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 Muslim woman actively participated in narrating, preserving, controlling and maintaining the hadith, along with her brother, the man who later became an inexhaustible representative of the effort to preserve, control, and narrate the Sunnah. Undoubtedly, the mothers of the believers, may God be pleased with them, had a great advantage in communicating Islam and spreading the Sunnah of the Prophet Especially among women, all of them heard from him, may God’s prayers and peace be upon him, and lived with him in the details of his life on the disparity between them in memorizing and narrating and publishing them. It narrated (378) recently, and it is considered the second narrator after the mother of the believers Aisha, may God be pl
... Show MoreBackground: In dentistry, dentist takes the advantages of soft lining materials due to the viscoelastic properties. The major problem is the adhesion of the soft liner with the denture base material. Materials and Methods: Heat cured of high impact acrylic resin specimens prepared with dimensions 75x13x13mm for shear bond strength test, soft lining material (Refit and Mollosil) with a 3-mm thickness and used to join each two acrylic blocks. Also four specimens with the same previous dimensions utilized for chemical and physical surface analysis. The specimens grouped as control (without plasma) and experiment (with oxygen plasma) treated high impact acrylic specimens. Results: Plasma treatment increased the shear bond strength for both Refi
... Show MoreThis research aims to examine the effectiveness of a teaching strategy based on the cognitive model of Daniel in the development of achievement and the motivation of learning the school mathematics among the third intermediate grade students in the light of their study of "Systems of Linear Equations”. The research was conducted in the first semester (1439/1440AH), at Saeed Ibn Almosaieb Intermediate School, in Arar, Saudi Arabia. A quasi-experimental design has been used. In addition, a (pre & post) achievement test (20 Questions) and a (pre & post) scale of learning motivation to the school mathematics (25 Items) have been applied on two groups: a control group (31Students), and an experimental group (29 Students). The resear
... Show MoreThe current research aims to show the impact of the international auditing standard IAS 540 in reducing income smoothing practices in Iraq. To achieve the objectives of the research, the researcher adopted a questionnaire for a sample of auditors in Iraq. Where 60 forms were distributed and after the questionnaire was retrieved and statistical analysis was done using the SPSS program, The research reached a number of results, the most important of which are: the existence of a statistically significant effect of the application of the international auditing standard IAS 540 in reducing income smoothing practices, The research recommended the necess
... Show Morebackground: human epidermal growth factor receptor-2 (her2/neu) is related to growth factor receptors with alkaline kinase activity and it is regarded as important prognostic and therapeutic factor that can depended on in breast cancer therapy. HER2/neu expression by immunohistochemistry (IHC) is submitted to a great in terob server inconsistency. Subsequently additional confirmatory tests for assessment of gene alterations and amplification status are needed for patients with early or metastatic breast cancer. In situ hybridization techniques and specifically Chromogenic in situ hybridization (CISH) was arise as a practical, cost-effective, and alternative to fluorescent in situ hybridization in testing for gene alterationAims of the study
... Show MoreFour samples of the Se55S20Sb15Sn10 alloy were prepared using the melting point method. Samples B, C and D were irradiated with (6.04×1010, 12.08×1010 and 18.12×1010 (n.cm-2s -1 ) of thermal neutron beam from a neutron source (241Am-9Be) respectively, while sample A was left not irradiated. The electrical properties were assessed both before and after the radiation. All irradiated and non-irradiated samples show three conduction mechanisms, at low temperatures, electrical conductivity is achieved by electron hopping between local states near the Fermi level. At intermediate temperatures, conduction occurs by the jumping of electrons between local states at band tails. At high temperatures, electrons transfer between extended stat
... Show MorePsoriasis is a long-lasting autoimmune disease that is characterized by swollen skin patches. Normally, these skin patches are dark, swollen, itchy and scaly. The single application of the innate TLR7/8 ligand Imiquimod (IMQ) in mice easily induces a dermatitis that closely resembles human psoriasis, critically dependent on the axis of IL-23/IL-17. Artemisia dracunculus prepared as an ointment and has been used topically to mice before imiquimod application. The results of the current study showed that A. dracunculus ointment can significantly reduce psoriasis area and severity index in (A. dracunculus ointment + imiquimod group as compared with both control group and (vehicle ointment + imiquimod) group.