Synthesis and antiprotozoal activity of nitazoxanide–N-methylbenzimidazole hybrids

A series of a novel hybrid compounds between nitazoxanide and N-methylbenzimidazole were synthesized starting from the corresponding N-methyl-2-nitroanilines. The new hybrid compounds (1–13) were evaluated in vitro against Giardia intestinalis, Entamoeba histolytica, Trichomonas vaginalis. NTZ, MTZ and ABZ were used as drug standards. Experimental evaluations revealed all of the new compounds (1–13) were active and showed strong activity against the three protozoa, particularly with E. histolytica where the IC₅₀ values ranged between 3 and 69 nM.Overall, compounds 2, 5, 7, 8, 9, 11 and 12 stood out with values lower than 87 nM for all three protozoa, comparatively better than the reference drugs.     

Soil Properties and Olive Cultivar Determine the Structure and Diversity of Plant-Parasitic Nematode Communities Infesting Olive Orchards Soils in Southern Spain

This work has studied for the first time the structure and diversity of plant-parasitic nematodes (PPNs) infesting olive orchard soils in a wide-region in Spain that included 92 locations. It aims at determining which agronomical or environmental factors associated to the olive orchards are the main drivers of the PPNs community structure and diversity. Classical morphological and morphometric identification methods were used to determine the frequency and densities of PPNs. Thirteen families, 34 genera and 77 species of PPNs were identified. The highest diversity was found in Helicotylenchus genus, with six species previously reported in Spain and with H. oleae being a first report. Neodolichorhynchus microphasmis and Diptenchus sp., Diphtherophora sp., and Discotylenchus sp., usually considered fungal feeders, were also reported for the first time associated to olive rhizosphere. PPNs abundance ranged from 66 to 16,288 individuals/500-cm³ of soil with Helicotylenchus digonicus being the most prevalent species, followed by Filenchus sp., Merlinius brevidens and Xiphinema pachtaicum. Nematode abundance and diversity indexes were influenced by olive cultivar, and orchard and soil management practices; while olive variety and soil texture were the main factors driving PPN community composition. Soil physicochemical properties and climatic characteristics most strongly associated to the PPN community composition included pH, sand content and exchangeable K, and maximum and minimum average temperature of the sampled locations. Our data suggests that there is a high diversity of PPNs associated to olive in Southern Spain that can exert different damage to olive roots depending on the olive variety and their abundance. Further analysis to determine the resistance levels of most common olive varieties to the prevalent PPNs in Spain will help to choose the most appropriate ones for the establishment of new plantations. This choice will take into consideration the specific soils and environments where those olive varieties will be established.     

Photolysis of water coupled to nitrate reduction by Nostoc muscorum subcellular particles.

The binding of tritiated guanylylimidodiphosphate ([³H]GMP-P(NH)P) to turkey erythrocyte ghosts was studied in parallel with the activation by GMP-P(NH)P of adenylate cyclase. The high affinity binding capacity for GMP-P(NH)P, 50 pmoles per mg protein, exceeds the estimated quantity of adenylate cyclase of 1 pmole per mg of protein. The rate of nucleotide binding is not affected by isoproterenol. Further, in the presence of the hormone the rate of binding is much slower than the rate of activation. Although the rate of dissociation of bound [³H]GMP-P(NH)P is negligible at 37°, it is increased dramatically by unlabeled GMP-P(NH)P, GTP, EDTA, ATP, AMP-P(CH₂)P, or p-aminophenylmercuric acetate. In contrast, the rate of decay of the GMP-P(NH)P-simulated state is not altered by these agents. Thus, the major fraction of GMP-P(NH)P binding to membranes is not relevant to cyclase activation.     

Fuzzy Index to Evaluate Edge Detection in Digital Images

In literature, we can find different metrics to evaluate the detected edges in digital images, like Pratt''s figure of merit (FOM), Jaccard’s index (JI) and Dice’s coefficient (DC). These metrics compare two images, the first one is the reference edges image, and the second one is the detected edges image. It is important to mention that all existing metrics must binarize images before their evaluation. Binarization step causes information to be lost because an incomplete image is being evaluated. In this paper, we propose a fuzzy index (FI) for edge evaluation that does not use a binarization step. In order to process all detected edges, images are represented in their fuzzy form and all calculations are made with fuzzy sets operators and fuzzy Euclidean distance between both images. Our proposed index is compared to the most used metrics using synthetic images, with good results.     

The Effect of Copper on the Color of Shrimps: Redder Is Not Always Healthier

The objective of this research is to test the effects of copper on the color of pacific white shrimp (Litopenaeus vannamei) in vivo. Forty-eight shrimps (L. vannamei) were exposed to a low concentration of copper (1 mg/L; experimental treatment) and forty-eight shrimps were used as controls (no copper added to the water). As a result of this experiment, it was found that shrimps with more copper are significantly redder than those designated as controls (hue _{(500–700 nm)}: P = 0.0015; red chroma _{(625–700 nm)}: P<0.0001). These results indicate that redder color may result from exposure to copper and challenge the commonly held view that highly pigmented shrimps are healthier than pale shrimps.     

Multivariate stabilizing sexual selection and the evolution of male and female genital morphology in the red flour beetle*

Male genitals are highly divergent in animals with internal fertilization. Most studies attempting to explain this diversity have focused on testing the major hypotheses of genital evolution (the lock-and-key, pleiotropy, and sexual selection hypotheses), and quantifying the form of selection targeting male genitals has played an important role in this endeavor. However, we currently know far less about selection targeting female genitals or how male and female genitals interact during mating. Here, we use formal selection analysis to show that genital size and shape is subject to strong multivariate stabilizing sexual selection in both sexes of the red flour beetle, Tribolium castaneum. Moreover, we show significant sexual selection on the covariance between the sexes for specific aspects of genital shape suggesting that male and female genitalia also interact to determine the successful transfer of a spermatophore during mating. Our work therefore highlights the important role that both male and female genital morphologies play in determining mating success and that these effects can occur independently, as well as through their interaction. Moreover, it cautions against the overly simplistic view that the sexual selection targeting genital morphology will always be directional in form and restricted primarily to males.     

Evolution of carotenoid metabolic capabilities during the early development of the European lobster Homarus gammarus (Linné, 1758)

The quantification of carotenoids during the early developmental stages of the European lobster Homarus gammarus, indicates a rapid decrease of pigment concentration, occurring immediately after hatching. Conversely, the carotenoid amount of the individual increases progressively at the end of larval stage I, as a result of an enhanced feeding activity. Free astaxanthin represents the bulk of carotenoids of the unhatched embryo (metanauplius), whereas larval, post-larval and juvenile stages exhibit the typical adult carotenoid pattern, in which astaxanthin esterified forms (diester and monoester) appear preponderant. The Artemia strain used as food material is not found to contain astaxanthin, while important amounts of canthaxanthin are observed; nevertheless, this carotenoid is not detected in the larvae, indicating that metabolic transformation capabilities are already occurring in freshly hatched individuals.     

Calcineurin-mediated Dephosphorylation of Synaptotagmin VI Is Necessary for Acrosomal Exocytosis

Regulated secretion is a fundamental process underlying the function of many cell types. In particular, acrosomal exocytosis in mammalian sperm is essential for egg fertilization. In general, exocytosis is initiated by a cytosolic calcium increase. In this report we show that calcium affects several factors during human sperm acrosomal exocytosis. By using an antibody that specifically recognizes synaptotagmin VI phosphorylated at the polybasic region of the C2B domain, we showed that a calcium-dependent dephosphorylation of this protein occurred at early stages of the acrosomal exocytosis in streptolysin O-permeabilized sperm. We identified the phosphatase as calcineurin and showed that the activity of this enzyme is absolutely required during the early steps of the secretory process. When added to sperm, an inhibitor-insensitive, catalytically active domain of calcineurin was able to rescue the effect of the specific calcineurin inhibitor cyclosporin A. This same domain dephosphorylated recombinant synaptotagmin VI C2B domain, validating this protein as a new substrate for calcineurin. When sperm were treated with catalytically active calcineurin before stimulation, exocytosis was inhibited, an effect that was rescued by the phosphomimetic synaptotagmin VI C2B-T418E,T419E mutant domain. These observations indicate that synaptotagmin must be dephosphorylated at a specific window of time and suggest that phosphorylated synaptotagmin has an active role at early stages of the acrosomal exocytosis.