquaculture disease control.     

Long‐term effects of climatic–hydrological drivers on macroinvertebrate richness and composition in two Mediterranean streams

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Antioxidant and prebiotic effects of dietary fiber co-travelers from sugar Kombu in healthy rats

The edible brown seaweed sugar Kombu (Saccharina latissima) is a good source of dietary fiber (DF) and associated compounds. Besides it presents antioxidant capacity in vitro due to their sulfated polysaccharides and polyphenols. The effect of a DF-rich sugar Kombu diet on biochemical parameters and antioxidant and prebiotic effects in healthy rats was evaluated. Thus, rats were fed either a basal diet or a supplemented one with 10 % sugar Kombu for 4 weeks. Several health-promoting effects were found such as a decrease in triglycerides (TGL) and uric acid (UrA), and an increase in antioxidant status both in serum and cecum. Regarding prebiotic effect, higher cecum weight and total short chain fatty acid (SCFA) content were evidenced in the seaweed-fed group, without significant differences on total bacterial count of feces. Sugar Kombu and sulfated polysaccharides from its DF could be used as functional ingredients for further nutraceutical applications.