5 research outputs found
Identification of a novel strain of green algae, <i>Parachlorella</i> sp binos (Binos). a
<p>, Microscopic image of <i>P.</i> sp <i>binos</i> (Binos) (x2000). <b>b</b>, India ink staining of <i>P.</i> sp <i>binos</i> (Binos) (x400). India ink was diluted with water to make a 10% solution. <b>c, d</b>, Phylogenetic analysis of members of the phylum Chlorophyta based on (<b>c</b>) 18S rRNA gene and (<b>d</b>) actin amino acid sequences. <b>e, f</b>, Transmission electron micrographs of (<b>e</b>) <i>P.</i> sp <i>binos</i> (Binos) and (<b>f</b>) <i>Chlorella</i> sp. <b>g</b>, Infrared spectra of the extracellular matrix of <i>P.</i> sp <i>binos</i> (red line) and purified sodium alginate (standard; black line) analyzed by Fourier transform infrared spectroscopy from 400 to 4000 cm<sup>−1</sup>.</p
Binding of radionuclides in contaminated water and soil samples from Fukushima. a
<p>, Soil and water soil samples were collected from Namie-machi, approximately 20 km from the Fukushima Daiichi Nuclear Plant. The upper photograph shows a signboard prohibiting entry to the 20 km exclusion zone. Gross radioactivity of ground samples measured using a Geiger-Müller counter was approximately 60 kcpm (lower photograph). Water samples (<b>b</b>) and soil-water extracts (<b>c</b>) contaminated by radioactive fallout were incubated with algal cells under illumination at 2000 lux for 8 h. Gross β radioactivity (closed bars) and γ radioactivity (open bars) from <sup>137</sup>Cs were measured by liquid scintillation and γ counters, respectively.</p
Binding of radioisotopes of cesium with <i>P.</i> sp <i>binos.</i> a
<p>, 10, 30, and 100 mg/ml of wet algal cells were incubated with 1.92 kBq of <sup>137</sup>CsCl at room temperature for 10 min. Radioactivity accumulated in algal cells were measured, and data are shown as % of total radioactivity (mean ± SD). *, <i>P</i><0.05, **, <i>P</i><0.01 (n = 4). <b>b</b>, After 10 min incubation, the radioactivities of pellets and supernatant were measured and the bound/free ratios were calculated (n = 4). <b>c</b>, Ten mg/ml of wet algal cells were incubated with nonradioactive CsCl (solid circles) or NaCl (open circles) and 1.92 kBq of <sup>137</sup>CsCl at room temperature for 10 min. Radioactivity accumulated in algal cells were measured, and data are shown as % of control uptake without nonradioactive CsCl. Non-linear curve fitting to the model of two binding sites with high and low affinities was performed using the CsCl and NaCl competition data (n = 4).</p
Radioiodine uptake by <i>P.</i> sp <i>binos</i> (Binos). a
<p>, Ten mg/ml of <i>P.</i> sp <i>binos</i> was incubated with 1.48 kBq of Na<sup>125</sup>I at room temperature under illumination at 2000 lux (open circles) or in the dark (solid circles) (n = 4). Radioactivity accumulated in algal cells were measured, and data are shown as maximal uptake. <b>b</b>, Algal cells incubated with Na<sup>125</sup>I at room temperature under illumination for 24 h. Radioactivity accumulated in algal cells were measured, and data are shown as % of total radioactivity. *, <i>P</i><0.05, **, <i>P</i><0.01 (n = 4). <b>c</b>, After 24 h incubation, pellet and supernatant radioactivities were measured and the bound/free ratios of <sup>125</sup>I were calculated (n = 4). <b>d</b>, Ten mg/ml of wet algal cells were incubated with nonradioactive NaI and 1.48 kBq of Na<sup>125</sup>I (n = 4). Radioactivity accumulated in algal cells were measured, and data are shown as % of control uptake without nonradioactive NaI <b>e</b>, Algal cells were incubated with or without 10 µM of hydrogen peroxide (H<sub>2</sub>O<sub>2</sub>) for 24 h (n = 3). <b>f, g</b>, After incubation of algal cells with 1 µM of sodium iodide for 24 h, elemental distribution of <sup>12</sup>C<sup>14</sup>N (f) and <sup>127</sup>I (g) on the section of algal cells were visualized by NanoSIMS. <b>h</b>, Marged image of <a href="http://www.plosone.org/article/info:doi/10.1371/journal.pone.0044200#pone-0044200-g002" target="_blank">Figure 2f and 2g</a>.</p
Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor
A novel orally bioavailable renin inhibitor, DS-8108b
(<b>5</b>), showing potent renin inhibitory activity and excellent
in vivo
efficacy is described. We report herein the synthesis and pharmacological
effects of <b>5</b> including renin inhibitory activity in vitro,
suppressive effects of ex vivo plasma renin activity (PRA) in cynomolgus
monkey, pharmacokinetic data, and blood pressure-lowering effects
in an animal model. Compound <b>5</b> demonstrated inhibitory
activities toward human renin (IC<sub>50</sub> = 0.9 nM) and human
and monkey PRA (IC<sub>50</sub> = 1.9 and 6.3 nM, respectively). Oral
administration of single doses of 3 and 10 mg/kg of <b>5</b> in cynomolgus monkey on pretreatment with furosemide led to dose-dependent
significant reductions in ex vivo PRA and sustained lowering of mean
arterial blood pressure for more than 12 h