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 L1-adaptive controller for controlling uncertain parameters and time-varying unknown parameters to control the position of a DC servomotor. For the purpose of comparison, the effectiveness of L1-adaptive controller for position control of studied servomotor has been examined and compared with another adaptive controller; Model Reference Adaptive Controller (MRAC). Robustness of both L1-adaptive controller and model reference adaptive controller to different input reference signals and different structures of uncertainty were studied. Three different types of input signals are taken into account; ramp, step and sinusoidal. The L1-adaptive controller ensured uniformly bounded
... Show MoreHygienic engineering has dedicated a lot of time and energy to studying water filtration because of how important it is to human health. Thorough familiarity with the filtration process is essential for the design engineer to keep up with and profit from advances in filtering technology and equipment as the properties of raw water continue to change. Because it removes sediment, chemicals, odors, and microbes, filtration is an integral part of the water purification process. The most popular technique for treating surface water for municipal water supply is considered fast sand filtration, which can be achieved using either gravity or pressure sand filters. Predicting the performance of units in water treatment plants is a basic pri
... Show MoreHygienic engineering has dedicated a lot of time and energy to studying water filtration because of how important it is to human health. Thorough familiarity with the filtration process is essential for the design engineer to keep up with and profit from advances in filtering technology and equipment as the properties of raw water continue to change. Because it removes sediment, chemicals, odors, and microbes, filtration is an integral part of the water purification process. The most popular technique for treating surface water for municipal water supply is considered fast sand filtration, which can be achieved using either gravity or pressure sand filters. Predicting the performance of units in water treatment plants is
... Show MoreTo perform a secure evaluation of Indoor Design data, the research introduces a Cyber-Neutrosophic Model, which utilizes AES-256 encryption, Role-Based Access Control, and real-time anomaly detection. It measures the percentage of unpredictability, insecurity, and variance present within model features. Also, it provides reliable data security. Similar features have been identified between the final results of the study, corresponding to the Cyber-Neutrosophic Model analysis, and the cybersecurity layer helped mitigate attacks. It is worth noting that Anomaly Detection successfully achieved response times of less than 2.5 seconds, demonstrating that the model can maintain its integrity while providing privacy. Using neutrosophic sim
... Show MoreSecnidazole was linked with ciprofloxacin as mutual prodrugs to get antibiotics with broader spectrum of activity, improved physicochemical properties and given by single dose to improve patient’s compliance. Furthermore, they provide structural modifications to overcome bacterial adaptation. The structures of the synthesized compounds were confirmed using FT-IR, mass spectrometry, elemental microanalysis (CHNO) and some physiochemical properties. This modification was led to an increase in Log P values for Mutual I (Log P 1.114) and Mutual II (Log P 1.97) compared with its values for Secnidazole (Log P -0.373) and ciprofloxacin (Log P -0.832). The solubility of prodrugs had been determined in different media, Mutual II showed 1
... Show MoreBackground: Although methotrexate (MTX) is a frequently used chemotherapy drug, its effectiveness is sometimes hampered by the drug's toxic consequences. Omega 7 is a monounsaturated fatty acid, with different anti-inflammatory, anti-diabetic anti-obesity applications, and its possible protective effects against MTX-induced blood toxicity were investigated in this study. Objective: Evaluation of possible protective effects of omega7 against MTX-induced blood toxicity. Methods: 30 mice were divided into five groups, the First group take liquid paraffin orallyfor 7 days for served as negative control and the second group take methotrexate (20mg/kg) intraperitoneallyto serve as a positive control,the third group takes omega 7 (100mg/kg
... Show MoreObjective: The objective of this study was to prepare nanosuspension of a practical water insoluble antiulcer drug which is lafutidine to enhance the solubility, dissolution rate with studying the effect of different formulation variables to obtain the best formula with appropriate physical properties and higher dissolution rate.Methods: Nanosuspension of lafutidine was prepared using solvent anti-solvent precipitation method using Polyvinylpyrrolidone K-90(PVP K-90) as the stabilizer. Ten formulations were prepared to show the effect of different variables in which two formulations showed the effect of stabilizer type, three formulations showed the effect of stabilizer concentration, two formulations showed the effect of combinatio
... Show MoreIn this research, the preparation of a chemically activated carbon from date stones by using electric and microwave assisted K2CO3 activation was studied. The effect of radiation power, radiation time, and impregnation ratio on the yield and Iodine number on the activated carbons was investigated. The activated carbon characterizations were examined by its surface area, pore structure analysis, bulk density, moisture content, ash content, iodine number, FTIR, and scanning electron microscopy (SEM). The adsorption capacity was also studied by adsorption of fluoroquinolones antibiotics, CIP, NOR, and LEVO, by the prepared activated carbon.
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