Derivation of site-specific environmental quality guideline values for fuel-contaminated soils on sub-Antarctic Macquarie Island.

Accidental fuel spills associated with the storage, transfer, and use of diesel fuel for power generation have occurred on sub-Antarctic Macquarie Island since the establishment of the island's research station in 1948. An extensive in situ remediation program was implemented by the Australian government from 2009 to 2016 that used nutrient addition and air sparging to enhance the microbial degradation of petroleum products. During this period, a range of ecotoxicological assessments were conducted to better understand the impacts of fuel in soils on native biota and their sensitivity.

Assessing risks from fuel contamination in Antarctica: Dynamics of diesel ageing in soil and toxicity to an endemic nematode.

Fuel spills are a major source of contamination in terrestrial environments in Antarctica. Little is known of the effects of hydrocarbon contaminants in fuels on Antarctic terrestrial biota, and how these change as fuel ages within soil. In this study we investigate the sensitivity of juveniles of the endemic Antarctic nematode Plectus murrayi to diesel-spiked soil.

Using an expert judgment response matrix to assess the risk of groundwater discharges from remediated fuel spill sites to the marine environment at sub-Antarctic Macquarie Island, Australia.

This study assesses toxicity of groundwater from remediated fuel spill sites, as the final phase of an environmental risk assessment of contaminated sites at sub-Antarctic Macquarie Island, Tasmania, Australia. To complement previous terrestrial ecotoxicological research, we determine risk to marine environments from residual biodegraded hydrocarbon contaminants in groundwater discharges. Direct toxicity assessments were conducted on 7 composite groundwater test solutions, adjusted to ambient seawater salinity.

Semi-Automated Analysis of Digital Photographs for Monitoring East Antarctic Vegetation.

Climate change is affecting Antarctica and minimally destructive long-term monitoring of its unique ecosystems is vital to detect biodiversity trends, and to understand how change is affecting these communities. The use of automated or semi-automated methods is especially valuable in harsh polar environments, as access is limited and conditions extreme. We assessed moss health and cover at six time points between 2003 and 2014 at two East Antarctic sites.

Sensitivity to Copper and Development of Culturing and Toxicity Test Procedures for the Antarctic Terrestrial Nematode Plectus murrayi.

Environmental quality guideline values and remediation targets, specific to Antarctic ecosystems, are required for the risk assessment and remediation of contaminated sites in Antarctica. Ecotoxicological testing with Antarctic soil organisms is fundamental in determining reliable contaminant effect threshold concentrations. The present study describes the development of optimal culturing techniques and aqueous toxicity test procedures for an endemic Antarctic soil nematode, Plectus murrayi, which lives within interstitial waters between soil particles.

Response of the Native Springtail Parisotoma insularis to Diesel Fuel-Contaminated Soils Under Field-Realistic Exposure Conditions at Subantarctic Macquarie Island.

A number of sites contaminated by petroleum hydrocarbons from past fuel spills are currently undergoing remediation on subantarctic Macquarie Island (under the jurisdiction of Tasmania, Australia). To assess the environmental risks these spills pose, and to establish remediation targets and guideline values, toxicity data for a range of native biota are required. The availability of data for local biota is limited, especially for soil invertebrates, which are critical to soil health.

Sensitivity of a Large and Representative Sample of Antarctic Marine Invertebrates to Metals.

There are limited data on the sensitivity to contaminants of marine organisms in polar regions. Consequently, assessments of the risk of contaminants to marine biota in polar environments typically include extrapolations from temperate and/or tropical species. This is problematic because the taxonomic composition of organisms differs between polar and temperate/tropical waters, and both the toxicity of chemicals and the physiology of organisms are very different at the stable low temperatures experienced in polar marine systems.

Moving beyond presence and absence when examining changes in species distributions.

Species distributions are often simplified to binary representations of the ranges where they are present and absent. It is then common to look for changes in these ranges as indicators of the effects of climate change, the expansion or control of invasive species or the impact of human land-use changes. We argue that there are inherent problems with this approach, and more emphasis should be placed on species relative abundance rather than just presence.

Sampling of Sea Ducks for Influenza A Viruses in Alaska during Winter Provides Lack of Evidence for Epidemiologic Peak of Infection.

Sampling of sea ducks for influenza A viruses in Alaska during winter provided no evidence for an epidemiologic peak of infection. Isolates were recovered, however, that provide information on viral diversity and dispersal that may not be realized through sampling efforts focused on other avian taxa.

Soil invertebrate community change over fuel-contaminated sites on a subantarctic island: An ecological field-based line of evidence for site risk assessment.

A number of fuel spills, of both recent and historic origins, have occurred on World Heritage-listed subantarctic Macquarie Island. Sites contaminated by mainly diesel fuels are undergoing remediation by the Australian Antarctic Division. The risks posed by these sites are being managed using a "weight of evidence" approach, for which this study provides a preliminary line of evidence for the ecological assessment component of this site management decision framework.

Impact of hydrocarbons from a diesel fuel on the germination and early growth of subantarctic plants.

Special Antarctic Blend (SAB) is a diesel fuel dominated by aliphatic hydrocarbons that is commonly used in Antarctic and subantarctic regions. The past and present use of SAB fuel at Australia's scientific research stations has resulted in multiple spills, contaminating soils in these pristine areas. Despite this, no soil quality guidelines or remediation targets have been developed for the region, primarily due to the lack of established indigenous test species and subsequent biological effects data.

Toxicity of fuel-contaminated soil to Antarctic moss and terrestrial algae.

Fuel pollution is a significant problem in Antarctica, especially in areas where human activities occur, such as at scientific research stations. Despite this, there is little information on the effects of petroleum hydrocarbons on Antarctic terrestrial biota. The authors demonstrate that the Antarctic mosses Bryum pseudotriquetrum, Schistidium antarctici, and Ceratodon purpureus, and the Antarctic terrestrial alga Prasiola crispa are relatively tolerant to Special Antarctic Blend (SAB) fuel-contaminated soil (measured as total petroleum hydrocarbons).

Phytoremediation of hydrocarbon contaminants in subantarctic soils: an effective management option.

Accidental fuel spills on world heritage subantarctic Macquarie Island have caused considerable contamination. Due to the island's high latitude position, its climate, and its fragile ecosystem, traditional methods of remediation are unsuitable for on-site clean up. We investigated the tolerance of a subantarctic native tussock grass, Poa foliosa (Hook.

Toxicity of diesel contaminated soils to the subantarctic earthworm Microscolex macquariensis.

Several fuel spills have occurred on subantarctic Macquarie Island (54°30' S 158°57' E) associated with storing fuel and generating power for the island's research station. The Australian Antarctic Division began full-scale, on-site remediation of these sites in 2009. To develop appropriate target concentrations for remediation, acute and chronic tests were developed with the endemic earthworm, Microscolex macquariensis, using avoidance, survival, and reproduction as endpoints.

Structure-activity relationship of pyrrole based S-nitrosoglutathione reductase inhibitors: carboxamide modification.

The enzyme S-nitrosoglutathione reductase (GSNOR) is a member of the alcohol dehydrogenase family (ADH) that regulates the levels of S-nitrosothiols (SNOs) through catabolism of S-nitrosoglutathione (GSNO). GSNO and SNOs are implicated in the pathogenesis of many diseases including those in respiratory, gastrointestinal, and cardiovascular systems. The pyrrole based N6022 was recently identified as a potent, selective, reversible, and efficacious GSNOR inhibitor which is currently in clinical development for acute asthma.

Discovery of potent and novel S-nitrosoglutathione reductase inhibitors devoid of cytochrome P450 activities.

The pyrrole based N6022 was recently identified as a potent, selective, reversible, and efficacious S-nitrosoglutathione reductase (GSNOR) inhibitor and is currently undergoing clinical development for the treatment of acute asthma. GSNOR is a member of the alcohol dehydrogenase family (ADH) and regulates the levels of S-nitrosothiols (SNOs) through catabolism of S-nitrosoglutathione (GSNO). Reduced levels of GSNO, as well as other nitrosothiols (SNOs), have been implicated in the pathogenesis of many diseases including those of the respiratory, cardiovascular, and gastrointestinal systems.

Structure-activity relationships of pyrrole based S-nitrosoglutathione reductase inhibitors: pyrrole regioisomers and propionic acid replacement.

S-Nitrosoglutathione reductase (GSNOR) is a member of the alcohol dehydrogenase family (ADH) that regulates the levels of S-nitrosothiols (SNOs) through catabolism of S-nitrosoglutathione (GSNO). GSNO and SNOs are implicated in the pathogenesis of many diseases including those in respiratory, cardiovascular, and gastrointestinal systems. The pyrrole based N6022 was recently identified as a potent, selective, reversible, and efficacious GSNOR inhibitor which is currently undergoing clinical development.

Discovery of s-nitrosoglutathione reductase inhibitors: potential agents for the treatment of asthma and other inflammatory diseases.

S-Nitrosoglutathione reductase (GSNOR) regulates S-nitrosothiols (SNOs) and nitric oxide (NO) in vivo through catabolism of S-nitrosoglutathione (GSNO). GSNOR and the anti-inflammatory and smooth muscle relaxant activities of SNOs, GSNO, and NO play significant roles in pulmonary, cardiovascular, and gastrointestinal function. In GSNOR knockout mice, basal airway tone is reduced and the response to challenge with bronchoconstrictors or airway allergens is attenuated.

Some like it wet - biological characteristics underpinning tolerance of extreme water stress events in Antarctic bryophytes.

Antarctic bryophyte communities presently tolerate physiological extremes in water availability, surviving both desiccation and submergence events. We investigated the relative ability of three Antarctic moss species to tolerate physiological extremes in water availability and identified physiological, morphological, and biochemical characteristics that assist species performance under such conditions. Tolerance of desiccation and submergence was investigated using chlorophyll fluorescence during a series of field- and laboratory-based water stress events.

1H-Pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes: a unique structural class of dopamine D4 selective ligands.

A series of novel 1H-pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes was prepared and screened at selected dopamine receptor subtypes. Compound 4 (NGB 4420) displayed high affinity and selectivity (>100-fold) for the D(4) over D(2) and other CNS receptors. This compound was identified as a D(4) antagonist via its attenuation of dopamine agonist-induced GTPgamma(35)S binding at D(4) receptor.

Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.

A series of chiral benzylpiperazinyl-1-(2,3-dihydro-indol-1-yl)ethanone derivatives were prepared and examined for their affinity at dopamine D(2) and D(4) receptors. Three compounds having D(2)/D(4) affinity ratios approximating that found for the atypical neuroleptic clozapine were further evaluated in behavioral tests of antipsychotic efficacy and motor side effects.

Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.

Optimization of the lead compound 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2,3-dihydro-indol-1-yl)-ethanone 1 by systematic structure-activity relation (SAR) studies lead to two potent compounds 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2-methy-2,3-dihydro-indol-1-yl)-ethanone 2n and 2-[-4-(4-chloro-benzyl)-piperazin-1-yl]-1-(2-methy-2,3-dihydro-indol-1-yl)-ethanone 7b. Their related synthesis was also reported.

6-(4-Benzylpiperazin-1-yl)benzodioxanes as selective ligands at cloned primate dopamine D(4) receptors.

A series of novel 6-(4-benzylpiperazin-1-yl)benzodioxanes were prepared and screened at selected dopamine receptor subtypes. 6-(4-[4-Chlorobenzyl]piperazin-1-yl)benzodioxane (2d) had high affinity and selectivity for the D(4) dopamine receptor subtype and was identified as a D(4) antagonist via its attenuation of dopamine-induced GTPgamma(35)S binding at the D(4) receptor.

trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.

The dopaminergic receptor profile of a series of trans-1-[(2-phenylcyclopropyl)methyl]-4-arylpiperazines was examined. Aromatic substitution patterns were varied with the goal of identifying a compound having affinities for the D(2) and D(4) receptors in a ratio similar to that observed for the atypical neuroleptic clozapine. The compounds (1S, 2S)-trans-1-[(2-phenylcyclopropyl)methyl]-4-(2, 4-dichlorophenyl)piperazine (5m) and (1S, 2S)-trans-1-[(2-phenylcyclopropyl)methyl]-4-(2, 4-dimethylphenyl)piperazine (5t) were selected for functional antagonists at D(2) and D(4) receptors and had a D(2)/D(4) ratio approximating that of clozapine; they proved inactive in behavioral tests of antipsychotic activity.

NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists.

N-(4-[4-¿2, 3-dichlorophenyl¿-1-piperazinyl]butyl)-3-fluorenylcarboxamide and N-(4-[4-¿2, 3-dichlorophenyl¿-1-piperazinyl]butyl)-2-biphenylenylcarboxamide were prepared in several steps from 2,3-dichloroaniline. These compounds were identified as highly selective dopamine D3 receptor antagonists.