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Despite enormous advancements in its management, cancer is the world's primary cause of mortality. Therefore, tremendous strides were made to produce intelligent theranostics with mitigated side effects and improved specificity and efficiency. Thus, we developed a pH-sensitive theranostic platform composed of dextran immobilized zinc oxide nanoparticles, loaded with doxorubicin and radiolabeled with the technetium-99m radionuclide (99mTc-labelled DOX-loaded ZnO@dextran). The platform measured 11.5 nm in diameter with −12 mV zeta potential, 88% DOX loading efficiency and 98.5% radiolabeling efficiency. It showed DOX release in a pH-responsive manner, releasing 93.1% cumulatively at pH 5 but just 7% at pH 7.4. It showed improved intracellular uptake, which resulted in a high growth suppressive effect against MCF-7 cancer cells as compared to the free DOX. It boasted a 4 times lower IC50 than DOX, indicating its significant anti-proliferative potential (0.14 and 0.55 μg ml−1, respectively). The in vitro biological evaluation revealed that its molecular mode of anti-proliferative action included downregulating Cdk-2, which provoked G1/S cell cycle arrest, and upregulating both the intracellular ROS level and caspase-3, which induced apoptosis and necrosis. The in vivo experiments in Ehrlich-ascites carcinoma bearing mice demonstrated that DOX-loaded ZnO@dextran showed a considerable 4-fold increase in anti-tumor efficacy compared to DOX. Moreover, by utilizing the diagnostic radionuclide (99mTc), the radiolabeled platform (99mTc-labelled DOX-loaded ZnO@dextran) was in vivo monitored in tumor-bearing mice, revealing high tumor accumulation (14% ID g−1 at 1 h p.i.) and reduced uptake in non-target organs with a 17.5 T/NT ratio at 1 h p.i. Hence, 99mTc-labelled DOX-loaded ZnO@dextran could be recommended as a rectified tumor-targeted theranostic platform. [ABSTRACT FROM AUTHOR]

This study focuses on the synthesis and preliminary bio-evaluation of [99mTc]-technetium tricarbonyl procainamide ([99mTc]-technetium tricarbony PA) as a viable cardiac imaging agent. The compound, [99mTc]-technetium tricarbony PA, was synthesized by labelling procainamide with a [99mTc]-technetium tricarbonyl core, yielding a high radiochemical yield and radiochemical purity of 98%. Under optimal circumstances, high radiochemical yield and purity were obtained utilizing [99mTc]-technetium tricarbonyl core within 30 min of incubation at pH 9, 200 µg substrate concentration, and 100 °C reaction temperature. The heart showed a high absorption of 32.39 ± 0.88% of the injected dose/g organ (ID/g), confirming the suitability of [99mTc]-technetium tricarbonyl PA as a viable complex for heart imaging. [ABSTRACT FROM AUTHOR]

Allantoin increases in different stress conditions and environment such as physical activity, amniotic fluids and oxidative stress. So, we inspired to explore the role of allantoin as a metabolic by-product in health improvement and protection using irradiation as simulator for oxidative stress. Allantoin was injected i.p. (100 mg/kg) in senile male rats in irradiated and non-irradiated groups in comparison to sham operated group. The studied parameters were superoxide dismutase, Glutathione reductase, Glutathione, total antioxidant capacity, collagenase, urea, creatine kinase, alanine transaminase, aspartate aminotransferase, triglycerides, total cholesterol, and HDL and LDL cholesterol. Allantoin in vitro antitumor activity was MTT assayed for some age dependent cancers. Allantoin showed improvement in all in vivo studied oxidative stress parameters. Allantoin showed an increase in lipogenesis was recorded as a hepatic energy targeting muscles. Allantoin improves aging process indicated by its collagenase inhibitory effect. Allantoin showed cytotoxicity against prostate, colon, intestinal ovarian and breast cancers and weak inhibitory against larynx cancer. Allantoin may be the possible mysterious key factor involved in health and aging improvement and cancer protection in stress conditions such as physically activity and radiation hazards. [ABSTRACT FROM AUTHOR]

One of the most famous techniques for stomach ulcer imaging is the nuclear imaging technique. We aim to focus on the synthesis of 125I-cimetidine (125I-cim) as an agent for peptic ulcer imaging. Cimetidine was labeled with Iodine-125 using a different oxidizing agent (Ch-T, NBS). All factors affecting the labeling yield were optimized. The radiochemical yield of 125I-cim was 98 ± 0.22% at optimum conditions. In vitro stability, in vivo biodistribution of 125I-cimetidine was studied in three groups: control group, pretreated group, and ulcer bearing group. In vivo biodistribution studies of 125I-cim revealed high uptake in the stomach ulcer, reaching about 75.4 ± 1.2% ID/g at 15 min post-injection, than pretreated groups compared to the control. The results showed the suitability of using 125I-cimetidine for stomach ulcer imaging. [ABSTRACT FROM AUTHOR]

The imaging of organs is very important in the field of diagnosis especially in case of liver diseases. In the present work, carnosine was successfully labeled with iodine-131 at room temperature in acidic medium using chloramine-T (Ch-T) as moderate oxidizing agent. The parameters affecting labeling of carnosine such as amount of oxidizing agent, amount of substrate, pH value of the reaction mixture, reaction temperature and reaction time, were investigated. The best conditions for formation of 131I-carnosine (131I-CAR) complex were 40 μg of chloramine-T (Ch-T), 75 μg of carnosine, pH 4 and 45 min reaction time at room temperature. The radiochemical yield for 131I-CAR complex was (91 ± 0.11) % at optimum conditions and the labeled complex was stable for 2 h after labeling process. Biodistribution study was achieved using three groups of rats (normal, treated by inactive carnosine and hepatotoxicity rats induced by CCl4). Hepatotoxicity of liver was evaluated using different biochemical markers such as ALT, AST and ALK.P. The 131I-CAR complex showed selective bio-localization in stomach and liver and its selectivity increases in acquired hepatotoxicity. The biological distribution indicates that the suitability of 131I-CAR as a potential hepatotoxicity imaging to detect hepatitis and medical prognosis. [ABSTRACT FROM AUTHOR]

Purpose: To evaluate the possible radioprotective effect of Costus speciosus and carnosine as natural antioxidants in order to control the hyperglycemia developed in male albino rats exposed to acute oxidative stress induced by gamma radiation. Methods: Twenty-eight adult male albino rats were divided into four groups. The first group was taken as a control group, while the three other groups were exposed to γ irradiation at a single 7.5 Gy dose. Furthermore, the rats in the second and third groups were i.p. injected with Costus speciosus root powder and carnosine, respectively. On the 3rd day, after irradiation, the serum levels of glucose, insulin, C peptide, copper, iron, calcium, total antioxidant capacity (TAC) and malondialdehyde (MDA) were measureded. Results: The results revealed that exposure to γ irradiation induced significant increases in serum glucose, iron, and malondialdehyde. However, the levels of serum calcium, copper, total antioxidant capacity and insulin significantly decreased (p < 0.05). A significant decrease was observed in C peptide in the exposed group, compared to control group. All the test parameters indicate improvement after treatment with Costus speciosus and carnosine (p < 0.05). Conclusion: Costus speciosus and carnosine ameliorate the effect of gamma radiation, indicating their role as antidiabetic agents and radioprotectors; however, Costus speciosus was critically more efficient than carnosine. [ABSTRACT FROM AUTHOR]

Levalbuterol was successfully radiolabeled with iodine using chloramine-T as an oxidizing agent via an electrophilic substitution reaction. The reaction parameters that affecting the labeling yield such as levalbuterol concentration, chloramine-T concentration, pH of the reaction medium and reaction time were studied in details. The radiochemical yield was 97.5 ± 0.5% and the radioiodinated compound was separated by HPLC. In vitro studies showed that the iodinated levalbuterol was stable for up to 24 h. The biodistribution in experimental animals showed that the lung uptake was 68.18 ± 0.17% at 5 min post injection which decreased with time until reached to 18.7 ± 0.12% at 2 h which was higher than other recent developed radiopharmaceuticals for lung imaging. The clearance pathways from the mice appear to proceed via both hepatobiliary and renal pathways. Predosing the mice with cold levalbuterol reduced the lung uptake to 20 ± 1.3% and further confirms the high specificity and selectivity of 125I-levalbuterol for the lung. [ABSTRACT FROM AUTHOR]

• Synthesis of Glutathione-coated selenium nanoparticles (GSH/SeNPs). • Antioxidant activity determination of (GSH/SeNPs) using DPPH assay. • Radiolabeling of (GSH/SeNPs) with technetium 99m (99mTc). • Determination of in-vitro stability of 99mTc-GSH/SeNPs complex. • In-vivo distribution in normal and solid tumor-bearing mice. Selenium nanoparticles (SeNPs) have become one of the most prospective and promising tools in the course of cancer diagnosis and therapy. Here we describe the synthesis of a novel radioactive platform for tumor imaging using selenium nanoparticles. SeNPs were synthetized using dithionite and glutathione as reducing and capping agent respectively with 5 mmol/L sodium selenite as a precursor and then SeNPs radiolabeled with technetium-99 m, the most common and famous radioactive isotope used for imaging purposes. A characteristic profile for the synthesized SeNPs was performed including size analysis, zeta potential, antioxidant activity, radiochemical yield and in-vivo biodistribution in normal and solid tumor bearing mice. Size analysis showed amorphous SeNP cores of a mean diameter of 21 ± 5 nm with a hydrodynamic size of 43 ± 8 nm and −28 mV zeta potential. The particles also showed a superior antioxidant activity of radical scavenging activity 55.6% according to DPPH assay, in addition, satisfying radiochemical yield up to 97 ± 1.5 was achieved. In vivo studies were applied on male Swiss albino mice that demonstrated a good biodistribution pattern in normal mice with a moderate accumulation in liver at 30 min post injection. Excellent T/NT ratios were obtained in solid tumor bearing mice throughout the experimental time points. The as-synthetized selenium nanoparticles demonstrated surprising and satisfying features which make them promising enough for tumor theranosis. [ABSTRACT FROM AUTHOR]