Regioselective,Solvent‐ and Metal‐Free Chalcogenation of Imidazo[1,2‐a]pyridines by Employing I2/DMSO as the Catalytic Oxidation System

Highly efficient molecular‐iodine‐catalyzed chalcogenations (S and Se) of imidazo[1,2‐a]pyridines were achieved by using diorganoyl dichalcogenides under solvent‐free conditions. This approach afforded the desired products that had been chalcogenated regioselectively at the C3 position in up to 96 % yield by using DMSO as an oxidant, in the absence of a metal catalyst, and under an inert atmosphere. This mild, green approach allowed the preparation of different types of chalcogenated imidazo[1,2‐a]pyridines with structural diversity. Furthermore, the current protocol was also extended to other N‐heterocyclic cores.     

Current advances in molecularly imprinted polymers and their release mechanisms in drug delivery systems

Molecularly imprinted polymer (MIP) has gained wide interest among researchers due to its unique molecular recognition of the template that is suitable as a drug carrier. Therefore, the preparation and formulation of the MIP are significant to suit the needs of the intended use. Due to its significance in drug delivery, this review aims to highlight various methods in the preparation of MIP, the composition for both controlled and stimuli-responsive drug delivery systems, and the release mechanism of the drugs. In drug delivery systems, MIP should have a sustained release performance as well as flexibility in surface modification for targeted delivery via a range of stimuli-responses, including  external stimuli (magnetic, light) and internal stimuli (pH, temperature, redox, biological). The properties of sustained release and targeted delivery of the MIP can improve the drug's therapeutic efficacy as well as the breakthrough for the tumor targeting application.     

Modes and Fields of Two Stacked Dielectric Resonators in a Cavity of an Electron Paramagnetic Resonance Probe

An electron paramagnetic resonance (EPR) probe consisting of two dielectric resonators (DRs) and a cavity (CV) is ideal for EPR experiments where both signal enhancement and tuning capabilities are required. The coupling of two DRs, resonating in their \({\text{TE}}_{01\delta }\) mode and a CV resonating in its \({\text{TE}}_{011}\) mode, is studied using energy-coupled mode theory (ECMT). The frequencies and eigenvectors of the three coupled modes are analytically derived. As predicted numerically, ECMT confirms that the \({\text{TE}}^{ + + - }\) and \({\text{TE}}^{ + - - }\) modes are indeed found to be degenerate at a specific distance between the two DRs \(d_{12}\). Additionally, the condition at which degeneracy occurs is specified. For a considerable range, the calculated frequency of the \({\text{TE}}^{ + + + }\) mode changes linearly with respect to \(d_{12}\). The \({\text{TE}}^{ + + + }\) mode showed a 500 MHz frequency change over a distance of 2 cm, when the resonance frequency is around 9.7 GHz. This enables the experimentalist to linearly tune the probe over this large frequency range. Finally the asymmetric configuration, where one of the resonators (DR2) is kept at the cavity center and the other one is allowed to move along the cavity axis, is studied. It is estimated that the frequency changes by 600 MHz over a distance of 1.5 cm. A formula for the magnitude of the magnetic field along the cavity axis, where the EPR samples are usually placed, is developed. This is crucial in determining the magnetic field in the vicinity of the sample and the probe’s filling factor.     

Structural and electrical study of Ce-substituted bismuth vanadate

Samples of Ce^IV-substituted bismuth vanadate, formulated as Bi₄Ce_xV_2−xO_{11−(x/2)−δ}; 0≤x≤0.30, were synthesized by solid-state reactions. The phase structure and electrical conductivity were investigated using X-ray powder diffraction, FT-IR, differential thermal analysis and AC impedance spectroscopy. For a low composition range, two phase transitions, α↔β and β↔γ, were exhibited in which the system mimics in most events the parent compound. Impedance analysis evidenced no relationship between the blocking effect of charge carriers and structural changes at ambient temperatures. However, the temperature dependence of conductivity was correlated with the stability region of various phases within the system.     

Multiple Spectroscopic,Docking and Cytotoxic Study of a Synthesized 2,2′ Bipyridin Phenyl Isopentylglycin Pt(II) Nitrate Complex: Human Serum Albumin and Breast Cancer Cell Line of MDA-MB231 as Targets

In the present study, the biological activities of a new synthesized Pt(II)-complex, 2,2′ bipyridinphenyl isopentylglycin Pt(II) nitrate was investigated via its interaction with the most important blood carrier protein of human serum albumin (HSA), using fluorescence and Far-UV circular dichroism (CD) spectroscopic techniques and also molecular docking. Moreover, cytotoxicity activity of the complex was studied against breast cancer cell line of MDA MB231 using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The Pt(II)-complex has a strong ability to quench the intrinsic fluorescence of HSA through a static quenching mechanism. According fluorescence quenching data, the binding parameters of the interaction were calculated and showed that hydrophobic interaction has an important role. The molecular docking results in coherent with fluorescence measurements illustrated that Pt(II) complex can bind to HSA at one position that located in the hydrophobic cavity of groove between drug site I and II. Also, experimental data on driving force in binding site was confirmed whereas theoretical results demonstrated Pt(II) complexinteract to HSA by hydrophobic interaction. Far-UV-CD results showed that Pt(II)-complex induced an increasing in the content of α-helical structure of the protein and stabilized it. Also, MTT assay represented growth inhibitory effect of the complex toward the breast cancer cell line.     

Completely automated multiresolution edge snapper--a new technique for an accurate carotid ultrasound IMT measurement: clinical validation and benchmarking on a multi-institutional database

The aim of this paper is to describe a novel and completely automated technique for carotid artery (CA) recognition, far (distal) wall segmentation, and intima-media thickness (IMT) measurement, which is a strong clinical tool for risk assessment for cardiovascular diseases. The architecture of completely automated multiresolution edge snapper (CAMES) consists of the following two stages: 1) automated CA recognition based on a combination of scale-space and statistical classification in a multiresolution framework and 2) automated segmentation of lumen-intima (LI) and media-adventitia (MA) interfaces for the far (distal) wall and IMT measurement. Our database of 365 B-mode longitudinal carotid images is taken from four different institutions covering different ethnic backgrounds. The ground-truth (GT) database was the average manual segmentation from three clinical experts. The mean distance ± standard deviation of CAMES with respect to GT profiles for LI and MA interfaces were 0.081 ± 0.099 and 0.082 ± 0.197 mm, respectively. The IMT measurement error between CAMES and GT was 0.078 ± 0.112 mm. CAMES was benchmarked against a previously developed automated technique based on an integrated approach using feature-based extraction and classifier (CALEX). Although CAMES underestimated the IMT value, it had shown a strong improvement in segmentation errors against CALEX for LI and MA interfaces by 8% and 42%, respectively. The overall IMT measurement bias for CAMES improved by 36% against CALEX. Finally, this paper demonstrated that the figure-of-merit of CAMES was 95.8% compared with 87.4% for CALEX. The combination of multiresolution CA recognition and far-wall segmentation led to an automated, low-complexity, real-time, and accurate technique for carotid IMT measurement. Validation on a multiethnic/multi-institutional data set demonstrated the robustness of the technique, which can constitute a clinically valid IMT measurement for assistance in atherosclerosis disease management.     

Labeling of new formulation of tin–sucralfate freeze-dried kit with technetium-99m and its biological evaluation

The present investigation deals with a simple preparation of new formulation of tin?Csucralfate freeze-dried kit (F.D.K.), to be directly labeled with ^99mTc at optimal pH value of 7.0. The lyophilized form containing 100?mg sucralfate and 11.3?mg dihydrated stannous chloride. Other optimal pH values of the preparation were found to be from 4.0 to 11.0. The range of sucralfate amount studied (50?C500?mg) not affected the radiochemical purity of the labeled complex. The radiochemical purity and the stability of the labeled preparation that assessed by filtration were more than 95%. ^99mTc sucralfate was radiochemical stable up to a specific activity of 1,000?mCi per gram which was more stable than earlier published value (700?mCi per gram) without any radiolytic decomposition. The biological behavior of ^99mTc-pertechnetate was evaluated in two groups of animals, the first group (neither fasted nor ulcerated) and the second group (fasted and ulcerated mice). The data of organ distribution of ^99mTc?Csucralfate in ulcerated fasted mice showed that more than 99% of the administered dose was accumulated in the stomach (87.92%) and intestine (11.43%). The radioanalytical results together with the in vivo-biological behavior of the labeled preparation demonstrate it??s stability, efficacy and usefulness in medical applications for the detection of gastrointestinal ulcers.     

Probing Proteins in Solution by Xe NMR Spectroscopy

The interaction of xenon with different proteins in aqueous solution is investigated by ¹²⁹Xe NMR spectroscopy. Chemical shifts are measured in horse metmyoglobin, hen egg white lysozyme, and horse cytochrome c solutions as a function of xenon concentration. In these systems, xenon is in fast exchange between all possible environments. The results suggest that nonspecific interactions exist between xenon and the protein exteriors and the data are analyzed in term of parameters which characterize the protein surfaces. The experimental data for horse metmyoglobin are interpreted using a model in which xenon forms a 1:1 complex with the protein and the chemical shift of the complexed xenon is reported (Locci et al., Keystone Symposia “Frontiers of NMR in Molecular Biology VI”, Jan. 9–15, 1999, Breckenridge, CO, Abstract E216, p. 53; Locci et al., XeMAT 2000 “Optical Polarization and Xenon NMR of Materials”, June 28–30, 2000, Sestri Levante, Italy, p. 46).     

Spreader-CDR system for efficient,reproducible, and frugal western blot

Efficient antibody incubation is a vital step for successful western blot. During the incubation, a thin antibody-depleted layer is created around the blotting membrane, which limits antibody binding. Although the conventional batch shaking method is ineffective against it, this layer can be easily disrupted by cyclic draining and replenishing (CDR) of the antibody solution during membrane incubation. Previously, we introduced a closed and rotating cylindrical chamber as a tool to implement CDR for western blots (rCDR). A new open bucket-style chamber was devised for easier operation and the possibility of process automation. Instead of rotation as in rCDR, rocking it back and forth achieved the CDR antibody incubation (R-CDR). The chamber was then equipped with a spreader-rod to facilitate the uniform movement of the antibody solution across the membrane surface. Hence, it was named spreader CDR (S-CDR). Compared to the batch incubation method, both the S-CDR and R-CDR devices produced significantly enhanced signals and developed faster results. There were several additional benefits of using the spreader-rod, which included uniform antibody binding across the membrane, reduced usage of antibodies, and the ability to recover results even from mishandled, creased membranes. The S-CDR device ensures better blots and can be easily implemented in existing western blot protocols.