Browsing by Author "Abd-Alla W.H."
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Item Molecular modeling and preclinical evaluation of radioiodinated tenoxicam for inflammatory disease diagnosis(Springer Netherlands, 2018) Sakr T.M.; Ibrahim I.T.; Abd-Alla W.H.; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; P.O. 13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt; Labelled Compound Department; Hot Labs Center; Atomic Energy Authority; P.O. 13759; Cairo; Egypt; Department of Pharmaceutical Chemistry; Faculty of Pharmacy; Misr University for Science & Technology; P.O. 77; 6th of October; EgyptAbstract: The aim of the presented study is to investigate a new promising radiopharmaceutical tracer able to visualize and differentiate inflammation versus infection in early stages. Radioiodinated tenoxicam (125I-tenoxicam) was prepared and its radiochemical yield and in vitro stability were assayed. The biodistribution studies were conducted on two different mice models: sterile inflammation and bacterial infection mice models. 125I-tenoxicam showed high T/NT accumulation in the inflammatory tissues revealing high selectivity to the inflammatory tissues in contrast to infection bearing mice. The docking study using CDOCKER protocol for tenoxicam and radioiodinated tenoxicam with COX enzymes was performed to confirm that radioiodinated tenoxicam still retaining COX enzymes selectivity. � 2018, Akad�miai Kiad�, Budapest, Hungary.Item Radioiodinated esmolol as a highly selective radiotracer for myocardial perfusion imaging: In silico study and preclinical evaluation(Elsevier Ltd, 2018) Sakr T.M.; Sanad M.H.; Abd-Alla W.H.; Salama D.H.; Saleh G.M.; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; P.O. Box 13759; Cairo; Egypt; Pharmaceutical Chemistry Department; Collage of Pharmaceutical Science and Drug Manufacturing; Misr University for Science & Technology; P.O. 77; 6th of October City; Giza; Egypt; Health Radiation Research department (Radiodiagnosis Unit); National Center for Radiation Research and Technology; Atomic Energy Authority; Cairo; EgyptChallenges facing cardiovascular imaging necessitate innovation of better radiopharmaceuticals to augment or replace the existing ones. This research assesses the ability and competency of radioiodinated esmolol as a potential cardio selective imaging agent. Radioiodinated esmolol was synthesized with 97.3 � 0.3% radiochemical yield and with high stability up to 48 h at room temperature as well as in rat serum. Molecular modeling study was performed to confirm the binding of iodinated esmolol to ?1-adrenergic receptor. Its biodistribution studies in normal Swiss albino mice showed high heart uptake (38.5 � 0.11%ID/g at 5 min p.i.), heart/liver ratio nearly 3.85:1 and heart/lungs ratio was about 7:1 at 5 min p.i. The evidenced selectivity of the radioiodinated esmolol to ?1-adrenoceptor was confirmed by prior injection of cold esmolol. Gamma camera biodistribution pattern showed that radioiodinated esmolol accumulated selectively in heart. � 2018 Elsevier LtdItem Radiosynthesis, molecular modeling studies and biological evaluation of 99mTc-Ifosfamide complex as a novel probe for solid tumor imaging(Taylor and Francis Ltd, 2018) Motaleb M.A.; El-Safoury D.M.; Abd-Alla W.H.; Awad G.A.S.; Sakr T.M.; Labelled Compounds Department; Hot Labs Center; Atomic Energy Authority; Cairo; Egypt; Pharmaceutical Chemistry Department; College of Pharmaceutical Sciences and Drug Manufacturing; Misr University for Science & Technology; Giza; Egypt; Pharmaceutics and Industrial Pharmacy Department; Faculty of Pharmacy; Ain Shams University; Cairo; Egypt; Radioactive Isotopes and Generator Department; Hot Labs Center; Atomic Energy Authority; Cairo; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; EgyptPurpose: Ifosfamide as a chemotherapeutic drug is used for the treatment of different cancer types. The purpose of this study is the preparation of 99mTc-ifosfamide complex to be evaluated as a potential candidate for tumor imaging. Materials and methods: The radiolabeling of ifosfamide with technetium-99m was carried out by mixing 4mg ifosfamide and 5 ?g of SnCl2.2H2O with 400 MBq Na99mTcO4 at pH 9 for 30 min at room temperature. Computer simulation studies were performed using Accelrys Discovery Studio 2.5 operating system to illustrate the interaction of ifosfamide and 99mTc-ifosfamide complexes with DNA. The in-vivo biodistribution of 99mTc-ifosfamide was studied in tumor-bearing Albino mice. Results: A new 99mTc-ifosfamide complex was synthesized with a good radiochemical yield of 90.3. 2.1% under the optimized conditions and exhibited in-vitro stability up to 2 h. Biodistribution studies showed good uptake in tumor site and high uptake in tumor site with T/NT ?3 after 60 min post-injection. Besides, the molecular docking study confirmed that the complexation of ifosfamide with technetium-99m does not abolish its binding to the target receptor. Conclusion: These promising results afford a new radiopharmaceutical that could be used as a potential tumor imaging. 2018, Copyright 2018 Taylor & Francis Group, LLC.