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.
In the present study, silver nanoparticles (AgNPs) were prepared using an eco-friendly method synthesized in a single step biosynthetic using leaves aqueous extract of Piper nigrum, Ziziphus spina-christi, and Eucalyptus globulus act as a reducing and capping agents, as a function of volume ratio of aqueous extract(100ppm) to AgNO3 (0.001M), (1: 10, 2: 10, 3: 10). The nanoparticles were characterized using UV-Visible spectra, X-ray diffraction (XRD). The prepared AgNPs showed surface Plasmon resonance centered at 443, 440, and 441 nm for sample prepared using extract Piper nigrum, Ziziphus spina-christi, and Eucalyptus respectively. The XRD pattern showed that the strong intense peaks
This study was aimed to extract the effective material from the dry nests of termites and detect its antibacterial activity against some pathogenic bacterial isolates and inhibit synthesis of its biofilm. Termites dry nests were collected and the effective material was extracted then the antibacterial activity was detected using the disc diffusion assay. Results were showed that the extract have antibacterial material from the Termites dry nests, this extract showed antibacterial activity against Gram positive bacteria (Staphylococcus aureus) at (21.5mm) and Gram negative bacteria ( Enterobacter sp. and Pseudomonas aeruginosa) at (26 mm and 20 mm) respectively by inhibiting their growth, as well as its effect on biofilm production o
... Show More4-amino-3-(4-(((4-hydroxy-3, 5dimethoxybenzyl) oxy) methyl) phenyl)-1, 2, 4-triazole-5-thione was synthesized by to method the first one from melt reaction of 4-(((4-hydroxy-3, 5-dimethoxybenzyl) oxy) methyl) benzoic acid with Thiocarbonyldihydrazide, the second method from convert the corresponded acid hydrazide to potassium 2-(4-(((4-hydroxy-3, 5-dimethoxybenzyl) oxy) methyl) benzoyl) hydrazinecarbodithioate salt then react with hydrazine hydrate. Newly Schiff base (7a-7f) were synthesized from reaction the 4-amino-1, 2, 4-triazol with substituted hydroxybenzaldehyde. The resulting compounds were characterized by IR, 1H-NMR, 13C-NMR, and HRMS data. 2, 2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assays
... Show Morecompound [1] was formed from the reaction of benzoin and benzaldehyde in the presence of ammonia, which was reacted with sodium hydride in DMF to obtain imidazole salt. This salt was reacted with adipoyl chloride to give compound [2]. Acid hydrazide derivative [3] was obtained from the reaction of compound [2] with hydrazine hydrate. After that Shiff bases [4-9] have been synthesized from the reaction of compound [3] with different aromatic aldehydes. These new formed compounds were diagnosed by 13C-NMR, 1H-NMR for some of them (in Ahl-Albate University in Jordan) and FT-IR spectroscopy (In Baghdad University). All of the prepared products have been studied their biological activities toward two kinds of bacteria. These products show
... Show MoreThe nuclear charge density distributions, form factors andcorresponding proton, charge, neutron, and matter root mean squareradii for stable 4He, 12C, and 16O nuclei have been calculated usingsingle-particle radial wave functions of Woods-Saxon potential andharmonic-oscillator potential for comparison. The calculations for theground charge density distributions using the Woods-Saxon potentialshow good agreement with experimental data for 4He nucleus whilethe results for 12C and 16O nuclei are better in harmonic-oscillatorpotential. The calculated elastic charge form factors in Woods-Saxonpotential are better than the results of harmonic-oscillator potential.Finally, the calculated root mean square radii usingWoods-Saxonpotentials ho
... Show MoreThe nuclear charge density distributions, form factors and
corresponding proton, charge, neutron, and matter root mean square
radii for stable 4He, 12C, and 16O nuclei have been calculated using
single-particle radial wave functions of Woods-Saxon potential and
harmonic-oscillator potential for comparison. The calculations for the
ground charge density distributions using the Woods-Saxon potential
show good agreement with experimental data for 4He nucleus while
the results for 12C and 16O nuclei are better in harmonic-oscillator
potential. The calculated elastic charge form factors in Woods-Saxon
potential are better than the results of harmonic-oscillator potential.
Finally, the calculated root mean square