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A cost-effective, scalable, and environmentally benign process is herein reported for the synthesis of pantoprazole sodium sesquihydrate: 5-(difluromethoxy)-2-[{(3,4-dimethoxy-2-pyridinyl)methyl}sulfinyl]-1 H -benzimidazole sodium sesquihydrate. At least two of the three main synthetic steps (coupling and oxidation) have been carried out for the first time in water, with no need to isolate and purify the intermediates, affording the corresponding pantoprazole sodium in good yield and purity. Minimum organic solvents, in terms of both the number of solvents and the volume of solvent used, are employed to make this process both economical and environment friendly. Furthermore, in situ transformation of pantoprazole sodium heterosolvate, due to the association between molecules of water and solvent used, to pantoprazole sodium sesquihydrate is described., Competing Interests: The authors declare no competing financial interest.

Ixeris dentata var. albiflora is considered as a potential therapeutic agent against mithridatism, calculous, indigestion, pneumonia, hepatitis, and tumors as well as good seasoned vegetable in Far East countries. Phytoene synthase (PSY), phytoene desaturase (PDS) ξ-carotene desaturase (ZDS), lycopene β-cyclase (LCYB), lycopene ε-cyclase (LCYE), ε-ring carotene hydroxylase (CHXB), and zeaxanthin epoxidase (ZDS) are vital enzymes in the carotenoid biosynthesis pathway. We have examined these seven genes from I. dentat a that are participated in carotenoid biosynthesis utilizing an Illumina/Solexa HiSeq 2000 platform. In silico analysis of the seven deduced amino acid sequences were revealed its closest homology with other Asteracea plants. Further, we explored transcript levels and carotenoid accumulation in various organs of I. dentata using quantitative real time PCR and high-performance liquid chromatography, respectively. The highest transcript levels were noticed in the leaf for all the genes while minimal levels were noticed in the root. The maximal carotenoid accumulation was also detected in the leaf. We proposed that these genes expressions are associated with the accumulation of carotenoids. Our findings may suggest the fundamental clues to unravel the molecular insights of carotenoid biosynthesis in various organs of I. dentata ., Competing Interests: The authors declare no conflict of interest.

Globally, plant-derivatives especially cereals and legumes are the major staple food sources for animals. The seeds of these crops comprise of phytic acid, the major repository form of the phosphorus, which is not digestible by simple-stomached animals. However, it is the most important factor responsible for impeding the absorption of minerals by plants that eventually results in less use of fertilizers that ultimately cause eutrophication in water bodies. Although abundant phosphorus (P) exists in the soils, plants cannot absorb most of the P due to its conversion to unavailable forms. Hence, additional P supplementation is indispensable to the soil to promote crop yields which not only leads to soil infertility but also rapid depletion of non-renewable P reservoirs. Phytase/phosphatase enzyme is essential to liberate P from soils by plants and from seeds by monogastric animals. Phytases are kind of phosphatases which can hydrolyse the indigestible phytate into inorganic Phosphate (Pi) and lower myo-inositol. There are several approaches to mitigate the problems associated with phytate indigestibility. One of the best possible solutions is engineering crops to produce heterologous phytase to improve P utilization by monogastric animals, plant nutrition and sustainable ecological developments. Previously published reviews were focused on either soil phytate or seed-phytate, related issues, but this review will address both the problems as well as phytate related ecological problems. This review summarizes the overall view of engineered phytase crops and their role in sustainable agriculture, animal nutrition and ecological development.

Spatially explicit approach is essential to prioritise the ecosystems for biodiversity conservation. In the present study, the conservation status of 20 protected areas of the Western Ghats of Kerala, India, was analysed based on long-term changes in forests (1975-1985-1995-2005-2013), landscape level changes in fragmentation and forest fires (2005-2015). This study has shown that a significant forest loss occurred in protected areas before declaration. Idukki is one of the major protected areas which showed a drastic reduction (18.83%) in its forest cover. During 1985-1995, Periyar tiger reserve had lost 24.19 km 2 core 3 forest area followed by Peppara (18.54 km 2 ), Parambikulam (17.93 km 2 ), Chimmony (17.71 km 2 ), Peechi-Vazhani (12.31 km 2 ) and Neyyar (11.67 km 2 ). An area of 71.33 km 2 of the protected area was affected by fires in 2014. Overall protected area-wise decadal analysis indicates Periyar has the highest number of fire incidences followed by Wayanad, Kurinjimala, Silent Valley and Eravikulam. Disturbances in the form of fires and fragmentation still exist and may have significant conservation threat to flora and fauna. Among protected areas, many are having a probability to go under threat or dynamic stage. Chinnar, Thattekkad and Kurinjimala sanctuaries are representing high levels of vulnerability, or they are near to decline stage. Habitat level monitoring of the anthropogenic disturbances can be efficiently useful for the strategic conservation planning. The present study has provided geospatial database on spatial patterns of deforestation, fragmentation and forest fires in protected areas of Kerala. Conservation prioritization approach based on these parameters will be useful for the strategic planning in the state of Kerala.

Allele-specific measurements of transcription factor binding from ChIP-seq data are key to dissecting the allelic effects of non-coding variants and their contribution to phenotypic diversity. However, most methods of detecting an allelic imbalance assume diploid genomes. This assumption severely limits their applicability to cancer samples with frequent DNA copy-number changes. Here we present a Bayesian statistical approach called BaalChIP to correct for the effect of background allele frequency on the observed ChIP-seq read counts. BaalChIP allows the joint analysis of multiple ChIP-seq samples across a single variant and outperforms competing approaches in simulations. Using 548 ENCODE ChIP-seq and six targeted FAIRE-seq samples, we show that BaalChIP effectively corrects allele-specific analysis for copy-number variation and increases the power to detect putative cis-acting regulatory variants in cancer genomes.

Background: One of the alarming difficulties in the field of hematology is the Coagulant disorders. Despite the availability of clinically proven existing anticoagulants, their limitations have prompted a continuous search for novel anticoagulants., Objective: The primary objective of the study is to synthesize a series of 2-amino-4H-chromen-4- ylphosphonate derivatives and to test their anticoagulant activity depending on PT measurements considering commercial heparin as positive control., Method: 2-Amino-4H-chromen-4-ylphosphonates were synthesized by the reaction of salicylaldehyde derivatives (1), malononitrile (2) and dialkyl phosphite (3) in ethanol using piperazine as a catalyst by ultra-sonication at room temperature. All the title compounds (4a-l) were tested for anticoagulant activity., Results: The results of the anticoagulant activity of the title compounds revealed that 4j, 4h and 4g showed prolonged prothrombin time 87.28, 81.81 and 78.42 sec when compared with that of the standard heparin which has prothrombin time of 121.50 sec., Conclusion: The findings from this study highlight that ultrasonication of the one pot three component reaction of salicylaldehyde derivatives, malononitrile and dialkyl phosphite with piperazine as a catalyst for the synthesis of 2-amino-4H-chromen-4-ylphosphonates is the best method. In vitro coagulant assay in terms of prothrombin time (PT) revealed that 4j, 4h and 4g possess promising anticoagulant properties. Other compounds (4a-l) were also found to have significant anticoagulant effect when compared with the heparin as positive control. Thus, these compounds qualify for further clinical studies to be used as the blood anticoagulants., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)

Introduction: Implant-supported prosthesis has high predictability and success and improves quality of life. This study aims at assessing awareness among the patients regarding implant-supported prosthesis., Materials and Methods: A cross-sectional study was conducted among 391 study participants. A structured questionnaire was distributed to assess implant-related awareness among the study participants. The questionnaires were analyzed for the responses., Results: Among the 391 respondents, 37.5% of the respondents reported having moderate knowledge regarding the tooth replacement options. Nearly 50% considered implants as a viable treatment option. The majority of them enlisted the dentist as the major source of information regarding implants, and media had a share of about 7.03% only. High cost was a major barrier in selecting implants as a treatment option., Conclusion: This survey showed that awareness among people was low regarding the dental implants. Efforts need to be directed to increase the awareness levels by utilizing media as a tool to achieve the target., Clinical Significance: A patient who is aware of the advantages of the implant-supported dentures will make an informed decision for better functional stability and retention of the denture, especially in the mandibular arch.

Bhutan is a mountainous country located in the Himalayan biodiversity hotspot. This study has quantified the total area under land cover types, estimated the rate of forest cover change, analyzed the changes across forest types, and modeled forest cover change hotpots in Bhutan. The topographical maps and satellite remote sensing images were analyzed to get the spatial patterns of forest and associated land cover changes over the past eight decades (1930-1977-1987-1995-2005-2014). Forest is the largest land cover in Bhutan and constitutes 68.3% of the total geographical area in 2014. Subtropical broad leaved hill forest is predominant type occupies 34.1% of forest area in Bhutan, followed by montane dry temperate (20.9%), montane wet temperate (18.9%), Himalayan moist temperate (10%), and tropical moist sal (8.1%) in 2014. The major forest cover loss is observed in subtropical broad leaved hill forest (64.5 km 2 ) and moist sal forest (9.9 km 2 ) from 1977 to 2014. The deforested areas have mainly been converted into agriculture and contributed for 60.9% of forest loss from 1930 to 2014. In spite of major decline of forest cover in time interval of 1930-1977, there is no net rate of deforestation is recorded in Bhutan since 1995. Forest cover change analysis has been carried out to evaluate the conservation effectiveness in "Protected Areas" of Bhutan. Hotspots that have undergone high transformation in forest cover for afforestation and deforestation were highlighted in the study for conservation prioritisation. Forest conservation policies in Bhutan are highly effective in controlling deforestation as compared to neighboring Asian countries and such service would help in mitigating climate change.

The Asian catfish, Clarias batrachus (Linnaeus, 1758), is a highly valued species endemic to India that is currently in drastic decline in most of its natural habitat. The present study was undertaken to document the genetic structure of populations of this species using mitochondrial DNA markers, specifically from the cytochrome B and D-loop regions. Specimens from eight wild populations were collected and analyzed from different regions in India. The genetic variation within and among populations was evaluated using a range of descriptive statistics. The analysis described here provides a broad and consistent view of population structure and demographic history of populations of C. batrachus. Although there was some genetic structuring consistent with regional differences, all eight populations examined here showed relatively low levels of genetic variation in terms of both haplotype and nucleotide diversities in the different analyses used. However, a number of private haplotypes were discovered, and this may provide valuable information for future selective breeding program and conservation management. The results may aid in the design and implementation of strategies for the future management of this endangered catfish C. batrachus in India.

Michael addition of indole derivatives with various substituted nitrostyrenes to yield β- indolylnitroalkanes is accomplished effectively under solvent free conditions using TiO2-SO4(2-) as efficient catalyst at 60 º C. All the synthesized compounds were screened for their antibacterial activity through in silico and in vitro methods. The molecular docking studies against FabH enzyme, a potential drug target of bacterial fatty acid biosynthetic pathway indicated the scope of developing them a new class of antimicrobial agents. Among the title compounds, 5h exhibited the highest dock score and the highest antibacterial activity when compared with other compounds and the standard drug Ampicillin. In addition, the compounds 5d, 5e, 5g, 5h, 5i, 5j and 5l showed significant inhibitory activity at different dose concentrations under in vitro conditions against the specified bacterial strains thus qualifying for further clinical evaluation so that they can be used as effective anti-bacterial agents.

India, a mega-diverse country, possesses a wide range of climate and vegetation types along with a varied topography. The present study has classified forest types of India based on multi-season IRS Resourcesat-2 Advanced Wide Field Sensor (AWiFS) data. The study has characterized 29 land use/land cover classes including 14 forest types and seven scrub types. Hybrid classification approach has been used for the classification of forest types. The classification of vegetation has been carried out based on the ecological rule bases followed by Champion and Seth's (1968) scheme of forest types in India. The present classification scheme has been compared with the available global and national level land cover products. The natural vegetation cover was estimated to be 29.36% of total geographical area of India. The predominant forest types of India are tropical dry deciduous and tropical moist deciduous. Of the total forest cover, tropical dry deciduous forests occupy an area of 2,17,713 km(2) (34.80%) followed by 2,07,649 km(2) (33.19%) under tropical moist deciduous forests, 48,295 km(2) (7.72%) under tropical semi-evergreen forests and 47,192 km(2) (7.54%) under tropical wet evergreen forests. The study has brought out a comprehensive vegetation cover and forest type maps based on inputs critical in defining the various categories of vegetation and forest types. This spatially explicit database will be highly useful for the studies related to changes in various forest types, carbon stocks, climate-vegetation modeling and biogeochemical cycles.

By considering the current regulatory requirement for an analytical method development, a reversed phase high performance liquid chromatographic method for routine analysis of etofenamate in dosage form has been optimized using analytical quality by design approach. Unlike routine approach, the present study was initiated with understanding of quality target product profile, analytical target profile and risk assessment for method variables that affect the method response. A liquid chromatography system equipped with a C18 column (250×4.6 mm, 5 μ), a binary pump and photodiode array detector were used in this work. The experiments were conducted based on plan by central composite design, which could save time, reagents and other resources. Sigma Tech software was used to plan and analyses the experimental observations and obtain quadratic process model. The process model was used for predictive solution for retention time. The predicted data from contour diagram for retention time were verified actually and it satisfied with actual experimental data. The optimized method was achieved at 1.2 ml/min flow rate of using mobile phase composition of methanol and 0.2% triethylamine in water at 85:15, % v/v, pH adjusted to 6.5. The method was validated and verified for targeted method performances, robustness and system suitability during method transfer.

Background: Appearance of the face is a great concern to everyone, as it is a significant part of self-image. The study analyzed the clinical crown dimensions of the maxillary anterior teeth with respect to their apparent mesiodistal widths, width-to-height ratio to determine whether golden proportion existed among the South Indian population., Materials and Methods: A total of 240 dentulous subjects were chosen for the study (120 males and 120 females) age ranging between 18 and 28 years. Full face and anterior teeth images of the subjects were made on specially designed device resembling a face-bow, mounted onto the wall under a standard light source. The width and height of the maxillary central incisors were measured on the stone casts using a digital caliper., Results: The mean perceived maxillary lateral incisor to central incisor width ratio was 0.67 in males and 0.703 in females. The mean perceived maxillary canine to lateral incisor width ratio was 0.744 in males and 0.714 in females. The mean width-to-height ratio of the maxillary central incisor was 79.49% in males and 79.197% in females., Conclusion: The golden proportion was not found between perceived mesiodistal widths of maxillary central and lateral incisors and nor between perceived mesiodistal widths of maxillary lateral incisors and canines. In the majority of subjects, the width-to-height ratio of maxillary central incisor was within 75-80%. There are no statistically significant differences in maxillary anterior teeth proportions between males and females. The results may serve as guidelines for treatment planning in restorative dentistry and periodontal surgery.

A mild and efficient Pd-catalyzed arylative domino carbocyclization of cyclohexadienone-containing 1,6-enynes is described. The reaction tolerates a variety of functionalized boronic acids to afford a cis-fused bicyclic framework containing an α,β-unsaturated ketone with excellent regio- and diastereoselectivity in good yields. The tandem process proceeds with β-arylation of propargylic ether followed by conjugate addition of a vinyl palladium intermediate and subsequent protonolysis of a palladium enolate.

The generation of excess reactive oxygen species (ROS) is one of the most common consequences of abiotic stress on plants. Glutathione reductase (GR, E.C. 1.6.4.2) and allied enzymes of the ascorbate-glutathione cycle play a crucial role to maintain the homeostatic redox balance in the cellular environment. GR plays an essential role in upholding the reduced glutathione pool under stress conditions. In the present study, a full-length GR cDNA and corresponding genomic clone was isolated from Pennisetum glaucum (L.) R. Br. The PgGR cDNA, encodes a 497-amino acid peptide with an estimated molecular mass of ~53.5 kDa. The PgGR peptide exhibits 54-89% sequence homology with GR from other plants and is cytoplasmic in nature. The PgGR enzyme was purified to near homogeneity, the recombinant protein being relatively thermostable and displaying activity in a broad range of temperature, pH and substrate concentrations. The PgGR transcript level was differentially regulated by heat, cold, salinity and methyl viologen-induced oxidative stress. The heterologously expressed PgGR protein in E. coli showed an improved protection against metal- and methyl viologen-induced oxidative stress. Our overall finding underscores the role of PgGR gene that responds to multiple abiotic stresses and provides stress tolerance in the experimental model (E. coli) which can be potentially used for the improvement of crops under abiotic stress conditions.

Monellin a sweet-tasting protein exists naturally as a heterodimer of two non-covalently linked subunits chain A and B, which loses its sweetness on denaturation. In this study, we validated the expression of a synthetic monellin gene encoding a single polypeptide chain covalently linking the two subunits under T7 and fruit-ripening-specific promoters in Escherichia coli and tomato fruits, respectively. Purified recombinant monellin protein retained its sweet flavour at 70 °C and pH 2. We developed 15 transgenic T0 tomato plants overexpressing monellin, which were devoid of any growth penalty or phenotypic abnormalities during greenhouse conditions. T-DNA integration and fruit-specific heterologous expression of monellin had occurred in these transgenic tomato lines. ELISA revealed that expression of monellin was 4.5% of the total soluble fruit protein. Functional analyses of transgenic tomatoes of T2-5 and T2-14 lines revealed distinctly strong sweetness compared with wild type. Monellin a potential non-carbohydrate sweetener, if expressed in high amounts in fruits and vegetables, would enhance their flavour and quality.

The thermostable phytase gene was isolated from Bacillus subtilis ARRMK33 (BsPhyARRMK33). The gene has an ORF of 1152 bp and that encodes a protein of 383 amino acids. Sequence analysis showed high homology with Bacillus sp. phytase proteins, but no similarity was found with other phytases. SDS-PAGE analysis exhibited a predicted molecular mass of 42 kDa. Homology modeling of BsPhyARRMK33 protein based on Bacillus amyloliquefaciens crystal structure disclosed its β-propeller structure. BsPhyARRMK33 recombinant plasmid in pET-28a(+) was expressed in Rosetta gami B DE3 cells and the maximum phytase activity 15.3 U mg(-1) obtained. The enzyme exhibits high thermostability at various temperatures and broad pH ranges. The recombinant protein retained 74% of its original activity after incubation at 95 °C for 10 min. In the presence of Ca(2+), the recombinant phytase activity was maximal where as it was inhibited by EDTA. The optimal pH and temperature for the recombinant phytase activity is achieved at 7.0 and 55 °C, respectively. Thermostable nature and wide range of pH are promising features of recombinant BsPhyARRMK33 protein that may be employed as an efficient alternative to commercially known phytases and thereby alleviate environmental eutrophication.

Deforestation in the biosphere reserves, which are key Protected Areas has negative impacts on biodiversity, climate, carbon fluxes and livelihoods. Comprehensive study of deforestation in biosphere reserves is required to assess the impact of the management effectiveness. This article assesses the changes in forest cover in various zones and protected areas of Nilgiri Biosphere Reserve, the first declared biosphere reserve in India which forms part of Western Ghats-a global biodiversity hotspot. In this study, we have mapped the forests from earliest available topographical maps and multi-temporal satellite data spanning from 1920's to 2012 period. Mapping of spatial extent of forest cover, vegetation types and land cover was carried out using visual interpretation technique. A grid cell of 1 km × 1 km was generated for time series change analysis to understand the patterns in spatial distribution of forest cover (1920-1973-1989-1999-2006-2012). The total forest area of biosphere reserve was found to be 5,806.5 km(2) (93.8 % of total geographical area) in 1920. Overall loss of forest cover was estimated as 1,423.6 km(2) (24.5 % of the total forest) with reference to 1920. Among the six Protected Areas, annual deforestation rate of >0.5 was found in Wayanad wildlife sanctuary during 1920-1973. The deforestation in Nilgiri Biosphere Reserve is mainly attributed to conversion of forests to plantations and agriculture along with submergence due to construction of dams during 1920 to 1989. Grid wise analysis indicates that 851 grids have undergone large-scale negative changes of >75 ha of forest loss during 1920-1973 while, only 15 grids have shown >75 ha loss during 1973-1989. Annual net rate of deforestation for the period of 1920 to 1973 was calculated as 0.5 followed by 0.1 for 1973 to 1989. Our analysis shows that there was large-scale deforestation before the declaration of area as biosphere reserve in 1986; however, the deforestation has drastically reduced after the declaration due to high degree of protection, thus indicating the secure future of reserve in the long term under the current forest management practices. The present work will stand as the most up-to-date assessment on the forest cover of the Nilgiri Biosphere Reserve with immediate applications in monitoring and management of forest biodiversity.

Polycaprolactone (PCL), a synthetic biocompatible and biodegradable polymer generally used as a scaffold material for tissue engineering applications. The high stiffness and hydrophobicity of the PCL fiber mesh does not provide significant cell attachment and proliferation in cardiac tissue engineering. Towards this goal, the study focused on a compound of PCL and oligomer hydrogel [Bisphenol A ethoxylated dimethacrylate (BPAEDMA)] processed into electrospun nanofibrous scaffolds. The composition, morphology and mechanical properties of the compound scaffolds, composed of varying ratios of PCL and hydrogel were characterized by scanning electron microscopy, infrared spectroscopy and dynamic mechanical analyzer. The elastic modulus of PCL/BPAEDMA nanofibrous scaffolds was shown to be varying the BPAEDMA weight fraction and was decreased by increasing the BPAEDMA weight fraction. Compound fiber meshes containing 75 wt % BPAEDMA oligomer hydrogel exhibited lower modulus (3.55 MPa) and contact angle of 25(o) . Rabbit cardiac cells cultured for 10 days on these PCL/BPAEDMA compound nanofibrous scaffolds remained viable and expressed cardiac troponin and alpha-actinin proteins for the normal functioning of myocardium. Cell adhesion and proliferations were significantly increased on compound fiber meshes containing 75 wt % BPAEDMA, when compared with other nanofibrous scaffolds. The results observed that the produced PCL/BPAEDMA compound nanofibrous scaffolds promote cell adhesion, proliferation and normal functioning of cardiac cells to clinically beneficial levels, relevant for cardiac tissue engineering., (© 2013 Wiley Periodicals, Inc.)

Background: Recent developments in deep (next-generation) sequencing technologies are significantly impacting medical research. The global analysis of protein coding regions in genomes of interest by whole exome sequencing is a widely used application. Many technologies for exome capture are commercially available; here we compare the performance of four of them: NimbleGen's SeqCap EZ v3.0, Agilent's SureSelect v4.0, Illumina's TruSeq Exome, and Illumina's Nextera Exome, all applied to the same human tumor DNA sample., Results: Each capture technology was evaluated for its coverage of different exome databases, target coverage efficiency, GC bias, sensitivity in single nucleotide variant detection, sensitivity in small indel detection, and technical reproducibility. In general, all technologies performed well; however, our data demonstrated small, but consistent differences between the four capture technologies. Illumina technologies cover more bases in coding and untranslated regions. Furthermore, whereas most of the technologies provide reduced coverage in regions with low or high GC content, the Nextera technology tends to bias towards target regions with high GC content., Conclusions: We show key differences in performance between the four technologies. Our data should help researchers who are planning exome sequencing to select appropriate exome capture technology for their particular application.

The voltage recovery in a spark gap for repetitive switching has been a long research interest. A two-pulse technique is used to determine the voltage recovery times of gas spark gap switch with argon gas. First pulse is applied to the spark gap to over-volt the gap and initiate the breakdown and second pulse is used to determine the recovery voltage of the gap. A pulse transformer based double pulse generator capable of generating 40 kV peak pulses with rise time of 300 ns and 1.5 μs FWHM and with a delay of 10 μs-1 s was developed. A matrix transformer topology is used to get fast rise times by reducing L(l)C(d) product in the circuit. Recovery Experiments have been conducted for 2 mm, 3 mm, and 4 mm gap length with 0-2 bars pressure for argon gas. Electrodes of a sparkgap chamber are of rogowsky profile type, made up of stainless steel material, and thickness of 15 mm are used in the recovery study. The variation in the distance and pressure effects the recovery rate of the spark gap. An intermediate plateu is observed in the spark gap recovery curves. Recovery time decreases with increase in pressure and shorter gaps in length are recovering faster than longer gaps.

A new class of hybrid molecules containing cinnamide subunit linked to benzophenone as inhibitors of tubulin polymerization were synthesized and evaluated for their anticancer potential. These hybrids exhibit anticancer activity with IC50 values ranging from 0.06 to 16.3μM. Compounds 4f and 4g possessing fluoro and trifluoromethyl on the cinnamido subunit showed significant cytotoxic activity with IC50 values 0.06 and 0.09μM against HeLa cell line, respectively. These compounds showed cell cycle arrest at G2/M phase of the cell cycle and inhibited tubulin polymerization followed by activation of caspase-3 activity and apoptotic cell death. Further in vitro tubulin polymerization assay showed that the level of tubulin inhibition was comparable to that of 2a for the compounds 4f and 4g. Moreover, Hoechst 33258 staining and DNA fragmentation assay suggested that these compounds induce cell death by apoptosis. Overall, the current study demonstrates that the synthesis of benzophenone linked cinnamide subunit conjugates as promising anticancer agents with G2/M arrest and apoptotic-inducing ability via targeting tubulin., (Copyright © 2014 Elsevier Ltd. All rights reserved.)

A highly diastereoselective total synthesis of (+)-pseudohygroline (1) starting from D-proline is described using Wittig olefination and MacMillan-alpha-hydroxylation as key reactions. (+)-Pseudohygroline is an important molecule in alkaloid chemistry as it was prepared as part of the first chemical proof of the absolute stereochemistry of biosynthetically important (+)-hygroline (2) and (+)-hygrine (3).

Analyzing the spatial extent and distribution of forest fires is essential for sustainable forest resource management. There is no comprehensive data existing on forest fires on a regular basis in Biosphere Reserves of India. The present work have been carried out to locate and estimate the spatial extent of forest burnt areas using Resourcesat-1 data and fire frequency covering decadal fire events (2004-2013) in Similipal Biosphere Reserve. The anomalous quantity of forest burnt area was recorded during 2009 as 1,014.7 km(2). There was inconsistency in the fire susceptibility across the different vegetation types. The spatial analysis of burnt area shows that an area of 34.2 % of dry deciduous forests, followed by tree savannah, shrub savannah, and grasslands affected by fires in 2013. The analysis based on decadal time scale satellite data reveals that an area of 2,175.9 km(2) (59.6 % of total vegetation cover) has been affected by varied rate of frequency of forest fires. Fire density pattern indicates low count of burnt area patches in 2013 estimated at 1,017 and high count at 1,916 in 2004. An estimate of fire risk area over a decade identifies 12.2 km(2) is experiencing an annual fire damage. Summing the fire frequency data across the grids (each 1 km(2)) indicates 1,211 (26 %) grids are having very high disturbance regimes due to repeated fires in all the 10 years, followed by 711 grids in 9 years and 418 in 8 years and 382 in 7 years. The spatial database offers excellent opportunities to understand the ecological impact of fires on biodiversity and is helpful in formulating conservation action plans.

Folate-sensitive fragile sites (FSFS) are a rare cytogenetically visible subset of dynamic mutations. Of the eight molecularly characterized FSFS, four are associated with intellectual disability (ID). Cytogenetic expression results from CGG tri-nucleotide-repeat expansion mutation associated with local CpG hypermethylation and transcriptional silencing. The best studied is the FRAXA site in the FMR1 gene, where large expansions cause fragile X syndrome, the most common inherited ID syndrome. Here we studied three families with FRA2A expression at 2q11 associated with a wide spectrum of neurodevelopmental phenotypes. We identified a polymorphic CGG repeat in a conserved, brain-active alternative promoter of the AFF3 gene, an autosomal homolog of the X-linked AFF2/FMR2 gene: Expansion of the AFF2 CGG repeat causes FRAXE ID. We found that FRA2A-expressing individuals have mosaic expansions of the AFF3 CGG repeat in the range of several hundred repeat units. Moreover, bisulfite sequencing and pyrosequencing both suggest AFF3 promoter hypermethylation. cSNP-analysis demonstrates monoallelic expression of the AFF3 gene in FRA2A carriers thus predicting that FRA2A expression results in functional haploinsufficiency for AFF3 at least in a subset of tissues. By whole-mount in situ hybridization the mouse AFF3 ortholog shows strong regional expression in the developing brain, somites and limb buds in 9.5-12.5dpc mouse embryos. Our data suggest that there may be an association between FRA2A and a delay in the acquisition of motor and language skills in the families studied here. However, additional cases are required to firmly establish a causal relationship.

Human serum albumin (HSA) is one of the most widely studied proteins and is an important plasma protein responsible for binding and transport of many exogenous and endogenous drugs. Coumarin derivatives play a critical role as anticancer, antidiabetic, anticoagulant, and analgesic agents. Here we have studied the cytotoxic activity of 7-hydroxycoumarin derivatives (7HC-1, 7HC-2, and 7HC-3) on mouse macrophage (RAW 264.7) cell lines. These studies revealed that 7-hydroxycoumarin derivatives caused an increased inhibition in growth of inflamed macrophages in a concentration-dependent manner with an IC50 of 78, 63, and 50 μM. Further studies, using fluorescence, circular dichroism spectroscopy, molecular docking, and molecular dynamics methods, show binding of 7HC (umbelliferone) derivatives with HSA at physiological pH 7.2. The binding constant of 7HC derivatives with HSA obtained from fluorescence emission was found to be K7HC-1 = 4.6 ± 0.01 × 10(4) M(-1), K7HC-2 = 1.3 ± 0.01 × 10(4) M(-1), and K7HC-3 = 7.9 ± 0.01 × 10(4) M(-1) which corresponds to -6.34 kcal/mol, -5.58 kcal/mol, and -6.65 kcal/mol of free energy. In contrast, the binding of these coumarin derivatives (7HC-1, 7HC-2, and 7HC-3) was almost negligible with α-1-glycoprotein (AGP). Circular dichroism (CD) studies revealed a decreased α-helix content with an increase in the β-sheets and random coils in HSA upon interaction with coumarin derivatives, suggesting a partial unfolding of the HSA secondary structure. Site probe studies with phenylbutazone (Site I) and ibuprofen (Site II) indicated that 7HC derivatives specifically bind to sub domains IIIA and IIIB of HSA which is further corroborated by molecular dynamics and docking studies suggesting that binding is specific in nature. The values of free energies and binding constants coincide for both experimental and in silico analysis and suggest that there are hydrophobic interactions when coumarin derivatives bind to HSA. Molecular dynamics studies showed that the HSA-coumarin complex reaches an equilibration state at around 3.5 ns which indicates that the HSA-coumarin complexes were stable. Thus these interactions play a central role in development of coumarin derivative-inspired drugs.

Background: The statistical profile reflects a global estimate of 5.1 million deaths in 2000, which was due to injuries that accounted for 10% of deaths due to all causes. Out of this, a quarter of injury-related deaths occurred in the South-East Asian region. Road Traffic Accident (RTA) is one among the top 5 causes of morbidity and mortality in South-East Asian countries. Most common cause of blunt abdominal trauma in India is road traffic accident followed by pedestrian accidents, abdominal blows, and fall from heights., Aims: To analyze the epidemiology and pattern of fatal thoraco-abdominal injuries in road traffic accidents., Materials and Methods: An autopsy-based cross-sectional study conducted. A purposive sampling technique was applied to select the study sample of 100 post-mortems of road traffic accident between November 2008 and May 2010 subjected to medico-legal autopsy at the department of Forensic Medicine, KIMS Hospital Bangalore., Results: The majority of the victims were aged 21 to 40 years, 50 (50.0%), most of the victims were male 92 (92.0%); and male/female ratio was 11.5:1. Commonest offending agents in heavy motor vehicles were 54 (54.0%). Bony cage sustained injuries were observed in 71; out of this, fractures of ribs were observed in 45 (63.3%) victims, clavicle in 14 (19.7%), sternum was 6 (8.4%), and vertebrae 6 (8.4%) of fatal road traffic accidents. Internal thoracic injuries were observed in 26 cases. Among internal thoracic injuries, lungs were the most commonly involved organ 24 (92.3%) followed by the heart 2 (7.6%). Lung sustained more lacerations 19 (79.1%) than contusions 5 (20.8%). Internal abdominal injuries were observed in 49 cases. In road traffic accidents, the most commonly injured abdominal organs were solid organs such as liver 16 (32.6%) followed by spleen 9 (18.3%)., Conclusions: Majority of the times in road traffic accidents, young and productive males were injured or lost their life. This study may help the planners to take safety measures, to implement strict traffic rules, to risk stratification in the susceptible population to educate the people, and the study of nature of offending agent in RTA can help the authorities to plan better availability of health care on roads.

Background: Nuclear receptors are a large structural class of transcription factors that act with their co-regulators and repressors to maintain a variety of biological and physiological processes such as metabolism, development and reproduction. They are activated through the binding of small ligands, which can be replaced by drug molecules, making nuclear receptors promising drug targets. Transcriptional regulation of the genes that encode them is central to gaining a deeper understanding of the diversity of their biochemical and biophysical roles and their role in disease and therapy. Even though they share evolutionary history, nuclear receptor genes have fundamentally different expression patterns, ranging from ubiquitously expressed to tissue-specific and spatiotemporally complex. However, current understanding of regulation in nuclear receptor gene family is still nascent., Methodology/principal Findings: In this study, we investigate the relationship between long-range regulation of nuclear receptor family and their known functionality. Towards this goal, we identify the nuclear receptor genes that are potential targets based on counts of highly conserved non-coding elements. We validate our results using publicly available expression (RNA-seq) and histone modification (ChIP-seq) data from the ENCODE project. We find that nuclear receptor genes involved in developmental roles show strong evidence of long-range mechanism of transcription regulation with distinct cis-regulatory content they feature clusters of highly conserved non-coding elements distributed in regions spanning several Megabases, long and multiple CpG islands, bivalent promoter marks and statistically significant higher enrichment of enhancer mark around their gene loci. On the other hand nuclear receptor genes that are involved in tissue-specific roles lack these features, having simple transcriptional controls and a greater variety of mechanisms for producing paralogs. We further examine the combinatorial patterns of histone maps associated with dynamic functional elements in order to explore the regulatory landscape of the gene family. The results show that our proposed classification capturing long-range regulation is strongly indicative of the functional roles of the nuclear receptors compared to existing classifications., Conclusions/significance: We present a new classification for nuclear receptor gene family capturing whether a nuclear receptor is a possible target of long-range regulation or not. We compare our classification to existing structural (mechanism of action) and homology-based classifications. Our results show that understanding long-range regulation of nuclear receptors can provide key insight into their functional roles as well as evolutionary history; and this strongly merits further study.

White spot syndrome caused by white spot syndrome virus (WSSV) is one of the most threatening diseases of shrimp culture industry. Previous studies have successfully demonstrated the use of DNA- and RNA-based vaccines to protect WSSV infection in shrimp. In the present study, we have explored the protective efficacy of antisense constructs directed against WSSV proteins, VP24, and VP28, thymidylate synthase (TS), and ribonucleotide reductase-2 (RR2) under the control of endogenous shrimp histone-3 (H3) or penaedin (Pn) promoter. Several antisense constructs were generated by inserting VP24 (pH3-VP24, pPn-VP24), VP28 (pH3-VP28, pPn-VP28), TS (pH3-TS, pPn-TS), and RR2 (pH3-RR2) in antisense orientation. These constructs were tested for their protective potential in WSSV infected cell cultures, and their effect on reduction of the viral load was assessed. A robust reduction in WSSV copy number was observed upon transfection of antisense constructs in hemocyte cultures derived from Penaeus monodon and Scylla serrata. When tested in vivo, antisense constructs offered a strong protection in WSSV challenged P. monodon. Constructs expressing antisense VP24 and VP28 provided the best protection (up to 90 % survivability) with a corresponding decrease in the viral load. Our work demonstrates that shrimp treated with antisense constructs present an efficient control strategy for combating WSSV infection in shrimp aquaculture.

A series of benzo[b]furans was synthesized with modification at the 5-position of the benzene ring by introducing C-linked substituents (aryl, alkenyl, alkynyl, etc.). These compounds were evaluated for their antiproliferative activities, inhibition of tubulin polymerization, and cell-cycle effects. Some compounds in this series displayed excellent activity in the nanomolar range against lung cancer (A549) and renal cell carcinoma (ACHN) cancer cell lines. (6-Methoxy-5-((4-methoxyphenyl)ethynyl)-3-methylbenzofuran-2-yl)(3,4,5-trimethoxyphenyl)methanone (26) and (E)-3-(6-methoxy-3-methyl-2-(1-(3,4,5-trimethoxyphenyl)vinyl)benzofuran-5-yl)prop-2-en-1-ol (36) showed significant activity in the A549 cell line, with IC₅₀ values of 0.08 and 0.06 μM, respectively. G₂/M cell-cycle arrest and subsequent apoptosis was observed in the A549 cell line after treatment with these compounds. The most active compound in this series, 36, also inhibited tubulin polymerization with a value similar to that of combretastatin A-4 (1.95 and 1.86 μM, respectively). Furthermore, detailed biological studies such as Hoechst 33258 staining, DNA fragmentation and caspase-3 assays, and western blot analyses with the pro-apoptotic protein Bax and the anti-apoptotic protein Bcl-2 also suggested that these compounds induce cell death by apoptosis. Molecular docking studies indicated that compound 36 interacts and binds efficiently with the tubulin protein., (Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Syntheses of a new series of biologically potent α-aminophosphonates were accomplished by one-pot Kabachnik-Fields reaction using TiO2-SiO2 as solid supported catalyst under microwave irradiation conditions. The chemical structures of all the newly synthesized compounds were confirmed by analytical and spectral (IR, 1H, 13C, 31P NMR, and mass) data. Their anticancer nature was evaluated by screening the in vitro activity on two human cancer cell lines, HeLa and SK-BR-3. Compounds 4i and 4o showed the best activity on these cancer cells even though the majority of the compounds, and particularly 4l and 4p, have good cytotoxic activity against them., (© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Off-pump coronary artery bypass involves precise manipulations for proper positioning the heart without causing hemodynamic compromise. Pericardial stay sutures exerting appropriate traction play an important role in off-pump surgery. We report a rare case in which a congenital pericardial defect was discovered after sternotomy in a patient undergoing off-pump coronary artery bypass.

Deforestation and fragmentation are important concerns in managing and conserving tropical forests and have global significance. In the Indian context, in the last one century, the forests have undergone significant changes due to several policies undertaken by government as well as increased population pressure. The present study has brought out spatiotemporal changes in forest cover and variation in forest type in the state of Odisha (Orissa), India, during the last 75 years period. The mapping for the period of 1924-1935, 1975, 1985, 1995 and 2010 indicates that the forest cover accounts for 81,785.6 km(2) (52.5 %), 56,661.1 km(2) (36.4 %), 51,642.3 km(2) (33.2 %), 49,773 km(2) (32 %) and 48,669.4 km(2) (31.3 %) of the study area, respectively. The study found the net forest cover decline as 40.5 % of the total forest and mean annual rate of deforestation as 0.69 % year(-1) during 1935 to 2010. There is a decline in annual rate of deforestation during 1995 to 2010 which was estimated as 0.15 %. Forest type-wise quantitative loss of forest cover reveals large scale deforestation of dry deciduous forests. The landscape analysis shows that the number of forest patches (per 1,000) are 2.463 in 1935, 10.390 in 1975, 11.899 in 1985, 12.193 in 1995 and 15.102 in 2010, which indicates high anthropogenic pressure on the forests. The mean patch size (km(2)) of forest decreased from 33.2 in 1935 to 5.5 in 1975 and reached to 3.2 by 2010. The study demonstrated that monitoring of long term forest changes, quantitative loss of forest types and landscape metrics provides critical inputs for management of forest resources.

A series of new diethyl(alkyl/aryl/heteroarylamino)(4-(pyridine-2-yl)phenyl)methylphosphonates (4a-t) were synthesized via three-component Kabachnik-Field's reaction of 4-(pyridin-2-yl)benzaldehyde, diethylphosphite and various primary amines, catalyzed by cupric acetate monohydrate [Cu(OAc)(2) ∙ H(2)O] under solvent-free and microwave irradiation conditions. Their computational docking analysis supported them as good therapeutic agents to the breast cancer aromatase enzyme and ascertained 4a, 4h, 4m, 4n, and 4t as potential molecules with good binding affinities varying from -9.0 to -9.6 kcal/mol and containing the 4-(pyridine-2-yl)phenyl moiety as a pharmacophore. Their in vitro screening performed for the anti-cell proliferation activity against MBC-MCF7 cells by MTT and Trypan blue assays confirmed 4m, 4n, and 4q as promising compounds to sustain a low percentage of cell viability at 20 µg/mL concentration. These compounds were also evaluated for their antioxidant activity by the DPPH method and the results established that compounds 4m, 4n, and 4q show around 10% higher activity than the standard antioxidant ascorbic acid., (Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Three LNA-based mercaptoacetamido-linked nonionic nucleoside dimers TL-S-T, T-S-TL, and TL-S-TL have been synthesized by HOBT and HBTU catalyzed condensation of silyl-protected 2-S-(thymidin-5 '-yl)mercaptoacetic acid or 2-S-(2 '-O,4 '-C-methylenethymidin-5 '-yl)mercaptoacetic acid with 3 '-amino-3 '-deoxy-5 '-O-DMT-2 '-O,4 '-C-methylenethymidine or with 3 '-amino-3 '-deoxy-5 '-O-DMT-β-thymidine followed by desilylation of the protected dimers. The 3 '-O-phosphoramidite derivative of one of the nucleoside dimers was successfully prepared by condensation with [P(-Cl)(-OCH2CH2CN)-N(iPr)2}] in DCM in the presence of N,N-diisopropylethylamine (DIPEA), which is a building block for the preparation of mercaptoacetamido-linked oligonucleotides of therapeutic applications.

Superoxide dismutases (SODs) form the foremost line of defense against ROS in aerobes. Pennisetum glaucum cDNA library is constructed to isolate superoxide dismutase cDNA clone (PgCuZnSOD) of 798 bp comprising 5'UTR (111 bp), an ORF (459 bp) and 3'UTR (228 bp). Deduced protein of 152 amino acids (16.7 kDa) with an estimated isoelectric point of 5.76 shared highest homology to cytoplasmic CuZnSODs from monocots i.e., maize, rice. Predicted 3D model reveals a conserved eight-stranded ß-barrel with active site held between barrel and two surface loops. Purified recombinant protein is relatively thermo-stable with maximal activity at pH 7.6 and shows inhibition with H(2)O(2) (4.3 mM) but not with azide (10 mM). In Pennisetum seedlings, abiotic stress induced PgCuZnSOD transcript up-regulation directly correlates to high protein and activity induction. Overexpression of PgCuZnSOD confers comparatively enhanced tolerance to methyl viologen (MV) induced oxidative stress in bacteria. Results imply that PgCuZnSOD plays a functional role in conferring oxidative stress tolerance to prokaryotic system and may hold significant potential to impart oxidative stress tolerance in higher plants through transgenic approach., (Copyright © 2012 Elsevier B.V. All rights reserved.)

Background: Mental health problems like depression, cognitive impairment, anxiety, sleep disorders, and so on, arising out of senility, neurosis, and living conditions are common in the geriatric population., Aims: To study the psychiatric morbidity among the rural elderly., Settings and Design: A community-based, cross-sectional study., Materials and Methods: A study was conducted on 800 rural elderly subjects, aged 60 years and more, living in ten randomly selected villages, served by the Rural Health Training Center (RHTC), Valadi, in Tamilnadu state, India. Cognitive functioning was assessed by the Mini Mental Status Examination (MMSE), and the depression by the Geriatric Depression Scale - Shorter version., Statistical Analysis: The data was analyzed with SPSS 16 version statistical software using proportions, and the chi-square., Results: A majority of the subjects were widows / widowers, illiterates, living with family, and showing economic dependency. The prevalence of cognitive impairment was 43.25%, with a mean MMSE score of 23.32±4.4, and the depression was 47.0% and 6.16±3.4. Cognitive impairment, depression, and a disturbed sleep pattern were associated with female sex, age, illiteracy, poverty, loneliness, and the low socioeconomic status of the family., Conclusions: The study showed a definite association between the sociodemographic factors and psychiatric morbidity. Encouraging the Non-governmental Organizations (NGOs) working for the elderly, running of separate geriatric clinics, and effective implementation of schemes like old age pension are some of the measures to be taken.

Total synthesis of (+)-anamarine a polyoxygenated δ-pyranone natural product was accomplished via cross-metathesis protocol starting from 3-butene-1-ol and glycidol. Other key features of this synthetic strategy include use of Sharpless asymmetric epoxidation, dihydroxylation, and deoxygenation-isomerization through allene rearrangement.

Broadening of the genetic base for identification and transfer of genes for resistance to insect pests and diseases from wild relatives of rice is an important strategy in resistance breeding programs across the world. An accession of Oryza nivara, International Rice Germplasm Collection (IRGC) accession number 105710, was identified to exhibit high level and broad-spectrum resistance to Xanthomonas oryzae pv. oryzae. In order to study the genetics of resistance and to tag and map the resistance gene or genes present in IRGC 105710, it was crossed with the bacterial blight (BB)-susceptible varieties 'TN1' and 'Samba Mahsuri' (SM) and then backcrossed to generate backcross mapping populations. Analysis of these populations and their progeny testing revealed that a single dominant gene controls resistance in IRGC 105710. The BC(1)F(2) population derived from the cross IRGC 105710/TN1//TN1 was screened with a set of 72 polymorphic simple-sequence repeat (SSR) markers distributed across the rice genome and the resistance gene was coarse mapped on chromosome 7 between the SSR markers RM5711 and RM6728 at a genetic distance of 17.0 and 19.3 centimorgans (cM), respectively. After analysis involving 49 SSR markers located between the genomic interval spanned by RM5711 and RM6728, and BC(2)F(2) population consisting of 2,011 individuals derived from the cross IRGC 105710/TN1//TN1, the gene was fine mapped between two SSR markers (RMWR7.1 and RMWR7.6) located at a genetic distance of 0.9 and 1.2 cM, respectively, from the gene and flanking it. The linkage distances were validated in a BC(1)F(2) mapping population derived from the cross IRGC 105710/SM//2 × SM. The BB resistance gene present in the O. nivara accession was identified to be novel based on its unique map location on chromosome 7 and wider spectrum of BB resistance; this gene has been named Xa33. The genomic region between the two closely flanking SSR markers was in silico analyzed for putatively expressed candidate genes. In total, eight genes were identified in the region and a putative gene encoding serinethreonine kinase appears to be a candidate for the Xa33 gene.

One pot three-component PEG-SO(3)H catalyzed reaction of 4-(Pyridin-4-yl)benzaldehyde and triethyl phosphite with various primary amines afforded α-aminophosphonates with high yields by the Kabachnik-Field's reaction. These new structurally diversified set of α-aminophosphonates (4a-j) were evaluated for their anti-tumor activity on human chronic myeloid leukemia cells (K 562), human colon carcinoma cells (Colo 205) along with non-cancerous human embryonic kidney cells (HEK 293). They showed moderate activity on both cancerous cells and non-cancerous cells., (Copyright © 2011 Elsevier Masson SAS. All rights reserved.)

A simple and efficient one pot synthesis of 2-amino-4H-chromen-4-yl phosphonate derivatives has been accomplished by the condensation of salicylaldehyde, malononitrile/ethylcyanoacetate and triethyl phosphite/trimethyl phosphite in the presence of molecular iodine as catalyst in water at room temperature. All the reactions were very clean and the products were obtained in very good to excellent yields. The title compounds are characterized by IR, 1H-, 13C-, 31P-NMR and mass spectra, also studied their antimicrobial and antioxidant activity.

A new series of novel bis[1, 2, 4]triazolo[3, 4-b][1, 3, 4]thiadiazines 7a-j has been synthesized by the reaction of [5, 5'-methylenebis(3-methylbenzofuran-7, 5-diyl)]bis[(4-amino-5-thioxo-4, 5-dihydro-1H-1, 2, 4-triazol-3-yl)methanone] (6) with a variety of phenacyl bromides in ethanol under reflux for 6 h. All the newly synthesized compounds were tested for in vitro activity against certain strains of bacteria such as Escherichia coli, Klebsiella pneumoniae, Shigella dysenteriae and Shigella flexneri. Compounds 7a, 7c and 7g were highly active against the entire organism employed. Compound 7c showed the activity higher than the standard drug neomycin, and almost equal to the streptomycin. Compounds 7a-j were also screened for their antifungal activity against Aspergillus niger, Candida albicans, Aspergillus flavus and Rhizopus oryzae. Compounds with methoxyphenyl moiety 7d and dichlorophenyl moiety 7f showed significant activity against the tested fungal strains.

A novel series of 2-(3, 5-dimethyl-1-phenyl-1H-4-pyrazolyl)-3-(aryl/heteroaryl)-1, 3-thiazolidin-4-one derivatives 4a-h has been synthesized readily in one-pot from 3, 5-dimethyl-1-phenyl-1H-4-pyrazolecarbaldehyde (3), and characterized via IR, NMR, MS and elemental analyses. Further, these compounds were screened for antibacterial (MIC) activity against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Staphylococcus pyogenes. Amongst them, compounds containing pyridyl 4g and pyrimidinyl 4h moiety exerted superior antibacterial activity against S. aureus and E. coli at the concentration of 6.25 µg/mL, which is less than the concentration of the standards neomycin and streptomycin, and emerged as potential molecules for further development.

Secalonic acid D (SAD), a cleft palate-inducing teratogen, has been shown to inhibit proliferation/cell cycle progression in association with alteration in the levels of cell cycle regulators, p21 and cyclin E. These studies were conducted to test the hypotheses that p21 and cyclin E play an important functional role in normal human embryonic palatal mesenchymal (HEPM) cell cycle and that their up- and down-regulation, respectively, by SAD is functionally significant to its cell cycle block. Using small interfering RNA (siRNA) to silence p21 gene and transient transfection to overexpress cyclin E in control & SAD-treated HEPM cells, cell proliferation was assessed using a combination of cell numbers, thymidine uptake, CDK2 activity and Ki-67 expression. The results showed that silencing of p21 gene, although increased cell proliferation/numbers and CDK2 activity in normal HEPM cells, failed to counteract SAD-induced anti-proliferative effect despite inducing partial recovery of CDK2 activity. Similar effects were apparent with cyclin E overexpression. It is concluded that p21 and cyclin E are important for normal HEPM cell proliferation. However, SAD-induced deregulation of either protein, singly, may not be sufficient to induce anti-proliferative effect. Involvement of other cell cycle proteins such as cyclin D1 or of multiple proteins in SAD-induced cell cycle block needs to be examined.

This study aims at determining the possible changes in intracellular calcium (Ca (i) (2+) ), plasma membrane calcium ATPase (PMCA) activity and phosphatidylserine (PS) along with glutathione (GSH) level in response to an oxidant challenge in vitro. Erythrocytes were isolated on Percoll and incubated with 2, 2'azobis (2-aminopropane) hydrochloride (AAPH) as well as with vitamin C preceding AAPH incubation. Membrane integrity in terms of hemolysis was negatively related to acetylcholine esterase (AChE) activity with the extent of reduction under OS being higher in the old erythrocyte than in the young. A divergent pattern was seen towards lower PMCA and higher (Ca (i) (2+) ) in the young and old cells. However, the PMCA activity in the stressed young cell was high when pre-treated with vitamin C. PS externalization in the young under OS is perhaps analogous to normal aging, with vitamin C preventing premature death. These findings suggest that young erythrocytes may benefit from vitamin C in therapies addressed towards the mechanisms underlying the reduced effects of OS.

A new series of tetraphenyl bisphosphonates have been elegantly synthesized by one-pot method and were characterized by elemental analysis, FTIR, 1H, 13C, 31P NMR, mass spectra and evaluated for their in vitro antibone resorptive activity by inhibiting growth of osteoclasts. Two bisphosphonates 3g and 3f showed marked inhibition ratio (8 μM and 10 μM) and emerged as lead compounds. All compounds were tested for their antioxidant (DPPH scavenging, reducing power and inhibition of lipid peroxidation). They exhibited potent in vitro antioxidant activity dose-dependently., (Copyright © 2011 Elsevier Masson SAS. All rights reserved.)

A seven year old female child presented with two episodes of vaginal bleeding and bilateral breast development. Examination showed normal anthropometric measurements and external genitalia of prepubertal type. Her 5-year old younger brother and her father had gynaecomastia. Search for a structural cause for precocious puberty was negative. Occupational exposure of her father to hormonal dust was identified as the cause. All pubertal changes reverted to normal after observing suitable precautions.

Accurate functional annotation of protein sequences is hampered by important factors such as the failure of sequence search methods to identify relationships and the inherent diversity in function of proteins related at low sequence similarities. Earlier, we had employed intermediate sequence search approach to establish new domain relationships in the unassigned regions of gene products at the whole genome level by taking Mycoplasma gallisepticum as a specific example and established new domain relationships. In this paper, we report a detailed comparison of the conservation status of the domain and domain architectures of the gene products that bear our newly predicted domains amongst 14 other Mycoplasma genomes and reported the probable implications for the organisms. Some of the domain associations, observed in Mycoplasma that afflict humans and other non-human primates, are involved in regulation of solute transport and DNA binding suggesting specific modes of host-pathogen interactions.