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Design, Synthesis, Characterization and Preliminary Anticancer Study for Methotrexate Silibinin Conjugates

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.

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Validity of Generalized Standard Addition Method for a Mixture of Amino Acid Analysis

A Modified version of the Generlized standard addition method ( GSAM) was developed. This modified version was used for the quantitative determination of arginine   (Arg) and glycine ( Gly) in arginine  acetyl salicylate – glycine complex . According to this method two linear equations were solved to obtain the amounts of (Arg) and (Gly). The first equation was obtained by spectrophotometic measurement of the total absorbance of (Arg) and (Gly) colored complex with ninhydrin . The second equation was obtained by measuring the total acid consumed by total amino groups of (Arg) and ( Gly). The titration was carried out in non- aqueous media using perchloric acid in glacial acetic acid as a titrant. The developed metho

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Publication Date
Sun Apr 03 2016
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Arterial stiffness index as a marker for the occurrence of atherosclerotic cardiovascular disease

Background: Arterial functional changes reflected by vascular stiffness might occur at early stages of cardiovascular disease before the morphological alterations reflected by increasing the intima media thickness and it is widely used as a very sensitive indicator of functional vascular damage.
Objectives: This study is aimed to correlate ultrasound detected vascular functional changes with the severity and extent of coronary artery disease.
Patients and methods: Sonographic scans were performed on 100 Patients (61males, 39 females) with an age range of (40-65years) for measuring carotid and brachial arteries end diastolic and end systolic diameters to calculate vascular stiffness index . Coronary CT angio

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Publication Date
Wed May 01 2019
Journal Name
Journal Of Engineering
Determination of the Optimum formula for Composite Motor Gasoline Octane Number Blending Enhancer

To decrease the dependency of producing high octane number gasoline on the catalytic processes in petroleum refineries and to increase the gasoline pool, the effect of adding a suggested formula of composite blending octane number enhancer to motor gasoline composed of a mixture of oxygenated materials (ethanol and ether) and aromatic materials (toluene and xylene) was investigated by design of experiments made by Mini Tab 15 statistical software. The original gasoline before addition of the octane number blending enhancer has a value of (79) research octane number (RON). The design of experiments which study the optimum volumetric percentages of the four variables, ethanol, toluene, and ether and xylene materials leads

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Publication Date
Fri Apr 21 2023
Journal Name
Technologies And Materials For Renewable Energy, Environment And Sustainability: Tmrees22fr
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Publication Date
Sat Nov 11 2023
Journal Name
مجلة كلية الامام الاعظم
Provisions for inheritance of agricultural lands (transfer of the right to dispose of)

Agricultural lands have great importance in people's lives, and their exploitation has a great impact on strengthening the national economy. Therefore, countries have given great importance to this sector, and because of the importance of this sector, the state has given large areas of these lands to the farmers to invest in agriculture, and among these farmers are those who died and left behind children who took up crafts. Agriculture, for fear that these agricultural lands would be abandoned and turned into waste lands, a land system was introduced called (regular distribu- tion), which corresponds to (legitimate inheritance). Under this system, these lands were trans- ferred to the children of farmers who died so that the process of inve

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Publication Date
Mon Jan 08 2024
Journal Name
Iraqi Journal For Computer Science And Mathematics
Applications for the groups S.U.T.(2,p) where p prime upper than 9

The problem of finding the cyclic decomposition (c.d.) for the groups ), where  prime upper than 9 is determined in this work. Also, we compute the Artin characters (A.ch.) and Artin indicator (A.ind.) for the same groups, we obtain that after computing the conjugacy classes, cyclic subgroups, the ordinary character table (o.ch.ta.) and the rational valued character table for each group.

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Publication Date
Tue Feb 05 2019
Journal Name
Journal Of The College Of Education For Women
Basic training requirements for teachers from the viewpoint of supervisors in Mafraq Governorate

This study aimed to reveal the stage for teachers of basic training needs from the perspective of workers in Mafraq Governorate, through a survey of a sample of counselors look at the Ajloun area schools reached (58) counselors.
To achieve the objective of the study was constructed questionnaire where they are finalized (18) items distributed on two dimensions (professional needs, performance requirements) and after confirmation of the validity and reliability have been applied to the sample where the results showed that training needs were high, both on a professional or per formative level .
The results also showed no statistically significant differences in the areas of tool due to gender, educational qualification. The study co

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Publication Date
Thu Jan 14 2021
Journal Name
Iraqi Journal Of Science
Boosting the Network Performance using Two Security Measure Scenarios for Service Provider Network

Network security is defined as a set of policies and actions taken by a network administrator in order to prevent unauthorized access, penetrated the defenses and infiltrated the network from unnecessary intervention. The network security also involves granting access to data using a pre-defined policy. A network firewall, on the other hand, is a network appliance that controls incoming and outgoing traffic by examining the traffic flowing through the network. This security measure establishes a secure wall [firewall] between a trusted internal network and the outside world were a security threat in shape of a hacker or a virus might have existed

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Publication Date
Mon Nov 01 2010
Journal Name
Iraqi Journal Of Physics
New Technique for Treatment of the dust accumulation from PV solar panels surface

One of the most important problems facing the world today is the energy problem. The solution was in finding renewable energy sources such as solar energy. The solar energy applications in Iraq is facing many problems . One of the most important problems is the accumulation of dust on the solar panels surface which causes decreasing its performance sharply. In the present work, a new technique was presented by using two-axis solar tracking system to reduce the accumulated dust on the solar panel surface and compared it with the fixed solar panels which installed at tilt angles 30° and 45°. The results indicated that the maximum losses of the output power due to accumulation of dust on the fixed solar panels is about 31.4% and 23.1% res

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Publication Date
Wed Feb 08 2023
Journal Name
Iraqi Journal Of Science
Calculation of Full Energy Peak Efficiency for HPGe Detector Using Monte Carlo Method

This research presents results on the full energy peak efficiency of a high purity germanium (HPGe) detector from point source as a function of photon energy and source-detector distance. The directions of photons emitted from the source and the photon path lengths in the detector were determined by Monte Carlo technique. A major advantage of this technique is the short computation time compared to the experiments. Another advantage is the flexibility for inputting detector-related parameters (such as source–detector distance, detector radius, length and attenuation coefficient) into the algorithm developed, thus making it an easy and flexible method to apply to other detector systems and configurations. It has been designed and writte

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