This 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, the highest enzyme activity at pH 8.5, and is most stable at pH 7.5 - 9, the enzyme also showed a full activity at a range of temperatures between 45-60 0C. Enzyme activity was strongly inhibited in the presence of mercuric chloride and copper sulphate, when added individually at a constant concentration. However, calcium chloride, manganese chloride and ferric chloride caused a little increase in enzyme activity while sodium azide had no effect on enzyme activity. Upon cytotoxic effect study through micro-cultured tetrazolium assay (MTT) against Caco-2 cell line. Purified cytosine deaminase was found to inhibit the growth of Caco-2 cancer cell line with an IC50 of 242.5 ?g/ml in a comparison to an IC50 of 1864 ?g/ml for crude enzyme. Besides, the enzyme didn’t show significant effect on WRL normal cell line.
Coumarin derivatives have shown different biological activities, such as antifungal, antibacterial antiinflammatory, and antioxidant activities, besides antibiotic resistance modulating effects, and anti-HIV, hepatoprotective, and antitumor effect. So, new coumarin derivatives (hydrazones and an amide) were synthesized through multisteps reactions. All the synthesized target compounds were characterized by FT-IR spectroscopy, 1HNMR analysis. The compounds then evaluated for their anti-bacterial activity by means of well-diffusion method against two gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae) and two gram-negative bacteria (E.coli and Pseudomonas aeruginosa). The highest activity was demonstr
... Show MoreIn this work, we focused on studying 1,4-naphthoquinones and their derivatives, and knowing the methods of preparing them using different auxiliary agents and forming derivatives containing heterocyclic rings, active groups and saturated rings containing heterogeneous elements . In addition, due to their strong antibacterial, antifungal and anticancer activity, 1,4-naphthoquinone compounds biological importance and are considered a source of various pharmaceutical compounds.
The development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1
... Show MoreZerumbone is a well-known compound having anti-cancer, anti-ulcer, anti-inflammatory and anti-hyperglycemic effects. During its use for the disease treatment, the membrane of erythrocyte can be affected by consumption of this bioactive compound. The current study was the first report of investigation of the hemolytic activities on human erythrocytes and cytotoxic profile of zerumbone. The toxicity of zerumbone on human erythrocytes was determined by in vitro hemolytic assay. Brine shrimp lethality assay was used to evaluate the cytotoxic effect of zerumbone at concentrations 10, 100 and 1000 μg/mL. The human erythrocyte test showed no significant toxicity at low concentrations, whereas hemolytic effect was amplified up to 17.5
... Show MoreZerumbone is a well-known compound having anti-cancer, anti-ulcer, anti-inflammatory and anti-hyperglycemic effects. During its use for the disease treatment, the membrane of erythrocyte can be affected by consumption of this bioactive compound. The current study was the first report of investigation of the hemolytic activities on human erythrocytes and cytotoxic profile of zerumbone. The toxicity of zerumbone on human erythrocytes was determined by in vitro hemolytic assay. Brine shrimp lethality assay was used to evaluate the cytotoxic effect of zerumbone at concentrations 10, 100 and 1000 μg/mL. The human erythrocyte test showed no significant toxicity at low concentrations, whereas hemolytic effect was amplified up to 17.5 % at
... Show MoreHere, we synthesized three new blended ligand complexes of chromium (III), iron (III), and lanthanum (III) ions with a Schiff base made from the condensation of [o-aminophenol and 2-hydroxyacetophenone in the presence of concentrated sulphoric acid (HL1)] as a primary ligand and o-nitroaniline (L2) as a secondary. The Schiff base and its dual ligand chelate were characterized using several spectroscopic studies, IR, 1HNMR, electronic and mass spectra, in addition to elemental analyses, molar conductivity measurements, and magnetic moments. The spectroscopic and analytical outcomes confirmed the formation of the chelates in a 1:1:1(L1: M: L2) ratio. Similarly, an octahedral structure became counseled for all chelates.
Lignans are natural products widely distributed in the plant kingdom. They are composed of two β-β-linked phenylpropane (shikimate-derived biogenetic subunits). Although the backbone of lignans is composed of phenylpropane units, there is enormous diversity in the structure of lignans leading to different classes of lignans, such as γ-butyrolactone derivatives, eg. Hymatairesinol, bicyclooctadiene derivatives, e.g. pinoresinol, tetrahydrofuran derivatives e.g.lariciresinol, di-arylbutandiol derivatives, e.g. secoisolariciresinol. Introduction of a further carbon –carbon linkage leads to a class of lignans collectively known as cyclolignans such as tetrahydro-naphthalene derivatives, for example podophyllotoxin. Lignans ha
... Show MoreIn this paper, some chalcone derivatives (C1, C2) were synthesized based on the reaction of equal amount of substituted acetophenone and substituted banzaldehyde in basic medium. Oxazine and thiazine derivatives were prepared from the reaction of chalcones (C1-C2) with urea and thiourea respectively in a basic medium. Pyrazole derivatives were prepared based on the reaction of chalcones with hydrazine mono hydrate or phenyl hydrazine in the presence of glacial acetic acid as a catalyst. The new synthesized compounds were identified using various physical techniques like1 H-NMR and FT-IR spectra.