bluuebunny/crossref_metadata_2025 huggingface dataset:
Synthesis and Biological Evaluation of Asiatic Acid Derivatives as Inhibitors of Glycogen Phosphorylases
Authors: Zhang Liying , Chen Jun , Gong Yanchun , Liu Jun , Zhang Luyong , Hua Weiyi , Sun Hongbin
Published: June 2009

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Twenty‐four asiatic acid derivatives have been synthesized and biologically evaluated as inhibitors of glycogen phosphorylase (GP). Within this series of compounds, asiatic acid benzyl ester (23; IC50=3.8 μM) exhibited more potent activity than its parent compound 1 (IC50=17 μM). SAR Analysis showed that asiatic acid (1) possessing a 2α‐OH function exhibited more potent GP inhibitory activity than eriantic acid B (27) which possesses a 2β‐OH function. Further lead optimization based on 1 is needed to find more effective asiatic acid derivatives as antidiabetic agents with protective effects against ischemic diabetic complications.
Secondary Metabolites and Cytotoxic Activities from the Stem Bark of Zanthoxylum nitidum
Authors: Yang Cheng‐Hui , Cheng Ming‐Jen , Lee Shiow‐Ju , Yang Cheng‐Wei , Chang Hsun‐Shuo , Chen Ih‐Sheng
Published: June 2009

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A dihydrobenzo[c]phenanthridine alkaloid, epizanthocadinanine A (1), together with 27 known compounds, including eight benzo[c]phenanthridines, i.e., oxynitidine (2), oxyavicine (3), oxychelerythrine (4), dihydrochelerythrine (5), 6‐acetonyldihydrochelerythrine (6), norchelerythrine (7), decarine (8), and arnottianamide (9); two 2‐quinolones, i.e., flindersine (10) and 4‐methoxy‐1‐methyl‐2‐quinolone (11); two furoquinolines, i.e., skimmianine (12) and γ‐fagarine (13); three aporphines, i.e., liriodenine (14), N‐acetyldehydroanonaine (15), and N‐acetylanonaine (16); six lignans, i.e., sesamin (17), episesamin (18), piperitol‐3,3‐dimethylallyl ether (19), xanthoxylol‐3,3‐dimethylallyl ether (20), savinin (21), and 2,3‐bis(3,4‐methylenedioxybenzyl)but‐2‐en‐4‐olide (22); three terpenoids, i.e., α‐cadinol (23), anticopalol (24), and spathulenol (25); one coumarin, i.e., aesculetin dimethyl ether (26); and two steroids, i.e., β‐sitosterol (27) and β‐sitostenone (28) were isolated from the stem bark of Zanthoxylum nitidum. Their structures were elucidated on the basis of extensive 1D‐ and 2D‐NMR as well as MS analyses. Moreover, the recently reported structures 2′–4′ of rhoifolines B and A, and ‘8‐methoxynorchelerythrine’, resp., isolated as new compounds from Z. rhoifolium and Z. nitidum, resp., could be assigned the revised structures 2–4 by reinvestigation of the spectroscopic data. In addition, the cytotoxicity of the isolates was evaluated on the MCF‐7, NCI‐H460, and SF‐268 cell lines. Among these isolates, liriodenine (14) was the most active compound against the MCF‐7, NCI‐H460, and SF‐268 cell lines with IC50 values of 2.19, 2.38, and 3.19 μg/ml, resp.
Anti‐Inflammatory, Antiproliferative, and Radical‐Scavenging Activities of Tolfenamic Acid and Its Metal Complexes
Authors: Kovala‐Demertzi Dimitra , Hadjipavlou‐Litina Dimitra , Primikiri Alexandra , Staninska Malgorzata , Kotoglou Chronis , Demertzis Mavroudis A.
Published: June 2009

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Some new complexes of tolfenamic acid (=2‐[(2‐methyl‐3‐chlorophenyl)amino]benzoic acid; Htolf) with potentially interesting biological activities are described. The complexes [Mn(tolf)2(H2O)2], [Co(tolf)2(H2O)2], [Ni(tolf2(H2O)2], [Cu(tolf)2(H2O)]2, and [Zn(tolf)2(H2O)] were prepared by the reaction of tolfenamic acid, a potent anti‐inflammatory drug, with metal salts. The radical‐scavenging activities of the complexes were evaluated using the 1,1‐diphenyl‐2‐picrylhydrazyl (DPPH) free radical‐scavenging assay. Their ability to inhibit soybean lipoxygenase, β‐glucuronidase, and trypsin‐induced proteolysis was studied. Their inhibitory effects on rat paw edema induced by carrageenin was studied and compared with those of tolfenamic acid. The complex [Zn(tolf)2(H2O)] exhibited the strongest in vivo inhibitory effect at 0.1 mm/kg Body Weight (BW; 93.0±0.9%), superior than the inhibition induced by tolfenamic acid at the same molar dose (76.0±0.9%). Tolfenamic acid and its metal complexes have been evaluated for antiproliferative activity in vitro against the cells of three human cancer cell lines, MCF‐7 (breast cancer cell line), T24 (bladder cancer cell line), and A‐549 (non‐small cell lung carcinoma), and a mouse fibroblast L‐929 cell line. The complexes [Mn(tolf)2(H2O)2] and [Cu(tolf)2(H2O)]2 have shown selectivity against T24 cell line. The IC50 values of these two complexes against T24 cancer cell lines are in a micromolar range similar or better to that of the antitumor drug cisplatin.
Acylated Oleanane‐Type Triterpene Saponins with Acceleration of Gastrointestinal Transit and Inhibitory Effect on Pancreatic Lipase from Flower Buds of Chinese Tea Plant (Camellia sinensis)
Authors: Yoshikawa Masayuki , Sugimoto Sachiko , Kato Yasuyo , Nakamura Seikou , Wang Tao , Yamashita Chihiro , Matsuda Hisashi
Published: June 2009

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The MeOH extract and its BuOH‐soluble fraction (crude saponin fraction) from the flower buds of Chinese tea plant (Camellia sinensis (L.) O. Kuntze; Fujian Province) were found to exhibit accelerating effects on gastrointestinal transit in mice and inhibitory effects against pancreatic lipase. From the BuOH‐soluble fraction, three new acylated oleanane‐type triterpene oligoglycosides, chakasaponins I, II, and III (1–3, resp.), were isolated together with 13 known compounds. The chemical structures 1–3 were elucidated on the basis of chemical and physicochemical evidence. Compounds 1–3 showed accelerating effects on gastrointestinal transit in mice and inhibitory effects against porcine pancreatic lipase (IC50=150–530 μM).
The relationship between cell membrane damage and lipid peroxidation under the condition of hypoxia‐reoxygenation: analysis of the mechanism using antioxidants and electron transport inhibitors
Authors: Yajima Daisuke , Motani Hisako , Hayakawa Mutsumi , Sato Yayoi , Sato Kaoru , Iwase Hirotaro
Published: June 2009

We consecutively observed lipid peroxidation and cell membrane damage under the condition of hypoxia‐reoxygenation (H/R) in cells and analyzed their mechanisms by using electron transport inhibitors and an antioxidant. In H/R experiments, lipid peroxidation and cell membrane damage were observed during the hypoxia phase. In the reoxygenation phase, lipid peroxidation stopped, while cell membrane damage did not. An antioxidant, n‐acetylcystein (NAC), and potassium cyanide (KCN) inhibited lipid peroxidation and cell membrane damage, while rotenone did not inhibit either of them. Although antimycin A did not inhibit lipid peroxidation, it inhibited cell membrane damage during the hypoxia phase but not during the reoxygenation phase. These results suggested that lipid peroxidation can affect cell membrane damage as a trigger during the hypoxia phase and the generation of oxidative stress can vary depending on the inhibition locations in the electron transport system. Copyright © 2009 John Wiley & Sons, Ltd.
Modification with Organometallic Compounds Improves Crossing of the Blood–Brain Barrier of [Leu5]‐Enkephalin Derivatives in an In Vitro Model System
Authors: Pinto Antonio , Hoffmanns Ulrich , Ott Melanie , Fricker Gert , Metzler‐Nolte Nils
Published: June 2009

Enkephalin peptides are thought to be suitable vectors for the passage of the blood–brain barrier (BBB). Modifications that do not alter the amino acid sequence are often used to improve the permeation through living membrane systems. As a new type of modification we introduce organometallic compounds, in particular ferrocene carboxylic acid. Derivatives of [Leu5]enkephalin were synthesised and labelled with organometallic compounds by using solid‐phase synthesis techniques. All new metal–peptide bioconjugates were comprehensively characterised by HPLC, NMR spectroscopy and mass spectrometry and found to be at least 95 % pure. For the first time, permeation coefficients in a BBB model for organometal–peptide derivatives were determined in this work. The uptake and localisation of fluorescein‐labelled enkephalins was monitored by fluorescence microscopy on three cancer cell lines. Octanol/H2O partition coefficients of the compounds were measured by HPLC. The introduction of the organometallic moiety enhances the uptake into cells and the permeation coefficient of [Leu5]‐enkephalin. This could be due to an increase in lipophilicity caused by the organometallic label. The metal–peptide conjugates were found to be nontoxic up to mMconcentrations. The low cytotoxicity encourages further experiments that could take advantage of the selectivity of enkephalin derivatives for opioid receptors.
Impact of intravascular ultrasound guidance in patients with acute myocardial infarction undergoing percutaneous coronary intervention
Authors: Maluenda Gabriel , Lemesle Gilles , Ben‐Dor Itsik , Collins Sara D. , Syed Asmir I. , Torguson Rebecca , Kaneshige Kimberly , Xue Zhenyi , Suddath William O. , Satler Lowell F. , Kent Kenneth M. , Lindsay Joseph , Pichard Augusto D. , Waksman Ron
Published: June 2009

Objectives: The aim of this study was to examine the utility of routine intravascular ultrasound (IVUS) guidance in patients with acute myocardial infarction (MI) undergoing percutaneous coronary intervention (PCI) with stent implantation. Background: Stent thrombosis (ST) is a serious complication of PCI with stent implantation for patients presenting with acute MI. Mechanical factors such as incomplete stent expansion and smaller stent diameters are known to correlate with ST and restenosis. IVUS guidance for stent deployment is reported to reduce these events in stable patients. Methods: We analyzed a cohort of 905 consecutive patients who underwent primary PCI for acute MI and were discharged alive. The clinical outcomes of 382 patients who underwent IVUS‐guided PCI were compared to those of 523 patients who did not. Patients who presented with cardiogenic shock and rescue PCI were excluded. The primary composite endpoint of death, MI, and target lesion revascularization at 1‐year follow‐up was systematically indexed and a propensity score was performed with regard to the use of IVUS‐guided PCI. Results: Patients undergoing IVUS‐guided PCI were older, more diabetic and hypertensive, but presented with less history of previous MI. The severity of coronary artery disease was balanced between both groups. The number of treated lesions and stents used was higher in the IVUS‐guided group, with a longer procedural duration. The overall rates of the composite primary outcome were similar (14.5% vs. 14.3%, P = 0.94) as were the rates of definite and probable stent thrombosis at 1 year (2.1% vs. 2.1%, P = 0.99) in the IVUS‐guided and no‐IVUS groups, respectively. After multivariate and propensity score adjustment, IVUS guidance was not an independent predictor for the primary endpoint. Conclusion: This study does not support the routine use of IVUS guidance for stent deployment in patients who present with acute MI and undergo primary PCI. © 2009 Wiley‐Liss, Inc.
First‐in‐man case report of the use of an Edwards‐Sapien valve to treat a regurgitant CoreValve aortic valve prosthesis
Authors: Taramasso Maurizio , Sharp Andrew S.P. , Maisano Francesco
Published: June 2009

Transcatheter aortic valve implantation is an alternative to conventional aortic valve replacement for patients at high surgical risk, with favorable procedural outcomes. Aortic regurgitation remains an off‐label indication. Recent case reports describe the successful use of a second CoreValve inside a malpositioned first CoreValve. In the current case, we report for the first time a valve‐in‐valve procedure for the treatment of a severely insufficient CoreValve prosthesis using the Edwards‐Sapien prosthesis. © 2009 Wiley‐Liss, Inc.
Antithrombotic strategies in patients on oral anticoagulant therapy undergoing percutaneous coronary intervention: A proposed algorithm based on individual risk stratification
Authors: Patti Giuseppe , Di Sciascio Germano
Published: June 2009

An increasing number of patients on chronic oral anticoagulant therapy undergo percutaneous coronary intervention. There is a lack of evidence‐based data and no practice guidelines are available about the optimal antithrombotic treatment of such patients after the procedure; thus, the adopted strategies are highly variable and are often left to the discretion of the attending physician. In this article, we review current evidence and propose an algorithm of antithrombotic strategies tailored to the individual patient, which takes into account the relative risks of bleeding, ischemic complications, and thromboembolism.© 2009 Wiley‐Liss, Inc.
Theoretical Study of the Stability of the DNA Duplexes Modified by a Series of Hydrophobic Base Analogues
Authors: Zendlová Lucie , Řeha David , Hocek Michal , Hobza Pavel
Published: June 2009

The geometries of a 13 mer of a DNA double helix (5′‐GCGTACACATGCG‐3′) were determined by molecular dynamics simulations using a Cornell et al. empirical force field. The bases in the central base pair (shown in bold) were replaced (one or both) by a series of hydrophobic base analogues (phenyl, biphenyl, phenylnaphathalene, phenylanthracene and phenylphenanthrene). Due to the large fluctuations of the systems, an average geometry could not be determined. The interaction energies of the Model A, which consisted of three central steps of a duplex without a sugar phosphate backbone, taken from molecular dynamics simulations (geometry sampled every 1 ps), were calculated by the self‐consistent charge density functional based tight‐binding (SCC‐DFTB‐D) method and were subsequently averaged. The higher the stability of the systems the higher the aromaticity of the base analogues. To estimate the desolvation energy of the duplex, the COSMO continuum solvent model was used and the calculations were provided on a larger model, Model B (the three central steps of the duplex with a sugar phosphate backbone neutralised by H atoms), taken from molecular dynamics simulations (geometry sampled every 200 ps) and subsequently averaged. The selectivity of the base analogue pairs was ascertained (Model B) by including the desolvation energy and the interaction energy of both strands, as determined by the SCC‐DFTB‐D method. The highest selectivity was found for a phenylphenanthrene. Replacing the nucleic acid bases with a base analogue leads to structural changes of the central pair. Only with the smallest base analogues (phenyl) does the central base pair stay planar. When passing to larger base analogues the central base pair is usually stacked.
Fifty Years of Chemical Research at Farmitalia
Authors: Arcamone Federico‐Maria
Published: June 2009

This review contains a brief description of the chemistry developed in Farmitalia and, after 1978, Farmitalia–Carlo Erba Research Laboratories, during the second half of the last century. It gives an overview of work that represents a significant part of the chemistry carried out in Italy during this period in the field of medicinal and natural product chemistry. This is particularly true when we consider in addition to the work done intramurally in the said laboratories, the work done by academic scientists in the frame of the various extramural collaborations. Only a fraction of the chemical research actually carried out is reported here as time and space dictated a selection. Subjects typically associated with Farmitalia and which gave rise to important scientific or therapeutic outcomes are given preference in this review.
Reliable Synthesis of Various Nucleoside Diphosphate Glycopyranoses
Authors: Wolf Saskia , Zismann Tanja , Lunau Nathalie , Meier Chris
Published: June 2009

A reliable and high yielding synthetic pathway for the synthesis of the biologically highly important class of nucleoside diphosphate sugars (NDP‐sugars) was developed by using various cycloSal‐nucleotides 1 and 9 as active ester building blocks. The reaction with anomerically pure pyranosyl‐1‐phosphates 2 led to the target NDP‐sugars 20–45 in a nucleophilic displacement reaction, which cleaves the cycloSal moiety in anomerically pure forms. As nucleosides cytidine, uridine, thymidine, adenosine, 2′‐deoxy‐guanosine and 2′,3′‐dideoxy‐2′,3′‐didehydrothymidine were used while the phosphates of D‐glucose, D‐galactose, D‐mannose, D‐NAc‐glucosamine, D‐NAc‐galactosamine, D‐fucose, L‐fucose as well as 6‐deoxy‐D‐gulose were introduced.
The Role of Building‐Block Metrics in the Halogen‐Bonding‐Driven Self‐Assembly of Calixarenes, Inorganic Salts and Diiodoperfluoroalkanes
Authors: Casnati Alessandro , Cavallo Gabriella , Metrangolo Pierangelo , Resnati Giuseppe , Ugozzoli Franco , Ungaro Rocco
Published: June 2009

Halogen bonding effectively co‐operates with ion–ion interactions in determining the supramolecular structure of three‐component heteromeric crystals comprising of calix[4]arenes, inorganic salts and diiodoperfluoroalkanes. The subtle interplay between these two types of interactions, as well as the influence of the valence of the metal ion, the “size” of the calixarene platform and the length of the perfluorocarbon module on the stoichiometry and overall supramolecular organisation of the ternary supramolecular architectures is discussed. The relevance to the overall packing of the size matching between the pitches along the cationic and anionic sub‐lattices is also discussed.
Supramolecular Chemistry at Interfaces: Molecular Recognition on Nanopatterned Porous Surfaces
Authors: Bonifazi Davide , Mohnani Stefan , Llanes‐Pallas Anna
Published: June 2009

Through the illustration of key examples that have recently appeared in the literature, the intention of this review is to provide a perspective of current advances on the molecular recognition at the interfaces aimed at the engineering of multifunctional organic‐based materials. The great interest in such systems has been motivated by the need to fabricate smaller and smaller components in order to improve, for example, the information storage capabilities of classical silicon‐based devices. Although great progress has been achieved on the exploitation of “top‐down” approaches, strong hope is now put on the development of hybrid devices in which the elementary components are replaced with single organic molecules. Nevertheless, the drive towards such devices is restricted by both their stability and difficulties to precisely control and manipulate the structural organisation at the molecular level. To overcome these restrictions, the use of nanotemplated surfaces featuring porous domains in which responsive functional molecules can be precisely accommodated at the single‐molecule level is one of the most promising approaches. In the first part of this manuscript, we therefore illustrate the main engineering strategies [1) through non‐covalent interactions, 2) surface‐confined covalent reactions and 3) assembly of pre‐organised cavities such as synthetic macrocycles] currently in use to create two‐dimensional (2D) patterned surfaces displaying porous structures at the nanoscale level. Such networks, featuring periodic hollow domains (controllable both in shape and size), are of particular significance as their cavities can be used as receptors for the recognition of remotely controllable functional molecules. In the second part, the confinement of molecular guests within the cavities is discussed, emphasising the selectivity and dynamics of key assemblies, with a particular focus on the biomolecular recognition and post‐assembly covalent functionalisation, which could provide the opportunity to fabricate devices currently beyond our reach on an unprecedented precision and efficiency. All the examples will be discussed in terms of structural organisation as studied by scanning tunnelling microscopy (STM) techniques.
Theoretical Studies on the Isomerizations of CH3NO2
Authors: YANG Lijuan , LI Xiaoyan , ZENG Yanli , MENG Lingpeng , ZHENG Shijun
Published: June 2009

The isomerizations of CH3NO2 (NM) have been investigated by density function theory (DFT) and electron density topological analysis methods. Nine isomers and eight isomerization channels were found. The connection relationship between the transition state (TS) and the isomers was confirmed by intrinsic reaction coordinate (IRC) tracing calculation. The calculation results show that in the CH3NO2→CH3ONOt process, the TS is a tight one (CH3NO2 does not break into CH3 and NO2 throughout the reaction), which is consistent with Arenass' results. A long structure transition region, which contains a four‐numbered ring → a five‐numbered ring → a four‐numbered ring → a five‐numbered ring structure, exists in CH3NOOc→CH2NOOH process. And it is the first time that a five‐numbered ring TS was found in reaction.
Improved QSPR Study of Diamagnetic Susceptibilities for Organic Compounds Using Two Novel Molecular Connectivity Indexes
Authors: MU Lailong , HE Hongmei , YANG Weihua
Published: June 2009

For predicting the molar diamagnetic susceptibilities of organic compounds, a variable molecular connectivity index mχ' and its converse index mχ'' based on adjacency matrix of molecular graphs and the variable atomic valence connectivity index δi' were proposed. The optimal values of parameters x, a, and y included in definition of δi', mχ' and mχ'' can be found by an optimization method. When x2.9, a1.10, and y0.36, a good five‐parameter model for the molar diamagnetic susceptibilities can be constructed from 0χ', 1χ', 2χ', 1χ'' and 2χ'' by using the best subset regression analysis method. The correlation coefficient r, standard error s, and average absolute deviation of the multilinear regression (MLR) model are 0.9930, 4.96 cgs, and 3.74 cgs, respectively, for the 721 organic compounds (training set). The cross‐validation by using the leave‐one‐out method demonstrates that the MLR model is highly reliable from the point of view of statistics. The average absolute deviation of predicted values of the molar diamagnetic susceptibility of another 360 organic compounds (test set) is 4.37 cgs for the MLR model. The results show that the current method is more effective than literature methods for estimating the molar diamagnetic susceptibility of an organic compound. The MLR method can provide an acceptable model for the prediction of the molar diamagnetic susceptibilities of organic compounds.
DNA‐binding Studies of Daunorubicin in the Presence of Methylene Blue by Spectroscopy and Voltammetry Techniques
Authors: HAJIAN Reza , SHAMS Nafiseh , PARVIN Afsaneh
Published: June 2009

The interaction of daunorubicin with calf thymus DNA has been investigated with the use of methylene blue dye as a spectral probe by the application of UV‐Vis spectrophotometry, spectrofluorometry and voltammetry. The voltammetric behavior of daunorubicin has been investigated at a glassy carbon electrode using cyclic and differential pulse voltammetry. Both UV‐vis spectrophotometry and cyclic voltammetry studies confirmed the intercalation reaction. The results showed that both daunorubicin and methylene blue molecules could intercalate into the double helix of DNA. The apparent binding constant of daunorubicin with DNA has been found to be 7.8 ×104 L·mol−1. The fluorescence signal of daunorubicin and methylene blue was quenched with DNA addition. The Stern‐Volmer equation was plotted based on the quenching fluorescence signal of daunorubicin.
A Simple Method Based on Harcourt‐Esson's Equation to Estimate the Critical Temperature of Thermal Explosion for Energetic Materials Using Non‐isothermal DSC
Authors: ZHAO Fengqi , HU Rongzu , GAO Hongxu
Published: June 2009

A method for estimating the critical temperature (Tb) of thermal explosion for energetic materials was derived from Semenov's thermal explosion theory and the non‐isothermal kinetic equation dα/dt=A0Tαf(α) based on Harcourt‐Esson's expression using reasonable hypotheses. The final formula is Tb=αTe0/(α−1), which is simple. The onset temperature (Tei) can be easily obtained from the non‐isothermal DSC curves, the value of Te0 can from the equation Tei=Te0+α1β1+α1βi2+α1βi3, the values of α can from the equation: lnβi=ln[A0/(a+1)G(α)+(a+1)lnTi], and then the value of Tb can be calculated. The result obtained with this method coincides completely with the value of Tb obtained by Zhang‐Hu‐Xie‐Li's method.
Thermodynamic Complexation of Dopamine with Zinc(II) in Media with Different Dielectric Constants
Authors: BAGHERI GH Azar
Published: June 2009

The complexation of zinc(II) with dopamine has been investigated by spectrophotometric measurements in mixed solvent system at an ionic strength of 0.2 mol·dm−3 sodium chloride, at (15±0.1), (25±0.1), (35±0.1)°C in a pH range of ca. 6 to ca. 7 with a high ratio of ligand to metal. The effect of solvent systems on protonation and complexation was discussed. Linear relationships were observed by plotting lg K versus 1/D, where K and D show stability and dielectric constants, respectively.
A Facile Approach to the Synthesis of Gold Nanoshells with Near Infrared Responsive Properties
Authors: LIU Shunying , LIANG Zhongshi , GAO Feng , YU Jiahui , LUO Shufang , CALATA Jesus N. , LU Guoquan
Published: June 2009

A very detailed study of the most important parameters that involved in the preparation of gold nanoshells with near infrared (NIR) absorption properties is reported. The importance of this work lies in the deep understanding of how each parameter contributes to the formation of gold nanoshells in terms of size, shell thickness, optical property and particle stability, which have not been emphasized in the literatures. Through detailed characterization by UV‐Vis spectroscopy, dynamic light scattering (DLS) and transmission electron microscopy (TEM) analysis, a facile approach to synthesize nanoshells with optimal optical properties in the NIR region was obtained. The amount of reagents, the ratio and condition of reagents, the reaction time, all played important roles in the formation of stable, narrow‐size distributed gold nanoshells with NIR absorption properties, which have significant applications to photothermal therapy of cancers in biomedical area.
A New Keggin Tungstocobaltate Decorated by Zinc(II) Complex Groups: [Zn(2,2′‐bipy)3]3{[Zn(2,2′‐bipy)2(H2O)]2‐[HCoW12O40]2}·H2O
Authors: WANG Hong , CHENG Cungui , TIAN Yumei
Published: June 2009

A new organic‐inorganic hybrid compound based on Keggin tungstocobaltate decorated by zinc(II) coordination groups, [Zn(2,2′‐bipy)3]3{[Zn(2,2′‐bipy)2(H2O)]2[HCoW12O40]2}·H2O (bipy=bipyridine), has been synthesized under hydrothermal conditions and characterized by elemental analyses, IR, TG analyses and X‐ray single crystal diffraction. This compound crystallizes in the orthorhombic system, space group C2/c with a=46.966(9) ?, b=14.358(3) Å, c=26.154(5) Å, α=β=γ=90°, V=17637(6) Å3, and Z=4. The result of structure determination shows that the crystal structure is constructed from a mono‐supporting Keggin tungstocobaltate polyanion {[Zn(2,2′‐bipy)2(H2O)]2[HCoW12O40]2}6−, three [Zn(2,2′‐bipy)3]2+ cations and one water molecule. It is interesting that [Zn(1)(2,2′‐bipy)3]2+ cations are held together into a helix chain through hydrogen‐bonding interactions. Additionally, the compound is stable in air and shows intense photoluminescence at room temperature.
Eletropolymerization of Niacinamide for Fabrication of Electrochemical Sensor: Simultaneous Determination of Dopamine, Uric Acid and Ascorbic Acid
Authors: ZHU Xiaohong , LIN Xiangqin
Published: June 2009

Two polymeric thin film modified electrodes, poly‐niacinamide/glassy carbon electrode (poly‐NA/GCE) and poly‐nicotinic acid/glassy carbon electrode (poly‐NC/GCE), have be fabricated at glassy carbon electrodes by simple electropolymerization of niacinamide (NA) in different potential scan ranges of cyclic voltammetry (CV). These two electrodes all showed catalytic ability towards the oxidation of dopamine (DA), uric acid (UA) and ascorbic acid (AA) by obvious reductions of overpotentials, giving well‐resolved voltammetric peaks, which allow simultaneously determination of DA, UA and AA. The poly‐NC/GCE showed even higher electrocatalytic activity than the poly‐NA/GCE. The electrochemical behavior of poly‐NC/GCE was investigated by CV and differential pulse voltammetry (DPV) for determination of DA, UA and AA. The linear ranges of the concentration for the determination of AA, DA and UA using DPV were 75–3000, 0.37–16 and 0.741–230 mol·L−1, respectively. The slopes of the linear calibration curves for the detection were estimated to be 5.6, 1140 and 102 mA·L·mol−1 for AA, DA and UA, respectively. The poly‐NC/GCE shows excellent sensitivity, good selectivity and antifouling properties.
Heterometal Clusters Ln2Na8(OCH2CH2NMe2)12(OH)2 as Homogeneous Catalysts for the Tishchenko Reaction
Authors: LI Lan , SHENG Hongting , XU Fan , SHEN Qi
Published: June 2009

The heterometal alkoxide clusters of Group 3 metal and lanthanides with sodium Ln2Na8(OCH2CH2NMe2)12(OH)2 (Ln=Y, lanthanide) were found to serve as highly active catalysts for the Tishchenko reaction of various aldehydes to form the corresponding esters. The reaction scope and the influence of lanthanide and sodium metal on the catalytic activity were investigated, and the proposed mechanism of the reaction was discussed.
Asymmetric Synthesis of (R)‐Fluoxetine: A Practical Approach Using Recyclable and in‐situ Generated Oxazaborolidine Catalyst
Authors: PADIYA Kamlesh , GAGARE Pravin , GAGARE Manjiri , LAL Bansi
Published: June 2009

A practical route for the synthesis of (R)‐fluoxetine·HCl (ee=96%) in 56% overall yield was described. The key intermediate (R)‐3‐chloro‐1‐phenyl‐1‐propanol was obtained by the asymmetric reduction of prochiral 3‐chloropropiophenone using in‐situ generated oxazaborolidine catalyst derived from (S)‐α,α‐diphenylprolinol. The chiral procatalyst (S)‐α,α‐diphenylprolinol was recovered quantitatively and recycled. An improved practical synthesis of (S)‐α,α‐diphenylprolinol was also discussed.
Synthesis, Characterization and Crystal Structure of Some Novel 1‐(3,5‐Dimethyl‐1H‐pyrazol‐1‐yl)‐3‐(substituted anilino)propan‐1‐ones
Authors: SAEED Aamer , HUSSAIN Shahid , ABBAS Naeem , BOLTE Michael
Published: June 2009

Michael addition of some substituted anilines to methyl acrylate in acidic medium afforded the methyl 3‐(substituted anilino)propionates (1a–1i), which on treatment with hydrazine hydrate in methanol were converted into corresponding 3‐(substituted anilino) propionohydrazides (2a–2i) in good yields. Microwave irradiation of the latter with pentane‐2,4‐dione afforded 1‐(3,5‐dimethyl‐1H‐pyrazol‐1‐yl)‐3‐(substituted anilino)propan‐1‐ones (3a–3i) under solventless conditions. The structures were confirmed by spectroscopic data, elemental analyses and in case of the 3h by single crystal X‐ray diffraction data.
Preparation and Characterization of Heat Sensitive Color‐developing Microcapsules
Authors: BA Xinwu , AN Puying , LU Shuang , LIU Guangtian
Published: June 2009

Heat sensitive color‐developing polyurethane microcapsules containing leucocompounds were prepared by interfacial polymerization. The effects of three determinative process parameters on the particle size distributions, surface morphologies, and heat sensitive color‐developing behavior of the microcapsules were investigated. As a result, the polyurethane microcapsules with a narrower distribution, rounder shape and better heat sensitive color‐developing property were prepared with increasing of the protective colloid content, emulsifying rate and emulsifier content. This was related with the surface roughness of the microcapsules.
Facile Syntheses of N‐Substituted Imidazoles and Benzotriazoles from Baylis‐Hillman Bromides
Authors: YE Dongyan , LI Jian , LI Chunju , JIA Xueshun
Published: June 2009

A facile synthesis of N‐substituted imidazole and benzotriazole derivatives from Baylis‐Hillman bromides with imidazole and benzotriazole at room temperature was reported. In view of the simple operation, mild reaction conditions, good to excellent yields, good regio‐ and stereoselectivity, the present method exhibited its superiority.
Chemical Modification of Poly(epichlorohydrin) Using Montmorillonite Clay
Authors: BEKKAR Fatima , BELBACHIR Mohamed
Published: June 2009

Cationic ring opening polymerization of epichlorohydrin (1) and acetic anhydride in the presence of Maghnite‐ H (Mag‐H+) as a catalyst afforded, ω‐diacetylated poly(epichlorohydrin) (P1) in a moderate yield and molecular weight without formation of side products and degradation. P1 was chemically modified with morpholine (2), piperidine (3) and pyrrolidine (4) into the corresponding new functional poly(epichlorohydrin)s (P2–P4) in a moderate reaction conversion . The conversion of P1 into P2–P4 was confirmed by using FTIR and NMR spectroscopy and the yield was calculated from the elemental analysis data according to the mole fraction concept. The obtained functional polymers were further characterized by thermal analysis which showed a substantial increase of the glass transition temperature (Tg). Thus, the chemical modification of α,ω‐acetylated PECH using Mag‐H+ offers a simple method for obtaining functional polymers. Mag‐H+ is a montmorillonite sheet silicate clay exchanged with proton.
Synthesis and Fluorescent Properties of Chiral Polymer Complexes Incorporating Bipyridine and Eu(III) or Gd(III)
Authors: ZONG Lili , MIAO Qian , LIU Yan , XU Jinqian , HUANG Xiaobo , CHENG Yixiang
Published: June 2009

Chiral polymer P‐1 was synthesized by the polymerization of (R)‐5,5′‐dibromo‐6,6'‐di(4‐trifluoromethyl‐ phenyl)‐2,2′‐bisoctoxy‐1,1'‐binaphthyl (R‐M‐1) with 5,5′‐divinyl‐2,2′‐bipyridine (M‐2) via Pd‐catalyzed Heck reaction. The polymer complexes P‐2 and P‐3 could be obtained by the bipyridyl coordination of P‐1 with Eu(TTA)3·2H2O and Gd(TTA)3·2H2O (TTA−=1‐(2‐thenoyl)‐3,3,3‐trifluoroacetonate). The chiral polymer P‐1 shows strong blue fluorescence due to the extended ‐electronic structure between the chiral repeating unit (R)‐6,6'‐di(4‐trifluoromethyl‐phenyl)‐2,2′‐bisoctoxy‐1,1'‐binaphthyl and the conjugated linker 2,2′‐bipyridyl (bpy) group via vinylene bridge. The Eu(III)‐containing polymer complex P‐2 can not only emit the polymer fluorescence, but also have the characteristic fluorescence of Eu(III) (5D0→7F2) under different exciting wavelengths. The Gd(III)‐containing polymer complex P‐3 only emits the polymer fluorescence. Based on the fluorescent properties of the polymer and RE(III)‐containing polymer complexes, it can be concluded that the chiral polymer does not transfer energy to Eu(III) or Gd(III) complex moiety but emits its own fluorescence.
Comparison of Anti‐bacterial Activity of Four Kinds of Alkaloids in Rhizoma Coptidis Based on Microcalorimetry
Authors: KONG Weijun , ZHAO Yanling , XIAO Xiaohe , JIN Cheng , LIU Yi , LI Zulun
Published: June 2009

The anti‐bacterial activities of four kinds of alkaloids in Rhizoma Coptidis, a traditional Chinese medicinal (TCM) herb, on Escherichia coli (E. coli) growth were investigated and compared by microcalorimetry. The four kinds of alkaloids were berberine, coptisine, palmatine and jatrorrhizine. The heat flow power‐time curves of E. coli growth in the presence of the four kinds of alkaloids were measured using an LKB‐2277 Bio‐activity monitor using a stop‐flow method, at 37°C. Then the thermal kinetic parameters such as, growth rate constant k, maximum power output of the log phase Pm,log and the stationary phase Pm,stat, growth inhibitory ratio I, generation time tg, total heat output of the log phase Qt,log and half‐inhibitory concentration of the drugs, IC50, were obtained from the curves. The four kinds of alkaloids had different anti‐E. coli activities. k, Pm,log and Qt,log of E. coli in the presence of the four kinds of alkaloids decreased with increasing concentrations of the alkaloids. Judged from the values of k, Pm,log, Qt,log, I and IC50, the experimental results revealed that the sequence of anti‐bacterial activities of the four kinds of alkaloids was berberine>coptisine>palmatine>jatrorrhizine. The functional groups methylenedioxy at C‐2 and C‐3 on phenyl ring improved anti‐bacterial activity more remarkably than methoxyl at C‐2 and C‐3 on the phenyl ring. However, the antibacterial activity did not vary significantly with methylenedioxy or methoxyl at C‐9 and C‐10 on the other phenyl ring.
Synthesis and Characterization of Novel Electroactive Poly(ether sulfone) via Oxidative Coupling Polymerization
Authors: CUI Lili , CHAO Danming , MAO Hui , LI Yongxin , ZHANG Junfeng , WANG Ce
Published: June 2009

By oxidative coupling polymerization a novel electroactive poly(ether sulfone), with fixed conjugated length of oligoaniline (phenyl‐capped aniline tetramer) in the main chain, was successfully synthesized. The structure of the electroactive poly(ether sulfone) was confirmed by FTIR, NMR spectroscopy and X‐ray powder diffraction (XRD). Electrochemical activity of the poly(ether sulfone) was tested in 1.0 mol·L−1 H2SO4 aqueous solution which shows two redox peaks. Moreover, the thermal properties of the poly(ether sulfone) were investigated by thermogravimetric analysis (TGA). Its electrical conductivity is about 1.37×10−7 S·cm−1 at room temperature upon preliminarily protonic‐doped experiment.
The Gender Differences in Baseline Characteristics and Statin Intervention Among Outpatients with Coronary Heart Disease in China: The China Cholesterol Education Program
Authors: Li Xiankai , Xu Yawei , Li Jue , Hu Dayi
Published: June 2009

Background

The China Cholesterol Education Program (CCEP) aimed to investigate the baseline characteristics of outpatients with coronary heart disease (CHD) according to gender, especially lipid levels, statin intervention, and rates of achieving their goal low‐density lipoprotein cholesterol (LDL‐C) level.

Methods

A total of 4778 CHD outpatients were enrolled from 52 centers in 6 Chinese cities from January 2006 to January 2007.

Results

Female outpatients were significantly older than male outpatients (66±10 vs 63±11 years, P <0.001). Male outpatients were more likely to smoke than female outpatients (P<0.001). Female outpatients had a higher prevalence of hypertension, diabetes mellitus, LDL‐C level, and total cholesterol level (all P values <0.001). About 82% of the participants received statin therapy. The LDL‐C levels were 3.06±1.08 mmol/L and 2.89±0.97 mmol/L in outpatients at high risk and very high risk respectively (P<0.001). Though there were higher rates of statin intervention, only 36.2% of the high risk outpatients got to the target LDL‐C level (<2.6 mmol/L); 10.9% of the very high risk outpatients achieved the optimal LDL‐C level (<1.82 mmol/L) suggested by National Cholesterol Education Program Adult Treatment Panel III. The rate of achieving target was only 42.2%, even when LDL‐C <2.6 mmol/L was the target level for patients at very high risk. Only 19.4% of the outpatients at very high risk achieved the target (LDL‐C <2.08 mmol/L) suggested by the updated Chinese guideline for CHD.

Conclusion

Although the outpatients received a higher rate of statin therapy, the rates of achieving the target were lower. There is still a significant gap between the guidelines and clinical practice in statin intervention among these CHD outpatients, particularly for women. Copyright © 2009 Wiley Periodicals, Inc.
Upstream High‐Dose Tirofiban Does Not Reduce Myocardial Infarct Size in Patients Undergoing Primary Percutaneous Coronary Intervention: A Magnetic Resonance Imaging Pilot Study
Authors: Song Young Bin , Hahn Joo‐Yong , Gwon Hyeon‐Cheol , Kim Jun Hyung , Lee Sang Yeub , Choe Yeon Hyeon , Choi Seung‐Hyuk , Choi Jin‐Ho , Lee Sang Hoon
Published: June 2009

Background

Primary percutaneous coronary intervention (PCI) is more effective than fibrinolytic therapy for ST‐segment elevation myocardial infarction (STEMI), but initial treatment delay to intervention is the main limitation of this strategy. Hypothesis: Upstream use of high‐dose tirofiban could reduce myocardial infarct size, using analysis of contrast‐enhanced magnetic resonance imaging (CE‐MRI).

Methods

Patients with STEMI within 12 hours after symptom onset were randomized to a facilitated PCI group (n = 19) or to a primary PCI group (n = 20). The primary endpoint was myocardial infarct size evaluated by the volume of delayed hyperenhancement on CE‐MRI at 1 month after index procedure.

Results

The baseline clinical characteristics were not significantly different between the 2 groups. Although the incidence of pre‐PCI thrombolysis in myocardial infarction (TIMI) flow grade 2 to 3 was significantly higher in the facilitated PCI group than in the primary PCI group (47.4% vs 15.0%, P = 0.03), the achievement of myocardial blush grade 2 to 3 or ST‐segment resolution at 30 minutes after procedure was not significantly different between the facilitated PCI and the primary PCI group (36.8% vs 40%, P = 0.84 and 31.6% vs 20%, P = 0.41, respectively). Infarct size on CE‐MRI was similar in the facilitated PCI group and the conventional primary PCI group (22.1% ± 11.7% vs 25.2% ± 13.2%, P = 0.44). At 6 months, the left ventricular ejection fraction (LVEF) on echocardiography was 52.6% ± 10.4% in the facilitated PCI group and 50.9% ± 9.8% in the primary PCI group (P = 0.68).

Conclusion

Despite the improvement of initial TIMI flow grade, the upstream use of high‐dose tirofiban did not reduce myocardial infarct size measured by CE‐MRI. Copyright © 2009 Wiley Periodicals, Inc.
Effect of Intracoronary Nicardipine on Cardiac Enzymes After Elective Percutaneous Coronary Intervention
Authors: Arora Sandeep , Alfayoumi Fadi , Khawaja Azimuddin Tareq , Dua Aashish , Srinivasan Venkatraman , Gradman Alan H.
Published: June 2009

Background

Elevation in cardiac enzymes after percutaneous coronary intervention (PCI) is common and is associated with adverse clinical outcomes.

Hypothesis

Administration of intracoronary nicardipine—a calcium channel blocker will reduce cardiac enzyme levels in patients undergoing elective PCI.

Methods

In a single center, prospective, double‐blind placebo‐controlled trial, 193 patients undergoing elective PCI (with or without stenting) for chronic stable angina and/or an abnormal stress test were randomized to receive 200 mcg of intracoronary nicardipine (n = 93) or saline solution (n = 100) prior to intervention. Cardiac enzyme levels were measured immediately and at 8 and 16 hours after the procedure. Major adverse clinical events (MACE) were assessed at 30 days and at 6 months.

Results

Incidence of periprocedural myonecrosis defined as elevation of troponin I levels > 1× the upper limit of normal was similar in both groups (placebo 15.4% vs drug 10.6%; P = 0.47). There was no significant difference in peak troponin I levels after PCI between the 2 groups (placebo 0.58 ng/mL ± 1.08 ng/mL vs drug 0.97 ng/mL ± 3.6 ng/mL; P = 0.35). Major adverse clinical events at 6 months were infrequent and not statistically different in the 2 groups (placebo 3.4% vs drug 1.2%; P = 0.52). Multivariate analysis revealed that pretreatment with nicardipine was not associated with reduction in the incidence of troponin I elevation (odds ratio [OR]: 0.54; 95% confidence interval [CI]: 0.18–1.6; P = 0.28).

Conclusions

In low‐risk patients undergoing elective PCI, intracoronary nicardipine administration did not produce a significant cardioprotective effect in reducing postprocedural cardiac enzymes leakage. Copyright © 2009 Wiley Periodicals, Inc.
Use of Bicycle Exercise Echocardiography for Unexplained Exertional Dyspnea
Authors: Singhal Shalabh , Yousuf Mian A. , Weintraub Neal L. , Shizukuda Yukitaka
Published: June 2009

Unexplained exertional dyspnea is a common and perplexing clinical problem. Myocardial ischemia and left ventricular systolic dysfunction are important cardiac causes, but are often not detected in these patients. Recently, exercise‐induced left ventricular diastolic dysfunction and exercised‐induced pulmonary hypertension have emerged as common alternative mechanisms. While conventional exercise treadmill echocardiography effectively diagnoses left ventricular systolic dysfunction and myocardial ischemia, it has limited ability to detect exercise‐induced diastolic dysfunction or pulmonary hypertension. The latest advances in exercise echocardiography, including utilization of tissue Doppler imaging and harmonic imaging, make noninvasive evaluation of both conventional and alternative cardiac causes of exertional dyspnea possible. These advancements, when coupled with newly designed supine exercise platforms for bicycle exercise echocardiography (BE), facilitate the detection of exercise‐induced diastolic dysfunction and pulmonary hypertension. Moreover, BE using supine ergometry additionally permits the dynamic evaluation of valvular function and interatrial shunting and detection of pulmonary arteriovenous fistula, uncommon but important causes of unexplained exertional dyspnea. Therefore, we propose that because of its superior diagnostic capabilities, BE should be included as part of a comprehensive cardiac evaluation of patients with unexplained exertional dyspnea. Copyright © 2009 Wiley Periodicals, Inc.
Bacteria and Fungi Levels in Various Indoor and Outdoor Environments in Ankara, Turkey
Authors: Mentese Sibel , Arisoy Münevver , Rad Abbas Yousefi , Güllü Gülen
Published: June 2009

In this study, different types of indoor environments (primary school, kindergarten, cafeteria, restaurant, dormitory, dwelling, office, sport salon, library, classroom, and laboratory) and their outdoor environments were investigated in terms of bioaerosol contamination. A total of 120 environments were investigated in Ankara, Turkey. The single‐stage Andersen sampler was used for viable bioaerosol sampling. During the sampling, indoor and outdoor temperature, relative humidity, and CO2 concentration were measured. Total bacteria counts (TBC) and fungi concentrations varied on a large scale within and between the sampling site groups (10–103 CFU/m3). The highest TBC levels were measured in kindergartens, primary schools, restaurants, high schools, and homes, while the highest mold levels were measured in kitchens, bathrooms, and offices. Micrococcus spp., Staphylococcus auricularis, and Bacillus spp. were predominant bacteria species and Penicillium spp., Aspergillus spp., and Cladosporium spp. were the most observed mold genera detected in the samples. Indoor‐to‐outdoor (I/O) ratios of the observed fungi counts were calculated as approximately around 1, and for bacteria counts these ratios were higher than 1. There was no statistical difference between indoor and outdoor mold levels, while a significant difference was found between indoor and outdoor bacteria levels (p < 0.001). A significant correlation between indoor CO2 and bioaerosols indicates insufficient ventilation.
Indoor Air Quality Benchmarking for Air Conditioned Offices
Authors: Hui Pui‐shan , Wong Ling‐tim , Mui Kwok‐wai
Published: June 2009

Maintaining acceptable indoor air quality (IAQ) for a healthy workplace is of major concern. Based on proper assessment methodologies and monitoring plans, policymakers have proposed indicators to address office IAQ. To streamline the assessment of office IAQ performance and offer incentives for maintaining better IAQ, this study proposes and investigates the feasibility of simple IAQ benchmarking using an IAQ indicator. The IAQ indicator is a benchmarking parameter derived from exposure concentrations of three selected common indoor air pollutants. This benchmark used a 5‐star rating system which assigned 1 star to the top 10% of samples with the highest levels of the three pollutants, 2 stars to the next 22.5%, 3 stars to the next 35%, 4 stars to the next 22.5% and 5 stars to the bottom 10%. The application of this benchmarking system was tested in 525 air conditioned offices in Hong Kong. Taking an existing IAQ certification scheme as a reference, the proposed benchmarking system proved to be useful in distinguishing offices with different IAQ labels, and illustrate the performance of office IAQ with different star ratings. Therefore, the proposed simple method can help promote better IAQ and serve as a screening assessment for IAQ in air conditioned offices of Hong Kong.