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.
.Curcumin (Cur) and L phenylalanine (Phy) compounds were used to prepare two mixed ligand complexes with Cr (III) and Fe (III) ions. The synthesized complexes are characterized by using conductivity measurement and different spectral methods like FT-IR and UV- Vis .Molar conductance and analytical studies confirmed that the complexes exhibit octahedral geometry., suggest that the complexes are formed in 1: 1 :2 [ L : Metal : 2phe ] ratio and they proposed to have the general formulae [M(Cur)(phe)2] Cl (M= Cr (III) and Fe (III) The compound dyeing method was studied and applied to acrylic fabric.The antibacterial activity of curcumin, phenylalanine and their mixed ligand complexes were examined on pathogenic bacterial strains and showed good
... Show MoreOil from Brassca campestris (local variety) was extracted with hexane using Soxhlet. The extracted oil was characterized and its antimicrobial activity was determined as well. The content of extracted oil was 40% with 0.5% of volatile oil .Oil was immiscible with polar solvent such as ethanol, acetone and water, while it was easily miscible with chloroform due to its hydrophobicity. The result of organoleptic tests revealed that the oil is clear yellow in color and odorless with acceptable taste. The oil was stable at 4 -25 C? for a month. Refractive index (RI) of oil was 1.4723 with density of 0.914, [both at 4-25 C?]. Boiling point 386 C?. Infra red spectroscopy (IR) indicated the presence of different chemical groups (C=C
... Show MoreThe fabrication of Solid and Hollow silver nanoparticles (Ag NPs) has been achieved and their characterization was performed using transmission electron microscopy (TEM), zeta potential, UV–VIS spectroscopy, and X-ray diffraction (XRD). A TEM image revealed a quasispherical form for both Solid and Hollow Ag NPs. The measurement of surface charge revealed that although Hollow Ag NPs have a zeta potential of -43 mV, Solid Ag NPs have a zeta potential of -33 mV. According to UV-VIS spectroscopy measurement Solid and Hollow Ag NPs both showed absorption peaks at wavelengths of 436 nm and 412 nm, respectively. XRD pattern demonstrates that the samples' crystal structure is cubic, similar to that of the bulk materials, with
... Show MoreEndoglucanase produced from Aspergillus flavus was purified by several steps including precipitation with 25 % ammonium sulphate followed by Ion –exchange chromatography, the obtained specific activity was 377.35 U/ mg protein, with a yield of 51.32 % .This step was followed by gel filtration chromatography (Sepharose -6B), when a value of specific activity was 400 U/ mg protein, with a yield of 48 %. Certain properties of this purified enzyme were investigated, the optimum pH of activity was 7 and the pH of its stability was 4.5, while the temperature stability was 40 °C for 60 min. The enzyme retained 100% of its original activity after incubation at 40 °C for 60 min; the optimum temperature for enzyme activity was 40 °C.
Objective: The aim of this study was to develop a bioadhesive gel of gatifloxacin for the treatment of periodontal diseases.Methods: Periodontal gels of gatifloxacin were prepared using different hydrophilic polymers such as carbopol 940 (CP 940), carboxymethyl cellulose (CMC) and hydroxypropylmethyl cellulose (HPMC) in varied concentrations, either alone or as a combination. The prepared gels were evaluated for their physical appearance, pH, drug content, viscosity, bioadhesiveness and in vitro drug release profile. The influence of the type and the concentration of polymer on the drug release as well as on viscosity and mucoadhesiveness of prepared gels were investigated.Results: The prepared gels showed acceptable physical proper
... Show MoreABSTRACT: In this research SnO2 thin films have been prepared by using hot plate atmospheric pressure chemical vapor deposition (HPCVD) on glass and Si (n-type) substrates at various temperatures. Optical properties have been measured by UV-VIS spectrophotometer, maximum transmittance about (94%) at 400 0C. Structure properties have been studied by using X-ray diffraction (XRD) , its shows that all films have a crystalline structure in nature and by increasing growth temperature from(350-500) 0C diffraction peaks becomes sharper and grain size has been change. Atomic force microscopy (AFM) uses to analyze the morphology of the Tine Oxides surface structure. Roughness & Root mean square for different temperature have been investigated. The r
... Show Moreتقدم هذه الدراسة وصفا للطريقة المستخدمة في تحضير الكربون المنشط (AC)من بقايا الشاي. تم دراسة الخواص الفيزيائية والكيميائية وكفاءة الامتزاز للكربون المنشط المحضر. تم إنتاج الكربون المنشط (AC) على مرحلتين: الاولى التنشيط باستخدام حامض الفوسفوريك (H3PO4) والثانية الكربنة عند درجة حرارة 450 درجة مئوية. استخدم الكربون المنشط لغرض امتصاص العقار الدوائي السيبروفلوكساسين(CIP) . تمت دراسة عدة عوامل تشغيلية بدرجة حرار
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The present investigation aimed to formulate a liquid self-microemulsifying drug delivery system (SMEDDS) of tacrolimus to enhance its oral bioavailability by improving its dispersibility and dissolution rate. Four liquid SMEDDS were prepared using maisine CC as oil phase, labrasol ALF as surfactant and transcutol HP as co-surfactant based on the solubility studies of tacrolimus in these components. The phase behavior of the components and the area of microemulsion were evaluated using pseudoternary phase diagrams. The formulations were also assessed for thermodynamic stability, robustness to dilution, self-emulsification time, drug content, globule size and polydispersity index. The prepared SMEDDS formulations exhibi
... Show MoreThis study aims to formulate azithromycin oleogel to locally treat skin infections such as acne vulgaris and skin wound infection. Providing a form of azithromycin that can be administered topically is highly desired to prevent unwanted systemic complications including diarrhea, nausea, and abdominal pain. Additionally, it will avoid first pass metabolism, improves patient acceptance, provides an alternative in nauseated patients, decreases the dose by direct contact with the pathological site, and provides a noninvasive and convenient mode of administration. Furthermore, for treating wound infections, the gel will act as a scaffold biomaterial for wound closure besides its antibacterial effect. Herein, we propose the use of grapeseed oil-b
... Show Moreتقدم هذه الدراسة وصفا للطريقة المستخدمة في تحضير الكربون المنشط (AC)من بقايا الشاي. تم دراسة الخواص الفيزيائية والكيميائية وكفاءة الامتزاز للكربون المنشط المحضر. تم إنتاج الكربون المنشط (AC) على مرحلتين: الاولى التنشيط باستخدام حامض الفوسفوريك (H3PO4) والثانية الكربنة عند درجة حرارة 450 درجة مئوية. استخدم الكربون المنشط لغرض امتصاص العقار الدوائي السيبروفلوكساسين(CIP) . تمت دراسة عدة عوامل تشغيلية بدرجة حرار
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