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.
New mixed ligand complexes of some metal ions Zn(II), Cd(II) and Hg(II) were prepared by reacting with mixture of two bidentate ligands [ HL = (P-methyl anilino) –P– chloro phenyl acetonitrile and en = ethylene diamine] in a molar ratio of 1:1:1[ M : HL : en] in ethanol . The ligand HL was previously prepared by Strecker’s procedure which includes the reaction of p- toluidine with P- chlorobenzaldehyde in the presence of KCN in acidic medium. The structures of new compounds were identified by elemental analyses, atomic absorption and thermal analyses TG/DTG in addition to FTIR and U.V-VIS. Spectra. The electrical conductivity measurements of metal complexes were also determined. From the obtained data the octahedral structure was s
... Show More
his project try to explain the using ability of spatial techniques for land cover change detection on regional level with the time parameter and did select for explain these abilities study case (Hewaizah marsh ) . this area apply to many big changes with the time. These changes made action on characters and behaviors of this area as well as all activities in it . This Project concerting to recognize the Using importance of remote sensing and GIS Methodology in data collecting for the changes of land use and the methodology for the analyses and getting the results for the next using as a base data for development and drawing the plans as well as in regional planning .This project focus on practical
... Show MoreResults showed that the optimum conditions for production of inulunase from isolate Kluyveromyces marxianus AY2 by submerged culture could be achieved by using inulin as carbon source at a concentration of 2% with mixture of yeast extract and ammonium sulphate in a ratio of 1:1 in a concentration of 1% at initial pH 5.5 after incubation for 42 hours at 30ºC.
In this paper, an analytical solution describing the deflection of a cracked beam repaired with piezoelectric patch is introduced. The solution is derived using perturbation method. A novel analytical model to calculate the proper dimensions of piezoelectric patches used to repair cracked beams is also introduced. This model shows that the thickness of the piezoelectric patch depends mainly on the thickness of the cracked beam, the electro-mechanical properties of the patch material, the applied load and the crack location. Furthermore, the model shows that the length of the piezoelectric patches depends on the thickness of the patch as well as it depends on the length of the cracked beam and the crack depth. The additional flexibil
... Show MoreThe industrial development and raise the level of income that has emerged clearly in the middle of the last century in many rich and medium rich countries has great influence on the risen of the health care level. Which led to a significant increase in the reconstruction of people over 65 years and this in turn has produced markets for products and services through modifications to the existing products to meet their physical needs. The importance of research also has the universal design of a comprehensive actually so that it covers as much as possible from human physical & cultural activities. The importance of research locally is to concentrate on this subject who has not been taken into consideration so far to accommodate the eld
... Show MoreThe magazine is one of the print media , which represents an important gateway to the wider world , due for its intellectual and cultural fun for the recipient affecting the everyday needs him in various directions . The cover of the magazine is the owner of appearance and impact of the first look the magazine , including the magnitude of the value of the functional and aesthetic pay the reader to the acquisition, as it seeks designed to attract the receiver and achieve better grades optical communication enabled this diversity vocabulary construction for the cover of the magazine and consistent with the idea of design .Ensure Current search four chapters , first chapter of which , the research problem and was questioning following what
... Show MoreIn this paper, an analytical solution describing the deflection of a cracked beam repaired with piezoelectric patch is introduced. The solution is derived using perturbation method. A novel analytical model to calculate the proper dimensions of piezoelectric patches used to repair cracked beams is also introduced. This model shows that the thickness of the piezoelectric patch depends mainly on the thickness of the cracked beam, the electro-mechanical properties of the patch material, the applied load and the crack location. Furthermore, the model shows that the length of the piezoelectric patches depends on the thickness of the patch as well as it depends on the length of the cracked beam and the crack depth. The additio
... Show MoreIn the postmodern era, the graphic design styles showed a new visualization method when the graphic designers had changed the traditional conditions by using design elements with new technics for photos, collage and comics illustration. The researcher assumes that the graphic design styles were affected by the art's movement at that period throw the same perspective of view for the concept presented in the art pieces and their entire message. Therefore, the researcher chooses field was the period of 1945-1970 in the USA for the (pop-art and conceptual-art) and explored the main visual effects that expressed the visual dialogue and compared them with the most common design styles ant the same period and location, the results of selected e
... Show MoreThe current research dealt with contrastive structures and the culture of reception in the design of interior spaces as embodying a rhetorical aspect that reveals formal values related to the meanings of beauty through the mechanisms of symbolism and interpretation that drives mental behavior and is in harmony with intellectual data and its performance function.
Hence, the research in the first chapter dealt with the research problem, the need for it, and the extent of the necessity that calls for studying contrastive structures in interior design and architecture, and touching and searching for what is the paradox and its representations for the recipient, in which the interior designer plays an active role in presenting the best cre
In this paper a new structure for the AVR of the power system exciter is proposed and designed using digital-based LQR. With two weighting matrices R and Q, this method produces an optimal regulator that is used to generate the feedback control law. These matrices are called state and control weighting matrices and are used to balance between the relative importance of the input and the states in the cost function that is being optimized. A sample power system composed of single machine connected to an infinite- bus bar (SMIB) with both a conventional and a proposed Digital AVR (DAVR) is simulated. Evaluation results show that the DAVR damps well the oscillations of the terminal voltage and presents a faster respo
... Show More