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.
Background: The vasoconstricting agents: nor-adrenaline and 5- hydroxytryptamine
(5-HT) have a stimulant action on smooth muscle contractility of the rat vas deferens.
Objective: This study aimed to investigate the effect of exposure to continuous
darkness and continuous light on the contractility of the vasa deferntia smooth
muscles from rats to applied nor-adrenaline and 5-HT.
Method: Male albino wistar rats were divided into 3 experimental groups. Group 1:
Control animals, were exposed to the ordinary photoperiod each day. Group 2: Rats
were kept in a dark room. Group 3: In a room under a bright artificial light.
All animals were killed after 4 weeks.
Results: Vasa deferentia preparations from continuous dar
This study aims to recognize the process of using computer in publicschools in Ma`an governorate in terms of hardware, capabilities, and teachers usage. It also aims to identify the most important obstacles those schools face from a teachers perspective.
The study sample consists of (150) teachers from different disciplines. The researcher prepared two questionnaires related to the research pivotal, then presented to a group of arbitrators to be used in this final form. The data was analyzed statistically and the study concluded that there is a shortage in the computer services provided to teachers, and there is a w
... Show MoreThe aim of the research is to study the effect of the roundhouse strategy on the achievement of fifth grade secondary school in physics and their pivotal thinking. The experiment has been applied for obtaining the data, which were processed statistically using the Statistical Package for Social Sciences, the results revealed that the students of the experimental group who studied using the roundhouse strategy was superior to the students of the control group who studied in the traditional method in the achievement exam. The results also show that there are statistically significant differences between the mean scores of the students of the experimental group and the control group in the pivotal thinking exam, in favor of the experimental gr
... Show MoreAbstract: Two different shapes of offset optical fiber was studied based on coreless fiber for refractive index (RI)/concentration (con.) measurement, and compare them. These shapes are U and S-shapes, both shapes structures were formed by one segment of coreless fiber (CF) was joined between two single mode (SMF) lead in /lead out with the same displacement (12.268µm) at both sides, the results shows the high sensitive was achieved in a novel S-shape equal 98.768nm/RIU, to our knowledge, no one has ever mentioned or experienced it, it’s the best shape rather than the U-shape which equal 85.628nm/RIU. In this research, it was proved that the offset form has a significant effect on the sensitivity of the sensor. Addi
... Show MoreBackground: Juvenile idiopathic arthritis (JIA) is a chronic disease of childhood. Increased prevalence of periodontal disease and dental caries in juvenile idiopathic arthritis is due to difficulties in executing good oral hygiene. This study was conducted to assess oral health status in patients with Juvenile idiopathic arthritis according to age and duration of illness. Materials and methods: A research was conducted among Juvenile idiopathic arthritis patients attending Baghdad Teaching Hospital with different age and both gender, underwent a clinical evaluation of their dental and oral condition. Diagnosis of dental caries was done according to the criteria of WHO (1997). Dental plaque, gingival condition, calculus were assessed by PI/
... Show MoreThe present study has conducted to investigate the effect of hot aqueous extract of seeds and leaves of fenugreek (Trigonella foenum-graecum) on embryonic development in Swiss albino mice morphologically , the results is showed throught dosage pregnant female orally after period 4, 8, 12days at the beginning of pregnancy by doses 100 , 200 , 300 mg/kg of body weight , the results showed normal period of pregnancy 21 days and abortion did not occur when the pregnant mice take the hot aqueous extract of leaves of fenugreek, but the pregnant mice that take the hot aqueous extract of seeds of fenugreek occurred abortion of embryos and showed some histopathological changes in ovaries and uterus such as congestion, hemorrhage, necrosis, odema,
... Show MoreMore than 450 distinct types of human papilloma virus recognized via recent molecular techniques. The low and high oncogenic risk-HPV genotypes have an association with a variety of benign and malignant tumors in the oropharyngeal and nasopharyngeal localizations. This study aimed to determine the rate of DNA detection of HPV genotype 6/11 in non-oncologic nasopharyngeal and palatine tonsillar tissues from pediatric patients subjected to adeno-tonsillectomies. A total number of 64 tissue specimens enrolled; 44 non-oncologic nasopharyngeal and palatine hypertrophied tissue specimens from 22 pediatric patients sustained combined adeno-tonsillectomies and compared to 20 nasal trimmed tissues with unremarkable pathological changes (in
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