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.
This research was aimed to the purification and characterization of cytosine deaminase as a medically important enzyme from locally isolated Escherichia coli; then studying its cytotoxic anticancer effects against colon cancer cell line. Cytosine deaminase was subjected to three purification steps including precipitation with 90% ammonium sulfate saturation, ion exchange chromatography on DEAE-cellulose column, and gel filtration chromatography throughout Sephadex G-200 column. Specific activity of the purified enzyme was increased up to 9 U/mg with 12.85 folds of purification and 30.85% enzyme recovery. Characterization study of purified enzyme revealed that the molecular weight of cytosine deaminase produced by E. coli was about 48 KDa,
... Show MoreThis study includes using green or biosynthesis-friendly technology, which is effective in terms of low cost and low time and energy to prepare V2O5NPs nanoparticles from vanadium sulfate VSO4.H2O using aqueous extract of Punica Granatum at a concentration of 0.1M and with a basic medium PH= 8-12. The V2O5NPs nanoparticles were diagnosed using several techniques, such as FT-IR, UV-visible with energy gap Eg = 3.734eV, and the X-Ray diffraction XRD was calculated using the Debye Scherrer equation. It was discovered to be 34.39nm, Scanning Electron Microscope (SEM), Transmission Electron Microscopy TEM. The size, structure, and composition of synthetic V2O5NPs were determined using the (EDX) pattern, Atomic force microscopy AFM. The a
... Show MoreBromocriptine mesylate is a semisynthetic ergot alkaloid derivative with potent dopaminergic activity, used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes ,the oral bioavailability is approximately 6%, therefore aim its prepare and evaluate bromocriptine mesylate as liquid self nano emulsifying drug delivery system to enhance its solubility , dissolution and stability . Solubility study was made in different vehicles to select the best excipients for dissolving bromocriptine mesylate. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1 ratios of surfactant and co-surfactant, four formulations were pre
... Show MoreOf the importance of the concept of ownership of real estate as the basic basis from which various projects are launched in various economic, tourism, and urban areas .... The need to research the diagnosis of real estate reality went astray in the difficulties, which played a decisive role in the process of urban development.
This leads us to the research problem of the difficulty of implementing urban development plans in many cases due to the absence of a clear methodology for organizing and modernizing the ownership of real estate and its coordination with the management of urban land and to achieve the objective
... Show MoreA tunable band pass filter based on fiber Bragg grating sensor using an in-fiber Mach-Zender interferometer with dual micro-cavities is presented. The micro-cavity was formed by splicing together a conventional single-mode fiber and a solid core photonic crystal fiber (SCPCF) with simple arc discharge technique. Different parameters such as arc power, length of the SCPCF and the overlap gap between samples were considered to control the fabrication process. The ellipsoidal air-cavity between the two fibers forms Fabry-Perot cavity. The diffraction loss was very low due to short cavity length. Ellipsoidal shape micro-cavities were experimentally achieved parallel to the propagation axis having dimensions of (24.92 – 62.32) μm of width
... Show MoreDigital commercial advertising depends on artistic formations to achieve attraction and arousal of attention, which is one of the most important communication factors that the designer seeks to achieve and is considered a key key to recognizing the beauty of the topic and its functional value. Reframe formal vocabulary.
The research included the introduction and includes the research problem and the need for it, which focused on the following question: What is the aesthetic role of artistic formation in the design of commercial advertising?
The aim of the research was: To reveal the aesthetic role of artistic formation in commercial advertising.
It also included the importance of research and research boundaries, as well as def
The change in the size of the droplets during the pesticide application process could have a negative impact on the percentage of drift or the losses of pesticides to the environment. One of the factors that could affect the droplet size produced from a single nozzle is the internal design of the nozzle itself, in addition to the wear of the nozzle orifice as a result of the usage time. In this research, three types of nozzles with different internal designs were used (Turbo TeeJet (TT), Turbo TwinJet (TTj 6011003), and Drift Guard (DG 11003)). The nozzles were subjected to an accelerated wear test for one hundred hours, and different droplet size parameters (Dv 0.1, Dv 0.5, Dv 0.9),
The concept of social graphic design is one of the most critical areas that highlight the designer's knowledge of social responsibility by employing design skills in community awareness. This study focused on defining social graphic design, the meaning, practices, and strategies for designing awareness posters. This study reviewed two examples of awareness posters that reflect the Saudi designer's practices. The results summarized that social graphic design is a concept not taught directly but gained from permanent practice in designing awareness posters that interact with community issues. The designer's understanding of his social events and their sensing in the visual form of a poster reflects the designer's social awareness. Social g
... Show More<span lang="EN-US">The need for robotics systems has become an urgent necessity in various fields, especially in video surveillance and live broadcasting systems. The main goal of this work is to design and implement a rover robotic monitoring system based on raspberry pi 4 model B to control this overall system and display a live video by using a webcam (USB camera) as well as using you only look once algorithm-version five (YOLOv5) to detect, recognize and display objects in real-time. This deep learning algorithm is highly accurate and fast and is implemented by Python, OpenCV, PyTorch codes and the Context Object Detection Task (COCO) 2020 dataset. This robot can move in all directions and in different places especially in
... Show MoreThe research aims to design a narrow-band frequency drive amplifier (1.5GHz -1.6GHz), which is used to boost the transmitter amplifier's input signal or amplify the GPS, GlONASS signals at the L1 band.
The Power Amplifier printed circuit board (PCB) prototype was designed using InGaP HBT homogeneous technology transistor and GaAs Heterojunction Bipolar Transistor (HBT) transistor. Two models have been compared; one of the models gave 16dB gain, and the other gave 23dB when using an input power signal (-15dBm). The PCB consumes 2.4W of power and has a physical dimension of 11 x 4 cm.