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 purpose of this research is to a treatment the impact of Views outliers to the estimators of a distributed arrival and service to the theory of queues and estimate the distribution parameters depending on the robust estimators, and when he was outliers greatest impact in the process of estimating the both distributions mentioned parameters, it was necessary to use way to test that does these data contain abnormal values or not? it was used the method ( Tukey ) for this purpose and is of the most popular ways to discover the outliers , it shows that there are views abnormal (outliers ) in the estimators of each of the distributional arrival and service, which have a significant impact on the calculation of these estimato
... Show MoreOtitis media with effusion (OME) is a common disease especially among young children (before school age) and it is one of the common causes of acquired hearing loss in childhood. Pediatric patients with OME are usually undernourished. The purpose of this study is to determine whether the serum levels of trace elements (zinc, copper, magnesium, iron) have a role in the development of OME in children. This study carried out on 55 children and subdivided them into two groups. Group 1 (patient group) consist of 30 children suffering from OME and group 2 (control group) included 25 apparently healthy children. Serum levels of zinc, copper, magnesium and iron were measured for both groups. Comparison the results between the two groups showed t
... Show MoreThis study expands the state of the art in studies that assess torsional retrofit of reinforced concrete (RC) multi-cell box girders with carbon fiber reinforced polymer (CFRP) strips. The torsional behavior of non-damaged and pre-damaged RC multi-cell box girder specimens externally retrofitted by CFRP strips was investigated through a series of laboratory experiments. It was found that retrofitting the pre-damaged specimens with CFRP strips increased the ultimate torsional capacity by more than 50% as compared to the un-damaged specimens subjected to equivalent retrofitting. This indicated that the retrofit has been less effective for the girder specimen that did not develop distortion beforehand as a result of pre-loading. From
... Show MoreHerein, we report designing a new Δ (delta‐shaped) proton sponge base of 4,12‐dihydrogen‐4,8,12‐triazatriangulene (compound
This paper analyzes the effect of scaling-up model and acceleration history on seismic response of closed-ended pipe pile using a finite element modeling approach and the findings of 1 g shaking table tests of a pile embedded in dry and saturated soils. A number of scaling laws were used to create the numerical modeling according to the data obtained from 1 g shake table tests performed in the laboratory. The current study found that the behaviors of the scaled models, in general have similar trends. From numerical modeling on both the dry and saturated sands, the normalized lateral displacement, bending moment, and vertical displacement of piles with scale factors of 2 and 35 are less than those of the pile with a scale factor of 1 and the
... Show MoreOne of the most important parameters determining structural members' durability and strength is the fire flame's influence and hazard. Some engineers have advocated using advanced analytical models to predict fire spread impact within a compartment and considering finite element models of structural components to estimate the temperatures within a component using heat transfer analysis. This paper presented a numerical simulation for a reinforced concrete beam’s structural response in a case containing Water Absorbing Polymer Spheres (WAPS) subjected to fire flame effect. The commercial finite element package ABAQUS was considered. The relevant geometrical and material parameters of the reinforced concrete beam model a
... Show MoreMedicinal plant life have performed an integral role in the development of human lifestyle being used as resources for the manufacturing of contemporary medicines, antibiotics. Microorganisms are responsible for many issues in industry and remedy because of biofilm formation. This study aimed to take a look at the results of Thymus vulgaris alcoholic extract on Staphylococcus aureus the causative marketers of acne in human particularly the women. The extract was acquired mixing 25 g of Thyme powder with 350 ml of 80% ethanol for 6 hours at 40°. Antimicrobial activities of the plant extract and integral oil towards the S. aureus were decided using the agar diffusion technique. The consequences proven that special concentrations of alcoholic
... Show MoreMutations in genes encoding proteins necessary for detoxifying oxidative stress products have been predicted to increase susceptibility to lung cancer (LC). Despite this, the association between waterpipe tobacco smoking (WP), genetic polymorphisms, and LC risk remains poorly understood. This is the first study to explore the relationship between WP tobacco smoking and these genetic factors. Previously, we investigated the association of GSTP1 SNPs (rs1695-A/G and rs1138272-C/T) with LC in Iraqi males who smoke WP. Here, we expanded our analysis to include GSTM1 (active/null) and GSTT1 (active/null) genotypes, both individually and in combination with GSTP1 SNPs. Multiplex PCR and RFLP-PCR assays were utilized to determine the genotypes of
... Show MoreThis research has presented a solution to the problem faced by alloys: the corrosion problem, by reducing corrosion and enhancing protection by using an inhibitor (Schiff base). The inhibitor (Schiff base) was synthesized by reacting of the substrates materials (4-dimethylaminobenzaldehyde and 4-aminoantipyrine). It was diagnosed by infrared technology IR, where the IR spectrum and through the visible beams proved that the Schiff base was well formed and with high purity. The corrosion behavior of carbon steel and stainless steel in a saline medium (artificial seawater 3.5%NaCl) before and after using the inhibitor at four temperatures: 20, 30, 40, and 50 C° was studied by using three electrodes potentiostat. The corrosion behavior
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