1-1-diphenyl-2-picrylhydrazyl and Carcinoma--Ehrlich-Tumor

Amaranthus (Amaranthaceae) has previously been reported to possess different bioactive phytochemicals including phenols, tannins and flavonoids. The current study was designed to evaluate the antioxidant, anti-proliferative and antimicrobial activity of stem and seed extracts of Amaranthus lividus (AL) and Amaranthus hybridus (AH), respectively.. Antioxidant activity of methanol extract was assessed by DPPH radical scavenging assay. Determination of lectin activity of Amaranthus extract was carried out using hemagglutination assay on mouse blood. A total of thirty six Swiss albino mice containing Ehrlich's ascites carcinoma (EAC) cells were treated with AL and AH extract at 25, 50 and 100 μg/ml/day/mouse for six days. Growth inhibitory activity was determined by haemocytometer counting of EAC cells using trypan blue dye and DAPI (4΄,6-diamidino-2-phenylindole) staining was used to assess apoptotic cells. Gene amplification study was conducted to observe the expression pattern of p53, Bax, Bcl-2 and caspase-3 mRNA using PCR (polymer chain reaction) technique. In vitro susceptibility of five pathogenic bacteria including Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, Salmonella typhi and Staphylococcus aureus was detected using disk diffusion assay.. The radical scavenging assay indicated that AH and AL possesses potent antioxidant potential, exhibiting IC50 value of 28 ± 1.5 and 93 ± 3.23 μg/ml, respectively. Hemagglutination assay revealed that AH and AL agglutinated mice blood at 1.565 and 3.125 μg/wall, respectively. Administration of AH and AL extract led to 45 and 43 % growth inhibition of EAC cells, respectively at 100 μg/ml with marked features of apoptosis including cell shrinkage, condensation of cytoplasm and aggregation of apoptotic bodies etc. Up-regulation of p53, Bax and caspase-3 and down-regulation of Bcl-2 mRNA in Amaranthus treated mice indicated mitochondria mediated apoptosis of EAC cells in comparison with control. None of the bacterial species showed susceptibility to the extract of both the Amaranthus species.. Our current findings suggest that both of the Amaranthus species have strong antioxidant, lectin and anti-proliferative activity on EAC cells. The current anticancer potential was observed due mainly to the mitochondria mediated apoptosis of EAC cells.

Topics: Amaranthus; Animals; Anti-Infective Agents; Antineoplastic Agents, Phytogenic; Antioxidants; Bangladesh; Biphenyl Compounds; Carcinoma, Ehrlich Tumor; Drug Screening Assays, Antitumor; Female; Indoles; Mice; Microbial Sensitivity Tests; Picrates; Plant Extracts; Vegetables

A new series of complexes of Ni(II), Co(II), Cu(II), Cd(II), Mn(II), Hg(II) and UO2(2+) derived from 2-acetylpyridine-α-naphthoxyacetylhydrazone (HA2PNA) have been prepared and characterized by elemental analyses, spectral (IR, UV-visible, ESR and (1)H NMR) as well as magnetic and thermal measurements. The data revealed that the ligand acts as neutral NO, NN and NNO or mono-negative NNO chelate. On the basis of electronic spectral and magnetic moment data, an octahedral geometry is suggested for Mn(II), Co(II), Ni(II) and UO2(2+) complexes and a square planar arrangement for Cu(II) complex. The bond length, bond angle, HOMO, LUMO, dipole moment and charges on the atoms have been calculated to confirm the geometry of the ligand and the investigated complexes. The kinetic parameters were determined for thermal degradation stages of some complexes using Coats-Redfern and Horowitz-Metzger methods. Also, the ligand and its complexes were screened against antibacterial, antioxidant using DPPH radical and antitumor activities using in vitro Ehrlich ascites assay.

Topics: Animals; Antineoplastic Agents; Antioxidants; Bacteria; Biphenyl Compounds; Carcinoma, Ehrlich Tumor; Coordination Complexes; Electron Spin Resonance Spectroscopy; Electrons; Free Radical Scavengers; Hemolysis; Hydrazones; Kinetics; Ligands; Magnetic Phenomena; Mice; Microbial Sensitivity Tests; Models, Molecular; Molecular Conformation; Naphthalenes; Picrates; Pyridines; Rats; Spectrophotometry, Infrared; Static Electricity; Structure-Activity Relationship; Thermogravimetry

roxburghii. Anticancer activity of MMR has been carried out on Ehrlich ascites carcinoma (EAC) cells with three different doses (20, 40 and 60 mg/kg/day) by observing different parameters such as tumor weight, survival time of EAC-bearing mice, growth inhibition of EAC cells, morphological changes and nuclear damage of EAC cells etc. whereas antioxidant activity was determined by measuring total antioxidant, DPPH free radical scavenging, ferrous reducing capacity assay. The extract showed highest anticancer activity at 60 mg/kg day¬-⁻¹(i.p.). It caused 81.4% (P<0.01) cells growth inhibition and reduced tumor burden significantly (78.5%; P<0.001) in comparison to control. It also increased life span of EAC-bearing mice significantly (73.5%; P<0.01). MMR treated EAC cells showed membrane blebbing, chromatin condensation, nuclear fragmentation (apoptotic feature) in Hoechst 33342 staining under fluorescence microscope. DNA fragmentation assay in agarose gel (1.5%) electrophoresis also rectified that it causes EAC cells death by apoptosis. MMR also exhibited moderate antioxidant properties in dose dependent manner. Thus, this plant can therefore be considering a resource for natural chemo-preventive drugs as well as a possible pharmaceutical supplement.

Topics: Animals; Antineoplastic Agents; Antioxidants; Apoptosis; Biphenyl Compounds; Carcinoma, Ehrlich Tumor; Cell Line, Tumor; DNA Fragmentation; Dose-Response Relationship, Drug; Lethal Dose 50; Male; Methanol; Mice; Phytotherapy; Picrates; Plant Extracts; Plant Leaves; Plants, Medicinal; Rubiaceae; Solvents; Time Factors; Tumor Burden

The chelating behavior of the ligand (H2APC) based on carbohydrazone core modified with pyridine end towards Cr(III), Mn(II) and Fe(III) ions have been examined. The (1)H NMR and IR data for H2APC revealed the presence of two stereoisomers syn and anti in both solid state and in solution in addition to the tautomeric versatility based on the flexible nature of the hydrazone linkage leading to varied coordination modes. The spectroscopic data confirmed that the ligand behaves as a monobasic tridentate in Cr(III) and Fe(III) complexes and as neutral tetradentate in Mn(II) complex. The electronic spectra as well as the magnetic measurements confirmed the octahedral geometry for all complexes. The bond length and angles were evaluated by DFT method using material studio program for all complexes. The thermal behavior and the kinetic parameters of degradation were determined using Coats-Redfern and Horowitz-Metzger methods. The antioxidant (DDPH and ABTS methods), anti-hemolytic and cytotoxic activities of the compounds have been screened. Cr(III) complex and H2APC showed the highest antioxidant activity using ABTS and DPPH methods. With respect to in vitro Ehrlich ascites assay, H2APC exhibited the potent activity followed by Fe(III) and Cr(III)complexes.

Topics: Animals; Antioxidants; Biphenyl Compounds; Carcinoma, Ehrlich Tumor; Chromium; Coordination Complexes; Electrons; Erythrocytes; Free Radical Scavengers; Hemolysis; Heterocyclic Compounds; Hydrazones; Iron; Kinetics; Ligands; Magnetic Resonance Spectroscopy; Manganese; Metals, Heavy; Mice; Models, Molecular; Molecular Conformation; Picrates; Pyridines; Rats; Spectrophotometry, Infrared; Thermodynamics; Thermogravimetry; Urea

The chelating behavior of ligands based on carbohydrazone core modified with pyridine end towards Co(II), Ni(II) and Cu(II) ions have been examined. The ligands derived from the condensation of carbohydrazide with 2-acetylpyridine (H(2)APC) and 4-acetylpyridine (H(2)APEC). The (1)H NMR, IR data and the binding energy calculations of H(2)APC revealed the presence of two stereoisomers syn and anti in the solid state and in the solution. The (1)H NMR, IR data and the binding energy calculations confirmed the presence of H(2)APEC in one keto form only in the solid state and in the solution. The spectroscopic data confirmed that H(2)APC behaves as a monobasic pentadentate in Co(II) and Cu(II) complexes and as mononegative tetradentate in Ni(II) complex. On the other hand, H(2)APEC acts as a mononegative tridentate in Co(II) complex, neutral tridentate in Ni(II) complex and neutral bidentate in Cu(II) complex. The electronic spectra and the magnetic measurements of complexes as well as the ESR of the copper complexes suggested the octahedral geometry. The bond length and bond angles were evaluated by DFT method using material studio program. The thermal behavior and the kinetic parameters of degradation were determined using Coats-Redfern and Horowitz-Metzger methods. The antioxidant (DDPH and ABTS methods), anti-hemolytic and in vitro Ehrlich ascites of the compounds have been screened.

Topics: Animals; Antineoplastic Agents; Antioxidants; Benzothiazoles; Biphenyl Compounds; Carcinoma, Ehrlich Tumor; Cobalt; Copper; Electron Spin Resonance Spectroscopy; Electrons; Erythrocytes; Free Radical Scavengers; Hemolysis; Hydrazones; Inhibitory Concentration 50; Kinetics; Ligands; Magnetic Resonance Spectroscopy; Mice; Models, Molecular; Nickel; Picrates; Pyridines; Rats; Spectrophotometry, Infrared; Sulfonic Acids; Thermogravimetry