Search results for "TOXICITY"

Cadmium as a transcriptional modulator in human cells

2010

Cadmium (Cd) is an underground mineral widely used in the steel industry, in plastics, and as a component of batteries. It is an industrial and environmental pollutant released as an air contaminant from fertilizers and, more prominently, in the form of wastewater. Food, drinking water, and, mainly, inhalation of smoke from cigarettes are sources of daily exposure of humans to the heavy metal. Although Cd has no known useful function for humans as well as other organisms, it appears to evoke in cells a number of responses that involve not only death signaling but also protective reactions against the toxicity. This finding prompted a number of experimental studies aimed to elucidate the cel…

Synthesis of 5H-pyrido[3,2-b]pyrrolizin-5-one tripentone analogs with antitumor activity

2018

Abstract Pyrrolizinones represent an interesting class of compounds with varied degrees of structural complexity and pharmacological activity. Among these, 9H-pyrido[2,3-b]pyrrolizin-9-one, tripentone analogs, recently reported by us, showed significant antiproliferative activity against human tumor cell lines, inducing apoptosis and not affecting viability of Caco-2 differentiated in normal intestinal-like cells. Considering their interesting biological activity, their 5H-pyrido[3,2-b]pyrrolizin-5-one analogs were efficiently synthesized in good to excellent yields (61–91%). All tripentone derivatives were tested to assess their cytotoxicity against two human tumor cell lines, HCT-116 (hum…

Toxicity of 4-chloro-o-cresol to fish. Light microscopy and chemical analysis of the tissue

1979

Comparative toxicity and cell-tissue distribution study on nanoparticular iron complexes using avian embryos and HepG2-cells

2007

In this study the toxicity and intracellular availability of iron from iron dextran (FeD), iron sucrose (FeS), and iron gluconate (FeG) was compared in organs of avian (turkey) embryos and in isolated cells (HepG2) in cell culture. Iron uptake was more pronounced in embryonic liver than in renal tissue. Cellular iron uptake in liver and kidney was more or less similar for the different compounds. Only some experiments showed slightly greater iron concentrations in liver and kidney with FeG compared with FeD and FeS. Significant differences were found in the survival ratios of the eggs and the embryo weights depending on the type of iron complex administered. The rank order of toxicities was…

Oxidation of carbidopa by tyrosinase and its effect on murine melanoma

2009

Oxidation of the anti-Parkinsonian agent carbidopa by tyrosinase was investigated. The products of this reaction were identified as 3-(3,4-dihydroxyphenyl)-2-methylpropanoic acid and 6,7-dihydroxy-3-methylcinnoline. These results demonstrate that after oxidation of the catechol moiety to an o-quinone either a redox exchange with the hydrazine group or a cyclization reaction occur. The cyclization product underwent additional oxidation reactions leading to aromatization. The cyclization reaction is undesired in the case of hydrazine-containing anti-melanoma prodrugs and will have to be taken into account in designing such compounds. Carbidopa was tested against B16(F10) melanoma cells in cul…

Metabolomics as a tool for the study of drug-induced hepatotoxicity

2015

Drug-induced liver injury (DILI) is a major health and economic problem and the leading cause of hepatic dysfunction, drug failure during clinical testing and post-market withdrawal of approved drugs. Pre-clinical testing should be able to detect potential hepatotoxins early in the drug development process in order to minimize health risks and financial losses. Several liver-derived in vitro models have been developed to be used in pharmacology and toxicology research to understand the mechanism of DILI and to evaluate potential hepatotoxicity of new chemical entities. Although they fail to reproduce the complexity of a whole organ, their low cost, high reproducibility, and the possibility …

High sensitivity of northern pike larvae to UV-B but no UV-photoinduced toxicity of retene

2003

In order to investigate whether increased UV-B radiation is a risk factor, a series of acute laboratory experiments was conducted with larval stages of the northern pike (Esox lucius L.), hatching in Nordic waters in May. Further, a comparative investigation on the acute phototoxicity of retene (7-isopropyl-1-methylphenanthrene), a PAH compound recently revealed to posses UV-B-induced phototoxicity in larval coregonids, was conducted with pike larvae. In semi-static experiment, larvae were pre-exposed to retene (3, 9, 30 and 82 microg/g), with relevant controls, for 24 h and then irradiated for 3 h once a day (two consecutive days) with three UV-B doses (CIE-weighted 1.0, 1.8 or 2.7 kJ/m2 p…

Histopathological responses of newly hatched larvae of whitefish (Coregonus lavaretus s.l.) to UV-B induced toxicity of retene

2003

Positively phototactic fish larvae may be exposed to increased ultraviolet-B (UV-B) radiation alone or, potentially and in addition, to polycyclic aromatic hydrocarbons (PAHs) such as retene (7-isopropyl-1-methylphenanthrene) at the egg or larval stages. Suspended and sedimental particulate material near pulp and paper mills may act as sources of retene in chemically contaminated lake areas. In laboratory conditions whitefish larvae were pre-exposed to retene (10, 32 and 100 microg/l), with relevant controls, and irradiated in semi-static tests for 3 h once a day (2 consecutive days) with two UV-B doses (CIE-weighted 2.8 or 5.4 kJ per m(2) per day) or with visible light only. These UV-B dos…

Pyrrolo[2,3-h]quinolinones: A new ring system with potent photoantiproliferative activity

2006

A new class of compounds, the pyrrolo[2,3-h]quinolin-2-ones, nitrogen isosters of the angular furocoumarin Angelicin, was synthesized with the aim of obtaining new photochemotherapeutic agents with increased antiproliferative activity and lower undesired toxic effects than the lead compound. Two synthetic pathways were approached to allow the isolation both of the dihydroderivatives 10-17 and of the aromatic ring system 23. Compounds 10-17 showed a remarkable phototoxicity and a great UVA dose dependence reaching IC(50) values at submicromolar level. Intracellular localization of these compounds has been evaluated by means of fluorescence microscopy using tetramethylrhodamine methyl ester a…

Confirmation of in situ exposure of fish to secondary treated bleached-kraft mill effluent using a laboratory simulation

1998

To corroborate the responses in whitefish (Coregonus Iavaretus L.) exposed to elemental chlorine free (ECF) bleached-kraft pulp mill effluent (BKME) in situ, a 30-d laboratory exposure was carried out at concentrations simulating the field conditions. The flow-through exposures were conducted at four secondary (activated sludge) treated effluent (STE) concentrations: 1.3, 2.3, 3.5, and 7%. To evaluate the role of the secondary treatment, fish were also exposed to one concentration (3.5%) of pretreated effluent (PTE) from the mill. Compared to the control, whitefish liver 7-ethoxyresorufin-O-deethylase (EROD) activity was twofold in fish exposed to 3.5% STE, which was similar to monooxygenas…