Preparation and Biological Evaluation of 99mtc-Sarafloxacin and 99mtc- Danofloxacin Complexes as a Model for Infection Imaging

Infection and inflammation remain a major cause of mortality and morbidity globally. This promotes research into better and more accurate diagnostic and therapeutic methods. This investigation focused on the labeling of sarafloxacin and danofloxacin for infection imaging. The radiolabeled antibiotic 99mTc-sarafloxacin and 99mTc-danofloxacin were assessed as an infection imaging agent in a mouse model. 99mTc-sarafloxacin and 99mTc-danofloxacin were obtained at pH 11 with a radiochemical yield of 96, 90%, respectively by adding 99mTc to 1 mg sarafloxacin or danofloxacin in the presence of 50 μg SnCl2.2H2O. Biodistribution studies in mice were carried out in experimentally induced infection in the left thigh using Staphylococcus aureus. Both thighs of the mice were dissected and counted, and the ratio of bacterial infected thigh/contralateral thigh was then evaluated. 99mTc-sarafloxacin and 99mTc-danofloxacin showed high uptake (T/NT=3.8±0.1 and 4.9±0.1, respectively) in the infectious lesion and abscess to normal muscle ratio indicating that 99mTcsarafloxacin and 99mTc-danofloxacin could be used for infection imaging

Influence of Nanosilver Synthesis Conditions on its Architecture

Silver nitrate reduction in presence of Ethylene glycol (EG) and Polyethylene glycol (PEG) represents one from the simplest techniques for silver nano-powder fabrication. Where EG act as reducing agent and PEG act as stabilizing agent. The impact of presence either the reducing agent or the stabilizing agent at the reaction media on the properties of synthesized silver were recorded. Regarding to the chain length of PEG was discovered to play the key role in the formation of nano-silver. Accordingly, the variation in the stabilizing agent (PEG) molecular weight on the morphological structures of produced silver was recorded. The formation of nano-silver was confirmed using UV–Vis spectroscopy. The UV–visible scanning results for the aqueous reaction medium containing silver ion has been demonstrated characteristics peak at 420nm that corresponding to the plasmon absorbance of silver nanoparticle. X-ray diffraction (XRD) was utilized to determine the crystalline structure of the prepared silver nano-powders. The crystalline structure of prepared nano-silver was produced in hexagonal, cubic crystal and face centered cubic configurations with different plane of orientation. Scanning electron micrographs of synthesized silver indicated that nano-silver were prepared in morphological structures as nanoparticle

Preparation and Biological Evaluation of 99mtc-Sarafloxacin and 99mtc- Danofloxacin Complexes as a Model for Infection Imaging

Infection and inflammation remain a major cause of mortality and morbidity globally. This promotes research into better and more accurate diagnostic and therapeutic methods. This investigation focused on the labeling of sarafloxacin and danofloxacin for infection imaging. The radiolabeled antibiotic 99mTc-sarafloxacin and 99mTc-danofloxacinwere assessed as an infection imaging agent in a mouse model. 99mTc-sarafloxacin and 99mTc-danofloxacin were obtained at pH 11 with a radiochemical yield of 96, 90%, respectively by adding 99mTc to 1 mg sarafloxacin or danofloxacin in the presence of 50 μg SnCl2.2H2O. Biodistribution studies in mice were carried out in experimentally induced infection in the left thigh using Staphylococcus aureus. Both thighs of the mice were dissected and counted and the ratio of bacterial infected thigh/contralateral thigh was then evaluated. 99mTc-sarafloxacin and 99mTc-danofloxacin showed high uptake (T/NT=3.8±0.1 and 4.9±0.1, respectively) in the infectious lesion and abscess to normal muscle ratio indicating that 99mTcsarafloxacin and 99mTc-danofloxacin could be used for infection imaging.Key words: sarafloxacin/ danofloxacin/ Technetium-99m/ Infection/ inflammation/ Diagnosi

Influence of Nanosilver Synthesis Conditions on its Architecture

Silver nitrate reduction in presence of Ethylene glycol (EG) and Poly Ethylene glycol (PEG) represents one from the simplest techniques for silver nano-powder fabrication. Where EG act as reducing agent and PEG act as stabilizing agent. The impact of presence either the reducing agent or the stabilizing agent at the reaction media on the properties ofsynthesized silver were recorded. Regarding to the chain length of PEG was discovered to play the key role in the formation of nano-silver. Accordingly, the variation in the stabilizing agent (PEG) molecular weight on the morphological structures of produced silver was recorded. The formation of nano-silver was confirmed using UV–Vis spectroscopy. The UV– visiblescanning results for the aqueous reaction medium containing silver ion has been demonstrated characteristics peak at 420nm that corresponding to the plasmon absorbance of silver nanoparticle. X-ray diffraction (XRD) was utilized to determine the crystalline structure of the prepared silver nano-powders.The crystalline structure of prepared nano-silver was producein hexagonal, cubic crystal and face centered cubic configurations with different plane of orientation. Scanning electron micrographs of synthesized silver indicated that nano-silver were prepared in morphological structures as nano-particle.Keywords: Silver, Nano-structures, Nano-material, Reduction, Characterization

Tissue p53-induced glycolysis and apoptosis regulator (TIGAR) is associated with oxidative stress in benign and malignant colorectal lesions

Background: Colorectal cancer (CRC) is the fourth leading cause of cancer-mortality worldwide. Tissue p53-induced glycolysis and apoptosis regulator gene (TIGAR) has an important role in cellular glycolysis and acts as an oncogene.Objectives: We aimed to investigate the diagnostic utility of TIGAR in both CRC and benign bowel deceases.Methods: One-hundred-eighty tissue samples were recruited and classified into 3 groups: group (1) 60 CRC samples from the tumor mass of colorectal cancer patients, group (2), 60 non-neoplastic colorectal tissue samples and group (3), 60 benign bowel lesions samples (ulcerative-colitis, Chron’s disease, adenoma, and familial adenomatous polyposis). The expressions of tissue mRNA and protein levels of TIGAR were determined. Levels of malondialdehyde and reduced glutathione were also measured.Results: Our results showed upregulated expressions of TIGAR gene and protein levels in CRC tissues and benign colonic lesions compared to non-tumor tissues (p < 0.0001). Their levels were higher in inflammatory bowel diseases compared to non-inflammatory benign lesions. There were significant relations among TIGAR expression, protein levels, TNM staging, and the presence of metastasis (p<0.0001). ROC curve analysis showed that TIGAR mRNA expression and its protein can discriminate between CRC and benign lesions and between benign bowel disease and controls.Conclusions: To the best of our knowledge this is the first study to assess the level of TIGAR in different benign bowel diseases. TIGAR might be involved in the pathogenesis of benign and malignant bowel diseases and could be a potential biomarker for diagnosis

Spectroscopic, thermodynamic, kinetic studies and oxidase/antioxidant biomimetic catalytic activities of tris(3,5-dimethylpyrazolyl)borate Cu(II) complexes

A series of copper(II) complexes, viz. [TpMeMeCu(Cl)(H2O)] (1), [TpMeMeCu(OAc)(H2O)] (2), [TpMeMeCu(NO3)] (3) and [TpMeMeCu(ClO4)] (4) containing tris(3,5-dimethylpyrazolyl)borate (KTpMeMe), have been synthesized and fully characterized. The substitution reaction of 1 with thiourea was studied under pseudo-first-order conditions as a function of concentration, temperature and pressure in methanol and acetonitrile as solvents. Two reaction steps that both depended on the nucleophile concentration were observed for both solvents. Substitution of coordinated methanol is about 40 times faster than the substitution of chloride. In acetonitrile, the rate constant for the displacement of coordinated acetonitrile was more than 20 times faster than the substitution of chloride. The reported activation parameters indicate that both reaction steps follow a dissociative mechanism in both solvents. On going from methanol to acetonitrile, the rate constant for the displacement of the solvent becomes more than 200 times faster due to the more labile acetonitrile, but the substitution mechanism remained to have a dissociative character. The antioxidant activities of 1–4 were evaluated for superoxide dismutase (SOD), glutathione-s-transferase (GST0 and glutathione reduced (GSH-Rd) activity. 1 and 2 were found to show (p < 0.05) the highest antioxidant activity in comparison to 3 and 4, which can be ascribed to the geometric configuration as well as the nature of the co-ligand. 1 showed catechol oxidase activity with turnover numbers of 20 min−1 and a coordination affinity for 3,5-DTBC of K1, = 31 mM−1. K1 is rather large and seems to be typical for faster biomimetic models, and also for the enzyme itself (25 mM−1). The reaction rate depended linearly on the complex concentration, indicating a first-order dependence on the catalyst concentration

Synthesis and antibacterial activity of 3-arylidene chromen-2, 4-dione derivatives

Abstract: Derivatives of 3-arylidene chromen-2, 4-dione 1 were synthesized to be used as a starting material for synthesizing some new fused heterocyclic compounds containing coumarin moiety. When compounds 1 reacted with hydrazine derivatives, hydroxylamine hydrochloride, urea, thiourea, semicarbazide and thiosemicarbazide it gave the corresponding compounds 2-5. Compound 4a, b reacted with methyl iodide in DMF and K2CO3 at room temperature to afford the corresponding 6a, b. All these compounds were screened InVitro for their antibacterial activity

Initial Characterization of the FlgE Hook High Molecular Weight Complex of

The spirochete periplasmic flagellum has many unique attributes. One unusual characteristic is the flagellar hook. This structure serves as a universal joint coupling rotation of the membrane-bound motor to the flagellar filament. The hook is comprised of about 120 FlgE monomers, and in most bacteria these structures readily dissociate to monomers (∼ 50 kDa) when treated with heat and detergent. However, in spirochetes the FlgE monomers form a large mass of over 250 kDa [referred to as a high molecular weight complex (HMWC)] that is stable to these and other denaturing conditions. In this communication, we examined specific aspects with respect to the formation and structure of this complex. We found that the Lyme disease spirochete Borrelia burgdorferi synthesized the HMWC throughout the in vitro growth cycle, and also in vivo when implanted in dialysis membrane chambers in rats. The HMWC was stable to formic acid, which supports the concept that the stability of the HMWC is dependent on covalent cross-linking of individual FlgE subunits. Mass spectrometry analysis of the HMWC from both wild type periplasmic flagella and polyhooks from a newly constructed ΔfliK mutant indicated that other proteins besides FlgE were not covalently joined to the complex, and that FlgE was the sole component of the complex. In addition, mass spectrometry analysis also indicated that the HMWC was composed of a polymer of the FlgE protein with both the N- and C-terminal regions remaining intact. These initial studies set the stage for a detailed characterization of the HMWC. Covalent cross-linking of FlgE with the accompanying formation of the HMWC we propose strengthens the hook structure for optimal spirochete motility