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.
Objective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs, like candesartan cilexetil (CC). CC is a class II drug used for the treatment of hypertension. Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β‑cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β‑cyclodextrin. Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were used to study compatibility. Results: The angle of repose determination showed good flow for most of the formulas, besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement sho
... Show MoreThe study aimed to purification of acid phosphatase (ACP) from sera of obesetype 2 diabetes mellitus patients, this study included from thirty T2DM patients and thirty control, purification process was done with several steps included precipitation with inorganic salt (NH4 ) 2SO4 30%-80%, dialysis, ion exchange chromatography by DEAE sepharose anion column and size exclusion chromatography by Sepharose 6B.ACP, BMI, FBS, HbA1c, Lipid profile, Urea, Creatinie, Insuline, Homa-IR were determined. Results showed the precipitate and concentrated protein appeared four peaks in ion exchange column. ACP located in the first and second peak with purification fold (21.1), (37.2) yield of enzyme and specific activity (173.3) IU/ml, which obtained a si
... Show MoreObjective: Matrix tablet approach is one of the delivery systems intended for poorly water-soluble drugs, like candesartan cilexetil (CC). CC is a class II drug used for the treatment of hypertension. Methods: Matrix tablets from (F1x to F18z) were prepared in the presence of β‑cyclodextrin. Matrix tablet formulation ensures control release of the drug and higher dissolution by β‑cyclodextrin. Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were used to study compatibility. Results: The angle of repose determination showed good flow for most of the formulas, besides having good compressibility. Weight variation test for all formulas showed accepted value. Drug content measurement sho
... Show MoreIn recent years, observed focus greatly on gold nanoparticles synthesis due to its unique properties and tremendous applicability. In most of these researches, the citrate reduction method has been adopted. The aim of this study was to prepare and optimize monodisperse ultrafine particles by addition of reducing agent to gold salt, as a result of seed mediated growth mechanism. In this research, gold nanoparticles suspension (G) was prepared by traditional standard Turkevich method and optimized by studying different variables such as reactants concentrations, preparation temperature and stirring rate on controlling size and uniformity of nanoparticles through preparing twenty formulas (G1-G20). Subsequently, the selected formula that pr
... Show MoreThis research was aimed to the purification and characterization of cytosine deaminase as a medically important enzyme from locally isolated Escherichia coli; then studying its cytotoxic anticancer effects against colon cancer cell line. Cytosine deaminase was subjected to three purification steps including precipitation with 90% ammonium sulfate saturation, ion exchange chromatography on DEAE-cellulose column, and gel filtration chromatography throughout Sephadex G-200 column. Specific activity of the purified enzyme was increased up to 9 U/mg with 12.85 folds of purification and 30.85% enzyme recovery. Characterization study of purified enzyme revealed that the molecular weight of cytosine deaminase produced by E. coli was about 48 KDa,
... Show MoreThis study aimed for isolation and identification of Candida glabrata and identifying some virulence factors. The distribution of patients with candidemia thrush showed that the age group 50-65 years old recorded the highest incidence of candidiasis in female and male with leukemia by 50% and 37.9 % respectively compared to the lowest incidence of candidiasis in the age group under 17 years old in female and male 8.8% and 13.5%, respectively. While the age group between 5-8 years was high, reaching 18 cases of oral candidiasis and 42% of children with leukemia compared with the age group, which was the least, that reached 9 cases, 21%. The highest incidence of C. glabrata was 59 isolates of females and males with leukemia, while C. kefyer w
... Show MoreManganese sulfate and Punica granatum plant extract were used to create MnO2 nanoparticles, which were then characterized using techniques like Fourier transform infrared spectroscopy, ultraviolet-visible spectroscopy, atomic force microscopy, X-ray diffraction, transmission electron microscopy, scanning electron microscopy, and energy-dispersive X-ray spectroscopy. The crystal's size was calculated to be 30.94nm by employing the Debye Scherrer equation in X-ray diffraction. MnO2 NPs were shown to be effective in adsorbing M(II) = Co, Ni, and Cu ions, proving that all three metal ions may be removed from water in one go. Ni(II) has a higher adsorption rate throughout the board. Co, Ni, and Cu ion removal efficiencie
... Show MoreManganese sulfate and Punica granatum plant extract were used to create MnO2 nanoparticles, which were then characterized using techniques like Fourier transform infrared spectroscopy, ultraviolet-visible spectroscopy, atomic force microscopy, X-ray diffraction, transmission electron microscopy, scanning electron microscopy, and energy-dispersive X-ray spectroscopy. The crystal's size was calculated to be 30.94nm by employing the Debye Scherrer equation in X-ray diffraction. MnO2 NPs were shown to be effective in adsorbing M(II) = Co, Ni, and Cu ions, proving that all three metal ions may be removed from water in one go. Ni(II) has a higher adsorption rate throughout the board. Co, Ni, and Cu ion removal efficiencies were 32.79%, 75
... Show MoreThe present study was conducted to estimate the antimicrobial activity and the potential biological control of the killer toxin produced by
This study includes using green or biosynthesis-friendly technology, which is effective in terms of low cost and low time and energy to prepare V2O5NPs nanoparticles from vanadium sulfate VSO4.H2O using aqueous extract of Punica Granatum at a concentration of 0.1M and with a basic medium PH= 8-12. The V2O5NPs nanoparticles were diagnosed using several techniques, such as FT-IR, UV-visible with energy gap Eg = 3.734eV, and the X-Ray diffraction XRD was calculated using the Debye Scherrer equation. It was discovered to be 34.39nm, Scanning Electron Microscope (SEM), Transmission Electron Microscopy TEM. The size, structure, and composition of synthetic V2O5NPs were determined using the (EDX) pattern, Atomic force microscopy AFM. The a
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