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ABSTRACT: The synthesis and molecular and supramolecular structures of the compound (6-amino-1-methyl-5-nitrosouracilato-N3)-triphenylphosphine-gold(I) with interesting abilities to inhibit tumor growth in an animal model of experimental glioma are reported. Thus, its antitumor properties, effects on both enzyme and non-enzyme antioxidant defense systems and the response of several biochemical biomarkers have been analyzed. After seven days of treatment, the gold compound decreased the tumor growth to ca. one-tenth and reduced oxidative stress biomarkers (thiobarbituric acid-reactive substances (TBARS) and protein oxidation levels) compared to animals treated with the vehicle. Also, gold compound maintained non-enzyme antioxidant defense systems as in non-tumor animals and increased enzyme antioxidant defenses, such as superoxide dismutase and glutathione peroxidase activities, and decreased catalase activity. Analysis of serum levels of electrolytes, nitrogenous compounds, glucose, lipids, total protein, albumin, transaminases and alkaline phosphatase indicated that gold compound treatment showed few adverse effects, while effectively inhibiting tumor growth through mechanisms that involved endogenous antioxidant defenses.
European journal of medicinal chemistry 04/2013; 64C:260-272. · 3.27 Impact Factor
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ABSTRACT: Hypercholesterolemia and low testosterone concentrations in men are associated with a high risk factor for atherosclerosis. It is known that cholesterol serves as the major precursor for the synthesis of the sex hormones. The bioactive peptides of the renin-angiotensin-system localized in the gonads play a key role in the relation between cholesterol and testosterone by modulating steroidogenesis and inhibiting testosterone production. In the present work, we evaluated the effects of diet-induced hypercholesterolemia on circulating testosterone levels and its relationship with the testicular RAS-regulating specific aminopeptidase activities in male mouse. A significant decrease in serum circulating levels of testosterone was observed after induced hypercholesterolemia. The changes found in aminopeptidase activities suggest a role of Ang III and Ang IV in the regulation of steroidogenesis.
General and Comparative Endocrinology 04/2011; 173(1):15-9. · 3.27 Impact Factor
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ABSTRACT: Three new Cd(II) complexes with the Schiff base ligand derived from the condensation 1+2 of 2,6-diacetylpyridine and 5,6-diamino-1,3-dimethyluracil have been "in template" synthesized. The molecular structures of complexes were determined by single-crystal X-ray diffraction. The metal center shows a very distorted mer-bis-tridentate CdN(6) octahedral geometry as consequence of the reduced bite angles of the ligand and the existence of long-distanced interactions with donor atoms in the neighbourhood. The luminescent properties of complexes in CH(3)CN solution were investigated showing the emission energies depend on the uracil part of the ligand. The evaluation of their biological properties against C6 glioma cell line indicates that cadmium(II) complexes could be an interesting tools to treat drug-resistant brain tumors.
Journal of inorganic biochemistry 09/2009; 103(8):1176-84. · 3.25 Impact Factor
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ABSTRACT: A number of new asymmetric azines derived from hydrazine and 6-acetyl-1,3,7-trimethyllumazine (lumazine=pteridine-2,4(1H,3H)-dione) and its derivatives with several aromatic aldehydes have been prepared and characterized by usual procedures (XRD, IR, (1)H and (13)C NMR). These were reacted with [ReCl(CO)(5)] to give the corresponding mononuclear chloro-fac-tricarbonylrhenium(I) [ReCl(CO)(3)L] compounds. The complexes were characterized by elemental analysis, thermogravimetry (TG) and differential scanning calorimetry (DSC), IR, (1)H and (13)C NMR. Furthermore, single-crystal X-ray diffraction studies have also allowed to report two different coordination modes of the ligands, which are strongly influenced by the basicity of the heteroatoms on the aromatic aldehyde; thus, the hydrazones derived from hydrazine and hydroxyaldehydes are linked to Re(I) through N5 atom from the pyrazine ring and the N61 one from the hydrazino group, whereas with the ligand derived from pyridin-2-carbaldehyde, the N62 atom of the hydrazino group and the N1 from the pyridine moiety are preferred ligand-to-metal binding sites. The study of the effects of the compounds on the growth of four human tumor cell lines (neuroblastoma NB69, glioma U373, and breast cancer MCF-7 and EVSA-T) suggests a modulator behaviour, according to the concentration, of cell growth due to their estrogen-like characteristics.
Journal of inorganic biochemistry 11/2008; 103(1):94-100. · 3.25 Impact Factor
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ABSTRACT: A series of mononuclear complexes with Co(II), Ni(II), Cu(II), Zn(II), Hg(II), Mo(VI) and Pd(II) containing the ligand derived from the 1:2 condensation of 2,6-diformyl-4-methylphenol and 5,6-diamino-1,3-dimethyluracil (hereafter denoted as BDFDAAU) were synthesized. The complexes were characterized by elemental analysis, thermogravimetry (TG) and differential scanning calorimetry (DSC), IR, (1)H, (13)C and (15)N NMR, UV-visible-near IR (UV-VIS-NIR), EPR and magnetic measurements. The deprotonated ligand in the phenolic oxygen shows a symmetric tridentate coordination mode through the two azomethine nitrogen atoms and the phenolic oxygen atom whereas the coordination of the neutral ligand takes place through the phenolic oxygen atom and one azomethine nitrogen atom. In the Mo(VI) complex, the ligand is bideprotonated in the phenolic oxygen and an amino group from one uracil unit; so, the coordination mode changes again into an asymmetric way: phenolic oxygen atom, one azomethine nitrogen atom and the nitrogen atom from the deprotonated amino group. The antiproliferative behaviour against the five human tumor cell lines (human neuroblastoma NB69, human breast cancer MCF-7 and EVSA-T, human glioma H4 and human bladder carcinoma cell line ECV) suggested a modulator behaviour, according to the concentration, of cell growth due to their estrogen-like characteristics.
Journal of Inorganic Biochemistry 05/2008; 102(4):647-55. · 3.35 Impact Factor
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ABSTRACT: New complexes of rhenium(I) with some 5-nitrosopyrimidines with general formula [ReCl(CO)3L] have been prepared and characterized by elemental analysis, conductivity measurements, IR and 1H, 13C and 15N NMR spectroscopic methods. The complexes appear to be monomeric and the pyrimidine ligands act in a neutral form. The structure of [ReCl(CO)3(DANU)].CH3CN has been solved by X-ray diffraction. The coordination environment around the Re(I) may be described as a distorted octahedron in which the ligand behaves in a bidentate fashion through N5 and O4 atoms, making a five-membered chelate ring. The coordination sphere is completed with three carbonyl groups in fac-arrangement and one chlorine atom. The evaluation of the antiproliferative behavior against five human tumor cell lines (human breast cancer MCF-7 and EVSA-T, human neuroblastoma NB69, human glioma H4 and human bladder carcinoma cell line ECV) suggested a modulator behavior of cell growth at low concentrations due to their estrogenic-like characteristics.
Journal of Inorganic Biochemistry 09/2005; 99(8):1637-45. · 3.35 Impact Factor
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ABSTRACT: The synthesis, spectroscopic (IR, 1H and 13C NMR, UV-Vis-NIR, EPR), magnetic measurements and biological studies of a number of complexes of Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Au(III) and Hg(II) of the Schiff base derived from the 1:2 condensation of 2,6-diformyl-4-methylphenol and 5-aminouracil, ((5-[[(3-[[(2,4-dioxopyrimidin-5(1H,3H)-yl)imino]methyl]-2-hydroxy-5-methylphenyl)methylene]amino]pyrimidine-2,4(1H,3H)-dione, hereafter denoted as BDF5AU) are reported. In all cases, the complexes appear to be monomeric. The deprotonated ligand in the phenolic oxygen atom shows a tridentate coordination mode through the two azomethine nitrogen atoms and the phenolic oxygen atom. The coordination of the neutral ligand takes place through the phenolic oxygen atom and one azomethine nitrogen atom and the carbonylic oxygen atom in fourth position of one uracil ring. The biological properties of some perchlorate complexes on the activity of some neutral, acid, basic and omega aminopeptidases (AP) are assayed, demonstrating a general inhibitory effect. Neutral and basic AP are mainly inhibited by Cu(II), Ni(II) and Cd(II) complexes, although tyrosyl-AP is activated by Zn(II) complex. Glutamyl-AP but not aspartyl-AP is inhibited by all the complexes assayed excepting Zn(II) complex. Finally, omega AP is inhibited by Ni(II) and Cd(II) complexes.
Journal of Inorganic Biochemistry 05/2003; 94(4):326-34. · 3.35 Impact Factor
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ABSTRACT: To assess the relative importance of soluble (Sol) and membrane-bound (M-B) components of aminopeptidase (AP) activities in local functions of male and female gonads.
Observational study.
University research.
Adult male and female Sprague-Dawley rats in the proestrous phase of the estrous cycle.
Samples from the right testis and the whole right ovary were dissected after perfusion with saline. The Sol and M-B fractions were obtained from these samples.
Fluorometric measurement of Sol and M-B AP activities using arylamide derivatives as substrates.
Highly significant differences between male and female gonads were observed. Sol AP activities showed a significant predominance in testes, whereas M-B AP activities were significantly higher in ovaries.
There was a discrepancy in the distribution of Sol and M-B AP activities between male and female gonads, which may imply a direct participation of sex steroids in AP activities. These results may reflect the relative importance of these enzymes in the testis and ovary and should be taken into account in evaluating the functional role of peptides locally produced in gonads.
Fertility and Sterility 05/2002; 77(4):802-4. · 3.56 Impact Factor
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ABSTRACT: A study of the relationship between the capillary column gas chromatographic retention times on two different columns (SE-54
and SE-52) for a group of trimethylsilyl ethers derived from 16 natural sterols found in olive oil and an initial set of 60
molecular descriptors was made. Three kinds of molecular descriptors were used: conventional, topological, and quantumchemical
parameters. By using multivariable regression, two empirical functions for each column were obtained, which were selected
on the basis of their respective statistical parameters. The first model relates the retention index with the quantum-chemical
descriptors and the second with both topological and conventional descriptors. In all cases, the correlation coefficients
of the empirical functions were higher than 0.9880, and the mean relative errors range between 2.88 and 3.24%. In any case,
both models could be used, although the second model could be more useful and preferable because it has higher R
2 values and a lower standard error percentage, giving slightly more exact results.
Journal of Oil & Fat Industries 05/2000; 77(6):627-630. · 1.77 Impact Factor
