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.
Piperine, a crystalline alkaloid compound isolated from Piper nigrum, piper longum, and other types of piper, has had many fabulous pharmacological advantages for preventing and treating some specific diseases, such as analgesic, anti-inflammatory, hepatoprotective, antimetastatic, antithyroid, immunomodulatory, antitumor, rheumatoid arthritis, osteoarthritis, Alzheimer's, and improving the bioavailability of other drugs. However, its potential for clinical use through oral usage is hindered by water solubility and poor bioavailability. The low level of oral bioavailability is caused by low solubility in water and is photosensitive, susceptible to isomerization by UV light, which causes piperine concentration to decrease. Many different
... Show MoreAssimilation is defined ,by many phoneticians like Schane ,Roach ,and many others, as a phonological process when there is a change of one sound into another because of neighboring sounds.This study investigates the phoneme assimilation as a phonological process in English and Arabic and it is concerned specifically with the differences and similarities in both languages. Actually ,this study reflects the different terms which are used in Arabic to refer to this phenomenon and in this way it shows whether the term 'assimilation ' can have the same meaning of 'idgham' in Arabic or not . Besides, in Arabic , this phenomenon is discussed from&nb
... Show MoreObjectives: The purpose of the study is to ascertain the relationship between the training program and the socio-demographic features of patients with peptic ulcers in order to assess the efficiency of the program on patients' nutritional habits.
Methodology: Between January 17 and October 30 of 2022, The Center of Gastrointestinal Medicine and Surgery at Al-Diwanyiah Teaching Hospital conducted "a quasi-experimental study". A non-probability sample of 30 patients for the case group and 30 patients for the control group was selected based on the study's criteria. The study instrument was divided into 4 sections: the first portion contained 7 questions about demographic information, the second sect
... Show MoreThe aerodynamic characteristics of the forward swept wing aircraft have been studied theoretically and an experimentally investigation for the wake field generated by this configuration have been carried out. Low order panel method with the Dirichlet boundary condition have been used to solve the case of the steady, inviscid and compressible flow. Two different panel method techniques have been employed: the source-doublet and the doublet method. The thickness for the various components was considered in the study. Prandtl-Glauert similarity rule has been used to account for the compressibility effects. Experimentally, a model was manufactured from wood with body length (290mm) and main wing span was (204mm). The primary objective of th
... Show MoreThe interactions of drug amoxicillin with maltose or galactose solutions with a variation of temperature have been discussed by taking in the volumetric and viscometric procedures. Physical properties [densities (ρ) and viscosities (η)] of amoxicillin (AMOX) aqueous solutions and aqueous solutions of two type saccharides (maltose and galactose 0.05m) have been measured at T = (298.15, 303.15 and 308.15) K under atmospheric pressure. The apparent molar volume (ϕv cm3mole-1) has been evaluated from density data and fitted to a Redlich-Mayer equation. The empirical parameters of the Mayer-Redlich equation and apparent molar volume at infinite dilution ذv were explicated in terms of interactions from type solute-solvent and solute
... Show MoreSurfaces quality is one of the most specified customer requirements for machine parts. The major indication of surfaces quality on machined parts is surface roughness. The research aim is to study the cutting conditions and their effects on the surface roughness. This paper utilizes regression models to predict surface roughness over the machining time for variety of cutting conditions in turning. In the experimental part for turning, different types of materials (Aluminum alloy, Copper alloy, and Gray cast iron) were considered with different cutting speed ( ) and feed rate ( ). A mathematical Model depending on statistical-mathematical method between surface roughness (Rz ) and cutting condition ( , ) were derived, for the three materials
... Show MoreThe interest in art for young ages is seen as an obvious breakthrough and as revealing of psychological and health feelings in addition to emotions, and it is a treatment for those who suffer from behavioral disorders. The problem arose with the following question: What is the role of artistic expression in diagnosing behavioral disorders for primary school pupils? The aim of the research is to detect the behavioral disorders in the artistic expression of the female students' paintings from the teachers' point of view. The descriptive analytical approach was adopted as it is the appropriate method for identifying and estimating the characteristics and features related to people, places and things, and analyzing situations or phenomena as a
... Show MoreThis research deals with the most important indicators used to measure the phenomenon of financial depth, beyond the traditional indicators, which are called quantitative indicators, which is shown to be inadequate to show the facts accurately, but it may come in the results of a counterfactual, although reliable in econometric studies done in this regard.
Therefore, this research has sought to put forward alternative indicators, is the structural indicators, and financial prices, and availability of financial instruments, and cost of transactions concluded, in order to measure the phenomenon of financial depth.
After using and analyzing data collected from countries the research
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