Synthesis, antimicrobial activity, and QSAR studies of furan-3-carboxamides

The synthesis and characterization of a new series of furan-3-carboxamides, from the aromatization of 4-trichloroacetyl-2,3-dihydrofuran to 3-trichloroacetyl furan followed by nucleophilic displacement of the trichloromethyl group or the corresponding carboxylic acid chloride by nitrogen-containing compounds, is presented. Preliminary in vitro antimicrobial activity of the title compounds was assessed against a panel of microorganisms including yeast, filamentous fungi, bacteria, and alga. Some of the furan-3-carboxamides exhibited significant in vitro antimicrobial activity. QSAR investigation was applied to find a correlation between the different physicochemical parameters of the compounds studied and their biological activity.     

Breath air analysis and its use as a biomarker in biological monitoring of occupational and environmental exposure to chemical agents

The analysis of exhaled air has several advantages since it is a noninvasive method applicable to a large number of toxic agents, in addition to being a simpler matrix than those of other biological samples such as urine and blood. However, it presents some challenges, such as the necessity of a more sensitive sampling procedure, since the chemical substances eliminated through exhaled air are unchanged in form, not being metabolized, and exhaled compounds are present at extremely low concentrations, i.e. in the nanomolar range. To improve the sensitivity and precision of measurement of the concentration of these substances in exhaled air, the sample usually has to be concentrated before assay by gas chromatography. To this end, the use of the solid-phase microextraction (SPME) technique has been proposed as an efficient sampling method. This paper presents a revision of breath analysis as a biomarker for occupational and environmental exposure to chemicals. The sampling methods and the potential use of SPME for determining chemical substances in exhaled air are discussed.     

CALCIUM‐INDUCED LIPID PEROXIDATION IS MEDIATED BY RHODNIUS HEME‐BINDING PROTEIN (RHBP) AND PREVENTED BY VITELLIN

Lipid peroxidation is promoted by the quasi‐lipoxygenase (QL) activity of heme proteins and enhanced by the presence of free calcium. Unlike mammalian plasma, the hemolymph of Rhodnius prolixus, a vector of Chagas disease, contains both a free heme‐binding protein (RHBP) and circulating lipoproteins. RHBP binds and prevents the heme groups of the proteins from participating in lipid peroxidation reactions. Herein, we show that despite being bound to RHBP, heme groups promote lipid peroxidation through a calcium‐dependent QL reaction. This reaction is readily inhibited by the presence of ethylene glycol tetraacetic acid (EGTA), the antioxidant butylated hydroxytoluene or micromolar levels of the main yolk phosphoprotein vitellin (Vt). The inhibition of lipid peroxidation is eliminated by the in vitro dephosphorylation of Vt, indicating that this reaction depends on the interaction of free calcium ions with negatively charged phosphoamino acids. Our results demonstrate that calcium chelation mediated by phosphoproteins occurs via an antioxidant mechanism that protects living organisms from lipid peroxidation.     

Evaluation of Cytotoxic and Anti-Inflammatory Activities of Extracts and Lectins from Moringa oleifera Seeds

Background

The extract from Moringa oleifera seeds is used worldwide, especially in rural areas of developing countries, to treat drinking water. M. oleifera seeds contain the lectins cmol and WSMoL, which are carbohydrate-binding proteins that are able to reduce water turbidity because of their coagulant activity. Studies investigating the ability of natural products to damage normal cells are essential for the safe use of these substances. This study evaluated the cytotoxic and anti-inflammatory properties of the aqueous seed extract, the extract used by population to treat water (named diluted seed extract in this work), and the isolated lectins cmol and WSMoL.

Methodology/Principal Findings

The data showed that the aqueous seed extract and cmol were potentially cytotoxic to human peripheral blood mononuclear cells, while WSMoL and diluted seed extract were not cytotoxic. The M. oleifera aqueous seed extract and the lectins cmol and WSMoL were weakly/moderately cytotoxic to the NCI-H292, HT-29 and HEp-2 cancer cell lines and were not hemolytic to murine erythrocytes. Evaluation of acute toxicity in mice revealed that the aqueous seed extract (2.000 mg/kg) did not cause systemic toxicity. The aqueous seed extract, cmol and WSMoL (6.25 µg/mL) and diluted seed extract at 50 µg/mL exhibited anti-inflammatory activity on lipopolyssaccharide-stimulated murine macrophages by regulating the production of nitric oxide, TNF-α and IL-1β. The aqueous seed extract reduced leukocyte migration in a mouse model of carrageenan-induced pleurisy; the myeloperoxidase activity and nitric oxide, TNF-α and IL-1β levels were similarly reduced. Histological analysis of the lungs showed that the extract reduced the number of leukocytes.

Conclusion/Significance

This study shows that the extract prepared according to folk use and WSMoL may be non-toxic to mammalian cells; however, the aqueous seed extract and cmol may be cytotoxic to immune cells which may explain the immunosuppressive potential of the extract.     

A new species of <Emphasis Type="Italic">Philodendron</Emphasis> Schott (<Emphasis Type="Italic">Araceae</Emphasis>) from Brazil — correction

Summary  Due to an oversight, the name Philodendron millerianum, was not validly published in a recent paper by Coelho & Sakuragui (2007). This error is corrected here and the location of the holotype and isotype confirmed.     

Can the Understory Affect the Hymenoptera Parasitoids in a Eucalyptus Plantation?

The understory in forest plantations can increase richness and diversity of natural enemies due to greater plant species richness. The objective of this study was to test the hypothesis that the presence of the understory and climatic season in the region (wet or dry) can increase the richness and abundance of Hymenoptera parasitoids in Eucalyptus plantations, in the municipality of Belo Oriente, Minas Gerais State, Brazil. In each eucalyptus cultivation (five areas of cultivation) ten Malaise traps were installed, five with the understory and five without it. A total of 9,639 individuals from 30 families of the Hymenoptera parasitoids were collected, with Mymaridae, Scelionidae, Encyrtidae and Braconidae being the most collected ones with 4,934, 1,212, 619 and 612 individuals, respectively. The eucalyptus stands with and without the understory showed percentage of individuals 45.65% and 54.35% collected, respectively. The understory did not represent a positive effect on the overall abundance of the individuals Hymenoptera in the E. grandis stands, but rather exerted a positive effect on the specific families of the parasitoids of this order.     

Seascape drivers of Macrocystis pyrifera population genetic structure in the northeast Pacific

At small spatial and temporal scales, genetic differentiation is largely controlled by constraints on gene flow, while genetic diversity across a species' distribution is shaped on longer temporal and spatial scales. We assess the hypothesis that oceanographic transport and other seascape features explain different scales of genetic structure of giant kelp, Macrocystis pyrifera. We followed a hierarchical approach to perform a microsatellite‐based analysis of genetic differentiation in Macrocystis across its distribution in the northeast Pacific. We used seascape genetic approaches to identify large‐scale biogeographic population clusters and investigate whether they could be explained by oceanographic transport and other environmental drivers. We then modelled population genetic differentiation within clusters as a function of oceanographic transport and other environmental factors. Five geographic clusters were identified: Alaska/Canada, central California, continental Santa Barbara, California Channel Islands and mainland southern California/Baja California peninsula. The strongest break occurred between central and southern California, with mainland Santa Barbara sites forming a transition zone between the two. Breaks between clusters corresponded approximately to previously identified biogeographic breaks, but were not solely explained by oceanographic transport. An isolation‐by‐environment (IBE) pattern was observed where the northern and southern Channel Islands clustered together, but not with closer mainland sites, despite the greater distance between them. The strongest environmental association with this IBE pattern was observed with light extinction coefficient, which extends suitable habitat to deeper areas. Within clusters, we found support for previous results showing that oceanographic connectivity plays an important role in the population genetic structure of Macrocystis in the Northern hemisphere.     

Gene silencing in Fucus embryos: developmental consequences of RNAi‐mediated cytoskeletal disruption

Brown algae (Phaeophyceae) are an important algal class that play a range of key ecological roles. They are often important components of rocky shore communities. A number of members of the Fucales and Ectocarpales have provided models for the study of multicellular evolution, reproductive biology and polarized development. Indeed the fucoid algae exhibit the unusual feature of inducible embryo polarization, allowing many classical studies of polarity induction. The potential of further studies of brown algae in these important areas has been increasingly hindered by the absence of tools for manipulation of gene expression that would facilitate further mechanistic analysis and gene function studies at a molecular level. The aim of this study was to establish a method that would allow the analysis of gene function through RNAi‐mediated gene knockdown. We show that injection of double‐stranded RNA (dsRNA) corresponding to an α‐tubulin gene into Fucus serratus Linnaeus zygotes induces the loss of a large proportion of the microtubule cytoskeleton, leading to growth arrest and disruption of cell division. Injection of dsRNA targeting β‐actin led to reduced rhizoid growth, enlarged cells and the failure to develop apical hair cells. The silencing effect on actin expression was maintained for 3 months. These results indicate that the Fucus embryo possesses a functional RNA interference system that can be exploited to investigate gene function during embryogenesis.