Small molecules drug conjugate mutual prodrug design (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide bond ; represent new interesting approaches for cancer treatment , the component of SMDC intended for targeting folate receptor , along with greater conservation of component until reaching the target tumor tissue . The designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were processed forward successfully by multistep reaction procedures , and by Thin Layer Chromatography (TLC) for preliminary detection of products and their intermediates, along with their purity. The structures of two final compounds and their intermediates were proclaimed by melting point measurement, infrared spectrometry and ¹HNMR analysis given results greatly correspond with theoretical proposed chemical structure of synthesized compounds. Furthermore, cytotoxic activity evaluation on cell line level had been done for two final compounds against human breast tumor cell (MCF-7) and human ovarian tumor cell (SKO-3) types of cancer cell line and the results were confirmed which show greater cytotoxic tumor activity of two final compounds, while compound VI possess optimal activity proportional with increased number of 6-MP molecules.
The aim of this study is to formulate and evaluate ezetimibe nanoparticles using solvent antisolvent technology. Ezetimibe is a practically water-insoluble drug which acts as a lipid lowering drug that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe prepared as nano particles in order to improve its solubility and dissolution rate.
Thirty formulas were prepared and different stabilizing agents were used with different concentrations such as poly vinyl pyrrolidone (PVPK-30), poly vinyl alcohol (PVA), hydroxy propyl methyl cellulose E5 (HPMC), and poloxamer. The ratios of drug to stabilizers used to prepare the nanoparticles were 1: 2, 1:3 and 1:4.
The prepared nanoparticles
... Show MoreDrug nanocrystals are nanoscopic crystals of the parent compound with dimensions less than 1 µm. A decrease in particle size will lead to an increase in effective surface area in the diffusion layer, which, in turn, increases the drug dissolution rate. Drug nanocrystals are one of the most important strategies to enhance the oral bioavailability of hydrophobic drugs.
Cefixime is the first member of what is generally termed the third generation orally active cephalosporins. These third generation cephalosporins are distinct from the older β-lactam antibiotics in their intensive antibacterial activity against a wide range of gram-negative bacteria.
The aim of this study is to prepare nanocrystals of cefixime as a caps
... Show MoreBackground: During acrylic resin processing, the mold must be separated from the surface of the gypsum to prevent liquid resin from penetrating into the gypsum, and water from the gypsum seeping into the acrylic resin. For many years, tin foil was the most acceptable separating medium, and because it's difficult to apply, a tin-foil substitute is used. In this study, olive oil is used as an alternative to tin foil separating medium for first time, and evaluating its effect as a separating medium on some mechanical properties such as (indentation hardness and transverse strength) of acrylic resins denture base comparing it with those processed using tin-foil and tin foil substitute such as (cold mold seal) separating medium. Materials and M
... Show MoreThe reaction of 1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one with one equivalent of 4-chlorophenol by coupling reaction afforded (E)-4-((5-chloro-2- hydroxyphenyl)diazenyl)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one. Then azo ligand was characterize using spectroscopic studies ( FTIR,UV-Vis, 1H and 13CNMR, Mass) also micro-elemental analysiz (C.H.N.O). Transition metal chelation with Co(II), Ni(II), Cu(II), and Zn(II) was investigated, revealing 1:2 metal-to-ligand stoichiometry with octahedral geometry. The biological, and industrial application for the azo ligand and it is complexes were evaluated, demonstrating antimicrobial activity against bacterial and fungal strains, with the Zn(II) complex exhibiting superior inhibition. Additionally,
... Show MoreBackground: C-reactive protein (CRP) is an acute phase protein that its plasma levels increase after trauma or surgery so it is used as an indicator for the level of inflammation after surgery. The objective of this study is to investigate pre- and post-operative levels of CRP in three types of oral surgical interventions (Apicoectomy, Impaction, and Impacted teeth exposure). Materials and Methods: A total number of (48) healthy individuals aged (20-60) years who needed oral surgical intervention for either (removal of impacted third molars, exposure of an impacted canine, or Apicoectomy). A 4ml venous blood was obtained from each patient at two occasions (pre-operatively at the day of operation and post-operatively after 48 hours), then ce
... Show MoreThe largest use of x-ray in medical by dentists, employers or persons that needed by patients with specific conditions, lead to higher exposure of x-ray that may cause many diseases. In the present work radiography films have been used in evaluating the efficiency of using unsaturated polyester polymer reinforced with lead oxide (PbO) as shield material for medical x-ray devices, many parameters studied like concentration and thickness that they are increasing the attenuation of x-ray in them. The results show that the attenuation of X-ray increasing with concentration of reinforced material and with thickness, and the optical density decreases with increasing concentration from 0% to 50%, we chose 30% as suitable concentration to increase
... Show MoreMost pathological effects of lead on the body are due to ability of lead to bind with important cellular molecules of various tissues and organs leading to formation abnormal molecules and thus to emergence of pathological conditions. To evaluation the risk to the health status of Iraqi workers who work in the batteries industry, expression of three types of calmodulin related genes were examined. Blood samples were collected from worker working in Iraqi industry of batteries (located in Al-Waziriya), then RNAs extraction were done thereby gene expression for Calcium/Calmodulin- dependent protein kinase2 (CaMKK2), C-X-C Chemokine receptor 4 (CXCR4) and mitogen activated protein kinase kinase 6 (MAP2K6) was done for each sample by using RT-q
... Show MoreIn this work an enzyme linked immunosorbent assay (ELISA) technique has been used for detection of some inflammatory markers in serum of acute coronary syndrome (ACS)-Patients Admitted to the cardiac care unit (CCU) of Iraqi Centre For Heart Diseases and Ibn AlNafees Teaching Hospital. The present method includes quantitative measurement of interleukine-6 (IL-6) and C-reactive protein (CRP), as their increase during symptoms may be responsible for identifying the mechanism of myocardial damag, in addition to their best performance than other quantitative tests perhaps due to their association with atherosclerotic process that belongs to the endothelial dysfunction. Aim of this study is to estimate the prevalence and correlation of IL-6 w
... Show MoreThis study involved the effect of anew nickel (II) complexs with formla [NiL2(H2O)2].2.5ETOH where L=Bis[5-(p-nitrophenyL)-4-phenyL-1,2,4-traizole-3-dithocarbamato hydrazide] diaqua. nickel(II). Ethanol(2.5).and anti-cancer drug cyclophosphamide on specific actifity of two Liver enzymes (GOT,GPT) in the (Liver,kidney) tissues and on the creatinine Level in the kidney byUtilizing an invivosystem in femalmice.The result showed that inhibition in the activity of GPT and GOT enzymes in theLiver and in both nickel (II) complex and cyclophosphamide drug (CP) . mice weretreated with three doses (90,180,320) µg/mouse for three days for each group.The Liver show's the highest rate of GPT inhibition was about 97.43% at180µg/mouse regarding the ki
... Show MoreAdipose tissue releases pro- and anti-inflammatory cytokines and hormones such as irisin, visfatin, and interleukin-6, which may be linked to periodontal diseases.
Our study aimed to determine salivary irisin, visfatin, and interleukin-6 levels in gingivitis and periodontitis patients, compare them with healthy periodontal patients, and evaluate the association between these biomarkers.