Theragnostic Cu/Cu Radioisotopes Production With RFT-30 Cyclotron.

Cu and Cu are theragnostic pair radionuclides with promising application in the nuclear medicine. Cu is PET nuclide for the non-invasive diagnosis and Cu is beta emitter for therapy of various cancers. This study discusses optimization efforts in the production of these radioactive coppers carried out with 30 MeV cyclotron.

Biological behavior of nanoparticles with Zr-89 for cancer targeting based on their distinct surface composition.

Nano-sized materials with properties that enable their internalization into target cells using passive targeting systems have been utilized with radioisotopes to track their pharmacokinetics in the body. Here, we report the incorporation of novel chelator-free Zr-89 using a hierarchical iron oxide nanocomposite (Zr-IONC). Characterization revealed that it had a rice-shape with a mean width of 160 nm.

TiO Decorated Low-Molecular Chitosan a Microsized Adsorbent for a Ge/Ga Generator System.

We report column material for a Ge/Ga generator with acid resistance and excellent adsorption and desorption capacity of Ge and Ga, respectively. Despite being a core element of the Ge/Ga generator system, research on this has been insufficient. Therefore, we synthesized a low molecular chitosan-based TiO (LC-TiO) adsorbent via a physical trapping method as a durable Ge/Ga generator column material.

Red Blood Cell Membrane Bioengineered Zr-89 Labelled Hollow Mesoporous Silica Nanosphere for Overcoming Phagocytosis.

Biomimetic nanoparticles (NPs) have been actively studied for their biological compatibility due to its distinguished abilities viz. long-term circulation, low toxicity, ease for surface modification, and its ability to avoid phagocytosis of NPs by macrophages. Coating the NPs with a variety of cell membranes bearing the immune control proteins increases drug efficacy while complementing the intrinsic advantages of the NPs.

Chitosan-TiO composite: A potential Ge/Ga generator column material.

A durable and ready to use Ge-Ga generator column material is required for its routine use in radiopharmaceutical procedures. The present work comprises preliminary studies for development and evaluation of chitosan-TiO based microsphere (C-TOM) composite towards its competence as a column material. The batch uptake studies showed higher distribution coefficients for Ge vis-à-vis Ga in the complete concentration range of HCl examined (0.

Development of Ga-SCN-DOTA-Capsaicin as an Imaging Agent Targeting Apoptosis and Cell Cycle Arrest in Breast Cancer.

Ga-labeled capsaicin using a DOTA (1,4,7,10-tetraazocyclododecane-N,N',N″,N'″-tetraacetic acid) derivative [Ga-SCN-Benzyl(Bn)-DOTA-capsaicin] was studied for the diagnosis of breast cancers, such as MCF-7 and SK-BR-3. The standard compound, Ga-SCN-Bn-DOTA-capsaicin, was also prepared and characterized by spectroscopic analysis. The binding affinity of Ga-SCN-Bn-DOTA-capsaicin was evaluated by using breast cancer cell lines (MCF-7, SK-BR-3) and colon cancer cell (CT-26); the biodistribution was carried out by using MCF-7-bearing nude mice, after which the positron emission tomography (PET) images were obtained at different time intervals (15-120 minutes).

Acid resistant zirconium phosphate for the long term application of Ge/Ga generator system.

The Ge/Ga generator system is an excellent source for producing ready-to-use Ga-68 in clinical Positron Emission Tomography (PET) applications. The column adsorbent is the key component for the Ge/Ga generator system. Therefore, several studies have been conducted to identify column materials with a stable and superior elution yield in an acidic eluent (0.

Discovery of boronic acid-based fluorescent probes targeting amyloid-beta plaques in Alzheimer's disease.

A boronic acid-based fluorescent probe was developed for diagnosis of amyloid-β (Aβ) plaques from Alzheimer's disease (AD). Probe 4c, which included boronic acid as a functional group, exhibited a significant increase (64.37-fold, FAβ/F0) in fluorescence intensity as a response to Aβ aggregates, with a blue shift (105nm) in the maximum emission wavelength.

Synthesis of Diacid-Assisted Indium Oxide Nanoparticles and Its CO Gas Sensing Activity.

Indium oxide (In2O3) is an extreme wide band-gap oxide material with unique electronic and optical properties that is used widely in solar cells, gas sensors and optoelectronic devices. In this study, two types of In2O3 nanostructures were prepared by a simple hydrothermal method using succinic acid (SA) or malonic acid (MA) as the assistant agents. The products were characterized by powder X-ray diffractions and scanning electron microscopy (SEM).

Development of fluorescent probes that bind and stain amyloid plaques in Alzheimer's disease.

β-amyloid (Aβ) plaques in the brain are composed of Aβ40 and Aβ42 peptides, and are the defining pathological feature of Alzheimer's disease (AD). Fluorescent probes that can detect Aβ plaques have gained increasing interest as potential tools for in vitro and in vivo monitoring of the progression of AD. In this study, chalcone-mimic fluorescent probe 5 was designed and prepared.

In-house development of an optimized synthetic module for routine [11C]acetate production.

[11C]Acetate, a radiotracer for PET imaging, is a promising radiopharmaceutical for overcoming the limitation of 2-deoxy-2-[18F]fluoro-D-glucose in a number of cancers. Here, the optimized automatic synthesis of [11C]acetate using an in-house-developed module under different conditions has been reported for routine production. [11C]CO2 was produced in a 16.

Synthesis and inhibitory effects of some novel 1,3-diarylprop-2-en-1-one analogues in Foxp3 expression: a novel class of anti-cancer candidates.

A series of novel analogues of 1,3-diarylprop-2-en-1-one (3a-m) were synthesized and evaluated for their inhibitory activity of FOX P3 gene expression and apoptosis in CD4(+)T cells that had been isolated from the spleen of 8 to 10 weeks old mice. The structure-activity relationship (SAR) of the R1 and R2 modification was studied to identify a candidate with the maximum potency. Of these compounds, 3d showed the highest inhibitory activity of FOX P3 gene expression and apoptosis (66.

Synthesis and characterization of a (68)Ga-labeled N-(2-diethylaminoethyl)benzamide derivative as potential PET probe for malignant melanoma.

Radiolabeled benzamides have been reported to be attractive agents for targeting malignant melanoma as they bind melanin and display high accumulation in melanoma cells. Herein, we report the synthesis and bioevaluation of a novel (68)Ga-labeled benzamide as a potential PET agent for malignant melanoma. The novel radiotracer was synthesized in good radiochemical yields (80% decay corrected yield) and high specific radioactivity (10 GBq/μmol).

Synthesis and evaluation of a novel 68Ga-labeled DOTA-benzamide derivative for malignant melanoma imaging.

Malignant melanoma displays a highly aggressive metastasis. Thus, early diagnosis of malignant melanoma is important for patient survival. We designed and synthesized a novel (68)Ga-labeled benzamide derivative that specifically binds to melanoma as demonstrated by its ability to bind to melanin.

Fluorescent 2-styrylpyridazin-3(2H)-one derivatives as probes targeting amyloid-beta plaques in Alzheimer's disease.

Amyloid plaques, which are primarily composed of aggregated amyloid-beta (Aβ) peptide, are the neuropathological hallmarks of Alzheimer's disease (AD). Fluorescent markers containing 2-styrylpyridazin-3(2H)-ones were developed to detect intracellular aggregated Aβ peptides. Nine compounds exhibited a greater than 10-fold increase of in emission spectra before and after mixing with Aβ aggregates compared with before mixing.

Design, synthesis, and anti-influenza viral activities of 1,3-diarylprop-2-en-1-ones: a novel class of neuraminidase inhibitors.

A series of 1,3-diarylprop-2-en-1-one derivatives 3a-v have been synthesized and evaluated for their ability to inhibit neuraminidase (NA). Among the prepared compounds, the less lipophilic derivative 3k showed the most potent in vitro inhibitory activity against NA with an IC(50) value of 1.5 μM.

Synthesis of novel phytosphingosine derivatives and their preliminary biological evaluation for enhancing radiation therapy.

Eight d-ribo-phytosphingosine derivatives were synthesized from d-ribo-phytosphingosine and diverse acyl chlorides with N,N-diisopropylethylamine in tetrahydrofuran for 1h at room temperature. Effect of these compounds on IR-induced cell death was evaluated on blood cancer cells (Jurkat). Among these, 3d showed the highest enhancement of radiosensitizing effect.

Design and evaluation of the tandem target for a simultaneous production of [11C]CH4 and [18F]-fluoride.

The tandem target for a simultaneous production of [11C]CH4 and [(18)F]-fluoride has been designed and evaluated. A separate recovery system has been applied for a simultaneous collection of [11C]CH4 and [(18)F]-fluoride after a bombardment. The [11C]CH4 target was placed in front, and the [18F]-fluoride target was posted successively.

In vivo targeting of ERG potassium channels in mice and dogs by a positron-emitting analogue of fluoroclofilium.

The antiarrhythmic clofilium is an efficient blocker of hERG1 potassium channels that are strongly expressed in the heart. Therefore, derivatives of clofilium that emit positrons might be useful tools for monitoring hERG1 channels in vivo. Fluoro- clofilium (F-clofilium) was synthesized and its channel-blocking properties were determined for hERG1 and hEAG1 channels expressed in HEK?293 cells and in Xenopus oocytes.