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.
This study includes a physiochemical and a spectrocpical characterization to some alkaloid compounds in the (ANAB AL- THEAB) plant (Solanum nigrun L.). It’s the most important medicinal herb belonging to the family (Solanaceae). Acid hydrolysis was performed by using limited conc. of Hcl and H2SO4, to obtain the aglycon part of previously separated steroidal componants as (A, B and C). The characterization of the(A,B and C) compounds indicates that they varied between them as the separated steroidal like-alkaloids, carried by using melting point (m.p.), thin layer chromatography (TLC), Infra -Red spectroscopy (IR) and Ultra violet-Visible spectroscopy (UV - Visible).High perfor
... Show MoreA new ligand complexes have been synthesis from reaction of metal ions of MnII , CoII , NiII , CuII , ZnII , CdII and PdII with schiff base [(E)-1-((2-amino-5-(3, 4, 5-trimethoxybenzyl) pyrimidin-4-ylimino) methyl) naphthalen-2-ol [HL)]. The prepared [HL] was characterized by FT-IR, UV-Vis spectroscopy, 1H13CNMR spectra Mass spectra and melting point. The compounds were characterized by techniques UV-Vis and FT-IR spectral studies, micro analysis (C.H.N), determination of atomic absorption, chloride content, molar conductivity measurements, magnetic susceptibility and melting point. The ligand acts as a monobasic tridentate, coordinating through deprotonated phenolic O and azomethine N atoms. The compounds are neutral electrolytic in dimeth
... Show MoreThis research presents a response surface methodology (RSM) with I‐optimal method of DESIGN EXPERT (version 13 Stat‐Ease) for optimization and analysis of the adsorption process of the cyanide from aqueous solution by activated carbon (AC) and composite activated carbon (CuO/AC) produced by pyro carbonic acid microwave using potato peel waste as raw material. Pyrophosphate 60% (wt) was used for impregnation with an impregnation ratio 3:1, impregnation time of 4 h at 25°C, radiant power of 700 W, and activation time of 20 min. Batch experiments were conducted to determine the removal efficiency of cyanide from aqueous solution to evaluate the influences of various experimental parameters su
Background: Although mammography is a powerful screening tool in detection of early breast cancer, it is imperfect, particularly for women with dense breast, which have a higher risk to develop cancer and decrease the sensitivity of mammogram, Automated breast ultrasound is a recently introduced ultrasonography technique, developed with the purpose to standardize breast ultrasonography and overcome some limitations of handheld ultrasound, this study aims to evaluate the diagnostic efficacy of Automated breast ultrasound and compare it with handheld ultrasound in the detection and characterization of breast lesions in women with dense breasts.
Objectives:<
... Show MoreBackground: Although mammography is a powerful screening tool in detection of early breast cancer, it is imperfect, particularly for women with dense breast, which have a higher risk to develop cancer and decrease the sensitivity of mammogram, Automated breast ultrasound is a recently introduced ultrasonography technique, developed with the purpose to standardize breast ultrasonography and overcome some limitations of handheld ultrasound, this study aims to evaluate the diagnostic efficacy of Automated breast ultrasound and compare it with handheld ultrasound in the detection and characterization of breast lesions in women with dense breasts. Objectives: To evaluate the diagnostic efficacy of Automated breast ultrasound and compare
... Show More