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.
Aннотация
В статье представлены явления полисемии и омонимии в специализированной терминосистеме, а именно в геодезической терминологии; определены предпосылки и причины возникновения полисемии и омонимии в профессиональном языке в области геодезии и кадастра; установлены различия и взаимосвязь между понятиями омонимия и полисемия; выделены главных типы полисемантических тер
... Show MoreThe aims of research is to know the effect of using the computer in
teaching physics to the fifth secondary grade on the achievement of the students and their retention of information .
The sample consists of ( 50 ) students in the fillh secondary grade (scicnti fie branch ) in Nassiriyah secondary school in Thi-qar governorate in ( 200 I - 2002 ) that chooses as random Iy and divided
to t>vo equivalent groups:control and experimental .
The researcher built the teaching plans of each group . The five lessons choice from curriculum , and desi b'Tl five computer teaching programs , and final achievement test from multip
... Show MoreObjective: To find out the relationship between vaginal bleeding during third trimester and pregnancy outcomes. Methodology: A purposive sample is "Non-probability" of (100) women who had diagnostic vaginal bleeding during third trimester (27-40wk) of pregnancy, and who visited the Bint Al-Huda Hospital for the period from 15th Feb. to 17th May 2015.Validity and reliability of questionnaire are determined through pilot study. Descriptive and inferential statistical procedures were used to analyze the data, and the data were collected by using interview technique, constructed questionnaire has been desig
The function of internal auditing has become an important function that aims at achieving objectives that are compatible with these developments and changes that have occurred in many countries in the world, which required the emergence of professional associations and institutes in the profession of internal auditing. Improve the guideline of the internal audit units issued by the Federal Audit Bureau to enhance the efficiency of internal audit performance in Iraqi government units. The researchers adopted the statistical method of proving the hypothesis by constructing a questionnaire that included three main axes: supporting the senior management in adopting the current guide, and the second being the importance of improving t
... Show MoreThe Research is interested in the detailed comparative study of certain selection of
Imam Alsamarqandi in some subjects of washing and touching the Gracious Quran.
The value of this study is that it is related to one aspect of the duties obliged on Muslim
like parity.
The study has tried to collect certain scholars’ opinions of eight doctrines with the
selection of Alsamarqandi to make a comp arson between them and to show how
Alsamarqandi is able to create legal laws from his sources to lead the researchers nto have
knowledge about the syllabi of the famous scientists.
Finally we ask God to bless to what is right and to accept this study and make it part of
our good deeds, Ameen.
A (b,t)-blocking set B in PG(2,q) is set of b points such that every line of PG(2,q) intersects B in at least t points and there is a line intersecting B in exactly t points. In this paper we construct a minimal (b,t)-blocking sets, t = 1,2,3,4,5 in PG(2,5) by using conics to obtain complete arcs and projective codes related with them.
Cardiovascular disorders are refer to the class of diseases that involve the heart or blood vessels (arteries and veins). While the term technically refers to any disease that affects the cardiovascular system. Cholesterol is classified as a sterol (a contraction of steroid and
... Show MoreDiversity of the aspects of analyzing a specific linguistic issue is considered to be a
familiar phenomenon in learning Arabic in which – at different levels- various linguistic
aspects and phases – sometimes – are involved in a linguistic issue . In this paper , the
problematic issues during linguistic analysis are taken into an account. The Holy Quran
interpretation books include many Quranic expressions which have a lot of meaning described
by different interpreters , from them this paper has selected only one expression ( = كفاتا
receptacle ) from the verse "Have we not made the earth a receptacle " ( Al- Mursalat verse 25
) , this paper believes that this expression is sufficient display the interpret
Organophosphorus insecticide and growth regulator namely Ethephon (2-chloroethylphosphonic acid) are widely used as a ripening process accelerator and a cultivation duration inhibitor. Pomegranate extract (PPE) has recently been taken into consideration due to its pharmacological effects especially those associated with renal diseases. Thus, this study aims to investigate the possible protective effect of PPE against ethephon-induced nephrotoxicity in rats. In this study four groups of adult male rats were divided into control group, PPE 400 mg/kg group, Ethephon 250 mg/kg group, and finally, PPE + Ethephon group (treated with the same dose of PPE group and Ethephon group). In the current study, kidney function parameters (KIM-1, creatin
... Show MoreIn a report by Transparency Organization in 2010, Iraq has 200 newspapers, magazines, sixty-seven radio stations and 45 satellite TV channels. The increase in these figures is measured in days or weeks and not months and years. This fact confirms the importance of studying content providers, especially youth sports content, for two reasons: the first is that young people constitute the highest percentage in Iraqi society, with all the potential involved in shaping the future aspects; the second reason is that for years sport has become an important pillar in people's lives not only in the entertainment aspect as it was seen in the past; Rather, sport has an influential presence in politi
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