Tag: Oxovanadium

DISCUSSION(4)

In sperm, an NADPH-depen-dent superoxide-generating system has been demonstrated. In addition, the ability of H2O2 generating Lactobacillus acidophilus, which is present in the vaginas of most normal women, can further potentiate the spermicidal activity of intravaginally applied oxovanadium(IV) complex. This is in contrast to the commercial vaginal detergent spermicide, N-9, which is selectively toxic to Lactobacilli. Furthermore, unlike N-9, the spermicidal activity of the oxovanadium(IV) complexes was not concomitantly associated with membrane disruption. buy cheap antibiotics

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The mechanism of sperm motility loss induced by oxo-vanadium(IV) complexes is yet to be determined. Both the vanadocenes(IV) and oxovanadium(IV) complexes also have antitumor activity. The antitumor effects of vanadium(IV) complexes are thought to be due to their reaction with the vanadyl-H2O2 system, which results in the generation of hydroxyl radicals in a Fenton-like reaction. In particular, the oxovanadium(IV) complex, after dissociation of phenanthroline rings, results in the formation of peroxocompounds that in the presence of H2O2 generate hydroxyl radicals. In support of this hypothesis is the observation that the vanadyl-phen complex induces hydroxyl radical-dependent DNA cleavage in the presence of H2O2. birth control yasmin

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DISCUSSION(2)

Structure-activity relationship analyses of 19 vanadocenes and 11 oxovanadium(IV) complexes clearly demonstrated that the spermicidal properties of these complexes were determined by the oxidation state of the vanadium(IV) atom. The various ancillary ligands linked by either carbon, nitrogen, or oxygen atoms to the central vanadium(IV) atom significantly contributed either to fine tuning of the spermicidal potency or enhancing the stability of these complexes in aqueous solution. buy flovent inhaler

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Our results provide unprecedented evidence that oxovana-dium(IV) complexes with 1,10-phenanthroline, 2,2′-bipyridyl, or 5′-bromo-2′-hydroxyacetophenone and their derivatives linked to vanadium(IV) via nitrogen or oxygen atoms have potent spermicidal activity against human sperm. The order of spermicidal efficacy for the 11 oxovanadium(IV) complexes synthesized and evaluated was as follows: VO(Cl-phen)2 > VO(phen)2 > VO(Br,OH-acph)2 > VO(Me2-phen) > VO(bipy)2 > VO(phen) > VO(Cl-phen) > VO(Me2-phen)2 > VO(Me2-bipy)2 > VO(Me2-bipy) > VO(bipy).

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RESULTS(8)

Next, TdT-mediated labeling of exposed 3′-OH termini of nuclear DNA with FITC-conjugated dUTP by the in situ TUNEL method was employed to demonstrate that oxo-vanadium(IV) complexes induced apoptosis in the sperm nuclear compartment. Figure 4, E and F, depicts the two-color flow cytometric contour plots of sperm nuclei of control sperm (E) treated with 0.1% DMSO and test sperm (F), respectively, treated with 100 ^M of VO(Cl-phen)2 in 0.1% DMSO after staining with FITC-dUTP and counterstaining with PI. More than 97% of VO(Cl-phen)2-treated sperm became apoptotic (TUNEL-positive) after 24 h of incubation (Fig. 4F). A 24-h exposure of sperm with any one of the 11 oxovanadium(IV) complexes evaluated resulted in a marked increase of TUNEL-positive cells, observed as a 43-98% (p < 0.05) increase in FITC-dUTP fluorescence (Table 3). buy ventolin inhalers

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Changes in the plasma membrane of the cell surface also appear early in cells undergoing apoptosis. In ap-optotic cells, the membrane phospholipid phosphatidyl serine is translocated from the inner to the outer leaflet of the plasma membrane, thereby exposing phosphatidyl serine to the external cellular environment. Annexin V binds to phosphatidyl serine residues that are exposed on the surface of cells undergoing apoptosis. The apoptosis-dependent surface binding of FITC-labeled recombinant human Annexin. buy cipro

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RESULTS(6)

Analysis by flow cytometry of the mitochondrial membrane potential changes occurring during apoptosis were analyzed with a A^m indicator, JC-1, a carbocyanine cationic dye, by following fluorescence associated with the uptake of JC-1 to evaluate A^m modifications. Motile sperm exhibited intense green and red fluorescence of JC-1 (Fig. 4A). It can be seen that a 3-h treatment with the oxovanadium(IV) complex VO(Cl-phen)2 resulted in an extinction of the red fluorescence (Fig. 4B), indicating that alteration occurred after VO(Cl-phen)2 treatment. A 3-h pretreatment of sperm with 7 of the 11 oxovanadium(IV) complexes resulted in variable decreases in A^m-related fluorescence observed as 31-73% reduction (p < 0.05) in JC-1 aggregate (orange/ green) fluorescence without concomitant reduction in JC-1 monomer (green) fluorescence (Table 3). flovent inhaler

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