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.
This paper deals with a Twin Rotor Aerodynamic System (TRAS). It is a Multi-Input Multi-Output (MIMO) system with high crosscoupling between its two channels. It proposes a hybrid design procedure that combines frequency response and root locus approaches. The proposed controller is designated as PID-Lead Compensator (PIDLC); the PID controller was designed in previous work using frequency response design specifications, while the lead compensator is proposed in this paper and is designed using the root locus method. A general explicit formula for angle computations in any of the four quadrants is also given. The lead compensator is designed by shifting the dominant closed-loop poles slightly to the left in the s-plane. This has the effect
... Show MoreComputer theoretical study has been carried out on the design of five electrode immersion electrostatic lens used in electron gun application. The finite element method (FEM) is used in the solution of the Poisson's equation fro determine axial potential distribution, the electron trajectory under Zero magnification condition . The optical properties : focal length ,spherical and chromatic aberrations are calculated,From studying the properties of the designed electron gun. we have good futures for these electron gun where are abeam current 4*10-4A can be supplied by using cathode tip of radius 100 nm.
This paper proposes improving the structure of the neural controller based on the identification model for nonlinear systems. The goal of this work is to employ the structure of the Modified Elman Neural Network (MENN) model into the NARMA-L2 structure instead of Multi-Layer Perceptron (MLP) model in order to construct a new hybrid neural structure that can be used as an identifier model and a nonlinear controller for the SISO linear or nonlinear systems. Two learning algorithms are used to adjust the parameters weight of the hybrid neural structure with its serial-parallel configuration; the first one is supervised learning algorithm based Back Propagation Algorithm (BPA) and the second one is an intelligent algorithm n
... Show MoreThe syntheses, characterizations and structures of three novel dichloro(bis{2-[1-(4-methoxyphenyl)-1H-1,2,3-triazol-4-yl-κN3]pyridine-κN})metal(II), [M(L)2Cl2], complexes (metal = Mn, Co and Ni) are presented. In the solid state the molecules are arranged in infinite hydrogen-bonded 3D supramolecular structures, further stabilized by weak intermolecular π…π interactions. The DFT results for all the different spin states and isomers of dichloro(bis{2-[1-phenyl-1H-1,2,3-triazol-4-yl-κN3]pyridine-κN})metal(II) complexes, [M(L1)2Cl2], support experimental measurements, namely that (i) d5 [Mn(L1)2Cl2] is high spin with S = 5/2; (ii) d7 [Co(L1)2Cl2] has a spin state of S = 3/2, (iii) d8 [Ni(L1)2Cl2] has a spin state of S =
... Show MoreRheumatoid arthritis (RA) is a common inflammatory disease that associated with increased morbidity and mortality due to accelerated atherosclerosis. Rosuvastatin is a unique hydroxy methyl glutaryl Co A (HMGCoA) reductase inhibitor that has anti inflammatory effects.
The aim of this study was to evaluate the effect of rosuvastatin as adjuvant therapy to methotrexate (MTX) on lipid profile and its possible cardioprotective effect in RA patients. A double blinded placebo controlled clinical trial with 8 weeks follow up periods at which 40 patients with active RA using MTX were randomized into 2 groups to receive either rosuvastatin 10mg or placebo as adjuvant therapy to MTX. In addition to twenty healthy subjects as control group.
... Show MoreThe preparation of the phenanthridine derivative compound was achieved by adopting an efficient one-pot synthetic approach. The condensation of an ethanolic mixture of benzaldehyde, cyclohexanone and ammonium acetate in a 2:1:1 mole ratio resulted in the formation of the title compound. Analytical and spectroscopic techniques were used to confirm the nature of the new compound. A mechanism for the formation of the phenanthridine moiety that is based on three steps has been suggested
SnS has been widely used in photoelectric devices due to its special band gap of 1.2-1.5 eV. Here, we reported on the fabrication of SnS nanosheets and the effect of synthesis condition together with heat treatment on its physical properties. The obtained band gap of the SnS nanosheets is in the rage of 1.37-1.41 eV. It was found that the photo-current density of a thin film comprised of SnS nanosheets could be enhanced significantly by annealing treatment. The maximum photo-current density of the stack structure of FTO/SnS/CdS/Pt was high as 389.5 mu A cm(-2), rendering its potential application in high efficiency solar hydrogen production.
Standards play a vital role in documenting the values of new test results in the form of tables. They are one of the basic requirements that the standardization process aims for as a complement to standardizing test procedures, and contribute to knowing the current reality of the student. The degree of readiness and level as a result of practicing different exercises for sports activities, in addition to the possibility of adopting it for comparison with his group or similar groups, classification, prediction and selection. Developing the skill of handling the football in the educational field is an important matter for achieving distinguished performance among students. This skill requires a level of accuracy, speed and control, and
... Show More