Preclinical evaluation of 188 Re-HYNIC-PSMA as a novel therapeutic agent

Journal of Radioanalytical and Nuclear Chemistry - In this study, optimized preparation, quality control, cell assessments and biostribution of 188Re-HYNIC-PSMA in normal rats and tumor bearing...     

Synthesis and antibacterial activity of ethyl 2-amino-6-methyl-5-oxo- 4-aryl-5,6-dihydro-4H-pyrano[3,2-c]quinoline-3-carboxylate

The three-component reaction of 4-hydroxy-1-methyl-2(1H)-quinolinone, aromatic aldehydes and ethyl cyanoacetate was carried out in the presence of a catalytic amount of 4-dimethyl aminopyridine(DMAP) in aqueous ethanol. The reactions result in the formation of pyranoquinoline derivatives in excellent yields. Antibacterial activity has been evaluated against Gram positive and Gram negative bacteria for some of the synthesized compounds. The results indicated that these compounds are moderately effective against bacterial growth and their effectiveness is highest against Pseudomonas aeruginosa.     

Parallel single-cell optical transit dielectrophoresis cytometer

In this work, we present an optical transit DEP flow cytometer for parallel single-cell analysis. Each cell's dielectric property is inferred from velocity perturbations due to DEP actuation in a microfluidic channel. Dual LED sources facilitate velocity measurement by producing two transit shadows for each cell passing through the channel. These shadows are detected using a 256-pixel linear optical array detector. Massively parallel analysis is possible as each pixel of the detector can independently analyze the passing cells. A wide channel (∼18 mm) was employed to carry many particles simultaneously, and the system was capable of detecting the velocity of over 200 cells simultaneously. We have achieved analysis rates for 10 µm diameter polystyrene spheres response exceeding 250 per second. With appropriate calibration, this DEP cytometer can quantitatively measure the dielectric response. The dielectric response (Clausius–Mossotti factor) of viable CHO cells was measured over the frequency range of 100 kHz to 6 MHz, and the obtained response matches the previously measured values by our group. The DEP cytometer uses simple modular components to achieve high throughput label-free single-cell dielectric analysis and can begin analyzing particles within 10 s after starting to pump the sample into the channel.     

Design,synthesis and antibacterial activity evaluation of novel 2-(4-((1-aryl-1H-1,2,3-triazol-4-yl)methoxy)phenyl)2-(2-oxoazetidin-1-yl)acetamide derivatives

In this paper, a novel series of 2-(4-((1-aryl-1H-1,2,3-triazol-4-yl)methoxy)phenyl)2-(2-oxoazetidin-1-yl)acetamide derivatives are synthesized in two steps. The first step involved Ugi multicomponent reaction of β-alanine, o-(propargyl)benzaldehyde and isocyanide derivatives. The product of this step, underwent a click 1,3-dipolar cycloaddition reaction with benzyl azide derivatives. The 2-(4-((1-aryl-1H-1,2,3-triazol-4-yl)methoxy)phenyl)2-(2-oxoazetidin-1-yl)acetamide product was characterized and their antibacterial activities were evaluated against various G-positive (Staphylococcus aureus and Bacillus subtilis) and G-negative (Pseudomonas aeruginosa and Escherichia coli) bacteria, using minimal inhibition concentration. The compounds showed very good antimicrobial activity and a number of products have been more active than ciprofloxacin.     

Sensitive Quantification of Fe(III) in Food Samples at Screen Printed Carbon Electrode Modified with Graphene and Piroxicam by Catalytic Adsorptive Voltammetry

A new disposable sensitive voltammetric sensor for the determination of Fe(III) based on a graphene (G) and piroxicam (Pir) modified screen printed carbon electrode (Pir/G/SPCE) has been developed. The developed method is based on accumulation of Fe(III) on the surface of the prepared sensor strip, formation a complex with Pir and subsequent reduction the adsorbed chelated Fe(III) at ?0.03 V (vs. Ag/AgCl) coupled with the catalytic enhancement of bromate. Characterizations of the modified electrode surface were performed by field emission scanning electron microscopy (FE‐SEM), energy dispersive X‐ray spectroscopy (EDX) and electrochemical impedance spectroscopy (EIS). Electrochemical behavior of the modified SPCEs was investigated by cyclic voltammetry (CV) and differential pulse voltammetry (DPV). Under the optimum conditions, the catalytic voltammetric method exhibited linear calibration plot in the concentration ranges of 1–100 ng mL^?1 and 100–3500 ng mL^?1 Fe(III) with a limit of detection of 0.3 ng mL^?1. The sensor strip displayed good reproducibility with 1.7 % relative standard deviation (RSD%). The developed method was successfully applied for the determination of iron in food samples such as vegetables, fruit, and cereal.     

Solubility prediction of deferiprone in N-methyl-2-pyrrolidone + ethanol mixtures at various temperatures using a minimum number of experimental data

Experimental solubility of deferiprone (DFP) in N-methyl-2-pyrrolidone (NMP) + ethanol (EtOH) mixtures at 293.2, 298.2, 303.2 and 308.2 K was determined and mathematically represented using various models. The trained versions of the van’t Hoff equation, its combined version with log-linear model, Jouyban–Acree model and a combination of van’t Hoff + Jouyban–Acree model were reported to simulate DFP solubility in the binary mixture compositions at various temperatures. The mean percentage deviation (MPD) was used as an accuracy criterion. The obtained overall MPDs for back-calculated and predicted solubility of DFP in NMP + EtOH mixtures varied from 1.1% to 3.2% and 2.6% to 6.6%, respectively. Some of apparent thermodynamic quantities for the dissolution processes of DFP are also reported.     

Optimized production,quality control and biodistribution assessment of <Superscript>166</Superscript>Ho–DOTATOC: a novel radiolabelled somatostatin analog

Nowadays, peptide receptor radionuclide therapy is used to treat a specific type of cancer called neuroendocrine tumors. In this research, the optimized conditions for ¹⁶⁶Ho-DOTATOC production are presented. The radiolabeled compound was prepared with the specific activity of 11.1 TBq/mmol and radiochemical purity of more than 99% (using ITLC and HPLC). Stability tests of the complex were investigated in room temperature and in human serum at 37 °C. Biodistribution studies in Syrian rats showed considerable accumulation in pancreas as the somatostatin receptor-positive tissue. ¹⁶⁶Ho-DOTATOC can be considered as a novel agent for treatment of somatostatin receptor-positive tumors.     

Composition of essential oils in subterranean organs of three species of Valeriana L

Essential oils from the subterranean organs of three species of Valeriana L. from Iran (Valeriana sisymbriifolia Vahl, Valeriana alliariifolia Adams and Valeriana officinalis L.) belonging to Valerianaceae family have been obtained by hydrodistillation and analysed by gas chromatography-mass spectrometry in order to discern the differences and similarities between the volatile chemical compositions of these species. More than 100 components were identified in essential oils of the studied plants (Supplementary Table S1--online only). The principal common constituents of the three species of Valeriana were spathulenol, limonene, γ-terpinene, vulgarone B and p-cymene. The main essential oil ingredients were α-selinene (7.83%) in V. sisymbriifolia, limonene (3.53%) in V. alliariifolia and spathulenol (13.33%), α-campholenal (11.48%), vulgarone B (8.38%) and valerenal (8.32%) in V. officinalis plants. Ageratochromene (precocene II), a chromene substance with antibacterial, antifungal, insecticidal and antijuvenile hormonal activities, was found at high levels (35.59% and 36.58%) in the essential oils of V. sisymbriifolia plants.