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 paper presents an analysis of selected qualitative characteristics of pellets produced from rape straw obtained from cultivations subjected to different fertilization treatments and from mixtures of straw selected for testing with crude glycerol obtained as a by-product from biodiesel production. The assessment focused on the following qualities of the obtained pellets: Moisture content, mechanical durability, heating value and main elements, that is, carbon, hydrogen, nitrogen, sulphur, chlorine and oxygen. The obtained results indicated that the different treatment regimens applied in spring rape cultivations had a significant impact on the physicochemical qualities of the straw. In terms of the heating value, traditional fer
... Show MoreThe enhancement of the thermal and thermo-hydraulic performance of a semi-circular solar air collector (SCSAC) is numerically investigated using porous semi-circular obstacles made of metal foam with and without longitudinal porous Y-shaped fins. Two 10 and 40 PPI porous material samples are examined. Three-dimensional models are built to simulate the performance of SCSAC: model (I) with clear air passage; model (II) with only metal foam obstacles, and model (III) with metal foam obstacles as well as porous Y-fins. COMSOL Multiphysics software version 6.2 based on finite element methodology is employed. A conjugate heat transfer with a (k-ε) turbulence model is selected to simulate both heat transfer and fluid flow across the entir
... 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 (
Abstract
The current research aims to identify the typical effect of Flower and Coscroft on expressive performance and the development of lateral thinking among literary fifth-grade students. To achieve the research objective, the researcher chose a sample of (90) female students from the fifth literary grade, with two experimental groups and a control group. The research groups are of six subjects. The research found that the two experimental groups have more expressive performance than the control group. Students of the first experimental group outperformed the students of the second experimental group in expressive performance and lateral thinking tests. In light of the findings of the research, the researcher
... Show MoreThe aim of the study is the assessment of changes in the land cover within Mosul City in the north of Iraq using Geographic Information Systems (GIS) and remote sensing techniques during the period (2014-2018). Satellite images of the Landsat 8 on this period have been selected to classify images in order to measure normalized difference vegetation index (NDVI) to assess land cover changes within Mosul City. The results indicated that the vegetative distribution ratio in 2014 is 4.98% of the total area under study, decreased to 4.77% in 2015 and then decreased to 4.54