Browsing by Author "Alaraby Salem M."

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Anti-Alzheimer potential, metabolomic profiling and molecular docking of green synthesized silver nanoparticles of Lampranthus coccineus and Malephora lutea aqueous extracts
(Public Library of Science, 2019) Youssif K.A.; Haggag E.G.; Elshamy A.M.; Rabeh M.A.; Gabr N.M.; Seleem A.; Alaraby Salem M.; Hussein A.S.; Krischke M.; Mueller M.J.; Abdelmohsen U.R.; Department of Pharmacognosy; Faculty of Pharmacy; Modern University for Technology and Information; Cairo; Egypt; Department of Pharmacognosy; Faculty of Pharmacy; Helwan University; Cairo; Egypt; Department of Pharmacognosy; Faculty of Pharmacy; Cairo University; Cairo; Egypt; Department of Pharmacology; National Research Centre; Cairo; Egypt; Department of Pharmaceutical Chemistry; October University for Modern Sciences and Arts (MSA); Cairo; Egypt; Julius-von-Sachs-Institute of Biosciences; Biocenter; Pharmaceutical Biology; University of W�rzburg; W�rzburg; Germany; Department of Pharmacognosy; Faculty of Pharmacy; Minia University; Minia; Egypt; Department of Pharmacognosy; Faculty of Pharmacy; Deraya University; Universities Zone; New Minia City; Minia; Egypt
The green synthesis of silver nanoparticles (SNPs) using plant extracts is an eco-friendly method. It is a single step and offers several advantages such as time reducing, cost-effective and environmental non-toxic. Silver nanoparticles are a type of Noble metal nanoparticles and it has tremendous applications in the field of diagnostics, therapeutics, antimicrobial activity, anticancer and neurodegenerative diseases. In the present work, the aqueous extracts of aerial parts of Lampranthus coccineus and Malephora lutea F. Aizoaceae were successfully used for the synthesis of silver nanoparticles. The formation of silver nanoparticles was early detected by a color change from pale yellow to reddish-brown color and was further confirmed by transmission electron microscope (TEM), UV�visible spectroscopy, Fourier transform infrared (FTIR) spectroscopy, dynamic light scattering (DLS), X-ray diffraction (XRD), and energy-dispersive X-ray diffraction (EDX). The TEM analysis of showed spherical nanoparticles with a mean size between 12.86 nm and 28.19 nm and the UV- visible spectroscopy showed ?max of 417 nm, which confirms the presence of nanoparticles. The neuroprotective potential of SNPs was evaluated by assessing the antioxidant and cholinesterase inhibitory activity. Metabolomic profiling was performed on methanolic extracts of L. coccineus and M. lutea and resulted in the identification of 12 compounds, then docking was performed to investigate the possible interaction between the identified compounds and human acetylcholinesterase, butyrylcholinesterase, and glutathione transferase receptor, which are associated with the progress of Alzheimer�s disease. Overall our SNPs highlighted its promising potential in terms of anticholinesterase and antioxidant activity as plant-based anti-Alzheimer drug and against oxidative stress. � 2019 Youssif et al. This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES
(Elsevier Masson SAS, 2019) Hassan G.S.; Abdel Rahman D.E.; Abdelmajeed E.A.; Refaey R.H.; Alaraby Salem M.; Nissan Y.M.; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Cairo University; Kasr Elini St.; Cairo; 11562; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; Badr University in Cairo; Badr City; Cairo; 11829; Egypt; National Cancer Institute; Cairo University; FomElkhalig; Kasr Elaini St.; Cairo; 11796; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University for Modern Sciences and Arts (MSA); Giza; Egypt
New pyrazole derivatives 2�5 were synthesized and evaluated for their COX-1 and COX-2 inhibitory activity in vitro. All compounds showed good inhibitory activity at a nanomolar level and most compounds exhibited selectivity towards COX-2 inhibition. Compounds 2a, 3b, 4a, 5b and 5e exhibited IC50 towards COX-2 enzyme of 19.87, 39.43, 61.24, 38.73 and 39.14 nM, respectively. Furthermore, compounds 3b, 4a, 5b and 5e exhibited a selectivity index of 22.21, 14.35, 17.47 and 13.10, respectively. The most active compounds were further subjected to in vivo anti-inflammatory assay. The tested compounds showed better or comparable activity to celecoxib as positive control. In order to explore their binding mode and selectivity behaviour, molecular docking in the active site of COX-2 was carried out for these derivatives. Analysis of the docked poses of the compounds showed that they adopt similar conformations to the highly selective COX-2 inhibitor, SC-558. The docking pose of compound 3b was confirmed by molecular dynamics. All the tested compounds exhibited potent inhibitory effect on the production of PGE2, in addition to their inhibition of COX-2 enzyme. � 2019 Elsevier Masson SAS
Radioiodinated doxorubicin as a new tumor imaging model: preparation, biological evaluation, docking and molecular dynamics
(Springer Netherlands, 2018) Ibrahim A.B.; Alaraby Salem M.; Fasih T.W.; Brown A.; Sakr T.M.; Labeled Compounds Department; Hot Labs Center; Atomic Energy Authority; Cairo; 13759; Egypt; Pharmaceutical Chemistry Department; Faculty of Pharmacy; October University of Modern Sciences and Arts (MSA); Giza; Egypt; Radioactive Isotopes and Generators Department; Hot Laboratories Centre; Atomic Energy Authority; Cairo; 13759; Egypt; Department of Chemistry; University of Alberta; Edmonton; Canada
Abstract: Non-invasive molecular imaging techniques are accruing more interest in the last decades. Several radiolabelling elements have been FDA-approved and are currently used to characterize tumors. In this study, the DNA intercalating agent doxorubicin was radiolabelled with 125I. Several parameters for the radiolabelling reaction were investigated and optimized. A maximum yield of 94 � 0.3% was reached after reacting 20�?g of doxorubicin with 200�?g Chloramine-T at pH 5 for 30�min. The in vivo stability of 125I-doxorubicin is validated by the low propensity for thyroid uptake in mice. The preclinical T/NT ratio was approximately 6.4 at 30 min. Docking and molecular dynamics confirmed that the radiolabelling of doxorubicin did not affect (or slightly improved its binding to DNA). Overall, 125I-doxorubicin was demonstrated to be a promising non-invasive probe for solid tumor imaging. Graphical Abstract: [Figure not available: see fulltext.]. � 2018, Akad�miai Kiad�, Budapest, Hungary.