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 aerial part of Ephedra foliata Family Ephedraceae have long been used in traditional medicine and now Ephedra species have medicinal, ecological, and commercial value. The variety of pharmacological actions of this plant is due to its chemical constituents. Ephedrine and
related alkaloids; are the newly potential medicinal value of Ephedra supplements for weight loss or performance improvement. Other pharmacological actions like antibacterial and antifungal effects of the phenolic acid compounds, the immunosuppressive action of the polysaccharides, and the antitumor action of flavonoids. The genus of this plant wildly distributed t
The present paper focuses on the nature of the different interactions between cometary nucleus and tail with solar wind. The dynamics of the comet will impose many features that provide unique behavior of the comet when entering the solar system. These features are reviewed in this paper and few investigations are made. The calculations made in this work represent the analysis and interpretation of the different features of the comet, such as perihelion and eccentricity dependence on the gas production rate, and the dependence of the latter on the composition of the comet nucleus. The dependences of the heliocentric, bow shock, contact surface, and stand-off distances with gas production rate for many types of comets that cover linear and n
... Show MoreBidentate Schiff base ligand 3-(3,4-Dihydroxy-phenyl)-2-[(4-dimethylamino-benzylidene)-amino]-2-methyl-propionic acid was prepared and characterized by spectroscopic techniques studies and elemental analysis. The Cd(II), Ni(II), Cu(II), Co(II), Cr(III),and Fe(III) of mixed-ligand complexes were structural explicate through Moler conductance , [FT-IR, UV-Vis & AAS], chloride contents, , and magnetic susceptibility measurements. Octahedral geometries have been suggested for all complexes. The Schiff base and its complexes were tested against various bacterial species, two of {gram(G+) and gram(G-)} were shown weak to good activity against all bacteria.
Background: Asthma is a disease of the airways characterized by chronic inflammation associated with airway hyper-responsiveness and airway wall remodeling. Aims of the study: The aims of this study was to determine the prevalence of oral manifestations , identify different microorganism from oral micro flora and determination of salivary IgA and salivary flow rate in asthmatic patients taking different dose of Prednisolone in comparison with control group. Subjects, materials and methods: The study included 17 patients under treatment with Prednisolone (10-20 mg),15 patients take (20-30 mg) of Prednisolone and other 18 patients take (30 – 40mg) of Prednisolone, and 25 healthy control group (10 male and 15 female). Results : The mo
... Show MoreDespite all the possibilities held by Iraq for the production of poultry , but there is low and clear in the level of production and a rise in costs and a decline in per capita consumption is due to a number of reasons, including poor investment , stop government subsides , dumping policies , market Bolmottagat imported , the contribution of the merchant squandering of national capacity , weak base material for the growth of this sector , the security situation and the crisis of energy and others .
Despite all this research has shown that there are great investment opportunities in this very sector of the market size and absorptive capacity of his and the growth of per capita income and level of cul
... Show MoreThis paper set forth the spatial suitability of the informal settlement supposed to be distributed by the Iraqis government to poor people. The Iraqi government identified 9 locations of informal settlement in Baghdad city and acceptance it as a reality as a help for them to getting home. In this paper I discovered the suitability of those locations which one will be suitable more than others for living. The analysis process was applied using the GIS environment – spatial analysis. According to the results, It has been identified as the most important measures to identify which one of these areas suitable for development for housing by using some criteria (Distance from the city center, Proximity from transport routes, Proximity of high v
... Show Moreفي البداية اود الاشارة الى ان فهم حقيقة الازمة هو ذو جانب فني يتعلق بالجينات الوراثية لنظام يملك في احيناته قدرة عالية على تفريخ المشتقات. هذا النظام الذي يزداد عقما وتدميرا يزداد قدرة على خلق النقود الائتمانية/المشتقات، وكلما اقتربنا اكثر من فهم هذا الجانب كلما اسقطت في ايدينا تلك التوصيفات الاكاديمية الجاهزة في نقص الرقابة والاشراف، تركيز المخاطر،....الخ التي تناولتها الكتابات الشائعة في معظم طروحات
... Show More Problem solving methods and mechanisms contribute to facilitating human life by providing tools to solve simple and complex daily problems. These mechanisms have been essential tools for professional designers and design students in solving design problems.
This research dealt with one of those mechanisms, which is the (the substance-field model model), as it has been mentioning that this mechanism is characterized by the difficulty of its application, which formed the main research problem. In home gardens (the sub-problem of research), an analysis of this problem was applied and then a solution was found to address it. The researcher used the 3dsmax program to implement the proposed design.
The most important research res
The effective insulation design of the stress grading (SG) system in form-wound stator coils is essential for preventing partial discharges and excessive heat generation under pulse-width modulation excitation. This paper proposes a method to find the optimal insulation design of the SG system aimed at reducing the dielectric and thermal stresses in the machine coil. The non-uniform transmission line model is used to predict the voltage propagation along the overhang, SG, and slot regions considering the variation in the physical properties of the insulation layers. The machine coil parameters for different insulation materials are calculated by using the finite element method. Two optimization algorithms, fmincon and particle swarm optimiz
... Show More