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.
Mass transfer correlations for iron rotating cylinder electrode in chloride/sulphate solution, under isothermal and
controlled heat transfer conditions, were derived. Limiting current density values for the oxygen reduction reaction from
potentiostatic experiments at different bulk temperatures and various turbulent flow rates, under isothermal and heat
transfer conditions, were used for such derivation. The corelations were analogous to that obtained by Eisenberg et all
and other workers.
Stuck pipe is a prevalent and costly issue in drilling operations, with the potential to cost the petroleum industry billions of dollars annually. To reduce the likelihood of this issue, efforts have been made to identify the causes of stuck pipes. The main mechanisms that cause stuck pipes include drill cutting of the formation, inappropriate hole-cleaning, wellbore instability, and differential sticking forces, particularly in highly deviated wellbores. The significant consequences of a stuck pipe include an increase in well costs and Non-Productive Time (NPT), and in the worst-case scenario, the loss of a wellbore section and down-hole equipment, or the need to sidetrack, plug, or abandon the well. This paper provides a comprehensive
... Show MoreThe present work aims to study the removal of dyes from wastewater by reverse osmosis process. Two dyes were used direct blue 6, and direct yellow. Experiments were performed with feed concentration (75 – 450 ppm), operation temperature (30 – 50 oC) and time (0.2 – 2.0 hr). The membrane used is thin film composite membrane (TFC). It was found that modal permeate concentration decreases with increasing feed concentration and time operating, while permeate concentration increases with increasing feed temperature. Also it was found that product rate increase with increasing temperature, but it decrease with increasing feed concentration and time. The concentration of reject solution showed an increase with increasing feed concentratio
... Show MoreMale reproductive health is intricately regulated by molecular and physiological processes, with the aryl hydrocarbon receptor (AhR) playing a crucial role. AhR is activated by various ligands and influences the onset and progression of diseases. The aim of this study was to evaluate the role of AhR on spermatogenesis in adult male rats were affected by resveratrol (RES) and CH223191, an AhR antagonist. The study include forty rats were randomly divided into four equal groups: Control group, DMSO group, RES group and AhR‾ group, the rats received respective treatments intraperitoneally twice weekly for 60 days, and various parameters related to male reproductive health were evaluated. The AhR that activation by the RES treatment w
... Show MoreThe construction industry plays a crucial role in the countries' economy, especially in the developed country. This point encourages the concerned institution to use new techniques and integrate many techniques and methods to maximize the benefits. The main objective of this research is to evaluate the use of risk management, value management, and building information modeling in the Iraqi construction industry. The evaluation process aims at two objectives. The direct objective was to evaluate the knowledge in risk management (RM), value management (VM), and building information modeling (BIM). The indirect objective was to support the participants with information related to the main items mentioned. The questionnaire
... Show MoreDue to severe scouring, many bridges failed worldwide. Therefore, the safety of the existing bridge (after contrition) mainly depends on the continuous monitoring of local scour at the substructure. However, the bridge's safety before construction mainly depends on the consideration of local scour estimation at the bridge substructure. Estimating the local scour at the bridge piers is usually done using the available formulae. Almost all the formulae used in estimating local scour at the bridge piers were derived from laboratory data. It is essential to test the performance of proposed local scour formulae using field data. In this study, the performance of selected bridge scours estimation formulae was validated and sta
... Show MoreParticulate matter (PM) emitted from diesel engine exhaust have been measured in terms of mass, using
99.98 % pure ethanol blended directly, without additives, with conventional diesel fuel (gas – oil),to
get 10 % , 15 %, 20 % ethanol emulsions . The resulting PM collected has been compared with those
from straight diesel. The engine used is a stationary single cylinder, variable compression ratio Ricardo
E6/US. This engine is fully instrumented and could run as a compression or spark ignition.
Observations showed that particulate matter (PM) emissions decrease with increasing oxygenate
content in the fuel, with some increase of fuel consumption, which is due to the lower heating value of
ethanol. The reduction in
The necessary optimality conditions with Lagrange multipliers are studied and derived for a new class that includes the system of Caputo–Katugampola fractional derivatives to the optimal control problems with considering the end time free. The formula for the integral by parts has been proven for the left Caputo–Katugampola fractional derivative that contributes to the finding and deriving the necessary optimality conditions. Also, three special cases are obtained, including the study of the necessary optimality conditions when both the final time and the final state are fixed. According to convexity assumptions prove that necessary optimality conditions are sufficient optimality conditions.
... Show MoreAerial manipulation of objects has a number of advantages as it is not limited by the morphology of the terrain. One of the main problems of the aerial payload process is the lack of real-time prediction of the interaction between the gripper of the aerial robot and the payload. This paper introduces a digital twin (DT) approach based on impedance control of the aerial payload transmission process. The impedance control technique is implemented to develop the target impedance based on emerging the mass of the payload and the model of the gripper fingers. Tracking the position of the interactional point between the fingers of gripper and payload, inside the impedance control, is achieved using model predictive control (MPD) approach.
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