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Design, Synthesis, Characterization and Preliminary Anticancer Study for Methotrexate Silibinin Conjugates
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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
Sat Jan 05 2019
Journal Name
Iraqi Journal Of Physics
Fabrication and characterization of porous silicon for humidity sensor application
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Porous Silicon (PS) layer has been prepared from p-type silicon by electrochemical etching method. The morphology properties of PS samples that prepared with different current density has been study using atom force measurement (AFM) and it show that the Layer of pore has sponge like stricture and the average pore diameter of PS layer increase with etching current density increase .The x-ray diffraction (XRD) pattern indicated the nanocrystaline of the sample. Reflectivity of the sample surface is decrease when etching current density increases because of porosity increase on surface of sample. The photolumenses (PL) intensity increase with increase etching current density. The PL is affected by relative humidity (RH) level so we can use

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Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and Characterization of Topical Letrozole Nanoemulsion for Breast Cancer
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Letrozole (LZL) is a non-steroidal competitive aromatase enzyme system inhibitor. The aim of this study is to improve the permeation of LZL through the skin by preparing as nanoemulsion using various numbers of oils, surfactants and co-surfactant with deionized water. Based on solubility studies, mixtures of oleic acid oil and tween 80/ transcutol p as surfactant/co-surfactant (Smix) in different percentages were used to prepare nanoemulsions (NS). Therefore, 9 formulae of (o/w) LZL NS were formulated, then pseudo-ternary phase diagram was used as a useful tool to evaluate the NS domain at Smix ratios: 1:1, 2:1 and 3:1.

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Publication Date
Tue Jan 01 2019
Journal Name
Energy Procedia
Fabrication and characterization of n- InSb Heterojunction for optoelectronic device
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Publication Date
Mon Jul 24 2023
Journal Name
Research Journal Of Pharmacy And Technology
Comparison of the effects of Methotrexate and Etanercept on RANKL and OPG as Bone Metabolism Biomarkers in patients with Rheumatoid Arthritis
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Rheumatoid arthritis is an autoimmune diseasecharacterized by chronic inflammationthat affects joints and cartilage. Bone complications such asRA-relatedosteoporosis are one of the most extra-articular manifestations. Many inflammatory mediators are released during RA disease pathophysiology; these mediators stimulate osteoclast genesis of bone by direct effects on RANKL and OPG. The study aimedto measure RANKL, OPG in RA patients treated with Etanercept only and other groups treated with Methotrexate onlyat baseline and after three months to evaluate bone state. An observational case-control prospective study was done on 30 RA patients who received MTX, 30 RA patients who received ETN, and 30 healthy,age-matched control groups. The

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Publication Date
Sun Sep 07 2014
Journal Name
Baghdad Science Journal
Study the effect of a new nikel (II) Complex and anticancer drug (cp) on Liver enzyme activity (GPT,GOT) and Creatinine level in Kidney of femal mice
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This study involved the effect of anew nickel (II) complexs with formla [NiL2(H2O)2].2.5ETOH where L=Bis[5-(p-nitrophenyL)-4-phenyL-1,2,4-traizole-3-dithocarbamato hydrazide] diaqua. nickel(II). Ethanol(2.5).and anti-cancer drug cyclophosphamide on specific actifity of two Liver enzymes (GOT,GPT) in the (Liver,kidney) tissues and on the creatinine Level in the kidney byUtilizing an invivosystem in femalmice.The result showed that inhibition in the activity of GPT and GOT enzymes in theLiver and in both nickel (II) complex and cyclophosphamide drug (CP) . mice weretreated with three doses (90,180,320) µg/mouse for three days for each group.The Liver show's the highest rate of GPT inhibition was about 97.43% at180µg/mouse regarding the ki

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Publication Date
Tue Oct 29 2024
Journal Name
Journal Of Advanced Pharmacy Education And Research
Evaluating the effects of different doses of fimasartan on methotrexate-induced renal inflammation in rats
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The nephrotoxicity induced by methotrexate is a severe condition that greatly affects its therapeutic potential and has a significant inflammatory component. Fimasartan is an angiotensin receptor blocker that offers organ-protective effects and may be useful in mitigating renal injury. The present study explored the anti-inflammatory potential of two doses of fimasartan against methotrexate-mediated nephrotoxicity. Albino rats were intraperitoneally administered a single methotrexate (20 mg/kg). Intraperitoneal treatment with fimasartan (5 or 10 mg/kg/day) was initiated on day two after methotrexate injection and continued for seven consecutive days. Methotrexate significantly increased serum urea, creatinine, and NGAL concentrations. It al

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Publication Date
Tue Jun 28 2011
Journal Name
Iraqi Journal Of Pharmacy
Effects of different concentrations of aqueous green tea extract against methotrexate-induced nephrotoxicity in rats
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Publication Date
Tue May 01 2018
Journal Name
Journal Of Physics: Conference Series
Fabrication and characterization study of ZnTe/n-Si heterojunction solar cell application
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Publication Date
Mon Jan 04 2021
Journal Name
Medico-legal Update
Study of Production and Characterization of Laccase Enzyme from Klebsiellapneumoniae K7 Isolate
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Sixty four local isolated of Klebsiella spp. have been isolated from environment samples (soil and water). These isolates were identified and diagnosis according to phenotype and biochemical tests. These isolates were subjected to primary and secondary screening, to select the isolate with the highest laccase activity. Fifteen isolates chosen from primary screening for screening their enzyme activity in secondary screening. It has been found the Klebsiella(K7) has the highest productivity of the enzyme (12 Unit/ml).Klebsiella(K7) isolate was diagnosis by Vitak 2 system, it was identified asK. pneumonia. The laccase purified was characterization, the experiments showed that: The molecular weight of laccase was 120KD and the optimum pH for th

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Publication Date
Wed Mar 25 2020
Journal Name
International Journal Of Drug Delivery Technology
Preparation, Characterization and In-Vitro Diffusion Study of Different Topical Flurbiprofen Semisolids
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Flurbiprofen (FLB) is chemically 2-(3- fluoro-4-phenyl phenyl) propanoic acid. It is a nonsteroidal anti-inflammatory drug (NSAID) used in the treatment of rheumatoid arthritis and osteoarthritis. Oral administration of this drug is associated with severe gastrointestinal side effects like ulceration and gastrointestinal bleeding. The solution to this problem lies in the fact that topically applied NSAIDs are safer than orally. This study aims to prepare different topical semisolid formulation of FLB as cream base (o/w), (w/o) and gel base using different gel-forming agents in different concentrations. Comparing characterization properties in addition to release and diffusion study for all the prepared formulas to select the best on

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