Preparation and biodistribution study of technetium-99m-labeled quercetin as a potential radical scavenging agent

Free radicals and oxidative stress are the primary causes of several chronic diseases such as cancer and heart disease. Quercetin is a natural compound with potent antioxidant activity. We have prepared and evaluated technetium-99m (^99mTc)-labeled quercetin as a potential radical scavenging radiotracer. A ^99mTc-quercetin complex was prepared using quercetin, SnCl₂ and Na^99mTcO₄ in a buffered solution over 30 min. The participation coefficient was measured in octanol and queues solutions. The stability was determined in phosphate buffered saline and serum. The biodistribution in normal mice was evaluated at 0.5, 2, 6 and 24 h post-injection. The radiochemical purity (>99%) was determined by thin layer chromatography (TLC) in normal saline solution as the mobile phase. It has a log P of 0.204. It was mainly cleared by the kidneys and showed negligible brain uptake at four time points measured post-injection. The pharmacological properties of quercetin, mainly its free radical scavenging, may potentially cat as a radiopharmaceutical agent for radical-targeted imaging of tissue with high levels of reactive oxygen species.     

Crystal structure of dinuclear azide-bridged copper(II) complex [Cu2((3,4-MeO-Ba)2En)2(μ1,1-N3)2(N3)2]{(3,4-MeO-Ba)2En=N,N′-Bis(3,4-dimethoxybenzylidene)-1,2-ethanediamine}

New dinuclear copper(II)-azido complex [Cu₂((3,4-MeO-Ba)₂En)₂(μ_1,1-N₃)₂(N₃)₂] (I) ((3,4-MeO-Ba)₂En = N,N′-bis(3,4-dimethoxybenzylidene)-1,2-diaminoethane) has been synthesized and characterized by elemental analyses, FT-IR spectroscopy, and X-ray single-crystal diffraction. Complex I consists of a dinuclear unit that represents a new example of a copper(II)-azido compound and the Cu²⁺ ions are bridged by two azido ions in a double end-on fashion, consisting of two terminally bonded azido ligands. The Schiff base ligand (3,4-MeO-Ba)₂En is chelated by two imino nitrogen atoms.     

Determination of Chlorophenoxy Acid Herbicides in Water Samples by Suspended Liquid-Phase Microextraction�CLiquid Chromatography

In this study, directly suspended liquid-phase microextraction was investigated for the extraction and determination of five chlorophenoxy acid herbicides in water samples. The optimized parameters for extraction of chlorophenoxy acid herbicides were 1 M HCl concentration in sample solution, solution temperature 20 °C, 45-min extraction time, 1,000 rpm stirring rate, 25 ??L extracting solvent volume and without NaCl addition. Under the optimum conditions, the enrichment factor ranged from 192 to 390. Calibration curves yielded good linearity (R ² > 0.999) and the linear range was 5.0?C500.0 ??g L^?1, limit of detection was 0.3?C0.4 ??g L^?1 and limit of quantification was 1?C2 ??g L^?1 for analytes and the relative standard deviations were in the range of 3?C10% (n = 3). Finally, the proposed method was successfully applied to the quantification of five chlorophenoxy acid herbicides in water samples and recovery was in the range of 74?C110%.     

Melamine Trisulfonic Acid (MTSA): A New Efficient Catalyst for the Chemoselective Methoxymethylation of Alcohols

Melamine trisulfonic acid, which is easily prepared by the reaction of melamine with neat chlorosulfonic acid, is able to efficiently catalyze the chemoselective methoxymethylation of alcohols with dimethoxymethane (DMM). All reactions were performed under mild and completely heterogeneous reaction conditions in good to high yields.     

ZnTe6O13, a new ZnO–TeO2 phase

Our investigations into the ZnO–TeO₂ system have produced a new phase, zinc(II) hexatellurium(IV) tridecaoxide, ZnTe₆O₁₃, with trigonal (R) symmetry, synthesized by repeated heating and cooling to a maximum temperature of 1053 K. The asymmetric unit consists of a Zn atom coordinated in a distorted octahedral fashion by two unique tellurium(IV) oxide units that form trigonal–bipyramidal TeO₄ and TeO₃₊₁ corner‐ and edge‐shared polyhedra. Except for the Zn and an O atom, which occupy 6c positions, all atoms occupy 18f general positions.     

Therapeutic drug monitoring of cefepime with micellar electrokinetic capillary chromatography: Assay improvement,quality assurance,and impact on patient drug levels

The improvement and performance of a micellar electrokinetic capillary chromatography assay for cefepime in human serum and plasma with a 50 μm id fused‐silica capillary elongated from 40 to 60 cm is reported. Sample preparation with dodecylsulfate protein precipitation at pH 4.5, the pH 9.1 separation medium, and the applied voltage were as reported previously [16]. The change resulted in a significant lower current, higher resolution, and increased detection time intervals. The performance of the assay with multilevel internal calibration was assessed with calibration and control samples. Quality assurance data of a 2‐year period assessed under the new conditions demonstrated the robustness of the assay. In serum samples of patients who received both cefepime and sulfamethoxazole, cefepime could not be detected due to the inseparability of the two compounds. The presence of an interference can be recognized by an increased peak width (width > 0.2 min), the appearance of a shoulder or an unresolved double peak. The patient data gathered during a 3‐year period reveal that introduction of therapeutic drug monitoring led to a 50% reduction of the median drug level. The data suggest that therapeutic drug monitoring can help to minimize the risk of major adverse reactions and to increase drug safety on an individual basis.     

99mTc-radiolabeled imidazo[2,1-b]benzothiazole derivatives as potential radiotracers for glioblastoma

This study presents [^99mTc]BPTG-1 and [^99mTc]BPTG-2 for glioblastoma imaging. In vitro cellular uptakes of these radiotracers were examined in SKOV-3, MCF-7, U87-MG, HT-29, and A549 cell lines. U87-MG cell line displayed the highest radiotracers uptakes. Biodistribution study in U87-MG tumor bearing mice revealed higher uptake of radiotracers in tumor than muscle and brain. Liver, intestine, and kidneys displayed the highest radioactivity uptakes. The main route of radiotracers elimination was hepatobiliary. Due to the brain uptake of these radiotracers, they are promising radiotracers for future studies in the diagnosis of glioblastoma.

     

On the Synthesis of Some 2-Arylhydrazono-3-oxothieno[2,3-<Emphasis Type="Italic">b</Emphasis>]pyridines by Reaction of Nitrilimines with 2-Mercaptonicotinic Acid

Summary. Nitrilimines prepared from N-arylhydrazono chlorides reacted with 2-mercaptonicotinic acid yielding the corresponding addition products, 2-[(2-oxo-1-arylhydrazonopropan-1-yl)mercapto] nicotinic acids, which were treated with 1,1-carbonyldiimidazole in THF affording by cyclocondensation the corresponding hitherto unknown 2-arylhydrazono-3-oxothieno[2,3-b]pyridines.     

Guaranteed cost nonlinear sampled-data control: applications to a class of chaotic systems

Nonlinear Dynamics - This paper addresses the guaranteed cost sampled-data controller synthesis and analysis problems with application to nonlinear chaotic systems. A linear parameter-varying (LPV)...