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.
In this work, nanostructure zinc sulfide (ZnS) thin films at temperature of substrate 450 oC and thickness (120) nm have been produced by chemical spray pyrolysis method. The X-Ray Diffraction (XRD) measurements of the film showed that they have a polycrystalline structure and possessed a hexagonal phase with strong crystalline orientation of (103). The grain size was measured using scanning electron microscope (SEM) which was approximately equal to 80 nm. The linear optical measurements showed that ZnS nanostructure has direct energy gap. Nonlinear optical properties experiments were performed using Q-switched 532 nm Nd:YAG laser Z-scan system. The nonlinear refractive index (n2) and nonlinear absorption coefficient (β) estimated for Z
... Show MoreMefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-t
... Show MoreThe Catharanthus roseus plant was extracted and converted to nanoparticles in this work. The Soxhlet method extracted alkaloid compounds from the plant Catharanthus roseus and converted them to the nanoscale. Chitosan polymer was used as a linking material and converted to Chitosan nanoparticles using Sodium TriPolyPhosphate (STPP). The extracted alkaloids were linked with Chitosan nanoparticles CSNPs by maleic anhydride to get the final product (CSNPs- Linker- alkaloids). The synthesized (CSNPs- Linker- alkaloids) was characterized using SEM spectroscopy UV–Vis., Zeta Potential, and HPLC High-Performance Liquid Chromatography. Scanning electron microscope (SEM) analysis shows that the Chitosan nanoparticles (CSNPs) have small dim
... Show MoreThe Schiff base (E)-2-(((2-(1H-benzo[d]imidazol-2-yl) phenyl) imino) methyl)-4-methylphenol (Lb) ligand with some metals(II) ion such as; Co, Cu, Cd, and Hg, were synthesis and characterized by the mass and 1 HNMR spectrometry for ligand Schiff base, the fourier-transform infrared spectroscop (FTIR), UV- visible and the flame atomic absorption (AA) spectrum, the CHN analysis, and the chlorine content, in addition to measuring the magnetic sensitivity of the complexes. All the complexes had octahedral geometry. The bioactivity activity for compounds against; Rhizopodium, Staphylococcus aureus, and Escherichia coli showed different efficacy towards these microorganisms
Transition metal complexes of Co(II), Ni(II), Cu(II), and Zn(II) with 2-(4-antipyrine azo)-4-nitroaniline derived from 4-aminoantipyrine and 4-nitroaniline were synthesized. Characterization of these compounds has been done on the basis of elemental analysis, electronic data, FT-IR, UV-Vis and 1HNMR, as well as magnetic susceptibility and conductivity measurements. The nature of the complexes formed were studied following the mole ratio and continuous variation methods, Beer's law obeyed over a concentration range (1×10-4 - 3×10-4 M). High molar absorbtivity of the complex solutions were observed. From the analytical data, the stoichiometry of the complexes has been found to be 1:2 (metal:ligand). On the basis of physicochemical data octa
... Show MoreThe new of compounds synthesized by sequence reactions starting from a reaction of 3-phenylenediamine or 4-phenylenediamine with chloroacetyl chloride to produce the compounds [I]a,b, then the compounds[I]a,b reacted with sodium azide to yield compounds[II]a,b that reacted 1,3-dipolarcycloaddition reaction with acrylic acid to give compounds [III]a,b these compounds reacted with methanol led to ester compounds[IV]a,b then reacted with hydrazine to give acid hydrazide [V]a,b . Finally compounds [V]a,b reacted with aromatic aldehydes to product shiff bases derivatives. The compounds characterized by mp. , IR, 1HNMR in addition to mass spectroscopy for some of them the liquid crystals properties were studied by using polarized optical microsco
... Show MoreThis article will address autoclave design considerations and
manufacturing working with high pressure low temperature
supercritical drying technique to produce silica aerogel. The design
elects carbon dioxide as a supercritical fluid (31.7 oC and 72.3 bar).
Both temperature and pressure have independently controlling
facility through present design. The autoclave was light weight (4.5
kg) and factory-made from stainless steel. It contains a high pressure
window for monitoring both transfer carbon dioxide gas to liquid
carbon dioxide and watching supercritical drying via aerogel
preparation process. In this work aerogel samples were prepared and
the true apparent densities, total pore volume and pore size
The Environmental Data Acquisition Telemetry System is a versatile, flexible and economical means to accumulate data from multiple sensors at remote locations over an extended period of time; the data is normally transferred to the final destination and saved for further analysis.
This paper introduces the design and implementation of a simplified, economical and practical telemetry system to collect and transfer the environmental parameters (humidity, temperature, pressure etc.) from a remote location (Rural Area) to the processing and displaying unit.
To get a flexible and practical system, three data transfer methods (three systems) were proposed (including the design and implementation) for rural area services, the fi
... Show MoreSCADA is the technology that allows the operator to gather data from one or more various facilities and to send control instructions to those facilities. This paper represents an adaptable and low cost SCADA system for a particular sugar manufacturing process, by using Programmable Logic Controls (Siemens s7-1200, 1214Dc/ Dc/ Rly). The system will control and monitor the laboratory production line chose from sugar industry. The project comprises of two sections the first one is the hardware section that has been designed, and built using components suitable for making it for laboratory purposes, and the second section was the software as the PLC programming, designing the HMI, creating alarms and trending system. The system will ha
... Show MoreAbstract
This paper presents mechanical and electrical design, and implementation process of industrial robot, 3-DoF type SCARA (selective compliment assembly robot arm),with two rotations and one translation used for welding applications.The design process also included the controller design which was based on PLC(programmable logic controller) as well as selection of mechanical and electrical components.The challenge was to use the available components in Iraq with reasonable costs. The robot mentioned is fully automated using programmable logic controller PLC(Zelio type SR3-B261BD),with 16inputs and 10 outputs. The PLC was implemented in FBD logic to obtain three different automatic motions with hi
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