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Aβ42 plaque formation is one of the preliminary pathologic events that occur post traumatic brain injury (TBI) which is also among the most noteworthy hallmarks of AD. Their pre symptomatic detection is therefore vital for better disease management. Chalcone–picolinic acid chelator derivative, 6‐({[(6‐carboxypyridin‐2‐yl)methyl](2‐{4‐[(2E)‐3‐[4‐(dimethyl amino)phenyl]prop‐2‐enoyl]phenoxy}ethyl)amino}methyl)pyridine‐2‐carboxylic acid, Py-chal was synthesized to selectively identify amyloid plaques formed post head trauma using SPECT imaging by stable complexation to 99mTc with > 97% efficiency without compromising amyloid specificity. The binding potential of the Py-chal ligand to amyloid plaques remained high as confirmed by in vitro binding assay and photophysical spectra. Further, the Py-chal complex stained amyloid aggregates in the brain sections of rmTBI mice model. In vivo scintigraphy in TBI mice model displayed high uptake followed by high retention while the healthy rabbits displayed higher brain uptake followed by a rapid washout attributed to absence of amyloid plaques. Higher uptake in brain of TBI model was also confirmed by ex vivo biodistribution analysis wherein brain uptake of 3.38 ± 0.2% ID/g at 2 min p.i. was observed for TBI mice model. This was followed by prolonged retention and more than twofold higher activity as compared to sham mice brain. This preliminary data suggests the specificity of the radiotracer for amyloid detection post head trauma and applicability of 99mTc labeled Py-chal complex for TBI-induced β-amyloid SPECT imaging. [ABSTRACT FROM AUTHOR]

A facile hydrothermal approach was used to synthesize a self-assembled tailored rod-shaped g-C3N4 anchored with molybdenum diselenide (MoSe2) flowers. Due to the presence of basic sites, MoSe2 can be loaded on the surface of the rod-type morphology of g-C3N4. The as-prepared materials were characterized using several techniques. The catalytic activities of the as-prepared g-C3N4/MoSe2 (CNM) composites were assessed by the catalytic reduction of harmful nitroarenes such as 4-nitrophenol (4-NP) and the organic dye rhodamine-B (RhB) together with NaBH4 in an aqueous solution. The as-synthesized CNM catalysts exhibit good performance toward both the catalytic reduction of 4-NP and degradation of the RhB dye. The results obtained indicate that among all the composites prepared, the CNM (6 : 1) shows the best reduction rate in 4-NP conversion, with a reduction efficiency of 99.70% in 6 min and degradation of RhB with 98% in 3 min. The synergic effect of MoSe2 flowers decorated on g-C3N4 promotes the electron transfer that is responsible for the highest catalytic reduction of 4-NP. The reduction and degradation mechanisms were also elucidated and discussed. The reusability study of the catalyst shows good results during the consecutive degradation and reduction experiments. Biocompatible studies on CNM (6 : 1) showed promising results for future prospects in biological applications. The material synthesized can serve as a novel heterogeneous catalyst for the removal of toxic contaminants and open new avenues for other useful applications. [ABSTRACT FROM AUTHOR]

Vascular endothelial growth factor co‐receptor neuropilin‐1, NRP‐1, is one of the prime tumor targets owing to its overexpression in numerous carcinomas. A peptidic conjugate, DO3A−Et‐RPAR was synthesized in 97% purity. It was labeled with 99mTc in 98% efficiency and specific activity of 3.62 MBq/nmol. The agent displayed minimal toxicity of 15% in healthy HEK293 cells at 0.5 mM concentration post 72 h incubation. 99mTc‐DO3A−Et‐RPAR was 98.6% stable in human serum up to 24 h post labeling. Cellular uptake assays exhibited maximum NRP‐1‐specific uptake (20±0.26% activity at 2 h) with low nanomolar affinity (KD = 9.21±0.36 nM) in U‐87 MG cells. In vivo blood kinetics study of radioconjugate establishes stability and rapid clearance from the bloodstream with biological half‐life of t1/2 (fast), 52±0.2 min; and t1/2 (slow), 13 h 10±0.4 min. Biodistribution studies carried out in U‐87 MG xenograft mice showed tumor to muscle ratio of 8.3 at 2 h p.i. [ABSTRACT FROM AUTHOR]

Correct staging is the most crucial for the treatment outcome in cancer management. Molecular imaging with 18F-fluoroestradiol (FES) positron emission tomography-computed tomography (PET-CT) targets estrogen receptor (ER) and may have a higher incremental value in diagnosis by aiding specificity. We enrolled 12 female breast cancer patients prospectively and did 18F-FES PET-CT and 18F-fluorodeoxyglucose (FDG) PET-CT within 1 week interval time. Lesion detection sensitivity was compared for a total number of lesions and for nonhepatic lesions only by McNemar test. 18F-FES PET-CT was taken as reference in case of indeterminate lesions. The incremental value reported by identifying 18F-FES exclusive lesions and by characterization of 18F-FDG indeterminate lesions. Spearman rank test was used to correlate ER expression and maximum standardized uptake value (SUVmax). Two ER-negative patients with no 18F-FES uptake were excluded. Ten ER-positive patients with 154 disease lesions were finally analyzed. 18F-FDG picked-up 142 lesions (sensitivity 92.21%), whereas 18F-FES picked-up 116 lesions (sensitivity 75.32%) and this difference was statistically significant. For nonhepatic lesions (n = 136) detectability, 18F-FDG picked-up 124 (sensitivity 91.18%), whereas 18F-FES picked-up 116 (sensitivity 85.29%) lesions and this difference was not statistically significant. Beside 12 exclusive lesions, 18F-FES characterized 41 (27.5%) 18F-FDG indeterminate lesions. Overall 18F-FES impacted 20% patient management. The positive trend was also seen with 18F-FES SUVmax with ER expression and negative with 18F-FDG SUVmax. We conclude, 18F-FDG has overall better sensitivity than 18F-FES PET-CT, however for nonhepatic metastasis difference was not significant. 18F-FES PET-CT better-characterized lesions and impacted 20% patient management. Therefore, 18F-FES PET-CT should be used with 18F-FDG PET-CT in strongly ER expressing patients for better specificity. [ABSTRACT FROM AUTHOR]