Synthesis of some novel androstanes as potential aromatase inhibitors

Novel pyrazole and isoxazole derivatives (6-9) were synthesized as a aromatase inhibitors. Pyrazole was synthesized from hydrazine hydrate and isoxazoles from hydroxylamine hydrochloride under different conditions. Molecular docking studies were carried out for the synthesized compounds. The best score was obtained for the compound (9) followed by compound (6) while compound (8) afforded poorest of the score. Aromatase inhibitory activity for compound (6) having pyrazole ring at 2,3 position showed highest activity followed by nitrile derivative (9). Isomeric forms of isoxazole (7 and 8) showed very poor activity compared to fadrozole and aminoglutethimide. Preliminary kinetic studies have shown that both of the active compounds (6 and 9) are reversible inhibitors of the enzyme.     

The patterns of population differentiation in a <Emphasis Type="Italic">Brassica rapa</Emphasis> core collection

With the recent advances in high throughput profiling techniques the amount of genetic and phenotypic data available has increased dramatically. Although many genetic diversity studies combine morphological and genetic data, metabolite profiling has yet to be integrated into these studies. For our study we selected 168 accessions representing the different morphotypes and geographic origins of Brassica rapa. Metabolite profiling was performed on all plants of this collection in the youngest expanded leaves, 5 weeks after transplanting and the same material was used for molecular marker profiling. During the same season a year later, 26 morphological characteristics were measured on plants that had been vernalized in the seedling stage. The number of groups and composition following a hierarchical clustering with molecular markers was highly correlated to the groups based on morphological traits (r = 0.420) and metabolic profiles (r = 0.476). To reveal the admixture levels in B. rapa, comparison with the results of the programme STRUCTURE was needed to obtain information on population substructure. To analyze 5546 metabolite (LC–MS) signals the groups identified with STRUCTURE were used for random forests classification. When comparing the random forests and STRUCTURE membership probabilities 86% of the accessions were allocated into the same subgroup. Our findings indicate that if extensive phenotypic data (metabolites) are available, classification based on this type of data is very comparable to genetic classification. These multivariate types of data and methodological approaches are valuable for the selection of accessions to study the genetics of selected traits and for genetic improvement programs, and additionally provide information on the evolution of the different morphotypes in B. rapa.     

Biologically synthesized fluorescent CdS NPs encapsulated by PHB

Here an attempt was made to biologically synthesize fluorescent cadmium sulfide nanoparticles and to immobilize the synthesized nanoparticles in PHB nanoparticles. The present study uses Brevibacterium casei SRKP2 as a potential producer for the green synthesis of CdS nanoparticles. Biologically synthesized nanoparticles were characterized and confirmed using electron microscopy and XRD. The size distribution of the nanoparticles was found to be 10-30 nm followed by which the consequence of time, growth of the organism, pH, concentration of CdCl(2) and Na(2)S on the synthesis of nanoparticles were checked. Enhanced synthesis and fluorescence emission of CdS nanoparticles were achieved at pH 9. The synthesized CdS NPs were immobilized with PHB and were characterized. The fluorescent intensity of the CdS nanoparticles remained unaffected even after immobilization within PHB nanoparticles.     

Novel probiotic Bifidobacterium longum subsp. infantis CECT 7210 strain active against rotavirus infections

Rotavirus is the leading cause of severe acute gastroenteritis among children worldwide. It is well known that breast-feeding and vaccination afford infants protection. Since breast-feeding has drastically decreased in developed countries, efforts have been focused on the potential use of probiotics as preventive agents. In this study, a novel Bifidobacterium longum subsp. infantis strain was isolated from infant feces and selected, based on its capacity to inhibit in vitro rotavirus Wa replication (up to 36.05% infectious foci reduction) and also to protect cells from virus infection (up to 48.50% infectious foci reduction) in both MA-104 and HT-29 cell lines. Furthermore, studies using a BALB/c mouse model have proved that this strain provides preliminary in vivo protection against rotavirus infection. The strain has been deposited in the Spanish Type Culture Collection under the accession number CECT 7210. This novel strain has the main properties required of a probiotic, such as resistance to gastrointestinal juices, biliary salts, NaCl, and low pH, as well as adhesion to intestinal mucus and sensitivity to antibiotics. The food safety status has been confirmed by the absence of undesirable metabolite production and in acute ingestion studies of mice. Overall, these results demonstrate that Bifidobacterium longum subsp. infantis CECT 7210 can be considered a probiotic able to inhibit rotavirus infection.     

Novel probiotic Bifidobacterium bifidum CECT 7366 strain active against the pathogenic bacterium Helicobacter pylori

Helicobacter pylori is considered one of the major risk factors underlying the development of gastritis and gastric and duodenal ulcers. Moreover, 50% of the population carries this bacterium, and consequently, when it is detected, eradication of H. pylori is strongly recommended. Regarding the use of probiotics as functional agents, several studies have shown that there is a direct relationship between the addition of certain probiotic bacteria and in vitro inhibition of H. pylori; however, in vivo studies showing bifidobacterial activity against H. pylori remain scarce. In this study, a Bifidobacterium bifidum strain which proved active in vitro against H. pylori has been isolated, with inhibition levels reaching 81.94% in the case of the supernatant and even 94.77% inhibition for supernatant purified by cationic exchange followed by an inverse phase. In vivo studies using a BALB/c mouse model have proved that this strain partially relieves damage to gastric tissues caused by the pathogen and also decreases the H. pylori pathogenicity ratio. This novel strain fulfills the main properties required of a probiotic (resistance to gastrointestinal juices, biliary salts, NaCl, and low pH; adhesion to intestinal mucus; and sensitivity to antibiotics). Furthermore, the absence of undesirable metabolites has been demonstrated, and its food safety status has been confirmed by acute ingestion studies in mice. In summary, the results presented here demonstrate that Bifidobacterium bifidum CECT 7366 can be considered a probiotic able to inhibit H. pylori both in vitro and in vivo.     

Taxonomic and Functional Metagenomic Profiling of the Microbial Community in the Anoxic Sediment of a Sub-saline Shallow Lake (Laguna de Carrizo, Central Spain)

The phylogenetic and functional structure of the microbial community residing in a Ca(2+)-rich anoxic sediment of a sub-saline shallow lake (Laguna de Carrizo, initially operated as a gypsum (CaSO(4)?×?2 H(2)O) mine) was estimated by analyzing the diversity of 16S rRNA amplicons and a 3.1?Mb of consensus metagenome sequence. The lake has about half the salinity of seawater and possesses an unusual relative concentration of ions, with Ca(2+) and SO (4) (2-) being dominant. The 16S rRNA sequences revealed a diverse community with about 22% of the bacterial rRNAs being less than 94.5% similar to any rRNA currently deposited in GenBank. In addition to this, about 79% of the archaeal rRNA genes were mostly related to uncultured Euryarchaeota of the CCA47 group, which are often associated with marine and oxygen-depleted sites. Sequence analysis of assembled genes revealed that 23% of the open reading frames of the metagenome library had no hits in the database. Among annotated genes, functions related to (thio) sulfate and (thio) sulfonate-reduction and iron-oxidation, sulfur-oxidation, denitrification, synthrophism, and phototrophic sulfur metabolism were found as predominant. Phylogenetic and biochemical analyses indicate that the inherent physical-chemical characteristics of this habitat coupled with adaptation to anthropogenic activities have resulted in a highly efficient community for the assimilation of polysulfides, sulfoxides, and organosulfonates together with nitro-, nitrile-, and cyanide-substituted compounds. We discuss that the relevant microbial composition and metabolic capacities at Laguna de Carrizo, likely developed as an adaptation to thrive in the presence of moderate salinity conditions and potential toxic bio-molecules, in contrast with the properties of previously known anoxic sediments of shallow lakes.     

A reconstruction of Palaeo‐Macaronesia,with particular reference to the long‐term biogeography of the Atlantic island laurel forests

Macaronesia is a biogeographical region comprising five Atlantic Oceanic archipelagos: the Azores, Madeira, Selvagen (Savage Islands), Canaries and Cape Verde. It has strong affinities with the Atlantic coast of the Iberian Peninsula and the north‐western fringes of Africa. This paper re‐evaluates the biogeographical history and relationships of Macaronesia in the light of geological evidence, which suggests that large and high islands may have been continuously available in the region for very much longer than is indicated by the maximum surface area of the oldest current island (27 Ma) – possibly for as long as 60 million years. We review this literature, attempting a sequential reconstruction of Palaeo‐Macaronesia from 60 Ma to the present. We consider the implications of these geological dynamics for our understanding of the history of colonization of the present islands of Macaronesia. We also evaluate the role of these archipelagos as stepping stones and as both repositories of palaeo‐endemic forms and crucibles of neo‐endemic radiations of plant and animal groups. Our principal focus is on the laurel forest communities, long considered impoverished relicts of the Palaeotropical Tethyan flora. This account is therefore contextualized by reference to the long‐term climatic and biogeographical history of Southern Europe and North Africa and by consideration of the implications of changes in land–sea configuration, climate and ocean circulation for Macaronesian biogeography. We go on to provide a synthesis of the more recent history of Macaronesian forests, which has involved a process of impoverishment of the native elements of the biota that has accelerated since human conquest of the islands. We comment briefly on these processes and on the contemporary status and varied conservation opportunities and threats facing these forests across the Macaronesian biogeographical region.     

Age and growth of sailfish Istiophorus platypterus (Shaw in Shaw and Nodder, 1792) from Mazatlan, Sinaloa, Mexico

Age and growth of the sailfish Istiophorus platypterus were determined for the area off Mazatlan coast, Sinaloa, in the Gulf of California, between September 2002 and August 2003. The lower jaw-fork length and total weight of 572 specimens were measured, and the fourth dorsal spine was collected to determine age. The monthly variation of the sample size displayed a well-defined seasonal pattern, which peaked during the warm period (May?CNovember) and declined during the rest of the year (temperate period). Significant differences were detected in the size structure by sex during the temperate period, with females displaying larger sizes and greater abundance (Female:Male = 3.35:1). In the warm period the size structure was similar, with the sex ratio reaching F:M = 0.73:1. This suggests a different sex-related recruitment in the fishing zone, with males moving more actively than females. While female size remained relatively unchanged over the year, male size increased during the warm period. Age was estimated using the number of growth rings on the cross-sectioned fourth dorsal spine, after the number of absorbed growth rings in the vascularized zone had been estimated. Nine age groups were identified; group-5 was the most abundant, representing 31% of the catch. The trend of the monthly change in the percentage of opaque-edge spines and the average of the marginal increase rate indicated that the formation of growth rings displayed an annual pattern. The von Bertalanffy growth model was adequately fitted to age and back-calculated length data. Significant differences were detected when growth was compared between sexes; females grew faster than males.     

Identification and Characterization of Toxigenic Fusaria Associated with Sorghum Grain Mold Complex in India

Fusarium species are dominant within the sorghum grain mold complex. Some species of Fusarium involved in grain mold complex produce mycotoxins, such as fumonisins. An attempt was made to identify Fusarium spp. associated with grain mold complex in major sorghum-growing areas in India through AFLP-based grouping of the isolates and to further confirm the species by sequencing part of α-Elongation factor gene and comparing the sequences with that available in the NCBI database. The dendrogram generated from the AFLP data clustered the isolates into 5 groups. Five species of Fusarium—F. proliferatum, F. thapsinum, F. equiseti, F. andiyazi and F. sacchari were identified based on sequence similarity of α-Elongation factor gene of the test isolates with those in the NCBI database. Fusarium thapsinum was identified as predominant species in Fusarium—grain mold complex in India and F. proliferatum as highly toxigenic for fumonisins production. Analysis of molecular variance (AMOVA) revealed 54% of the variation in the AFLP patterns of 63 isolates was due to the differences between Fusarium species, and 46% was due to differences between the strains within a species.