The spectrum of clinical efficacy of Methotrexate (MTX) is broad in that MTX is used in the treatment of certain cancers, severe psoriasis and rheumatoid arthritis.Various mechanisms by which cancer cells grown in tissue culture become resistant to anticancer drugs. The use of multiple drugs with different mechanisms of entry into cells and different cellular targets allows for effective chemotherapy and high cure rates. In an efforts to develop effective strategies that increase the therapeutic potential of anticancer drugs with less systemic toxicity ,are being directed towards the investigation of dietary supplements and other phytotherapeutic agents for their synergistic efficacy in combination with anticancer drugs. A promising approach to improve the cancer cell selectivity of methotrexate is the chemical transformation into reversible derivatives which convert the conjugate to the parent drug by virtue of enzyme within cancer tissue. The present study includes the synthesis of two derivatives of methotrexate which are :-Schiff base methotrexate-silibinin conjugate ( compound 5), and Methotrexate-silibinin conjugate (compound 6).The synthesis of the target compounds was accomplished following multistep reaction procedures. The chemical reactions were followed up and purity of the products was checked by TLC. The structures of the final compounds and their intermediates were characterized and identified by their melting points, infrared spectroscopy, 1H-NMR and elemental microanalysis(C H N S).The anticancer activity of these compounds was investigated by HEP-2 cell line(Larynx carcinoma), which showed that compounds 5 and 6 have the higher activity than methotrexate or silibinin alone.These are promising data for the discovery of new anticancer agents in future. These compounds may deliver the parent drug selectively into the cancer cells to be hydrolyzed by enzymes that are elevated in tumor tissues compared with normal tissues . Keywords: Methotrexate, Silibinin, Cancer treatment resistance, Folate receptor, Cancer cell targeting.
Here, we synthesized three new blended ligand complexes of chromium (III), iron (III), and lanthanum (III) ions with a Schiff base made from the condensation of [o-aminophenol and 2-hydroxyacetophenone in the presence of concentrated sulphoric acid (HL1)] as a primary ligand and o-nitroaniline (L2) as a secondary. The Schiff base and its dual ligand chelate were characterized using several spectroscopic studies, IR, 1HNMR, electronic and mass spectra, in addition to elemental analyses, molar conductivity measurements, and magnetic moments. The spectroscopic and analytical outcomes confirmed the formation of the chelates in a 1:1:1(L1: M: L2) ratio. Similarly, an octahedral structure became counseled for all chelates.
Aceclofenac (AC) is an orally active phenyl acetic acid derivative, non-steroidal anti-inflammatory drug with exceptional anti-inflammatory, analgesic and antipyretic properties. It has low aqueous solubility, leading to slow dissolution, low permeability and inadequate bioavailability. The aim of the current study was to prepare and characterize AC-NS-based gel to enhance the dissolution rate and then percutaneous permeability. NS.s were prepared using solvent/antisovent precipitation method at different drug to polymer ratios (1:1, 1:2, and 1:3) using different polymers such as poly vinyl pyrrolidone (PVP-K25), hydroxy propyl methyl cellulose (HPMC-E5) and poloxamer® (388) as stabilizer
... Show MoreThe new compounds of pyrazolines were synthesized from the reaction of different acid hydrazide with ethylacetoacetate and ethanol under reflux. These compounds were obtained from many sequence reactions. The 4-acetyl-5-methyl-2,4-dihydro-3H-pyrazol-3-one compounds synthesized from the reaction of 5-methyl-2,4-dihydro-3H-pyrazol-3-one with acetyl chloride in calcium hydroxide and 1,4-dioxane. Finaly, Schiff bases were prepared via condensation reaction of products of mono- and tri ketone derivatives[IV]a, b with phenyl hydrazines as presented in (Scheme 1, 2). The synthesized compounds were identification by using FTIR, NMR and Mass spectroscopy (of some of them).
The aim of this study was the discrimination of Salmonella isolated from chicken and their feed and drinking water for the epidemiological control of salmonellosis. Totally, 289 samples, including 217 chicken cloaca swabs, 46 water, and 26 feed samples were collected from five different farms in Karbala governorate, Iraq. Conventional bacteriology tests, API 20E, Vitek 2, and serology were used for bacterial identification. Random amplified polymorphic DNA (RAPD)-polymerase chain reaction (PCR) was applied to analyze the genetic relationships among Salmonella isolates. The isolation rate of Salmonella spp. was 21.1% (61/289). While the water samples constituted the highest rate (30.4%), a rate of
... Show MoreBased on nonlinear self- diffraction technique, the nonlinear optical properties of thin slice of matter can be obtained. Here, nonlinear characterization of nano-fluids consist of hybrid Single Wall Carbon Nanotubes and Silver Nanoparticles (SWCNTs/Ag-NPs) dispersed in acetone at volume fraction of 6x10-6, 9x10-6, 18x10-6 have been investigated experimentally. Therefore, CW DPSS laser at 473 nm focused into a quartz cuvette contains the previous nano-fluid was utilized. The number of diffraction ring patterns (N) has been counted using Charge - Coupled- Device (CCD) camera and Pc with a certain software, in order to find the maximum change of refractive index ( of fluids. Our result show that the fraction volume of 18x10-6 is more nonli
... Show MoreLiquid electrodes of domperidone maleate (DOMP) imprinted polymer were synthesis based on precipitation polymerization mechanism. The molecularly imprinted (MIP) and non-imprinted (NIP) polymers were synthesized using DOMP as a template. By methyl methacrylate (MMA) as monomer, N,Nmethylenebisacrylamide (NMAA) and ethylene glycol dimethacrylate (EGDMA) as cross-linkers and benzoyl peroxide (BP) as an initiator. The molecularly imprinted membranes were synthesis using acetophenone (APH), di-butyl sabacate (DBS), Di octylphthalate (DOPH) and triolyl phosphate (TP)as plasticizers in PVC matrix. The slopes and limit of detection of l
... Show Morefour coordinated complexes for divalent metal ions : Mn, Fe, Co, Ni, Cu and Cd have been synthesized using bidentate Schiff base ligand type (NN)formed by the condensation of o-phenylenediamine , p- methylbenzadehyde and furfural in methanol. The ligand was reacted with divalent metal chloride forming complexes of the types :[M(L)Cl2] where : MII=Mn, Fe, Ni, Cu, and Cd . These new compounds were characterized by elemental analysis, spectroscopic methods (FT-IR, U.V-Vis, 1HNMR (for ligand only and atomic absorption) , magnetic susceptibility, chloride content along with conductivity measurement. These studies revealed that the geometry for all complexes about central metal ion is tetrahedral.
In this paper, the system of the power plant has been investigated as a special type of industrial systems, which has a significant role in improving societies since the electrical energy has entered all kinds of industries, and it is considered as the artery of modern life.
The aim of this research is to construct a programming system, which could be used to identify the most important failure modes that are occur in a steam type of power plants. Also the effects and reasons of each failure mode could be analyzed through the usage of this programming system reaching to the basic events (main reasons) that causing each failure mode. The construction of this system for FMEA is dependi
... Show MoreLiquid-crystalline organic semiconductors exhibit unique properties that make them highly interesting for organic optoelectronic applications. Their optical and electrical anisotropies and the possibility to control the alignment of the liquid-crystalline semiconductor allow not only to optimize charge carrier transport, but to tune the optical property of organic thin-film devices as well. In this study, the molecular orientation in a liquid-crystalline semiconductor film is tuned by a novel blading process as well as by different annealing protocols. The altered alignment is verified by cross-polarized optical microscopy and spectroscopic ellipsometry. It is shown that a change in alignment of the