Search results for "Metabolite"

Automated Determination of Paroxetine and Its Main Metabolite by Column Switching and On-Line High-Performance Liquid Chromatography

1994

An automated column-switching method coupled to isocratic high-performance liquid chromatography has been developed for simultaneous determination of blood levels of paroxetine and its nonconjugated main metabolite BRL 36610. The lower limits of detection were 9-15 nmol/L (3-5 ng/ml) and linearity between drug concentration and detector response was found for 0-1,500 nmol/L (0-500 ng/ml). The method could be applied to the analysis of serum samples obtained from depressed patients who were treated with daily oral doses of 20 or 40 mg of paroxetine. After the 20-mg dose, the mean blood level of paroxetine was 69 nM (23 ng/ml), whereas the metabolite BRL 36610 was detectable in only one of 5 …

In silico methods for metabolomic and toxicity prediction of zearalenone, α-zearalenone and β-zearalenone.

2020

Zearalenone (ZEA), α-zearalenol (α-ZEL) and β-zearalenol (β-ZEL) (ZEA's metabolites) are co/present in cereals, fruits or their products. All three with other compounds, constitute a cocktail-mixture that consumers (and also animals) are exposed and never entirely evaluated, nor in vitro nor in vivo. Effect of ZEA has been correlated to endocrine disruptor alterations as well as its metabolites (α-ZEL and β-ZEL); however, toxic effects associated to metabolites generated once ingested are unknown and difficult to study. The present study defines the metabolomics profile of all three mycotoxins (ZEA, α-ZEL and β-ZEL) and explores the prediction of their toxic effects proposing an in silico w…

Studies on the Biosynthesis of Paraherquamide: Synthesis and Incorporation of a Hexacyclic Indole Derivative as an Advanced Metabolite

2001

Imidazo[2,1-b] [1,3,4]thiadiazoles with antiproliferative activity against primary and gemcitabine-resistant pancreatic cancer cells

2020

A new series of eighteen imidazo [2,1-b] [1,3,4]thiadiazole derivatives was efficiently synthesized and screened for antiproliferative activity against the National Cancer Institute (NCI-60) cell lines panel. Two out of eighteen derivatives, compounds 12a and 12h, showed remarkably cytotoxic activity with the half maximal inhibitory concentration values (IC50) ranging from 0.23 to 11.4 μM, and 0.29–12.2 μM, respectively. However, two additional compounds, 12b and 13g, displayed remarkable in vitro antiproliferative activity against pancreatic ductal adenocarcinoma (PDAC) cell lines, including immortalized (SUIT-2, Capan-1, Panc-1), primary (PDAC-3) and gemcitabine-resistant (Panc-1R), elici…

Multibiomarker approach to fipronil exposure in the fish Dicentrarchus labrax under two temperature regimes

2020

12 pages, 5 figures, 3 tables, supplementary data https://doi.org/10.1016/j.aquatox.2019.105378

Determination of metabolite concentrations in human brain tumour biopsy samples using HR-MAS and ERETIC measurements.

2009

Accurate determination of the concentration of the metabolites contained in intact human biopsies of 10 glioblastoma multiforme samples was achieved using one-dimensional 1H high-resolution magic angle spinning (HR-MAS) NMR combined with ERETIC™ (electronic reference to in vivo concentrations) measurements. The amount of sample used ranged from 6.8 to 12.9 mg. Metabolite concentrations were measured in each sample using two methods: with DSS (2,2-dimethyl-2-silapentane-5-sulfonate sodium salt) as an internal reference and with ERETIC™ as an external electronically generated reference. The ERETIC™ signal was shown to be highly reproducible and did not affect the spectral quality. The concent…

Secoiridoids and Iridoids from Morinda asteroscepa

2020

The new 2,3-secoiridoids morisecoiridoic acids A (1) and B (2), the new iridoid 8-acetoxyepishanzilactone (3), and four additional known iridoids (4–7) were isolated from the leaf and stem bark methanol extracts of Morinda asteroscepa using chromatographic methods. The structure of shanzilactone (4) was revised. The purified metabolites were identified using NMR spectroscopic and mass spectrometric techniques, with the absolute configuration of 1 having been established by single-crystal X-ray diffraction analysis. The crude leaf extract (10 μg/mL) and compounds 1–3 and 5 (10 μM) showed mild antiplasmodial activities against the chloroquine-sensitive malaria parasite Plasmodium falciparum (…

Metabolic profiling of ripe olive fruit in response to moderate water stress

2013

a b s t r a c t The concentrations of different metabolites in olive (Olea europaea (L.)) fruit at harvest can be affected by water availability, with significant consequences on the composition and the quality of the resulting oil. The aim of the present study was to profile the metabolic composition of ripe olives (cv. Cipressino) grown under water-stress and irrigated conditions applied during the last part of the fruit developmental cycle (from pit hardening to commercial harvest). The imposed conditions resulted in a moderate water stress (−3.5 MPa) at the end of the experimental period. Samples (pulp + skin) of fruit collected at the stage of complete epicarp pigmentation were analyze…

Substantial Fat Loss in Physique Competitors Is Characterized by Increased Levels of Bile Acids, Very-Long Chain Fatty Acids, and Oxylipins.

2022

Funder: Finnish Foundation for Cardiovascular Research

Simultaneous determination of levodopa methyl ester, levodopa, 3-O-methyldopa and dopamine in plasma by high-performance liquid chromatography with e…

1994

A new procedure is described for the simultaneous determination of levodopa methyl ester (LDME) and its biotransformation products levodopa (L-DOPA), 3-O-methyldopa (3-OMD) and dopamine (DA) in stabilized plasma samples, using reversed-phase high-performance liquid chromatography. A coulometric detector equipped with a dual-electrode system operating in the redox mode was used to simultaneously quantitate all compounds. This system generated a double signal monitored by a dual-channel acquisition data system and allowed quantitation of compounds at the nanogram level. The intra- and inter-assay precision varied in the 2.4-6.9% and 3.2-9.1% ranges respectively, whereas the recoveries were cl…