Synthesis and Characterisation of a Boron-Rich Symmetric Triazine Bearing a Hypoxia-Targeting Nitroimidazole Moiety

Boron Neutron Capture Therapy (BNCT) is a binary therapy that promises to be suitable in treating many non-curable cancers. To that, the discovery of new boron compounds able to accumulate selectively in the tumour tissue is still required. Hypoxia, a deficiency of oxygen in tumor tissue, is a great challenge in the conventional treatment of cancer, because hypoxic areas are resistant to conventional anticancer treatments. 2-Nitroimidazole derivatives are known to be hypoxia markers due to their enrichment by bioreduction in hypoxic cells. In the present work, 2-nitroimidazole was chosen as the starting point for the synthesis of a new boron-containing compound based on a 1,3,5-triazine skeleton. Two o-carborane moieties were inserted to achieve a high ratio of boron on the molecular weight, exploiting a short PEG spacer to enhance the polarity of the compound and outdistance the active part from the core. The compound showed no toxicity on normal human primary fibroblasts, while it showed noteworthy toxicity in multiple myeloma cells together with a consistent intracellular boron accumulation

Risk assessment of war wrecks – a comprehensive approach investigating four wrecks containing munitions in the German Bight/North Sea

Shipwrecks and dumped munition continue to be a major hazard, both in the North Sea but also on a global scale. Research within the EU Interreg project North Sea Wrecks (NSW), in cooperation with the German Aerospace Centre, Institute for the Protection of Maritime Infrastructures (DLR), is generating new insights into the status of wrecks, the potential leakage of pollutants from remaining munitions loads and the effects of contamination on exposed marine organisms in the North Sea environment. Further, historical documents are generated from archives to describe ship’s history and sinking scenario. These historical findings were compared to models and images of the visual inspections of the wrecks. Further, samples of water, sediment and organisms are being analysed for traces of explosives. Combining the results of these different fields of research allows for a better understanding of the environmental risks deriving from these wrecks. This process is shown below by focusing on the wreck of the German light cruiser SMS MAINZ, which sank in 1914. Data were compared to three additional wrecks situated also within the southern German Bight. Available data about the wrecks were preliminary assessed using a wreck risk model. Finally, wrecks were ranked according to their potential environmental risk

Energetic Compounds in the Trophic Chain—A Pilot Study Examining the Exposure Risk of Common Eiders (Somateria mollissima) to TNT, Its Metabolites, and By-Products

The Baltic and North Seas still contain large amounts of dumped munitions from both World Wars. The exposure of the munition shells to the seawater causes corrosion, which leads to the disintegration of shells and a leakage of energetic compounds, including the highly toxic 2,4,6-trinitrotoluene (TNT), and consequently threatening the marine environment. To evaluate the risk of accumulation of energetic compounds from conventional munitions in the marine food chain, we analyzed the presence of TNT and its metabolites 2-amino-4,6-dinitrotoluene (2-ADNT) and 4-amino-2,6-dinitrotoluene (4-ADNT) as well as their byproducts 1,3-dinitrobenzene (1,3-DNB) and 2,4-dinitrotoluene (2,4-DNT) in different tissues (including muscle, liver, kidney, brain, and bile) from 25 Common Eiders (Somateria mollissima) from the Danish Baltic Sea. Tissues were prepared according to approved protocols, followed by GC-MS/MS analysis. None of the aforementioned energetic compounds were detected in any of the samples. This pilot study is one of the first analyzing the presence of explosive chemicals in tissues from a free-ranging predatory species. This study highlights the need for continuous monitoring at different levels of the trophic chain to increase our knowledge on the distribution and possible accumulation of energetic compounds in the marine environment in order to provide reliable data for decision-making tools and risk assessments

Synthesis and Characterisation of a Boron-Rich Symmetric Triazine Bearing a Hypoxia-Targeting Nitroimidazole Moiety

Boron Neutron Capture Therapy (BNCT) is a binary therapy that promises to be suitable in treating many non-curable cancers. To that, the discovery of new boron compounds able to accumulate selectively in the tumour tissue is still required. Hypoxia, a deficiency of oxygen in tumor tissue, is a great challenge in the conventional treatment of cancer, because hypoxic areas are resistant to conventional anticancer treatments. 2-Nitroimidazole derivatives are known to be hypoxia markers due to their enrichment by bioreduction in hypoxic cells. In the present work, 2-nitroimidazole was chosen as the starting point for the synthesis of a new boron-containing compound based on a 1,3,5-triazine skeleton. Two o-carborane moieties were inserted to achieve a high ratio of boron on the molecular weight, exploiting a short PEG spacer to enhance the polarity of the compound and outdistance the active part from the core. The compound showed no toxicity on normal human primary fibroblasts, while it showed noteworthy toxicity in multiple myeloma cells together with a consistent intracellular boron accumulation