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.
Sphingolipids are key components of eukaryotic membranes, particularly the plasma membrane. The biosynthetic pathway for the formation of these lipid species is largely conserved. However, in contrast to mammals, which produce sphingomyelin, organisms such as the pathogenic fungi and protozoa synthesize inositol phosphorylceramide (IPC) as the primary phosphosphingolipid. The key step involves the reaction of ceramide and phosphatidylinositol catalysed by IPC synthase, an essential enzyme with no mammalian equivalent encoded by the AUR1 gene in yeast and recently identified functional orthologues in the pathogenic kinetoplastid protozoa. As such this enzyme represents a promising target for novel anti-fungal and anti-protozoal drugs. Given
... Show MoreIn our article, three iterative methods are performed to solve the nonlinear differential equations that represent the straight and radial fins affected by thermal conductivity. The iterative methods are the Daftardar-Jafari method namely (DJM), Temimi-Ansari method namely (TAM) and Banach contraction method namely (BCM) to get the approximate solutions. For comparison purposes, the numerical solutions were further achieved by using the fourth Runge-Kutta (RK4) method, Euler method and previous analytical methods that available in the literature. Moreover, the convergence of the proposed methods was discussed and proved. In addition, the maximum error remainder values are also evaluated which indicates that the propo
... Show MoreAutorías: Ghassan Adeeb Abdulhasan, Falih Hashim Fenjan, Hussein Jabber Abood. Localización: Revista iberoamericana de psicología del ejercicio y el deporte. Nº. 3, 2022. Artículo de Revista en Dialnet.
The evolution of the Internet of things (IoT) led to connect billions of heterogeneous physical devices together to improve the quality of human life by collecting data from their environment. However, there is a need to store huge data in big storage and high computational capabilities. Cloud computing can be used to store big data. The data of IoT devices is transferred using two types of protocols: Message Queuing Telemetry Transport (MQTT) and Hypertext Transfer Protocol (HTTP). This paper aims to make a high performance and more reliable system through efficient use of resources. Thus, load balancing in cloud computing is used to dynamically distribute the workload across nodes to avoid overloading any individual r
... Show MoreA pseudo-slug flow is a type of intermittent flow characterized by short, frothy, chaotic slugs that have a structure velocity lower than the mixture velocity and are not fully formed. It is essential to accurately estimate the transition from conventional slug (SL) flow to pseudo-slug (PSL) flow, and from SL to churn (CH), by precisely predicting the pressure losses. Recent research has showed that PSL and CH flows comprise a significant portion of the conventional flow pattern maps. This is particularly true in wellbores and pipelines with highly deviated large-diameter gas-condensate wellbores and pipelines. Several theoretical and experimental works studied the behavior of PSL and CH flows; however, few models have been suggested to pre
... Show MoreThis research presents a new algorithm for classification the
shadow and water bodies for high-resolution satellite images (4-
meter) of Baghdad city, have been modulated the equations of the
color space components C1-C2-C3. Have been using the color space
component C3 (blue) for discriminating the shadow, and has been
used C1 (red) to detect the water bodies (river). The new technique
was successfully tested on many images of the Google earth and
Ikonos. Experimental results show that this algorithm effective to
detect all the types of the shadows with color, and also detects the
water bodies in another color. The benefit of this new technique to
discriminate between the shadows and water in fast Matlab pro
Background: Currently there are four general approaches to correct refractive errors: refractive corneal surgery, crystalline lens surgery and implantation of an intraocular lens in anterior or posterior chamber. Aim: To evaluate the predictability, safety and stability of toric phakic implantable collamer lens implantation to correct moderate to high myopic astigmatism. Methods: Sixty eyes of 40 patients underwent implantation of a toric implantable collamer lens (V4c design) in the Eye Specialty Private Hospital, Baghdad, Iraq were studied. The mean spherical refraction was -11.32±3.17 diopter (D) with a range of -6.00 to -18.00 D and a mean cylinder of -2.61±1.16 with range of -1.00 to -5.50 D. The outcome measures that evaluat
... Show MoreThe Electric Discharge (EDM) method is a novel thermoelectric manufacturing technique in which materials are removed by a controlled spark erosion process between two electrodes immersed in a dielectric medium. Because of the difficulties of EDM, determining the optimum cutting parameters to improve cutting performance is extremely tough. As a result, optimizing operating parameters is a critical processing step, particularly for non-traditional machining process like EDM. Adequate selection of processing parameters for the EDM process does not provide ideal conditions, due to the unpredictable processing time required for a given function. Models of Multiple Regression and Genetic Algorithm are considered as effective methods for determ
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