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Here, we report the synthesis of cobalt-doped copper oxide nanoparticles (CuO–NPs) via combustion strategy with lime juice as a reductant at relatively low temperature of 600 °C and at shorter duration of 3 h. Powder X-ray diffraction (XRD) results revealed that, every compound was in monoclinic structure with space group C12/C1 (No. 15) and average particle size were found to be 18–21 nm. These NPs were used to evaluate the antimycobacterial activity against “Mycobacterium tuberculosis H37Rv ATCC 27294”, “Mycobacterium abscessus ATCC 19977”, “Mycobacterium fortuitum ATCC 6841”, “Mycobacterium chelonae ATCC 35752” and anticancer activity on MDA-MB-231. Antioxidant activity was evaluated by DPPH method. The results showed that, doping CuO with cobalt improved the antimycobacterial, anticancer and scavenging activities of CuO–NPs.

BACKGROUND Excessive alcohol consumption is a global health burden and requires a better understanding of its neurobiology. A lower density of brain microtubules is found in alcohol-related human brain disease postmortem and in rodent models of chronic alcohol consumption. Here, we report in vivo imaging studies of microtubules in brain using our recently reported Positron Emission Tomography (PET) tracer, [11C]MPC-6827, in chronic alcohol-consuming adult male C57BL/6 J mice and control mice. METHODS In vivo PET imaging studies of [11C]MPC-6827 (3.7 ± 0.8 MBq) were performed in two groups of adult male mice: (1) water-consuming control mice (n = 4) and (2) mice that consumed 20% alcohol (w/v) for 4 months using the intermittent 2-bottle choice procedure that has been shown to lead to signs of alcohol dependence. Dynamic 63 min PET images were acquired using a microPET Inveon system (Siemens, Germany). PET images were reconstructed using the 3D-OSEM algorithm and analyzed using VivoQuant version 4 (Invicro, MA). Tracer uptake in ROIs that included whole brain, prefrontal cortex (PFC), liver and heart was measured and plotted as %ID/g over time (0-63 min) to generate time-activity curves (TACs). RESULTS In general, a trend for lower binding of [11C]MPC-6827 in the whole brain and PFC of mice in the chronic alcohol group was found compared with control group. No group difference in radiotracer binding was found in the peripheral organs such as liver and heart. CONCLUSIONS This pilot study indicates a trend of loss of microtubule binding in whole brain and prefrontal cortex of chronic alcohol administered mice brain compared to control mice, but no loss in heart or liver. These results indicate the potential of [11C]MPC-6827 as a PET ligand for further in vivo imaging investigations of AUD in human.

Nine non-alkaloid constituents viz., sitostenone (1), β-sitosterol (2), naringenin (3), aromadendrin (4), matairesinol (5), vanillic acid (6), ferulic acid (7), protocatechuic acid (8) and sitoster...

A single crystal of vitamin-C-doped lithium sulfate (VCLSM) was grown at room temperature from aqueous solution by slow evaporation method. The as-grown crystals were found to be transparent and yellow in color. Powder X-ray diffractogram of the pure and doped crystals was recorded and various planes were identified for their corresponding reflections. The X-ray diffraction (XRD) analysis validated the crystalline nature of the samples. Single crystal X-ray diffraction study revealed the structure of the crystals and also revealed their monoclinic crystal system with space group P21. The vibrational modes of different functional groups present in the compound were analyzed using Fourier transform infrared (FTIR) spectral analysis. Thermal characteristics study of the crystal was carried out by thermogravimetric analysis (TGA) and differential thermal analysis (DTA) techniques, which clearly showed that the materials have high thermal stability even after doping. Optical transmittance spectrum using UV–Vis–NIR spectrometer showed that the grown crystal is highly transparent in the whole visible and Infrared (IR) region. Second-harmonic generation (SHG) property was confirmed for both pure and doped crystals by Kurtz’s powder test using Nd:YAG Laser.

In this paper, adipic acid crystals were grown using slow evaporation method in aqueous solution of l-alanine at room temperature. X-ray diffraction investigation shows that the crystal belongs to P21/n space group. EDAX study confirms the occurrence of elements in the crystal. The crystal is thermally stable up to 124 °C. Further, the grown crystals were exposed to Co-60 gamma radiations with different doses of 1 Mrad, 3 Mrad, and 5 Mrad at normal room temperature. After gamma irradiation, a small change in the intensity and a slight shift in the Powder X-Ray Diffraction (PXRD) peaks were seen. UV–visible analysis reveals an increase in reflectance after gamma irradiation. Increase in dielectric constant, dielectric loss, and AC conductivity was observed by dielectric studies. Second Harmonic Generation (SHG) efficiency of the crystal is 0.42 times that of the standard Potassium Dihydrogen Phosphate (KDP) crystal and is increased moderately up to the gamma irradiation dosage of 3 Mrad.

Combinations of antiangiogenic and cytotoxic agents show promising results in the treatment of cancer. However, there is a lack of single agent with both antiangiogenic and cytotoxic activities for clinical application. AG-488 aka FLAG-003 is a novel ligand with established antiangiogenetic properties via activation of receptor thymidine kinase (RTK) and anti-tubulin properties in tumor cells. AG-488 is also reported to reduce tumor volume and prolong survival in preclinical animal models of glioblastoma multiforme, breast cancer and is in clinical stage. Higher expression of RTKs and tubulins is reported in various cancers. This study reveals the development of [

Nine non-alkaloid constituents viz., sitostenone (

A novel vicinal diepoxide of alloaureothin was isolated from Streptomyces sp. NIIST-D31 strain along with three carboxamides, p-aminobenzoic acid and 1,6-dimethoxyphenazine. Exhaustive 2D NMR analysis and analysis of experimental, theoretical CD spectra aided in establishing the structure of compound 1. Compound 1 inhibits adipogenesis and accumulation of lipid droplets during the differentiation of 3T3-L1 cells.

Background Serotonin 1A (5-HT1A) receptors are implicated in the pathogenesis of several psychiatric and neurodegenerative disorders motivating the development of suitable radiotracers for in vivo positron emission tomography (PET) neuroimaging. The gold standard PET imaging agent for this target is [carbonyl-11C]WAY-100635, labeled via a technically challenging multi-step reaction that has limited its widespread use. While several antagonist and agonist-based PET radiotracers for 5-HT 1A receptors have been developed, their clinical translation has been hindered by methodological challenges and/or and non-specific binding. As a result, there is continued interest in the development of new and more selective 5-HT1A PET tracers having a relatively easier and reliable radiosynthesis process for routine production and with favorable metabolism to facilitate tracer-kinetic modeling. The purpose of the current study was to develop and characterize a radioligand with suitable characteristics for imaging 5-HT1A receptors in the brain. The current study reports the in vitro characterization and radiosyntheses of three candidate 5-HT1A receptor antagonists, DF-100 (1), DF-300 (2) and DF-400 (3), to explore their suitability as potential PET radiotracers. Results Syntheses of 1–3 and corresponding precursors for radiolabeling were achieved from isonicotinic, picolinic acid or picolino nitrile. In vitro binding studies demonstrated nanomolar affinity of the compounds for 5-HT1A receptors. Binding of 1–3 for other biogenic amines, neurotransmitter receptors, and transporters was negligible with the exception of moderate affinities for α1-adrenergic receptors (4–6-fold less potent than that for 5-HT1A receptor). Radioligands [11C]1–3 were efficiently prepared by 11C-O-methylation of the corresponding phenolic precursor in non-decay corrected radiochemical yields of 7–11% with > 99% chemical and radiochemical purities. Dynamic PET studies in rats demonstrated negligible brain uptake of [11C]1 and [11C]2. In contrast, significant brain uptake of [11C]3 was observed with an early peak SUV of 4–5. However, [11C]3 displayed significant off-target binding attributed to α1-adrenergic receptors based on regional distribution (thalamus>hippocampus) and blocking studies. Conclusion Despite efficient radiolabeling, results from PET imaging experiments limit the application of [11C]3 for in vivo quantification of 5-HT1A receptors. Nevertheless, derivatives of compound 3 may provide a scaffold for alternative PET radiotracers with improved selectivity for 5-HT 1A receptors or α1-adrenergic receptors.

Poor control on the exfoliation of covalent organic frameworks (COFs) remains a disadvantage for their application as two-dimensional nanosheets. An equally important problem is the reversible control at the available surface charges on COFs. Herein, a strategy for the reversible exfoliation, re-stacking, and surface-charge control of a propidium iodide based ionic covalent organic framework, PI-TFP, using cucurbit[7]uril (CB[7]) induced molecular recognition, is reported. The surface charge on PI-TFP facilitates its initial self-exfoliation. However, complexation with CB[7] resulted in re-stacking with concomitant decrease in zeta potential from +28±3.0 to +0.004±0.003 mV. Addition of 1-adamantylamine hydrochloride (AD) facilitates decomplexation of PI-TFP from CB[7], resulting in exfoliation and an increase in zeta potential to +24±3.0 mV. Such control on the exfoliation, re-stacking, and the associated regulation of the surface charge in PI-TFP was exploited for controlling bacterial growth. Thus, the activity of E. coli and S. aureus bacteria obtained with the self-exfoliated PI-TFP could be reversibly controlled by the CB[7]/AD pair.

Objective: The objective of this study was to evaluate the uptake and specificity of [11C]MPC-6827, a MT targeted PET ligand in prostate, glioblastoma and breast cancer cells. Methods: [11C]MPC-6827 was synthesized by reacting corresponding desmethyl precursors with [11C]CH3I in a GE-FX2MeI/FX2M radiochemistry module. In vitro binding of [11C]MPC-6827 was performed in breast cancer MDA-MB-231, glioblastoma (GBM) patient-derived tumor (GBM-PDX), GBM U251 and prostate cancer 3 (PC3) cell lines at 37 °C in quadruplicate at 5, 15, 30, 60, and 90 minute incubation time. The nonspecific bindings were determined by incubation with unlabeled microtubule targeting agents MPC-6827, HD-800, colchicine, paclitaxel and docetaxel (5.0 mM). Results: [11C]MPC-6827 provided the highest binding in the breast cancer cell, MDA-MB-231, among all the cells studied, with 90% specific binding. [11C]MPC-6827 binds to glioblastoma PDX and U251 cells with ~50% and 40% specific binding, whereas, prostate cancer cell line, PC3 cells showed 40% specific binding. [11C]MPC-6827 also exhibits binding to the taxane and colchicine binding sites of MTs, in MDA-MB-231 cells. Conclusion: These data indicate that [11C]MPC-6827 can be a promising PET radiotracer for preclinical imaging of the brain and peripheral cancers.

In multi-user MIMO, the capacity achieving techniques are precoding strategies usually accomplish affordable overall performance with much lower intricacy. Linear precoding strategies include zero-forcing (ZF) precoding customized for low-rate feedback of channel state information (CSI). Non-linear precoding is designed essentially dependent on the concept of dirty paper coding (DPC), which indicates that any recognized interference on the transmitter might be subtracted without the chastisement of radio resources if a definitive precoding scheme can be carried out on the transmit signal. The block diagonalization (BD) is a linear precoding approach for multi-user multi-input multi-output (MU-MIMO) broadcast channels, that's capable of completely get rid of the multi-user interference (MUI), but it isn't computationally efficient. This paper proposes the block diagonalization approach in order to achieve the MIMO broadcast channel capacity. The intricacy analysis recommends that the proposed approach is more efficient than the other precoding techniques in terms of the quantity of required computations.