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.
Abstract
The grey system model GM(1,1) is the model of the prediction of the time series and the basis of the grey theory. This research presents the methods for estimating parameters of the grey model GM(1,1) is the accumulative method (ACC), the exponential method (EXP), modified exponential method (Mod EXP) and the Particle Swarm Optimization method (PSO). These methods were compared based on the Mean square error (MSE) and the Mean Absolute percentage error (MAPE) as a basis comparator and the simulation method was adopted for the best of the four methods, The best method was obtained and then applied to real data. This data represents the consumption rate of two types of oils a he
... Show MoreThe author addresses the issue of the linguoculturological component in the process of teaching Russian to Arabic students, focuses on the peculiarities of the national character of students. The author also refers to the long-standing ties of Russian and Arab cultures, thus emphasizing the relevance of this aspect for the current state and situation of the Russian language in Arab countries.
Автор статьи обращается к вопросу лингвокультурологической составляющей в процессе преподавания русского языка арабским студентам, останавливается на особенностях национального хара
... Show MoreThe technological developments in the field of communication have witnessed considerable impact in the variables which exist in following up and conveying the events which link it’s meaning to political implications. This makes a number of satellite channels depend on the techniques of propaganda and use them in the news bulletins to achieve political aims and ends related to its formational directives where those channels allotted a considerable time in its programming transmission map to concentrate on the security and political status to complete the image of the informational scene according to the logic of its propaganda and styles in processing news for daily events.The technological developments in the field of communication hav
... Show MoreResearch aims (Quality and originality in scientific research from the point of view of the participants in the course (qualification of scholars of Bayt al-Hikma) To find out how satisfied the participants about the training course held by the house of wisdom (research community), To develop and maximize the capacity of researchers in the field of writing scientific research, As well as establishing frameworks and concepts and standards related to quality and authenticity scientific research, The role played by this kind of research in the service of the movement of the human journey towards progress and prosperity.
On this basis was the research community, their number was (23) common t
... Show MoreBackground: This study aimed to examine the efficacy of methylene blue (MB) and toluidine blue O (TBO) photodynamic therapy (PDT) as adjuncts to root surface debridement (RSD). Methods: This split-mouth, randomized, controlled clinical trial included eighteen patients, and a total of 332 sites (control = 102, MB = 124 and TBO = 106) were examined. Two sessions of PDT were completed at baseline and two weeks after RSD. Clinical parameters of bleeding on probing (BOP), plaque index (PI), probing pocket depth (PPD), and clinical attachment level (CAL) were measured pre- and post-treatment. Results: PPD and BOP reductions in sites treated by RSD with adjunctive photosensitizers (MB and TBO) were significantly higher than in control site
... Show MoreIn this research the specific activity of natural radionuclides 226Ra, 232Th and 40K were determined by sodium iodide enhanced by thallium NaI(TI) detector and assessed the annual effective dose in Dielac 1 and 2 and Nactalia 1 and 2 for children of less than 1 year which are available in Baghdad markets. The specific activity of 40K has the greater value in all the types which is in the range of allowed levels globally that suggested by UNSCEAR. The mean value of annual effective doses were 2.92, 4.005 and 1.6325 mSv/y for 226Ra, 232Th and 40K respectively.
Background: Oil refinery workers are continuously exposed to numerous hazardous materials. Petroleum contains the heavy metals as a natural constituent or as additives. These metals induce the production of ROS which associated with an oxidative damage to DNA, proteins, and lipids. This study was conducted to assess the salivary levels of heavy metals, salivary oxidative status, oral immunological activity (salivary sIgA) and assessment of the oral findings among the workers of Al-Daura oil refinery in Baghdad city. Subjects, Materials and Methods: This study was done in Al-Daura oil refinery; samples consist of 60 workers involved in refinery processes (study group) and 20 non-workers (control group). Oral examination and saliva collection
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