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.
The research includes attempts to prepare anthranil ic acid (C7H7N02) complexes with some metals: [Pd (II), Fe(ll), and Fe (Ill)) which have been characterized by using:
Thermal stability (melti ng point, d composition poit), molar conductivity, IR, UV-visible spectra, elemental analysis (C-H-N) and magnetic properties. The general formula has been given for the prepared complexes:-
- M(C2H6N02)2 Where M= [Pd(ll), Fe(TI), Hg(ll)]
:.. M(C1H6N02)l Where M= [Fe(llf)]
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 MoreBeta-lactamase was purified from local isolate Klebsiella pneumonia by several steps included precipitation with ammonium sulphate at 20-40% saturation, DEAE- ion exchange chromatography and gel filtration on Sephacryl S-200 column. The obtained purification fold and recovery were 32.66; 47.04% respectively. The characterization of the purified beta-lactamase showed that the molecular weight was about 4000 daltons as determined by gel filtration.Purified enzyme had an optimal pH of 7 for activity and an optimal stability between pH 6.5-7.5, results shows that the optimal temperature appear to be 35 ? C .During storage the enzyme retained 72% at -20 ? C and retained 25% of the activity at the same period at 4 ? C.
Probiotics are live microbes that give many health benefits to human beings and animals, the most studied and commonly used probiotics are Gram-positive bacteria; lactobacilli and bifidobacteria. At nowadays, Lactobacillus spp. constitute more than two-thirds of the total numbers of probiotic species. The present study aimed to characterize Lactobacillus that locally isolated from human mouth and feces as probiotics. A total of three Lactobacillus isolates; Lactobacillus fermentum Lb2, Lactobacillus rhamnosus Lb9, and Lactobacillus paracasei Lb10 were investigated in respect to acid and bile salts tolerance, antibiotics susceptibility, and cell surface hydrophobicity in vitro using bacterial adhesion to hydrocarbons method. In compa
... Show MoreSUMMARY. – Absorption, flourescence, quantum yield and lifetime of rhodamine B in chloroform, methanol and dimethyl sulfoxide were measured. A comparison was done of these quantities with those for solid solutions, which are obtained by mixing constant volume proportions of dye at a concentration of 1×10–4M/l with different volume proportions from the concentrated solution of polymer in chloroform and dimethyl sulfoxide. The results showed that the addition of polymer to liquid concentrated solutions (1×10–4M/l) of rhodamine B dye from expecting, which leads to development of active medium for laser dye at high concentration, increase the spectra shift toward high energies, and the luminescence quantum yield but decreasing radiative
... Show MoreLeucine amino peptidases (LAP; EC 3.4.11.1) constitute a diverse set of exopeptidases that catalyze the hydrolysis of leucine residues from the amino-terminal of protein or peptide substrates, (LAP) are present in animals, plants, and microbes. In this study, leucine amino peptidase was purified partial from Arachis hypogaea seeds by using gel filtration chromatography Sephadex G-100. The enzyme was purified 3.965 fold with a recovery of 29.4%. Its pH and temperature optimum were(8.7) and (37oC), respectively. The results show novel properties of LAP from Arachis hypogaea L. or peanut. The Km value for LAP (77 mM), with V max (1538 m mole min-1). We recommend a separate isoenzymeof the enzyme (LAP) from Arachis hypogaea on L. peanut seeds a
... 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 MoreBioavailability is the objective for an optimum formulation. The target of the analysis is to maximize both the fluidity and disintegration profile of class II weakly compounds that are water-soluble. Anti-dyslipidemia drug rosuvastatin calcium (RC) (bioavailability 20%) through formulating as nanofibers (NFs) using electrospinning (ES) technology. Twenty formulas were prepared, and different polymers and polymer combinations with various concentrations were used such as polyethylene oxide (PEO) polyvinyl pyrrolidine (PVPK-30), and hydroxypropyl methylcellulose (HPMC). Three distinct groups of maximum parameters, including polymeric solution, electrospinning method, and ambient parameter, are capable of influencing the creation alon
... Show MorePoly [2-methoxy-5-(2-ethylhexyloxy)-1, 4-phenylenevinyl] (MEH-PPV) thin films were created in this study using both spin coating and drop casting processes. MEH-PPV thin films generated by Ferric Chloride (FeCl3) doping (0.03, 0.06, 0.09, and 0.12 wt%) were studied for some physical features using Fourier-Transform Infrared Spectroscopy (FTIR), Field Emission Scanning Electron Microscopy (FE-SEM), and Energy Dispersive X-ray Spectroscopy (EDX). An FTIR test showed that there was no chemical reaction that occurred between Ferric Chloride (FeCl3) and MEH-PPV, but rather a physical one, that is, an organic material composite occurred. As for FE-SEM, the pure sample MEH-PPV formed uniformly, but when FeCl3 was added by weight, we have differ
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