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 paper, turbidimetric and reversed-phase ultra-fast liquid chromatography (UFLC) methods were described for the quantitative determination of ephedrine hydrochloride in pharmaceutical injections form. The first method is based on measuring the turbidimetric values for the formed yellowish white precipitate in suspension status in order to determine the ephedrine hydrochloride concentration. The suspended substance is formed as a result of the reaction of ephedrine hydrochloride with phosphomolybdic acid which was used as a reagent. The physical and chemical characteristics of the complex were investigated. The calibration graphs of ephedrine were established by turbidity method. While the second method (UFLC) was conducted using the
... Show MoreGypseous soils are considered one of the most problematic soils. The skirted foundation is an alternative technology that works to improve the bearing capacity and reduce settlement. This paper investigates the use of square skirted foundations resting on gypseous soil subjected to concentric and eccentric vertical load with eccentricity values of 4, 8, and 17 mm in 16 experimental model tests. To obtain the results by using this type of foundation, a small-scale physical model was designed to obtain the load–settlement behavior of the square skirted foundation; the dimension of the square footing is 100 mm × 100 mm with 1 mm thickness, the skirt depth (
This experiment presented essential oils by GC/MS, pigment content, and their antioxidant activities as well as sensory evaluation of delight samples. Limonene (66.88%) was the most prevalent yield. The peels of clementine had DPPH and ABT Scavenging activity. All levels of pigment extract had better scores for all sensory values and recorded acceptable scores in terms of appearance, color, aroma, and overall acceptability compared to control delight. Besides, delight samples containing 15 mg astaxanthin pigment extract showed maximum sensory scores compared to other samples and control delight. On the other hand, the product was less acceptable to the panelists compared to control in the case of the addition of 3.75 mg astaxanthin pigme
... Show MoreRecently, there has been an increase in the prevalence of ulcerative colitis (UC), and inflammatory bowel diseases (IBD) worldwide, especially in certain recently industrialized countries like China and In¬dia. Globally, the prevalence of UC, a chronic illness that affects the large intestine, is rising. Fifty adherent invasive Escherichia coli (AIEC) isolates were identified from ulcerative colitis biopsy samples originating from the Gastrointestinal tract (GIT) and Hepatology teaching hospitals/medical city in Baghdad City. The test’s results demonstrated that the AIEC isolates had a high level of resistance to the majority of the an-tibiotics under investigation. Enterobacterial Repetitive Intergenic Consensus (ERIC-PCR) and m
... Show MoreUnderstanding the effects of fear, quadratic fixed effort harvesting, and predator-dependent refuge are essential topics in ecology. Accordingly, a modified Leslie–Gower prey–predator model incorporating these biological factors is mathematically modeled using the Beddington–DeAngelis type of functional response to describe the predation processes. The model’s qualitative features are investigated, including local equilibria stability, permanence, and global stability. Bifurcation analysis is carried out on the temporal model to identify local bifurcations such as transcritical, saddle-node, and Hopf bifurcation. A comprehensive numerical inquiry is carried out using MATLAB to verify the obtained theoretical findings and und
... Show MoreThe object of research is studying Raman scattering technique, photoluminescence and some optical properties of silver nanoparticles created by eco-friendly technique which independent on a long time, effort, energy and high temperatures, and with the highest adsorption capacity in order to achieve a high inhibition to paralyze the activity of the bacterial wall, by achieving the highest surface plasmon resonance (SRR). Silver nanoparticles were prepared using Matricaria Flower extract. Characterization of silver nanoparticles and detection of their effectiveness against microbial using two types of bacteria (Escherichia Coli and Staphylococcus aureus ), these nanoparticles were measured using a number of measurements, X-ray diffrac
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