ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Background: Infectious diseases, as well as cancer, are the leading causes of death worldwide. Dr... more Background: Infectious diseases, as well as cancer, are the leading causes of death worldwide. Drug resistance usually results in their treatment requiring a combination of two or more drugs. Objective: Oleanolic-based hybrid compounds were prepared via esterification and characterized using FTIR, NMR and LC-MS. In vitro antibacterial and in vitro cytotoxicity studies were performed. Method: Oleanolic acid was hybridized with selected known pharmaceutical scaffolds via the carboxylic acid functionality in order to develop therapeutics with increased biological activity. Antibacterial activity was determined using the micro-dilution assay against selected Gram-positive and Gram-negative bacteria and cytotoxicity using the sulforhodamine B assay. Results: Compound 8 displayed potent antibacterial effect against five strains of bacteria, such as Bacillus subtilis, Staphylococcus aureus, Proteus vulgaris, Klebsiella oxytoca, and Escherichia coli, with MIC values of 1.25, 0.078, 0.078, 1...
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
BACKGROUND Toxicity data regarding combinational exposure of humans to arsenic, cadmium and mercu... more BACKGROUND Toxicity data regarding combinational exposure of humans to arsenic, cadmium and mercury is scarce. Although hepatotoxicity has been reported, limited information is available on their mechanistic underpinnings. The cytotoxic mechanisms of these metals were determined in HepG2 hepatocarcinoma cell lines after individual and combinational exposure. METHODS HepG2 cells were exposed to heavy metals (sodium arsenite, cadmium chloride, and mercury chloride) individually or in combination for 24 h, after which cell density, mitochondrial membrane potential (ΔΨm), reactive oxygen species (ROS), reduced glutathione (GSH), adenosine triphosphate (ATP) and caspase-3/7 activity was assessed. RESULTS AND DISCUSSION Cadmium (IC50 = 0.43 mg/L) and the combination (0.45 mg/L, arsenic reference) were most cytotoxic, followed by arsenic (6.71 mg/L) and mercury (28.23 mg/L). Depolarisation of the ΔΨm and reductions in ROS, GSH and ATP levels occurred. Arsenic, cadmium and the combination increased caspase-3/7 activity, while mercury reduced it. CONCLUSION The combination produced a greater, albeit mechanistically similar, cytotoxicity compared to individual metals. Cytotoxicity was dependent on altered mitochondrial integrity, redox-status, and bioenergetics. Although the combination's cytotoxicity was associated with caspase-3/7 activity, this was not true for mercury. Heavy metal interactions should be assessed to elucidate molecular underpinnings of cytotoxicity.
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Background: Infectious diseases, as well as cancer, are the leading causes of death worldwide. Dr... more Background: Infectious diseases, as well as cancer, are the leading causes of death worldwide. Drug resistance usually results in their treatment requiring a combination of two or more drugs. Objective: Oleanolic-based hybrid compounds were prepared via esterification and characterized using FTIR, NMR and LC-MS. In vitro antibacterial and in vitro cytotoxicity studies were performed. Method: Oleanolic acid was hybridized with selected known pharmaceutical scaffolds via the carboxylic acid functionality in order to develop therapeutics with increased biological activity. Antibacterial activity was determined using the micro-dilution assay against selected Gram-positive and Gram-negative bacteria and cytotoxicity using the sulforhodamine B assay. Results: Compound 8 displayed potent antibacterial effect against five strains of bacteria, such as Bacillus subtilis, Staphylococcus aureus, Proteus vulgaris, Klebsiella oxytoca, and Escherichia coli, with MIC values of 1.25, 0.078, 0.078, 1...
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
BACKGROUND Toxicity data regarding combinational exposure of humans to arsenic, cadmium and mercu... more BACKGROUND Toxicity data regarding combinational exposure of humans to arsenic, cadmium and mercury is scarce. Although hepatotoxicity has been reported, limited information is available on their mechanistic underpinnings. The cytotoxic mechanisms of these metals were determined in HepG2 hepatocarcinoma cell lines after individual and combinational exposure. METHODS HepG2 cells were exposed to heavy metals (sodium arsenite, cadmium chloride, and mercury chloride) individually or in combination for 24 h, after which cell density, mitochondrial membrane potential (ΔΨm), reactive oxygen species (ROS), reduced glutathione (GSH), adenosine triphosphate (ATP) and caspase-3/7 activity was assessed. RESULTS AND DISCUSSION Cadmium (IC50 = 0.43 mg/L) and the combination (0.45 mg/L, arsenic reference) were most cytotoxic, followed by arsenic (6.71 mg/L) and mercury (28.23 mg/L). Depolarisation of the ΔΨm and reductions in ROS, GSH and ATP levels occurred. Arsenic, cadmium and the combination increased caspase-3/7 activity, while mercury reduced it. CONCLUSION The combination produced a greater, albeit mechanistically similar, cytotoxicity compared to individual metals. Cytotoxicity was dependent on altered mitochondrial integrity, redox-status, and bioenergetics. Although the combination's cytotoxicity was associated with caspase-3/7 activity, this was not true for mercury. Heavy metal interactions should be assessed to elucidate molecular underpinnings of cytotoxicity.
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