Search results for "Heterocyclic Compounds"

Molecular docking and oxidation kinetics of 3-phenyl coumarin derivatives by human CYP2A13.

2021

CYP2A13 enzyme is expressed in human extrahepatic tissues, while CYP2A6 is a hepatic enzyme. Reactions catalysed by CYP2A13 activate tobacco-specific nitrosamines and some other toxic xenobiotics in lungs.To compare oxidation characteristics and substrate-enzyme active site interactions in CYP2A13 vs CYP2A6, we evaluated CYP2A13 mediated oxidation characteristics of 23 coumarin derivatives and modelled their interactions at the enzyme active site.CYP2A13 did not oxidise six coumarin derivatives to corresponding fluorescent 7-hydroxycoumarins. The Km-values of the other coumarins varied 0.85-97 µM, Vmax-values of the oxidation reaction varied 0.25-60 min-1, and intrinsic clearance varied 26-…

SINTESI ED ATTIVITÀ ANTINEOPLASTICA DI NUOVI COMPOSTI ETEROCICLICI

2004

New efficient artemisinin derived agents against human leukemia cells, human cytomegalovirus and Plasmodium falciparum: 2nd generation 1,2,4-trioxane…

2015

Abstract In our ongoing search for highly active hybrid molecules exceeding their parent compounds in anticancer, antimalaria as well as antiviral activity and being an alternative to the standard drugs, we present the synthesis and biological investigations of 2nd generation 1,2,4-trioxane-ferrocene hybrids. In vitro tests against the CCRF-CEM leukemia cell line revealed di-1,2,4-trioxane-ferrocene hybrid 7 as the most active compound (IC50 of 0.01 μM). Regarding the activity against the multidrug resistant subline CEM/ADR5000, 1,2,4-trioxane-ferrocene hybrid 5 showed a remarkable activity (IC50 of 0.53 μM). Contrary to the antimalaria activity of hybrids 4–8 against Plasmodium falciparum …

Tetrathiafulvalene-Capped Hybrid Materials for the Optical Detection of Explosives

2013

[EN] Mesoporous silica microparticles capped with TTF moieties and containing a ruthenium dye in the pores were used for the turn-on optical detection of the nitroaromatic explosives Tetryl and TNT via a selective pore uncapping and release of the entrapped dye.

Functional C1-inhibitor diagnostics in hereditary angioedema: Assay evaluation and recommendations

2008

Hereditary angioedema (HAE) is an autosomal dominant disease characterized by recurrent episodes of potentially life-threatening angioedema. The most widespread underlying genetic deficiency is a heterozygous deficiency of the serine protease inhibitor Cl esterase inhibitor (C1-Inh). In addition to low C4 levels, the most important laboratory parameter for correct diagnosis of HAE or angioedema due to acquired C1-Inh deficiency is reduced C1-Inh function (fC1-Inh). No direct recommendations about the assays for fC1-Inh or sample handling conditions are available, although this would prove especially useful when a laboratory first starts to offer assays on fC1-Inh for HAE diagnosis. In the p…

Investigations on the content indole-3-acetic spruce needles of healthy and damaged trees of various sites

1993

Summary Surveys were made on the concentration of indole-3-acetic acid (IAA) in spruce trees of various sites. The concentrations of the hormone were specified with a radioimmunoassay after the needle extract had been purified in several steps. The content of IAA in needles of damaged trees was distinctly lower than the content in needles of healthy trees. Another feature was the annual rythm of the IAA content with the maximum of concentration in June. A distinct diurnal course with highest level of concentration during the early afternoon hours was also observed. The diurnal rhythm of the damaged trees was clearly lower. The supposition is that the lower IAA content is responsible for a p…

Induction of alkaloid diversity in hybrid plant cell cultures

1999

The treatment of Rauwolfia serpentina x Rhazya stricta somatic hybrid cell suspension culture with 100 μM of methyl jasmonate led to a general increase in indole alkaloid content and to qualitative changes in the alkaloid pattern. The content of Six alkaloids were investigated with respect to their content in both the cell biomass and nutrition medium. Intracellular 17-O-acetyl-norajmaline content on the 5th day after treatment had increased about 40-fold compared with the control culture. The respective concentrations of the other alkaloids increased by a factor of two to five. In total 26 indole alkaloids were identified in extracts of the methyl jasmonate-treated culture by TLC, UV, MS a…

Production of cyclopiazonic acid by molds isolated from Taleggio cheese

1999

Twenty-seven strains of Penicillium were isolated from the rind of Taleggio, a typical Italian cheese, so that we could test their capacity to produce cyclopiazonic acid (CPA); all strains produced CPA. The production was strongly influenced by the strain variety and growth conditions. Strains incubated at 25 degrees C for 7 days always produced CPA in mannitol broth, with concentrations ranging from 0.02 to 1 microg/ml, whereas only 33% of strains grown in yeast-extract broth produced CPA, with a maximum value of 0.1 microg/ml. In milk, maximum production (1.6 microg/ml) was observed after 14 days of incubation at 25 degrees C. In order to evaluate the presence of the toxin and its capacit…

Roquefortine C occurrence in blue cheese.

2001

Several strains of Penicillium are used for the production of mold-ripened cheeses, and some of them are able to produce mycotoxins. The aims of the research were the determination of roquefortine C and PR toxin in domestic and imported blue cheeses, the identification of the penicillia used as starter, and the investigation of their capacity for producing toxins in culture media. Roquefortine C was always found in the cheeses at levels ranging from 0.05 to 1.47 mg/kg, whereas the PR toxin was never found. The identification of the fungal strains present in the domestic cheeses included Penicillium glabrum, Penicillium roqueforti, and Penicillium cyclopium in the Gorgonzola "dolce" and Peni…

Production of halogenated compounds by Bjerkandera adusta.

1994

International audience; The white-rot fungusBjerkandera adusta produces volatile chlorinated phenyl compounds. The main compounds identified were 3-chloro-4-methoxybenzaldehyde (3-chloro-p-anisaldehyde), 3-chloro-4-methoxybenzyl alcohol (3-chloro-p-anisyl alcohol), 3,5-dichloro-4-methoxybenzaldehyde (3,5-dichloro-p-anisaldehyde), and 3,5-dichloro, 4-methoxybenzyl alcohol (3,5-dichloro-p-anisyl alcohol).p-Anisaldehyde, veratraldehyde and the corresponding alcohols,p-anisyl alcohol and veratryl alcohol were produced simultaneously. Even with a very low concentration of chloride in the medium (<>–5 m), chlorinated aromatic compounds were still observed. Addition of bromide to the culture mediu…