Inhibitors of prostaglandin biosynthesis from Dalbergia odorifera.

The root heartwood of Dalbergia odorifera T. Chen (Leguminosae) is a Chinese medicinal drug (Japanese name koshinko) used for a stagnant blood syndrome (stagnation of disordered blood; Japanese, oketsu). In addition to 10 known compounds, five new phenolic compounds, isomucronustyrene and hydroxyobtustyrene (cinnamylphenols), (+)-isoduartin (isoflavan), odoriflavene (isoflav-3-ene) and (-)-odoricarpan (pterocarpan) were isolated and their structures were elucidated on the basis of chemical and spectroscopic methods. Of the fifteen compounds isolated, cinnamylphenols, isoflavans, isoflavene and benzoic acid derivative significantly inhibited prostaglandin biosynthesis as well as platelet aggregation induced by arachidonic acid.     

Validation of a method for predicting the precision, limit of detection and range of quantitation in competitive ELISA.

The mathematical model for predicting the precision, limit of detection (LOD) and range of quantitation (ROQ) in a competitive enzyme-linked immunosorbent assay (ELISA) proposed by Hayashi et al. (Anal. Chem., 2004, 76, 1295) was validated. The model describes the relative standard deviation (RSD) of concentration estimates by the RSDs of pipetting volumes of analyte, enzyme-conjugated antigen, antibody and substrate solutions, and the standard deviation (SD) of inherent absorbances between the wells in an ELISA plate. For 6 kinds of direct competitive ELISA kits, the LOD and ROQ predicted by the model agreed well with those obtained by experiments with real samples. It was also confirmed that the model is applicable to the prediction of uncertainty that depends on the pipetting error of the viscous antiserum solution. The model was demonstrated to be useful for estimating the LOD and ROQ of competitive ELISA.     

Pharmacokinetics of the nitroxide PCA measured by in vivo EPR

PCA (2,2,5,5-tetramethylpiperidine-1-oxyl-3-carboxylic acid) is a relatively stable free radical which has been shown to be useful as a contrast agent for nuclear magnetic resonance imaging and as an imaging/spectroscopy agent for EPR. In an effort to determine the role of the liver and kidney in the pharmacokinetics of PCA, using low frequency in vivo EPR spectroscopy, we followed the clearance of PCA after intravenous injection in mice: under normal conditions, with a restricted blood supply to the kidneys, after exposure to an acute hepatotoxin CCl₄, and after exposure to lipopolysaccharide (endotoxin). The observed pharmacokinetics fit a two-component model. The fast component was dramatically affected when the renal vessels were restricted, while CCl₄ and endotoxin had a smaller but significant effect. The half times of the slow components were not significantly different (p>0.05) in the groups treated by renal blood flow occlusion, CCl₄, or LPS, compared with the control group. In conclusion, we find that the pharmacokinetics of PCA need to be completely described in term of a two component model: the fast component of the decay is mainly due to the elimination by the kidneys and also is affected by the time for the initial distribution; the slow component is related to the bioreduction of the nitroxide. In addition to the liver other tissues can also effectively metabolize PCA. The effect of oxygen on the rate of metabolism is modest at most.     

The mutagenic constituents of Rubia tinctorum.

Twenty compounds were isolated from the roots of Rubia tinctorum which are used as a commercial source of madder color. Among these compounds, mollugin (1), 1-hydroxy-2-methylanthraquinone (2), 2-ethoxymethylanthraquinone(11), rubiadin (13), 1,3-dihydroxyanthraqunone (14), 7-hydroxy-2-methylanthraquinone (16), lucidin (17), 1-methoxymethylanthraquinone (18) and lucidin-3-O-primeveroside (19) showed mutagenicity with Salmonella typhimurium TA 100 and/or TA 98. Since the mutagenic compounds isolated are anthraquinone derivatives with the exception of compound 1, structure-mutagenicity relationships of the anthraquinones were also studied. The results suggested that the greatest activity is exhibited by 1,3-dihydroxyanthraquinones possessing methyl or hydroxylmethyl group on carbon 2.     

Green synthesis of bio-ethyl acetate over Egyptian natural red clay as a highly active,selective, and eco-friendly catalyst

The present work focused on the utilization of Egyptian red clay (ERC) without any treatment as a highly efficient, selective, and eco-friendly catalyst for synthesis of bio-ethyl acetate in the gas phase. The best conditions used in conventional fixed bed reactor were 130 cm³/min total flow rate of air with 1.6 and 2.1 vol% bio-ethanol and bio-acetic acid, respectively, 1 g clay catalyst calcined at 300 and 225°C reaction temperature. Under these conditions, the conversions to ester achieved were about 80 and 98% after 5 and 30 min, respectively, from the initial admission of the reactants into the reactor. The amount and type of surface acidity were identified by isopropanol reaction and chemisorption of basic probes. The results demonstrated that the majority of intermediate strength of BrØnsted acid sites are the key role for the dehydration reaction toward ester formation. The virgin and annealed clay solids were characterized using X-ray fluorescence (XRF), thermogravimetry (TG) and differential thermal analysis (DTA), Fourier transform infrared (FTIR), X-ray diffraction (XRD), and N₂ sorption.     

Optical time-domain analog pattern correlator for high-speed real-time image recognition

The speed of image processing is limited by image acquisition circuitry. While optical pattern recognition techniques can reduce the computational burden on digital image processing, their image correlation rates are typically low due to the use of spatial optical elements. Here we report a method that overcomes this limitation and enables fast real-time analog image recognition at a record correlation rate of 36.7 MHz--1000 times higher rates than conventional methods. This technique seamlessly performs image acquisition, correlation, and signal integration all optically in the time domain before analog-to-digital conversion by virtue of optical space-to-time mapping.     

Experimental study on interfacial area transport of a vertical downward bubbly flow

In relation to the development of the interfacial area transport equation, local flow measurements of vertical downward air–water flows in a pipe with an inner diameter of 50.8 mm were performed at three axial locations of z/D=6.50, 34.0, and 66.5 as well as ten radial locations from r/R=0 to r/R=0.9 using a multi-sensor probe. In the experiment, the superficial liquid velocity and the void fraction ranged from –0.620 m/s to –2.49 m/s and from 0.21% to 8.4%, respectively. The dependence of the interfacial area transport on the liquid velocity, void fraction, and bubble size is discussed in detail.     

Chiral analyses of dextromethorphan/levomethorphan and their metabolites in rat and human samples using LC-MS/MS

In order to develop an analytical method for the discrimination of dextromethorphan (an antitussive medicine) from its enantiomer, levomethorphan (a narcotic) in biological samples, chiral analyses of these drugs and their O-demethyl and/or N-demethyl metabolites in rat plasma, urine, and hair were carried out using LC-MS/MS. After the i.p. administration of dextromethorphan or levomethorphan to pigmented hairy male DA rats (5 mg/kg/day, 10 days), the parent compounds and their three metabolites in plasma, urine and hair were determined using LC-MS/MS. Complete chiral separation was achieved in 12 min on a Chiral CD-Ph column in 0.1% formic acid–acetonitrile by a linear gradient program. Most of the metabolites were detected as being the corresponding O-demethyl and N, O-didemethyl metabolites in the rat plasma and urine after the hydrolysis of O-glucuronides, although obvious differences in the amounts of these metabolites were found between the dextro and levo forms. No racemation was observed through O- and/or N-demethylation. In the rat hair samples collected 4 weeks after the first administration, those differences were more clearly detected and the concentrations of the parent compounds, their O-demethyl, N-demethyl, and N, O-didemethyl metabolites were 63.4, 2.7, 25.1, and 0.7 ng/mg for the dextro forms and 24.5, 24.6, 2.6, and 0.5 ng/mg for the levo forms, respectively. In order to fully investigate the differences of their metabolic properties between dextromethorphan and levomethorphan, DA rat and human liver microsomes were studied. The results suggested that there might be an enantioselective metabolism of levomethorphan, especially with regard to the O-demethylation, not only in DA rat but human liver microsomes as well. The proposed chiral analyses might be applied to human samples and could be useful for discriminating dextromethorphan use from levomethorphan use in the field of forensic toxicology, although further studies should be carried out using authentic human samples.     

Abelian quotients of monoids of homology cylinders

A homology cylinder over a surface consists of a homology cobordism between two copies of the surface and markings of its boundary. The set of isomorphism classes of homology cylinders over a fixed surface has a natural monoid structure and it is known that this monoid can be seen as an enlargement of the mapping class group of the surface. We now focus on abelian quotients of this monoid. We show that both the monoid of all homology cylinders and that of irreducible homology cylinders are not finitely generated and moreover they have big abelian quotients. These properties contrast with the fact that the mapping class group is perfect in general. The proof is given by applying sutured Floer homology theory to homologically fibered knots studied in a previous paper.     

Synthetic studies of carbapenem and penem antibiotics. II. Synthesis of 3-acetyl-2-azetidinones by (2 + 2) cycloaddition of diketene and Schiff bases.

It was found that (2 + 2) cycloaddition reaction of diketene with Schiff bases was effectively promoted by imidazole as a catalyst to afford 3-acetyl-2-azetidinone derivatives 4. As an application of this new method, a practical asymmetric synthesis of 4 and its conversion into (3S,4S)-4-carboxy-1-(di-p-anisylmethyl)-3-[(R)-1-hydroxyethyl]-2- azetidinone, which is a key intermediate for the synthesis of carbapenem and penem antibiotics, were accomplished.