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 this research, optical communication coding systems are designed and constructed by utilizing Frequency Shift Code (FSC) technique. Calculations of the system quality represented by signal to noise ratio (S/N), Bit Error Rate (BER),and Power budget are done. In FSC system, the data of Nonreturn- to–zero (NRZ ) with bit rate at 190 kb/s was entered into FSC encoder circuit in transmitter unit. This data modulates the laser source HFCT-5205 with wavelength at 1310 nm by Intensity Modulation (IM) method, then this data is transferred through Single Mode (SM) optical fiber. The recovery of the NRZ is achieved using decoder circuit in receiver unit. The calculations of BER and S/N for FSC system a
... Show MoreProsthetic hands are compensatory devices for the hand amputees as a result of injury, various accidents or birth deformities, types of prosthetic hand vary depending on the mechanism they operate and how they perform. There are common types in use that are characterized by their complex mechanisms, which are difficult for the amputee to use or exclude use because of their high cost, therefore the aim of this research is to design an artificial hand that is suitable in terms of simplicity of use and low cost and similar to a natural hand with regard to dimensions and shape that operated in the mechanism of links. This research involves Stress and strain analysis of the prosthetic hand and its fingers that modelled from (Petg CR)
... Show MoreThis paper proposes a new structure of the hybrid neural controller based on the identification model for nonlinear systems. The goal of this work is to employ the structure of the Modified Elman Neural Network (MENN) model into the NARMA-L2 structure instead of Multi-Layer Perceptron (MLP) model in order to construct a new hybrid neural structure that can be used as an identifier model and a nonlinear controller for the SISO linear or nonlinear systems. Weight parameters of the hybrid neural structure with its serial-parallel configuration are adapted by using the Back propagation learning algorithm. The ability of the proposed hybrid neural structure for nonlinear system has achieved a fast learning with minimum number
... Show MoreSixty four local isolated of Klebsiella spp. have been isolated from environment samples (soil and water). These isolates were identified and diagnosis according to phenotype and biochemical tests. These isolates were subjected to primary and secondary screening, to select the isolate with the highest laccase activity. Fifteen isolates chosen from primary screening for screening their enzyme activity in secondary screening. It has been found the Klebsiella(K7) has the highest productivity of the enzyme (12 Unit/ml).Klebsiella(K7) isolate was diagnosis by Vitak 2 system, it was identified asK. pneumonia. The laccase purified was characterization, the experiments showed that: The molecular weight of laccase was 120KD and the optimum pH for th
... Show MoreFlurbiprofen (FLB) is chemically 2-(3- fluoro-4-phenyl phenyl) propanoic acid. It is a nonsteroidal anti-inflammatory drug (NSAID) used in the treatment of rheumatoid arthritis and osteoarthritis. Oral administration of this drug is associated with severe gastrointestinal side effects like ulceration and gastrointestinal bleeding. The solution to this problem lies in the fact that topically applied NSAIDs are safer than orally. This study aims to prepare different topical semisolid formulation of FLB as cream base (o/w), (w/o) and gel base using different gel-forming agents in different concentrations. Comparing characterization properties in addition to release and diffusion study for all the prepared formulas to select the best on
... Show MoreThe aim of this paper, study the effect of carbon nanotubes on the electrical properties of polyvinylchloride. Samples of polyvinylchloride carbon nanotubes composite prepared by using hot press technique. The weight percentages of carbon nanotubes are 0,5,10 and 20wt.%. Results showed that the D.C electrical conductivity increases with increasing of the weight percentages of carbon nanotubes. Also, the D.C electrical conductivity changed with increase temperature for different concentrations of carbon nanotubes. The activation energy of D.C electrical conductivity is decreased with increasing of carbon nanotubes concentration.
In this work ester derivatives were synthesized by the reaction of imidazole derivatives (C1) with ethylchloroacetate in ethanol and NaOH to give the corresponding (C2) .While compound (C3) acetohydrazide was synthesized by the reaction of ester derivatives (C2) with hydrazine hydrat in ethanol. Compound (C3) from the reaction with different aromatic aldehydes in absolute ethanol gave the Schiff′s bases (C4,C5). The product compounds were characterized by FT-IR, U.V and 1HNMR spectra and the biological activities were studied as antibacterial.