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.
Leucine 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 MoreLactococcus lactis ssp. lactis isolated from raw milk was used for titanium dioxide (TiO2) nanoparticles biosynthesis. Biosynthesized TiO2 nanoparticles were characterized using UV-vis spectroscopy, Atomic Force Microscopy (AFM) (1.97 nm), X-ray diffraction (XRD) appa-ratus, Field Emission Scanning Electron Microscopy (FE-SEM), Energy dispersive X-ray anal-ysis (EDX) spectra and Fourier Transform Infrared Spectroscopy (FTIR). Result was 408.21 cm-1 that belong to anatase Titania. L. lactis ssp. Lactis isolates had the ability to synthesize TiO2 nanoparticles, the characterization results presented that the biosynthesized nanoparti-cles were at wavelength (344-347) nm; approving the formation of anatase phase of TiO2 NPs; spherical c
... Show MorePolymers, being one of the most important materials in dentistry, offer great physical and mechanical qualities, as well as good biocompatibility. Aim of this study was done to evaluate the Polyetherketoneketone and Polyetherketoneketone polymer composite material used as dental implant through tensile strength, Fourier Transform Infrared analysis FTIR, and wettability). Polyetherketoneketone composites (Polyetherketoneketone and Strontium-containing hydroxyapatite) with selected weight percentage ratios of (0, 10%, 20%, 30%), were fabricated using a compression molding technique”, The study involved Samples preparation (sheets) shaped and form into the desired shape according to standard for tests which included tensile strength,
... Show MoreThe 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)]
Nano particles of Cadmium Oxide (CdO) thin films were prepared by spray pyrolysis technique. The synthesized film is annealed at (200 , 300, 450) o C for 3 hours . The XRD and AFM for the analysis of its structural and micro-structural characteristic has been preformed. The average grain size was found to be about 32.50 nm .There is a preferred orientation along (200) plane with texture coefficient 1.79, 1.644, 1.763 and 1.792 for deposited and annealed films, corresponding to grain size 57,58 ,51 and 51 nm. The variations of stress with temperature is ranged from 0.157 - 0.376 GPa .
Seven strains of Rhizobium leguminosarum bv. vicide were isolated
and purified from the root nodules of faba bean (Viciae faba) plants
collected from different agroclimatic locations in Baghdad and Diyala
provinces of Iraq. Screening of these strains gives four salinity tolernat strains which tolerate 1-5% sodium chloride supplement mannitol to salt yeast extract (M Y) medium. Colony forming units for the four tolerant strains under stress conditions were significantly reduced in comparison with those under normal conditions. Different tests were used to study the surface properties of stress tolerant strains under normal and stress conditions. No differences were found in the production of lipopolysaccharid
Nano crystalline copper sulphide (Cu2S) thin films pure and 3% Bi doped were deposited on glass substrate by thermal evaporation technique of thickness 400±20 nm under a vacuum of ~ 2 × 10− 5 mbar to study the influence of annealing temperatures ( as-deposited, and 573) K on structural, surface morphology and optical properties of (Cu2S and Cu2S:3%Bi). (XRD) X-ray diffraction analysis showed (Cu2S and Cu2S:3%Bi) films before and after annealing are polycrystalline and hexagonal structure. AFM measurement approves that (Cu2S and Cu2S:3%Bi) films were Nano crystalline with grain size of (105.05-158.12) nm. The optical properties exhibits good optical absorption for Cu2S:3%Bi films. Decreased of optical band gap from 2.25 to 2 eV after dop
... 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 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.
Bioavailability 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
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