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.
The electronic payment systems are considered the most important infrastructure for the work of banks, particularly after a steady and remarkable development in information and communication technology, Which created the reality of the work of the infrastructure for these systems and these systems also become one of the most important components of infrastructure for the work of banks, cause it is one of the most important channels through which the transfer of cash, financial instruments between financial institutions in general and banking in particular.
In order to achieve the objectives of the research, the most important to identify the concept of electronic payment systems, and its divisions, and th
... Show MoreThis research was conducted to measure the safety of heat stable enterotoxin a (STa) produced by enterotoxigenic Escherichia coli, through studying its toxic effect on human blood lymphocyte, since it showed a promising effect in reducing the proliferation of colorectal cancer cells. the cytogenetic effects of (STa) by using five different concentrations (100, 200, 400, 800 and 1600μg/ml) in comparison with negative (PBS, Phosphate buffer saline) and positive (MMC, Mitomycin C) at concentration of 5μg/ml, controls on human blood lymphocytes obtained from both (10) normal healthy persons and (20) colorectal cancer patients was measured by employing the following parameters: mitotic index, blast index, chromosomal aberrations and micronucle
... Show MoreThere are many techniques that can be used to estimate the spray quality traits such as the spray coverage, droplet density, droplet count, and droplet diameter. One of the most common techniques is to use water sensitive papers (WSP) as a spray collector on field conditions and analyzing them using several software. However, possible merger of some droplets could occur after they deposit on WSP, and this could affect the accuracy of the results. In this research, image processing technique was used for better estimation of the spray traits, and to overcome the problem of droplet merger. The droplets were classified as non-merged and merged droplets based on their roundness, then the merged droplets were separated based on the average non-m
... Show MoreOsteoarthritis is the most prevalent arthritic disease and a leading cause of disability. The pathogenesis of osteoarthritis involves multiple etiologies, including variable degree of synovial inflammation. Metformin and pioglitazone could potentially reduce the levels and activity of inflammatory mediators. This may consider as a new therapeutic approach added to the current used drugs in an attempt to decrease the pain, inflammation, and improve daily activity and quality of life in patients with knee osteoarthritis.
This study designed to evaluate the clinical utility of using metformin or pioglitazone as anti-inflammatory agents in combination with non-steroidal anti-inflammatory drugs (NSAID) of selective type of cyclooxygen
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This research aims to assess the practice of physical activities by people with intellectual disabilities and its challenges during the Coronavirus (COVID-19) pandemic from their families' point of view. The research sample consisted of (87) individuals from families with intellectual disabilities in the Makkah region. The sample was selected by the simple random method where the researcher used the descriptive analytical approach. A questionnaire of (32) items was used as the research tool to collect data. The findings of the study showed that the assessment level of practicing physical activities by people with intellectual disabilities was low. The public facilities dimension ranked first with a moder
... Show MoreCancer stay to be one of the leading causes of death throughout the world due to a limited success to use treatments. The new synthesized metal complexes with formula: [Ni L2 (H2O)2]. 2.5 E t OH and [Cd L2]. ½ H2O Where L = Bis [ 5 – ( P – nitrophenyl ) - 4 – phenyl 1 , 2 , 4 – trazol – 3 – dithiocarbamato hydrazide ] and the aqueous extract of Teucrium polium L.(TP) plant (Ja,adahin Arabic) were examined against growth cells of hepatocellular Carcinoma cell Line ( HeP2 ). The cytotoxicity assay of cancer cell line was used for determination of inhibition rate with three concentrations; (62.5, 105 and 250 µg /200µl). The aqueous extract of TP plant induced death of cancer cells by significant elevation of the inhib
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