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:
Recently, there is a widespread attention about the service at the level of each of the research and academic studies, and at the organizational level as well. The subject of orientation towards the service aspect is starting to be of this attention being of the modern subjects, relatively, which appeared at the end of the last century, as well as the link of this subject with the relationship between the organization and its customers, and how to provide high quality services to get their satisfaction. Thus, the specialists from researchers were interested in this field to develop an appropriate scale to measure the organizational orientation toward service, and it was the most prominen
... Show MoreLa disciplina sémantica siendo una rama de la lingüística y relacionada con los significados que residen detrás de los vocablos sería muy intereseante ser estudiada y investigada, sobre todo cuando tratamos de penetrarnos dentro de la evolución semántica y los motivos por los que se suceden estos cambios. Pues, es injusto dejar de dar una definición aclaratoria sobre esta disciplina y sus componentes.
El significado de los léxicos que se forma por un conjunto de semas o rasgos significativos mínimos. Sin embargo, no todos esos semas son igualmente intervenidos por los hablantes de una comunidad lingüística, sino que hay algunos de ellos que siempre están presentes, mientras que otros varían. Es decir, el significado
... Show MoreThe aim of the research is to explain the nature of the relationship between the dimensions of the strategic recovery of the service represented by (compensation, speed of response, apology, initiative (defining the problem) and the strategic goals of the company represented in (profitability, growth, community service, employee satisfaction) in the National Insurance Company, it has been approved The questionnaire as a tool to collect data and information from the sample of (58) who are in (department manager, M. department director, division official, unit official) and the statistical program (spss) was used in calculating (arithmetic mean, standard deviation, coefficient of variation, coefficient of Correlation, t-test, varia
... Show MoreThe research aims to shed light on banking liberalization and explain its impact on attracting customers, especially since Iraq adopted this policy after (2003) due to the changes that occurred, as the Central Bank of Iraq granted flexibility to banks in setting the interest rate on deposits and loans as well as allowing the entry of foreign banks in the local environment. The research relied on the analytical method for the dimensions of banking liberalization represented by (liberating interest rates, liberating credit, legal reserve requirements, entering foreign banks, privatization) as well as the factors affecting the attraction of customers, and a number of Iraqi banks listed in the Iraqi Stock Exchange were selected as a
... Show MoreThe aim of this work is oriented to increase film cooling effectiveness value through numerical investigations for flow of Mach number not more than 0.3 around vane surface, to find the effects of inclination and compounds angles of round holes in staggered rows on adiabatic film cooling effectiveness of vane suction side. Multi cylindrical film cooling hole cases were studied with pitch ratio P/d =2 and 3, local blowing ratios M=0.382, 0.77 and 1.14, inclination angles a=30° and 45°, compound angles β= 0°, 15°, 30° and 45° and local momentum ratios I= 0.084, 0.34 and 0.756 for better cooling process.
A numerica
... Show MoreThis research dealt with the subject of negotiation skills of employees in public relations departments which is one of many skills supposed to be available to these employees. These skills combined help in the success of the job of public relations departments; and give them an important and vital role within the roles distributed in the departments of any government institution wither is governmental or non-governmental.
Negotiation is a skill that requires intelligence, tact, culture, information, intuition, and knowing to use the means of communication to access the information that is useful in reaching satisfactory results
... Show MoreIntroduction and Aim: Pseudomonas aeruginosa is a nosocomial infection with an ability to develop high levels of antibiotic resistance. The efflux pump system is one of the mechanisms that is linked to multidrug resistance in P. aeruginosa. In this study, we employed siRNA loaded on gold nanoparticles against the MexA efflux pump gene to decrease the MexA gene expression in P. aeruginosa and estimated antibiotic resistance after gene silencing. Materials and Methods: This study examined four strains of P. aeruginosa isolated from patients in various hospitals in Baghdad. Bacteria isolated were identified by biochemical tests and Vitek compact 2 system. Single-stranded siRNA (33bp) designed in this study was loaded onto gold
... Show MoreThis study aimed to identify the perceived mental image of volunteering, and its relationship to volunteer motivation among a sample of Al-Quds Open University students, as well as to identify the differences in the perceived mental image of volunteering due to variables (gender, year of study, place of residence, college). The researcher has used relational descriptive approach. The researcher has used two questionnaires, the first was used to measure the perceptive mental image of volunteering, and the second to measure the motivation towards volunteering, and the study population may consist of all students of Al-Quds Open University Hebron Branch during the first semester of the academic year 2021/2020 and their number (3462)Male and
... Show MoreTraumatic radial nerve injury in humeral shaft fracture is the most common traumatic nerve injury in long-bone fracture, with overall prevalence 2-18%, ranging from traction to complete transection. Spontaneous recovery may reach 88%. The aim of the study is to assess the sensitivity & specificity of the ultrasound to detect the radial nerve injury and to see if this can be used as a diagnostic test. This is a prospective study on 17 adult patients with a closed fracture of the humeral shaft, dividing into two groups, the first group of 7 patients had signs and symptoms of radial nerve palsy at presentation and the second group of 10 patients had intact radial nerve function was considered as a control group. All these patients had at leas
... Show MoreThis paper presents a comparison study on thermal performance conic cut twist tape inserts in laminar flow of nanofluids through a constant heat fluxed tube. Three tape configurations, namely, quadrant cut twisted tape (QCT), parabolic half cut twisted tape (PCT), and triangular cut twisted (VCT) of twist ratio= 2.93 and cut depth= 0.5 cm were used with 1% and 2% volume concentration of SiO2/water and TiO
... Show More