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
This work is considered the first study for the components of the Iraqi Leucaena leucocephala plant, where the different phytochemical compounds that present in the aerial parts were identified by using the gas chromatography/mass spectrometry technique (GC/MS). The type of the components and their concentration will differ according to the part of the plant used and the method of extraction (hot and cold). This study made a comparison in lupeol concentration that was identified and isolated from petroleum ether fractions of Leucaena leucocephala by using Gas Chromatography/Mass Spectrometry (GC/MS), High-performance thin-layer chromatography (HPTLC), and Preparative High-Performance Li
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There has been a heated controversy over the role the financial policy plays and how sufficient it is in affording the financial burden. This burden is known as the operational current expenses which the governments of various countries mainly afford, despite the discrepancy in the government’s economic policy. After the deterioration and deficit in the state budget in all countries nowadays, it was necessary to find an appropri
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Objectives: To find out the association between enhancing learning needs and demographic characteristic of (gender, education level and age).
Methods: This study was conducted on purposive sample was selected to obtain representative and accurate data consisting of (90) patients who are in a peroid of recovering from myocardial infarction at Missan Center for Cardiac Diseases and Surgery, (10) patients were excluded for the pilot study, Data were analyzed using descriptive statistical data analysis approach of frequency, percentage, and analysis of variance (ANOVA).
Results: The study finding shows, there was sign
... Show MoreThe research aims to identify the effect of the training program that is based on integrating futuristic thinking skills with classroom interaction patterns on mathematics teachers in order to provide their students with creative solution skills. The research sample consisted of 31teachers (15 teachers for the experimental group and 16 for the control groups). The researcher developed a measure for the academic self-efficacy consisting of (39) items. Its validity, reliability, coefficient of difficulty and discriminatory power were estimated. To analyze the findings, the researcher adopted the Mann-Whitney (U) test and the effect size, and the findings were as follows: There is a statistically significant difference at the significance leve
... Show MoreThe present paper(Spacio-Temporal Relations in the Translated Text in Both Russian and Arabic) focuses on the spacio-temporal effect in the translated text; it is possible to compose the translation text simultaneously with the process of the composing the original text. This is carried out during the simultaneous consecutive translation. And, the time and place of composing the translation might greatly differ from the time and place of composing the original textt. The translator may tackle a text of an ancient time and written in a language which might have changed, and may thus appear as another language where the author might have talked on behalf of a people who had lived or are living in apparently different geographic
... Show MoreThis research was carried out to evaluate the activity of crude juice of Olive on some cytogenetic parameters in mice like chromosomal aberration (CAs) and micronuclei formation(MN). The results showed that there was no significant difference between the crude juice (green and black)in CAs(3.77,4.10)and MN(0.25,0.25) in comparison with negative control (3.39,0.22)respectively. The interaction effect between the crude before and after treatment with mutagen MMC showed that the crude is one of the vital inhibitors of the mutagen by its ability in reducing the percentages of both the CAs and MN in bone marrow cells in mice.
Background: Oral anticoagulation medication, warfarin and non-vitamin k antagonist oral anticoagulants (NOAC) may require long term use which may affect patients’ satisfaction with their treatment and their quality of life (QOL). Objective: To compare the quality of life and treatment satisfaction among groups of patients using different anticoagulant therapies (warfarin and NOAC). Patients and methods: A cross-sectional study was performed at Ibn Al-Bitar Hospital for cardiac surgery in Baghdad in the period between December 2022 to May 2023. The study population included a convenient sample of patients receiving either warfarin or non-vitamin k antagonist oral anticoagulants treatment. The Arabic version of the short form 12
... Show MoreIn this study, the effect of intersecting ribs with inclined ribs on the heat transfer and flow characteristics of a high aspect ratio duct has been numerically investigated. The Relative roughness pitch (P/e) is 10 and the Reynolds number range from 35,700 to 72,800. ANSYS (Fluent-Workbench 18.0) software has been utilized to solve the Reynolds averaged Navier-Stokes (RANS) equations with the Standard k-ε turbulence model. Three ribbed models have been used in this study. Model 1 which is a just inclined ribs, Model 2 which has a single longitudinal rib at the center with inclined ribs and Model 3 which has two longitudinal ribs at the sides. The results showed that the heat transfer rate has been enhanced when the int
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Summary of the jurisprudence research
Praise be to God, Lord of the Worlds, and prayers and peace be upon the Master of the Messengers, our master Muhammad, and upon his pure family, and his ignorant and ignorant companions, and those who followed them in goodness until the Day of Judgment.
Then:
The many jurisprudential aspects that the Shafi’i imams said are of great importance, because these aspects are nothing but the opinions of venerable jurists who have reached a high degree of knowledge until they have become among the owners of faces. And among them are the Shafi’i jurists, the jurists may differ among themselves, either because there is no text about their imam in a
... Show MoreThis study was carried out at the Poultry Research Station belong to state Board of Agricultural Research, Ministry of Agriculture, Abu Ghraib. The duration of this study was from 28 November 2013 to 15 May 2014 to evaluate the effect of supplementation different levels of organic selenium(Se-yeast) and inorganic selenium (Selenium selenite) on some productive performances of broiler breeder and selenium levels in plasma ,egg (yolk,albumin). The study included 336 female broiler breeder and 28 males (Ross 308 and arbor acres), 42 weeks old were randomly distributed to 7 dietary treatments experiment with 2 replicates / treatment (24 females and 2 male birds /replicate). The duration of the experiment was 24 weeks, and treatments were as the
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