Novel Biginelli dihydropyrimidines with potential anticancer activity: A parallel synthesis and CoMSIA study

Novel Biginelli dihydropyrimidines of biological interest were prepared using p-toluene sulphonic acid as an efficient catalyst. All the thirty-two synthesised dihydropyrimidines were evaluated for their in vitro antioxidant activity using DPPH method. Only, compounds 28 and 29 exhibited reasonably good antioxidant activity. Furthermore, the synthesised Biginelli compounds were subjected for their in vitro anticancer activity against MCF-7 human breast cancer cells. The title compounds were tested at the concentration of 10 μg. Compounds exhibited activity ranging from weak to moderate and, from moderate to high in terms of percentage cytotoxicity. Among them, compounds 10 and 11 exhibited significant anticancer activity. In order to elucidate the three-dimensional structure–activity relationships (3D QSAR) towards their anticancer activity, we subjected them for comparative molecular similarity indices analysis (CoMSIA). Illustration regarding their synthesis, analysis, antioxidant activity, anticancer activity and 3D QSAR study is described.

Effect of magnetic and electrical fields on dendritic freezing of aqueous solutions of sodium chloride

Aqueous solutions of sodium chloride were solidified under the influence of magnetic and electrical fields using two different freezing systems. In the droplet system, small droplets of the solution are introduced in an organic liquid column at −20°C which acts as the heat sink. In the unidirectional freezing system the solutions are poured into a tygon tube mounted on a copper chill, maintained at −70°C, from which the freezing initiates. Application of magnetic fields caused an increase in the spacing and promoted side branching of primary ice dendrites in the droplet freezing system, but had no measurable effect on the dendrites formed in the unidirectional freezing system. The range of electric fields applied in this investigation had no measurable effect on the dendritic structure. Possible interactions between external magnetic and electrical fields have been reviewed and it is suggested that the selective effect of magnetic fields on dendrite spacings in a droplet system could be due to a change in the nucleation behaviour of the solution in the presence of a magnetic field.

Generation of High Magnetic Fields Using Thyristors

This paper describes the use of high-power thyristors in conjunction with a low-voltage supply for generating pulsed magnetic fields. A modular bank of electrolytic capacitors is charged through a programmable solid-state power supply and then rapidly discharged through a bank of thyristors into a magnetizing coil. The modular construction of capacitor banks enables the discrete control of pulse energy and time. Peak fields up to 15 telsa (150 KOe) and a half period of about 200 microseconds are generated through the discharges. Still higher fields are produced by discharging into a precooled coil ( 77°K). Measurement method for a pulsed field is described.

Evaluating pasture species for less fertile soils in a subtropical aseasonal low rainfall zone

Grasses, legumes, saltbushes and herbs were evaluated at 6 sites in southern inland Queensland to identify potential pasture and forage plants for use on marginal cropping soils. The region experiences summer heat waves and severe winter frosts. Emphasis was on perennial plants, and native species were included. Seedlings were transplanted into the unfertilized fields in either summer or autumn to suit the growing season of plants, and watered to ensure estab-lishment. Summer-growing grasses were the most successful group, while cool season-growing perennials mostly failed. Summer legumes were disappointing, with Stylosanthes scabra and Indigofera schimperi performing best. Some lines such as I. schimperi and the Eragrostis hybrid cv. Cochise were assessed as potential weeds owing to low animal acceptance. Native Rhynchosia minima grew well at some sites and deserves more study. Cenchrus ciliaris was always easy to establish and produced the highest yields. Persistence of some Digitaria and Bothriochloa species, Eragrostis curvula and Fingerhuthia africana at specific sites was encouraging, but potential weediness needs careful assessment. Standard species were identified to represent the main forage types, such as Austrostipa scabra for cool season-growing grasses, for incorporation into future trials with new genetic materials. The early field testing protocol used should be considered for use elsewhere, if unreliable rainfall poses a high risk of establishment failure from scarce seed.

Biological management of the invasive Vachellia nilotica ssp. indica (Benth.) Kyal. & Boatwr. (Fabales: Mimosoideae) in tropical Australia: stress-inducing potential of Anomalococcus indicus Ramakrishna (Insecta: Hemiptera: Coccoidea: Lecanodiaspididae), an agent of promise

Vachellia nilotica ssp. indica (hereafter, V. n. indica) is an important tree weed in Australia. Its dense populations induce undesirable changes in the vast areas of northern Australia. Because chemical and mechanical management options appear unviable for various reasons, biological management of this tree is considered a better option. Among the many trialled arthropods in Australian context, Anomalococcus indicus, a lecanodiaspid native to India, has been identified as a potent-candidate, since in India, its native terrain, it is the most widespread and occurs throughout the year. Severe infestations of A. indicus cause defoliation, wilting and death of branches, and occasionally the tree. Populations of A. indicus have been brought into Australia and are being tested for its host specificity under quarantine conditions. This article reports the physiological damage and stress it inflicts in the shoots of V. n. indica. Younger-nymphal instars of A. indicus feed on cortical-parenchyma cells of young stems, whereas the older instars and adults feed from the phloem of old stems. Two conspicuous responses of V. n. indica arising in response to the feeding action of A. indicus are changes in the cell-wall dynamics and irregular cell divisions. The feeding action of A. indicus elicits a sequence of reactions in the stem tissues of V. n. indica such as differentiation of thick-walled elements in the outer cortical parenchyma, differential thickening of cells with supernumerary layers of either suberin or lignin, proliferations of parenchyma and phloem, wall thickening and obliteration of inner lumen of phloem cells, and the sieve plates plugged with callosic deposits. The responses are the culminations of interaction between the virulence factor (one or more of the salivary proteins?) from A. indicus and the resistance factor in V. n. indica. We have analysed structural changes in the context of their functions, by comparing the feeding action of A. indicus with that of other hemipteroids. From the level of stress it induces, this study confirms that A. indicus has the potential to be an effective biological management of V. n. indica in Australia. © 2014 © 2014 Taylor & Francis and Aboricultural Association.

Impact of nitrification inhibitor (DMPP) on soil nitrous oxide emissions from an intensive broccoli production system in sub-tropical Australia

Vegetable cropping systems are often characterised by high inputs of nitrogen fertiliser. Elevated emissions of nitrous oxide (N2O) can be expected as a consequence. In order to mitigate N2O emissions from fertilised agricultural fields, the use of nitrification inhibitors, in combination with ammonium based fertilisers, has been promoted. However, no data is currently available on the use of nitrification inhibitors in sub-tropical vegetable systems. A field experiment was conducted to investigate the effect of the nitrification inhibitor 3,4-dimethylpyrazole phosphate (DMPP) on N2O emissions and yield from broccoli production in sub-tropical Australia. Soil N2O fluxes were monitored continuously (3 h sampling frequency) with fully automated, pneumatically operated measuring chambers linked to a sampling control system and a gas chromatograph. Cumulative N2O emissions over the 5 month observation period amounted to 298 g-N/ha, 324 g-N/ha, 411 g-N/ha and 463 g-N/ha in the conventional fertiliser (CONV), the DMPP treatment (DMPP), the DMMP treatment with a 10% reduced fertiliser rate (DMPP-red) and the zero fertiliser (0N), respectively. The temporal variation of N2O fluxes showed only low emissions over the broccoli cropping phase, but significantly elevated emissions were observed in all treatments following broccoli residues being incorporated into the soil. Overall 70–90% of the total emissions occurred in this 5 weeks fallow phase. There was a significant inhibition effect of DMPP on N2O emissions and soil mineral N content over the broccoli cropping phase where the application of DMPP reduced N2O emissions by 75% compared to the standard practice. However, there was no statistical difference between the treatments during the fallow phase or when the whole season was considered. This study shows that DMPP has the potential to reduce N2O emissions from intensive vegetable systems, but also highlights the importance of post-harvest emissions from incorporated vegetable residues. N2O mitigation strategies in vegetable systems need to target these post-harvest emissions and a better evaluation of the effect of nitrification inhibitors over the fallow phase is needed.

Influence of interleukin-1 beta on platelet-poor plasma clot formation: A potential impact on early bone healing

Objectives Hematoma quality (especially the fibrin matrix) plays an important role in the bone healing process. Here, we investigated the effect of interleukin-1 beta (IL-1β) on fibrin clot formation from platelet-poor plasma (PPP). Methods Five-milliliter of rat whole-blood samples were collected from the hepatic portal vein. All blood samples were firstly standardized via a thrombelastograph (TEG), blood cell count, and the measurement of fibrinogen concentration. PPP was prepared by collecting the top two-fifths of the plasma after centrifugation under 400 × g for 10min at 20°C. The effects of IL-1β cytokines on artificial fibrin clot formation from PPP solutions were determined by scanning electronic microscopy (SEM), confocal microscopy (CM), turbidity, and clot lysis assays. Results The lag time for protofibril formation was markedly shortened in the IL-1β treatment groups (243.8 ± 76.85 in the 50 pg/mL of IL-1β and 97.5 ± 19.36 in the 500 pg/mL of IL-1β) compared to the control group without IL-1β (543.8 ± 205.8). Maximal turbidity was observed in the control group. IL-1β (500 pg/mL) treatment significantly decreased fiber diameters resulting in smaller pore sizes and increased density of the fibrin clot structure formed from PPP (P < 0.05). The clot lysis assay revealed that 500 pg/mL IL-1β induced a lower susceptibility to dissolution due to the formation of thinner and denser fibers. Conclusion IL-1β can significantly influence PPP fibrin clot structure, which may affect the early bone healing process.

Beasts on Fields. Human-Wildlife Conflicts in Nature-Culture Borderlands

Human-wildlife conflicts are today an integral part of the rural development discourse. In this research, the main focus is on the spatial explanation which is not a very common approach in the reviewed literature. My research hypothesis is based on the assumption that human-wildlife conflicts occur when a wild animal crosses a perceived borderline between the nature and culture and enters into the realms of the other. The borderline between nature and culture marks a perceived division of spatial content in our senses of place. The animal subject that crosses this border becomes a subject out of place meaning that the animal is then spatially located in a space where it should not be or where it does not belong according to tradition, custom, rules, law, public opinion, prevailing discourse or some other criteria set by human beings. An appearance of a wild animal in a domesticated space brings an uncontrolled subject into that space where humans have previously commanded total control of all other natural elements. A wild animal out of place may also threaten the biosecurity of the place in question. I carried out a case study in the Liwale district in south-eastern Tanzania to test my hypothesis during June and July 2002. I also collected documents and carried out interviews in Dar es Salaam in 2003. I studied the human-wildlife conflicts in six rural villages, where a total of 183 persons participated in the village meetings. My research methods included semi-structured interviews, participatory mapping, questionnaire survey and Q- methodology. The rural communities in the Liwale district have a long-history of co-existing with wildlife and they still have traditional knowledge of wildlife management and hunting. Wildlife conservation through the establishment of game reserves during the colonial era has escalated human-wildlife conflicts in the Liwale district. This study shows that the villagers perceive some wild animals differently in their images of the African countryside than the district and regional level civil servants do. From the small scale subsistence farmers point of views, wild animals continue to challenge the separation of the wild (the forests) and the domestics spaces (the cultivated fields) by moving across the perceived borders in search of food and shelter. As a result, the farmers may loose their crops, livestock or even their own lives in the confrontations of wild animals. Human-wildlife conflicts in the Liwale district are manifold and cannot be explained simply on the basis of attitudes or perceived images of landscapes. However, the spatial explanation of these conflicts provides us some more understanding of why human-wildlife conflicts are so widely found across the world.

Does gait speed indicate prosthetic walking potential following lower limb amputation?

Background: Gait speed is an indicator of walking ability, morbidity and mortality; and is a reliable, valid and sensitive outcome measure commonly used in the rehabilitation setting. Gait speed is a quick and efficient assessment method; yet, to date, there has been little investigation of its potential use in populations with lower limb amputation.

Remote sensing of boreal land cover: estimation of forest attributes and extent

Remote sensing provides methods to infer land cover information over large geographical areas at a variety of spatial and temporal resolutions. Land cover is input data for a range of environmental models and information on land cover dynamics is required for monitoring the implications of global change. Such data are also essential in support of environmental management and policymaking. Boreal forests are a key component of the global climate and a major sink of carbon. The northern latitudes are expected to experience a disproportionate and rapid warming, which can have a major impact on vegetation at forest limits. This thesis examines the use of optical remote sensing for estimating aboveground biomass, leaf area index (LAI), tree cover and tree height in the boreal forests and tundra taiga transition zone in Finland. The continuous fields of forest attributes are required, for example, to improve the mapping of forest extent. The thesis focus on studying the feasibility of satellite data at multiple spatial resolutions, assessing the potential of multispectral, -angular and -temporal information, and provides regional evaluation for global land cover data. Preprocessed ASTER, MISR and MODIS products are the principal satellite data. The reference data consist of field measurements, forest inventory data and fine resolution land cover maps. Fine resolution studies demonstrate how statistical relationships between biomass and satellite data are relatively strong in single species and low biomass mountain birch forests in comparison to higher biomass coniferous stands. The combination of forest stand data and fine resolution ASTER images provides a method for biomass estimation using medium resolution MODIS data. The multiangular data improve the accuracy of land cover mapping in the sparsely forested tundra taiga transition zone, particularly in mires. Similarly, multitemporal data improve the accuracy of coarse resolution tree cover estimates in comparison to single date data. Furthermore, the peak of the growing season is not necessarily the optimal time for land cover mapping in the northern boreal regions. The evaluated coarse resolution land cover data sets have considerable shortcomings in northernmost Finland and should be used with caution in similar regions. The quantitative reference data and upscaling methods for integrating multiresolution data are required for calibration of statistical models and evaluation of land cover data sets. The preprocessed image products have potential for wider use as they can considerably reduce the time and effort used for data processing.

Perennial pastures for marginal farming country in southern Queensland. 2. Potential new grass cultivar evaluation

Trials in the Condamine-Balonne basin, Australia, compared 11 promising perennial pasture grass accessions (4 Bothriochloa, 2 Cenchrus, 2 Urochloa and 1 each of Digitaria, Eragrostis and Panicum species) against the best similar commercial cultivars on the basis of ease of establishment from seed, persistence once established, forage yield and ease of seed production. Accessions sown at a site were determined by prior experience with them on a range of soils. High quality seed was relatively easy to produce for both Urochloa species and for Eragrostis curvula CPI 30374 but problematic for the Bothriochloa spp. Once established, all accessions persisted for 3–5 years and most were well grazed, but adequate establishment was sometimes a problem with Panicum stapfianum and Bothriochloa ewartiana. The dry matter yield ratings of the non-commercial lines were similar to those of the commercial equivalents of the same species. While agronomically valuable, none of the promising new grasses was considered worthy of commercialization at this point because their strengths did not warrant the setting up of a seed-production business in competition with current commercial enterprises. Long-standing cultivars such as Gayndah buffel and Nixon sabi grass continued to exhibit their superior pasture qualities.

Methane in Australian agriculture: current emissions, sources and sinks, and potential mitigation strategies

Methane is a potent greenhouse gas with a global warming potential ∼28 times that of carbon dioxide. Consequently, sources and sinks that influence the concentration of methane in the atmosphere are of great interest. In Australia, agriculture is the primary source of anthropogenic methane emissions (60.4% of national emissions, or 3260kt-1methaneyear-1, between 1990 and 2011), and cropping and grazing soils represent Australia's largest potential terrestrial methane sink. As of 2011, the expansion of agricultural soils, which are ∼70% less efficient at consuming methane than undisturbed soils, to 59% of Australia's land mass (456Mha) and increasing livestock densities in northern Australia suggest negative implications for national methane flux. Plant biomass burning does not appear to have long-term negative effects on methane flux unless soils are converted for agricultural purposes. Rice cultivation contributes marginally to national methane emissions and this fluctuates depending on water availability. Significant available research into biological, geochemical and agronomic factors has been pertinent for developing effective methane mitigation strategies. We discuss methane-flux feedback mechanisms in relation to climate change drivers such as temperature, atmospheric carbon dioxide and methane concentrations, precipitation and extreme weather events. Future research should focus on quantifying the role of Australian cropping and grazing soils as methane sinks in the national methane budget, linking biodiversity and activity of methane-cycling microbes to environmental factors, and quantifying how a combination of climate change drivers will affect total methane flux in these systems.

Mössbauer Lineshape in the Presence of Radio-Frequency Fields

A general expression for the Mössbauer lineshape in the presence of a radio frequency field is derived. As an example the effect of the rf field on Fe57 nuclei is discussed for a situation where the 3/2 sublevel of 14.4 keV state of Fe57 is selectively populated. At resonance, both the diagonal and non-diagonal matrix elements contribute to the correlation function. As a result, in addition to a slight rf induced distortion of the main Mössbauer line. additional transition lines are obtained. Thus the present calculation supports the experimental observations of Heiman et al.

The leaf-feeding geometrid Isturgia disputaria (Guenee)-A potential biological control agent for prickly acacia, Vachellia nilotica subsp. indica (Benth.) Kyal. & Boatwr. (Mimosaceae) in Australia

Prickly acacia (Vachellia nilotica subsp. indica), a native multipurpose tree in India, is a weed of National significance, and a target for biological control in Australia. Based on plant genetic and climatic similarities, native range surveys for identifying potential biological control agents for prickly acacia were conducted in India during 2008-2011. In the survey leaf-feeding geometrid, Isturgia disputaria Guenee (syn. Tephrina pulinda), widespread in Tamil Nadu and Karnataka States, was prioritized as a potential biological control agent based on field host range, damage potential and no choice test on non target plant species. Though the field host range study exhibited that V. nilotica ssp. indica and V. nilotica ssp. tomentosa were the primary hosts for successful development of the insect, I. disputaria, replicated no - choice larval feeding and development tests conducted on cut foliage and live plants of nine non-target acacia test plant species in India revealed the larval feeding and development on three of the nine non-target acacia species, V. tortilis, V. planiferons and V. leucophloea in addition to the V. nilotica ssp. indica and V. nilotica ssp. tomentosa. However, the proportion of larvae developing into adults was higher on V. nilotica subsp. indica and V. nilotica subsp. tomentosa, with 90% and 80% of the larvae completing development, respectively. In contrast, the larval mortality was higher on V. tortilis (70%), V. leucophloea (90%) and V. planiferons (70%). The no-choice test results support the earlier host specificity test results of I. disputaria from Pakistan, Kenya and under quarantine in Australia. Contrasting results between field host range and host use pattern under no-choice conditions are discussed.

The host range of three biotypes of Dactylopius tomentosus (Lamarck) (Hemiptera: Dactylopiidae) and their potential as biological control agents of Cylindropuntia spp. (Cactaceae) in Australia

The host range of two newly imported biotypes of Dactylopius tomentosus and their potential as biological control agents of Cylindropuntia spp. were investigated. A third biotype (imbricata) of D. tomentosus previously released in Australia to control C. imbricata was also screened to determine if it will feed on other species of Cylindropuntia occurring in Australia. Efficacy trials were conducted to evaluate the ability of the biotypes to retard the growth or kill those plant species supporting development of four or more individuals in the host test trials. The host range of the three biotypes of D. tomentosus was restricted to the genus Cylindropuntia. However, the biotypes showed varying degrees of specificity within this genus. The imbricata biotype was the only biotype to develop on Australian C. rosea provenances, albeit with a range of developmental success on all C. rosea provenances tested. The Spanish provenance supported the highest development success followed by Grawin (NSW), Lorne Station (NSW) while the least preferred was the Mexican provenance. The rosea and cholla biotypes were unsuitable candidates to control C. rosea in Australia. However, the efficacy trials showed that the cholla biotype had a high impact on four of the eight naturalised Cylindropuntia species in Australia. This biotype established rapidly and the sustained feeding of one fecund female and her progeny killed potted plants of C. imbricata and C. fulgida at week 18. This biotype has the potential to be an effective agent against C. fulgida, C. imbricata, C. kleiniae and C. tunicata and, as a consequence, an application seeking its release in Australia has been lodged.