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.
Some metal ions (Mn
+2
, Fe
+2
,Co
+2
,Ni
+2
,Cu
+2
, Cd
+2
and Hg
+2
) complexes of N-acetyl
Tryptophan( AcetrpH) and (2, 2′-bipyridine) (2, 2′-Bipy)have been synthesized and then
characterized on the basis of their FT-IR, UV-Vis spectroscopy, magneticsuscptibity
conductivity measurements and atomic absorption;from the results obtained and the propsed
molecular structure for these complexes as octahedral geometry,the following general formula
has been given for the prepared complexes.
[M
+n
(Acetrp)2(2, 2′-Bipy)].
Where M= Mn
+2
, Fe
+2
,Co
+2
,Ni
+2
,Cu
+2
, Cd
+2
,Hg
+2
(Acetrp)
-=Ligand ion(N-acetyl
The problem of the research came through the following question (what is the effectiveness of active design in contemporary industrial products), and it emphasized the importance of research to make society with its members in a positive state of activity, and what can help the industrial product design to achieve this, but the goal of the study is (determining the characteristics and principles of design Active and its effectiveness in the industrial product), and the study was determined by industrial products related to daily, recreational and sports activity, The researcher relied on a form to determine the axes of analysis for the sample models, in order to reach the results of the research, the most important of which are: Realiz
... Show MoreDue to the importance of Laser usage in the field of skin diseases Like removing. the cicatrix (acne causes). skin lines, cone spots, two laser systems have underwent a study and evaluation for their use in treatingthe skin diseases.
The research deals with desigrrating an optical system .The system is for concentrating the laser beam C02 with a wave length of
10.6 micrometer Descriptions of 1he system and value of the
perfonnance
... Show MoreTwo Prototypes of Transversely Excited at atmospheric pressure (TEA) Nitrogen laser systems (One Stage Blumlein Circuit and Two Stage Blumlein Circuit) were fabricated and operated. High voltage power supply with variable operating voltage (0-20 kv) and operating current (1-3A) was built and tested successfully. The gas flow rate of 15 L/ min and 10 L/ min for OSBC and TSBC was used. The performance of the fabricated systems was studied extensively reaching to the optimum operating conditions. The obtained laser output energy for the first system has linear relationship with the applied voltage. The maximum output energy was about (1.14 mJ) with (10.40) ns pulse duration and the half-wave divergence angle was about (0.1455 m rad). In the
... Show MoreThis work involves synthesis of novel Schiff bases derivatives contining isoxazoline or pyrazoline units starting with chalcons . 4-Aminoacetophenone was reacted with 3-nitrobenzaldehyde in basic medium giving chalcone [I] by claisen-schemidt reaction. The chalcone [I] was reacted with hydroxylamine hydrochloride giving isoxazoline [II] in basic medium. The chalcone [I] could also react with hydrazitne hydrate to give pyrazoline [III] . The novel Schiff bases with structural formula [IV] and [V] were prepared by the reaction of amino compounds ; isoxazoline [II] and pyrazolines [III] with p-substituted aldehydes or p-subsituted ketones, respectively in dry benzene using drops of glacial acetic acid as a cat
... Show MoreMercury-lead-antimony based superconductors with the formula Hg0.5 Pb0.5xSbxBa2Ca2Cu3O8+δ (x=0, 0.10 and 0.15) have been prepared by useing three step solid state reaction processes. Electrical resistivity, using four probe technique, is used to find the transition temperature Tc. It is found from that sample Hg0.5 Pb0.5Ba2Ca2Cu3O8.437 is semiconductor , sample Hg0.5 Pb0.4Sb0.1Ba2Ca2Cu3O8.353 is normal state with metallic behaviors, while sample Hg0.5 Pb0.35Sb0.15Ba2Ca2Cu3O8.233 is superconducting state with critical transition temperature (Tc) is 126K. X-ray diffraction (XRD) analysis showed a tetragonal structure with decrease in the c-axis lattice constant for the samples doped with Sb as compared with these which have no Sb
... Show MoreThe operating characteristics of optoelectronic devices depend critically on the properties physical of the constituent materials, interesting compound has been focused on this research formed from group III and V of the periodic table. Thin film n-InSb heterjuntion were successfully fabricated on p-Si substrates by thermal evaporation technique at different annealing temperature (as prepared, 400,500,600) °C. The effect of annealing temperature on the structural, surface morphology, optical and optoelectronic properties of InSb films were investigated and studied. The crystal structure of the film was characterized by X-ray diffraction and techniques. AFM techniques inspect the surface morphology of InSb films, the study presented the val
... Show MoreLetrozole (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.