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Az Zāwīyah, Libya

Adali T.,Near East University | Bentaleb A.,Near East University | Elmarzugi N.,University of Technology Malaysia | Elmarzugi N.,University of Tripoli | Hamza A.M.,National Medical Research Center
International Journal of Biological Macromolecules | Year: 2013

The main aim of this study is to provide understanding for the interaction modes and the binding affinity based on the study of PEG 400 that binds to ctDNA. The effects of the PEG-400-to-ctDNA ratio, pH, incubation time and thermal stability of ctDNA on PEG-ctDNA biocomplex formation were studied. UV-vis-NIR absorption analysis indicated that PEG forms a complex with ctDNA via a mechanism other than intercalation. The results of thermal denaturation studies showed that the PEG-ctDNA biocomplex helix was stabilised, with a resulting increase in the PEG-ctDNA melting temperature. FTIR analysis indicated that the PEG binds to ctDNA through weak to moderately strong hydrophilic and hydrophobic interactions with the base pairs of ctDNA. TEM micrographs showed that the addition of PEG to ctDNA caused ctDNA to condense with PEG molecules into an irregular aggregate structure. These results demonstrate that the PEG-ctDNA biocomplex has potential applications in biomedical sciences. © 2013 Elsevier B.V.

Ali Elmarzugi N.,University of Technology Malaysia | Ali Elmarzugi N.,University of Tripoli | Ibrahim Keleb E.,University of Tripoli | Taleb Mohamed A.,University of Tripoli | And 5 more authors.
Jurnal Teknologi (Sciences and Engineering) | Year: 2013

The utilization of natural products for their pharmaceutical and nutraceuticals purposes have high value in prevention and treatment of myriad illness. In pharmaceutical industry the formulation of natural products into an effective and stable dosage form necessitate evaluation of the processing techniques required and the properties of the product obtained. Therefore the objective of the present study was to prepare and evaluate lettuce leaves Lactuca sativa granules in a view to develop solid dosage forms. Lettuce leaves were washed with water, one batch was dried in open air and the other one in oven and grinded into fine powder. Dried powdered lettuce leaves were granulated without and with polyvinylpyrrolidone (PVP) at various water concentrations. The prepared granules were evaluated for its particle size distribution, bulk density, tapped density, hausners index, Carr's index, friability, flowability and water absorption. The influence of water concentration, PVP addition and drying methods on the granule properties were also investigated. The results obtained showed that lettuce granules possess good flow properties and can be used as a candidate for the formulation of solid dosage forms particularly tablets. © 2013 PenerbitUTM Press. All rights reserved.

Ahmed M.A.,Long Island University | Azam F.,NIMS University | Rghigh A.M.,University of Tripoli | Gbaj A.,National Medical Research Center | Zetrini A.E.,National Medical Research Center
Journal of Pharmacy and Bioallied Sciences | Year: 2012

Purpose: 2-(3-benzoyl phenyl)propanohydroxamic acid (2) and 2-{3-[(hydroxyimino)(phenyl)methyl]phenyl}propanoic acid (3) were synthesized from non-steroidal anti-inflammatory drug, ketoprofen as dual-mechanism drugs. Materials and Methods: Structures of the synthesized compounds were established by IR, 1 H NMR, and mass spectroscopy. Both compounds were screened for their anti-inflammatory activity in rat paw edema model and in vitro antitumor activity against 60 human tumor cell lines. Flexible ligand docking studies were performed with different matrix metalloproteinases and cyclooxygenases to gain an insight into the structural preferences for their inhibition. Results: Compound (2) proved out to be more potent than ketoprofen in rat paw edema model. Both compounds showed moderate anticancer activity ranging from 1% to 23% inhibition of growth in 38 cell lines of 8 tumor subpanels at 10 μM concentration in a single dose experiment. Hydroxamic acid analogue was found to be more potent than ketoximic analogue in terms of its antitumor activity. Conclusion: Analysis of docking results together with experimental findings provide a good explanation for the biological activities associated with synthesized compounds which may be fruitful in designing dual-target-directed drugs that may inhibit cyclooxygenases and MMPs for the treatment of cancer.

Kadirvel M.,University of Manchester | Salem Abudalal A.,National Medical Research Center | Rajendran R.,University of Manchester | Gbaj A.,National Medical Research Center | And 2 more authors.
Carbohydrate Research | Year: 2012

Ester prodrugs have the potential to eliminate the gastrotoxicity associated with the carboxylic acid group of indomethacin. 4,6-Bis-O-2′- [1′-(4″-chlorobenzoyl)-5′-methoxy-2′-methyl-1′H- indol-3′-acetyl]-myo-inositol-1,3,5-orthoacetate (2) was synthesised and evaluated as a COX-2 inhibitor. It adopts a conformationally restricted chair with two indomethacin groups in the sterically hindered 1,3-diaxial positions. Acid-induced cleavage of the orthoacetate lock of the prodrug leads to a ring flip of the myo-inositol ring with the two indomethacin groups now in 1,3-diequatorial positions. This increases the susceptibility of hydrolysis of the ester groups to release indomethacin under acidic conditions. The long half-life (152 min) of decomposition of (2) at ∼pH 1-2 suggests that it may bypass the stomach with minimal hydrolysis upon oral administration. Indomethacin ester (2) was completely stable at pH 4.0-8.5 over 24 h at 37°C and showed comparable activity to indomethacin in a COX-2 assay (pH 8.0). © 2012 Elsevier Ltd. All rights reserved.

Yeltokova M.,Astana Medical University | Zharliganova D.,Astana Medical University | Shaidarov M.,Astana Medical University | Bakhtin M.,Astana Medical University | And 5 more authors.
Radiation Protection Dosimetry | Year: 2015

To explore the possibility to use the lens extract as an in vitro stimulator to conduct a test of stimulated leukergy in liquidators of the accident consequences (LAC) on Chernobyl Nuclear Power Plant (CNPP) with a cataract in the long-term period. The study sample included 72 men-LAC on CNPP, at the age from 42 to 65 y, who have a cataract. The comparison group consisted of 60 men, with a cataract, of the same age, and who were not exposed to radiation. The control group was composed of 60 men, at the age of 42-58 y without lens pathology. Phenomenon of the stimulated leukergy was revealed in persons who had been exposed to radiation in the dose of 18.2±0.58 cGy and was observed in 5.7-8.05 % (P < 0.001), suggesting a continued high auto-aggression to the lens antigens, and the strength of cell-mediated immunity. © The Author 2015.

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