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.
سرطان البنكرياس هو مرض ذو معدل وفيات مرتفع، ولا يزال التشخيص المبكر لسرطان البنكرياس يمثل تحديًا. يظل معدل البقاء النسبي لمدة 5 سنوات أقل من 8%، والاستراتيجيات العلاجية غير فعالة في زيادة معدلات بقاء المريض على قيد الحياة. في خلايا سرطان البنكرياس، ارتبطت مقاومة العلاج بالتغيرات الجينية التي تؤدي إلى ظهور مسارات خلوية شاذة؛ ولذلك، هناك ما يبرر ايجاد استراتيجيات جديدة لعلاج هذا المرض. هنا، سعينا لاستكشاف
... Show MoreATTAPULGITE clay was modified in this study by the graphene oxide sheets and the clay was diagnosed before and after modification using several techniques (Fourier-transform infrared spectroscopy FT-IR, X-ray powder diffraction XRD, Scanning electron microscope SEM , energy dispersive spectroscopy EDX ) ,The surface of the attapulgite clay (before (Ata) after modification by graphene oxide (Ata-GO) ) was applied to adsorption of the Alizarin dye from its water solutions through the application of several kinetic models (pseudo first-order model , pseudo second -order model , intraparticle diffusion model ),It was found that the practical results follow pseudo second -order model. The process of modification on the surface of the mud has imp
... Show MoreThe topic of context is one of the important topics, which was mentioned as a concept in several fields and different fields, and there were many points of view that defined that concept.
He specified the title of the research (design contexts in the design of the interior space), as the research sought to identify the concept of context in the interior design of the spaces of sewing workshops. The research was divided into four chapters:
The first chapter, which consists of the methodological framework, the problem of research and the need for it, the importance of research, the goal and limits of research for sewing workshops for vocational schools from (2020-2021).
The second chapter: consists of previous studies and the theo
synthesis and characterization of New Bidentate schiff base Ligand Type(NO)Donor Atoms Derived from isatin and 3-Amino benzoic acid and Its complexes with Co(||),Cu(||),Cd(||)and Hg(||)Ions
Nanomaterials, including nanoparticles such as iron oxide nanoparticles, have received great attention from researchers due to their unique properties and applications. There are several diverse methods, including chemical, physical, and green biological methods, to prepare iron oxide nanoparticles. The green method was chosen because it is safer, purer, and less toxic compared to other methods. Therefore, the green method is a promising and environmentally friendly method in the near future. The aqueous extract of Iraqi orange leaves was used to prepare nano iron oxide, it was examined structurally and spectrally by several techniques (X-ray diffraction- XRD, Fourier transform infrared - FT-IR, field emission scanning electron micr
... Show MoreAbstract
The goal of current research to describe and diagnose the level of attention of doctors to design and regulatory dimensions, (strategic vision, organizational structure, organizational processes, business systems, personnel), and the performance of hospitals and dimensions, in six hospitals in medicine and selected a sample for research, as well as identify organizational design effect in the performance of hospitals and dimensions (efficiency, the development of human resources, patient satisfaction, achieve financial results, quality of health care).
Research has focused in part theoretical on key variables to look organizational des
... Show MoreBackground: Frovatriptan succinate (FVT) is an effective medication used to treat migraines; however, available oral formulations suffer from low permeability; accordingly, several formulations of FVT were prepared. Objective: Prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosome gel. Methods: Binary ethosomes were prepared using different concentrations of phospholipid PLH90, ethanol, propylene glycol, and cholesterol by thin film hydration and characterized by particle size, zeta potential, and entrapment efficiency. Furthermore, in-vitro, in-vivo, ex-vivo, pharmacokinetics, and histopathological studies were done. Results: Regarding FVT-loaded BE, formula (F9) demonstrated the best paramet
... Show MoreThe research includes the synthesis and identification of the mixed ligands complexes of M(II) Ions in general composition [M(Lyn)2(phen)] Where L- lysine (C6H14N2O2) commonly abbreviated (LynH) as a primary ligand and 1,10-phenanthroline(C12H8N2) commonly abbreviated as "phen," as a secondary ligand . The ligands and the metal chlorides were brought in to reaction at room temperature in ethanol as solvent. The reaction required the following molar ratio [(1:1:2) (metal): phen:2 Lyn -] with M(II) ions, were M = Mn(II),Cu(II), Ni(II), Co(II), Fe(II) and Cd(II). Our research also includes studying the bio–activity of the some complexes prepared against pathogenic bacteria Escherichia coli(-),Staphylococcus(-) , Pseudomonas (-), Bacillus (-)
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