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.
Research Summary:
Seeking happiness and searching for it have been among the priorities of mankind from the beginning of his creation and will remain so until the end of this world, and even in the next life, he seeks happiness, but the difference is that a person can work in this world to obtain it, but in the next life he is expected to get what he done in this world. And among these reasons are practical actions that a person undertakes while he intends to draw close to God Almighty, so they lead him to attain his desired perfection, and to attain his goals and objectives, which is the minimum happiness in this life, and ultimate happiness after the soul separates the body, and on the day of the judgment, Amon
... Show MoreThis paper includes a comparison between denoising techniques by using statistical approach, principal component analysis with local pixel grouping (PCA-LPG), this procedure is iterated second time to further improve the denoising performance, and other enhancement filters were used. Like adaptive Wiener low pass-filter to a grayscale image that has been degraded by constant power additive noise, based on statistics estimated from a local neighborhood of each pixel. Performs Median filter of the input noisy image, each output pixel contains the Median value in the M-by-N neighborhood around the corresponding pixel in the input image, Gaussian low pass-filter and Order-statistic filter also be used. Experimental results shows LPG-PCA method
... Show MoreThe current research seeks to identify the most important humanitarian issues of a sacred and very important group in all the heavenly religions and human societies, namely the elderly, to identify their significant problems and health problems, and What are the effects of these problems on their mental health and which is the ultimate goal of human resources in All parts of the world? The study relied on what is available from the sources in the literature starting from the messages of heaven and the Islamic religion followed with humanitarian, social, legal and psychological postulates. The research included four systematic chapters included the definition research and identification of the problem, importance, objectives and terminolo
... Show MorePrediction of accurate values of residual entropy (SR) is necessary step for the
calculation of the entropy. In this paper, different equations of state were tested for the
available 2791 experimental data points of 20 pure superheated vapor compounds (14
pure nonpolar compounds + 6 pure polar compounds). The Average Absolute
Deviation (AAD) for SR of 2791 experimental data points of the all 20 pure
compounds (nonpolar and polar) when using equations of Lee-Kesler, Peng-
Robinson, Virial truncated to second and to third terms, and Soave-Redlich-Kwong
were 4.0591, 4.5849, 4.9686, 5.0350, and 4.3084 J/mol.K respectively. It was found
from these results that the Lee-Kesler equation was the best (more accurate) one
This investigation was conducted to recognize the structure for (RHETI version 2.5 1999) by using exploratory and confirmatory factor analysis. Sample of (620) student of Al-Mustansrya University were administered the (RHETI).
The data of their responses was analyzed by using (PAF) and oblique rotating .
The findings explored (9) factors as one factor for each type and (184) items were loaded by the factors: (60) item for feeling center, (61) items for instinctive center and (63) items for thinking center.
Results of confirmatory factorial analysis supported a model designed by the researcher depended upon a theoretical views of Riso and Hudson
... Show MoreSentiment analysis refers to the task of identifying polarity of positive and negative for particular text that yield an opinion. Arabic language has been expanded dramatically in the last decade especially with the emergence of social websites (e.g. Twitter, Facebook, etc.). Several studies addressed sentiment analysis for Arabic language using various techniques. The most efficient techniques according to the literature were the machine learning due to their capabilities to build a training model. Yet, there is still issues facing the Arabic sentiment analysis using machine learning techniques. Such issues are related to employing robust features that have the ability to discrimina
... Show MoreLeading edge serration is now a well-established and effective passive control device for the reduction of turbulence–leading edge interaction noise, and for the suppression of boundary layer separation at high angle of attack. It is envisaged that leading edge blowing could produce the same mechanisms as those produced by a serrated leading edge to enhance the aeroacoustics and aerodynamic performances of aerofoil. Aeroacoustically, injection of mass airflow from the leading edge (against the incoming turbulent flow) can be an effective mechanism to decrease the turbulence intensity, and/or alter the stagnation point. According to classical theory on the aerofoil leading edge noise, there is a potential for the leading edge blowi
... Show MoreThe research aims to identify the level of functional engagement and hope-based thinking of kindergarten teachers, identify if there is a significant difference in functional engagement and hope-based thinking in terms of specialization and years of service for kindergarten teachers, identify if there is a significant correlation between functional engagement and hope-based thinking of kindergarten teachers. The current research is determined by kindergarten teachers in the Second Rusafa Baghdad Education Directorate for the academic year (2022-2023). In order to achieve the objectives of the research, the researcher prepared a functional engagement scale, which consists of (45) items in three areas: Perceptual and functional engagement
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