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.
Sildenafil, tadalafil, and vardenafil are phosphodiesterase type 5 enzyme (PDE-5) inhibitors used for the treatment of male erectile dysfunction. This present study aims to investigate 55 herbal products indicated for men’s sexual health from the Malaysian market for adulteration of PDE-5 inhibitors and analogues. The screening and identification of 20 PDE-5 inhibitors and analogues in herbal products of various forms (powder, capsules, tablets, and pastels) were conducted using gas chromatography–electron impact-mass spectrometer (GC-EI-MS). The analysis has shown that 19 herbal products were adulterated with PDE-5 inhibitors and analogues. Unique ion fragmentations and the presence of molecular
... Show MoreNumerous integral and local electron density’s topological parameters of significant metal-metal and metal-ligand bonding interactions in a trinuclear tetrahydrido cluster [(Cp* Ir) (Cp Ru)2 (μ3-H) (μ-H)3]1 (Cp = η5 -C5Me5), (Cp* = η5 -C5Me4Et) were calculated and interpreted by using the quantum theory of atoms in molecules (QTAIM). The properties of bond critical points such as the delocalization indices δ (A, B), the electron density ρ(r), the local kinetic energy density G(r), the Laplacian of the electron density ∇2ρ(r), the local energy density
... Show MoreThe research aims to achieve proof of convergence between optimal costs and standard costs in calculating costs for the economic unit, support efforts aimed at adopting optimal costs in cost accounts and accounting thought in general, and achieve benefit from the theory of convergence between optimal costs and standard costs in the field of achieving actual costs in The economic unit in order to reduce and converge, and this came to address the possibility of adopting the concept of optimal costs in the production costs calculations for the purposes of rationalizing administrative decisions, and rationalizing the preparation of financial statements within management accounting.
The research concluded that
... Show MoreAugmented reality technology is a modern technique used in all fields, including: medicine, engineering and education, and has received attention from officials in the educational process at present; The focus of this research is on the degree of use of augmented reality among field experience students in the project's optimal investment program for teaching staff and their difficulties, applied to a sample of 75 students, through a questionnaire prepared by the researcher as a tool to determine the degree of use, as well as difficulties. The researcher addressed the subject through two main axes to determine the degree of use, as well as the difficulties preventing teachers and learners from using this technique. The results of the rese
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The logistic regression model is one of the nonlinear models that aims at obtaining highly efficient capabilities, It also the researcher an idea of the effect of the explanatory variable on the binary response variable. &nb
... Show MoreThe concept of deficit in public budget becomes a chronic economic phenomenon in most of the world, whether the advanced countries or developing countries. Despite the difference in the visions of the economic schools to accept or reject the deficit in public budget but the opinion that prevailed is the necessity of the state to reduce the public spending which led to a continuous deficits in the public budget which consequently increased the government borrowing ,increase income taxes and wealth, consequently this weakened the in motivation in private investment which contributed to the increase of in factionary stagnation , so that governments have to cover the lack of local funding sources which become difficult to be eq
... Show MoreRecords of two regionalized variables were processed for each of porosity and permeability of reservoir rocks in Zubair Formation (Zb-109) south Iraq as an indication of the most important reservoir property which is the homogeneity,considering their important results in criterion most needed for primary and enhanced oil reservoirs.The results of dispersion treatment,the statistical incorporeal indications,boxes plots,rhombus style and tangents angles of intersected circles indicated by confidence interval of porosity and permeability data, have shown that the reservoir rocks of Zubair units (LS),(1L) and (DJ) have reservoir properties of high quality,in contrast to that of Zubair units (MS) and (AB)which have reservoir properties of less q
... Show MoreAn experiment in the semester, the second semester of the academic year (2022-2023), and the data used was not processed (the second test for two independent, inaccurate samples, the Bermon correlation coefficient, and the Spearman correlation coefficient), and the following results were reached: There is a statistically significant difference at the level of ( 0) average, 05) between the third grade who studied the plan for asking cluster questions, and between the average of those who studied the special feature according to the traditional method of selecting achievement, and enjoyed completing the specialization, choosing the experimental group, because the strategy of asking cluster questions is one of the externalities that... Lear
... Show MoreThe research aims to clarify the role that psychological ownership, through its dimensions, plays in deterring the effects of toxic leadership, through its dimensions, in the Ministry of Industry and Minerals. The research started with a basic problem represented by the following question: "Using psychological ownership and its application in deterring the negative effects of toxic leadership." The research used the descriptive-analytical method. The sample was randomly selected from workers in some selected companies affiliated with the Ministry of Industry and Minerals in Baghdad, and the sample size reached 124 individuals. One of the most important results is that there is an effect of the psychological ownership variable, based on the
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