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Computational structure-activity relationship analysis of non-peptide inducers of macrophage tumor necrosis factor-alpha production.
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Previously, we screened a series of arylcarboxylic acid hydrazide derivatives for their ability to induce macrophage tumor necrosis factor alpha (TNF-alpha) production and identified 16 such compounds. In the present study, we evaluated 23 additional arylcarboxylic acid hydrazides and found that
Bromine levels in tissue lipids of rats fed brominated fatty acids.
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Rats have been fed diets containing either 0.8% brominated corn oil or 0.5% of the ethyl ester of 9,10-dibromostearate or 9,10,12,13-tetrabromostearate. The brominated compounds were incorporated into semisynthetic diets and animals were observed after feeding periods of 5 days to 3 months. With the
Biological activity of some 4-anilinoquinazolines: cytotoxic, genotoxic and antiprotease effects, induction of necrosis and changes of actin cytoskeleton.
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Fourteen substituted 4-anilinoquinazolines have been tested for cytotoxic effect and structure activity relationships. The most active derivatives were substituted by chlorine or bromine group in the aromatic ring, in the pyrimidine ring by morpholine group and in the aniline skeleton by nitro group
Bromine-inhalation mimics ischemia-reperfusion cardiomyocyte injury and calpain activation in rats.
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Halogens are widely used highly toxic chemicals that pose potential threat to humans due to their abundance. Halogens such bromine (Br2) cause severe pulmonary and systemic injuries however, the mechanisms of their toxicity are largely unknown. Here we demonstrate that Br2 and reactive brominated
Effect of bromine and chlorine positioning in the induction of renal and testicular toxicity by halogenated propanes.
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A series of halogenated propanes were studied for renal and testicular necrogenic effects in the rat and correlated to their ability to induce in vivo renal and testicular DNA damage and in vitro testicular DNA damage. 1,2-Dibromo-3-chloropropane (DBCP) and 1,2,3-tribromopropane were most potent in
2-Bromo-5-hydroxyphenylporphyrins for photodynamic therapy: photosensitization efficiency, subcellular localization and in vivo studies.
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BACKGROUND
Photodynamic therapy (PDT) is a therapeutic modality capable of inducing cell death by oxidative stress through activation of a sensitizer by light. Aryl-porphyrin with hydroxyl groups are good photosensitizers and presence of bromine atoms can enhance the photodynamic activity through
Hepatotoxicity of brominated benzenes: relationship between chemical structure and hepatotoxic effects in acute intoxication of mice.
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Brominated benzenes appear in the environment and human tissues. Their detection in the environment may be as a result of their usage, e.g. hexabromobenzene (HBB), and as products of HBB degradation or metabolism. The aim of this study was to compare liver impairment in acute intoxication of mice
Chemical burns: our 10-year experience.
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A review of 173 patients with chemical burns admitted to our burn unit was carried out during the years 1976-85. Most burns were work related (83 per cent). The majority of patients were men aged 21-50 years (mean age = 29.6 years). The mean total body surface area involved was 3.6 per cent (range =
Carbon monoxide contributes to the cytokine-induced inhibition of surfactant synthesis by human type II pneumocytes.
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BACKGROUND
An increase in cyclic guanosine 3',5'-monophosphate (cGMP) due to nitric oxide generation is known to participate in the mediation of the tumor necrosis factor alpha (TNF-alpha) effect in type II cells. Because guanylyl cyclase can be activated also by carbon monoxide (CO), in this study
Panniculitis due to potassium bromide.
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Potassium bromide again is well known to be surprisingly effective in patients with severe myoclonic epilepsy in infants (SME). Rare side effects on the skin reappeared, such as the febrile nodular panniculitis (Weber-Christian syndrome). In 1993 we described the first three cases of necrotizing
Structure-activity relationship of ochratoxin A and synthesized derivatives: importance of amino acid and halogen moiety for cytotoxicity.
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The enigma why the mycotoxin ochratoxin A (OTA) impairs cell and organ function is still not solved. However, an interaction with target molecules is a prerequisite for any observed adverse effect. This interaction depends on characteristics of the target molecule as well as on the OTA molecule
Toxicology of brominated fatty acids: metabolite concentration and heart and liver changes.
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Rats were fed for 35 days diets containing 2% of either brominated corn oil (BCO), monoglyceride of dibromostearate (DBS), monoglyceride of tetrabromostearate (TBS) or a mixture of the two monoglycerides (BMG) which provided proportions of brominated acids comparable to that of the BCO. Hearts from
The toxicity of brominated sesame oil and brominated soybean oil in miniature swine.
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Miniature swine were fed brominated sesame oil at dietary levels of 0, 5, 25, 50 or 500 mg/kg of body weight for 17 weeks and brominated soybean oil at levels of 0, 5, 50 or 500 mg/kg of body weight for 28 weeks. Growth rate and food intake were decreased only at the high dose level in the
Anti-Inflammatory Activity and Structure-Activity Relationships of Brominated Indoles from a Marine Mollusc.
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Marine molluscs are rich in biologically active natural products that provide new potential sources of anti-inflammatory agents. Here we used bioassay guided fractionation of extracts from the muricid Dicathais orbita to identify brominated indoles with anti-inflammatory activity, based on the
Inhibition of microtubule assembly in tumor cells by 3-bromoacetylamino benzoylurea, a new cancericidal compound.
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We have synthesized a new compound, 3-bromoacetylamino benzoylurea (3-BAABU), which showed strong cancericidal activity by inducing irreversible mitotic arrest and subsequently apoptosis in human T cell leukemic cells (CEM), human biphenotypic leukemic cells (SP), a human prostate cancer cell line
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