bluuebunny/crossref_metadata_2025_split huggingface dataset:
Galactose Encapsulated Multifunctional Nanoparticle for HepG2 Cell Internalization
Authors: Lai Chian‐Hui , Lin Chia‐Yi , Wu Huan‐Ting , Chan Hau‐Shien , Chuang Yung‐Jen , Chen Chien‐Tien , Lin Chun‐Cheng 
Published: September 2010

AbstractThe fluorescent dye Cy3 and galactose derivatives are covalently assembled with different ratios on the surfaces of magnetic nanoparticles (MNPs) to produce multifunctional HepG2 cancer cell–targeting agents and the effect of ligand spatial orientation on the MNP surface is investigated on targeting specificity. By using a mixture of bis‐N‐hydroxysuccinimide ester (a bifunctional linker) and OSu‐activated Cy3 (w/w = 30:1), stable and quantifiable fluorescent MNPs (Cy3@MNPs) are synthesized that could be subsequently loaded with galactosyl ligands. A mono‐antennary and two different tri‐antennary galactosyl ligands are individually immobilized on Cy3@MNPs, and the uptake efficiencies of the resulting galactosyl Cy3@MNPs by HepG2 and HeLa cells are investigated using confocal microscopy. The confocal images show that galactosyl Cy3@MNPs are sprayed over cytoplasm of the HepG2 cells, indicating that the MNP uptake occurs via receptor‐mediated endocytosis that is followed by release from endosomes. The results also reveal that the ligand spatial orientation affects the efficiency of the receptor‐mediated endocytosis and one of the tri‐antennary galactosyl ligands shows the best uptake efficiency owing to the optimal spatial presentation of the galactosyl moieties. Overall, it is shown that the MNP is a good ligand carrier and that, when pre‐assembled, the multivalent ligand structure enhances the interactions between the surface ligands of the MNPs and receptors of HepG2 cells. Additionally, the galactosyl Cy3@MNPs are not cytotoxic, indicating that they may potentially be used for in vivo applications.
Sustained Release of a Monoclonal Antibody from Electrochemically Prepared Mesoporous Silicon Oxide
Authors: Andrew Jennifer S. , Anglin Emily J. , Wu Elizabeth C. , Chen Michelle Y. , Cheng Lingyun , Freeman William R. , Sailor Michael J. 
Published: September 2010

AbstractNanostructured mesoporous silica (SiO2) films are used to load and release the monoclonal antibody bevacizumab (Avastin) in vitro. A biocompatible and biodegradable form of mesoporous SiO2 is prepared by electrochemical etching of single crystalline Si, followed by thermal oxidation in air at 800°C. Porous SiO2 exhibits a negative surface charge at physiological pH (7.4), allowing it to spontaneously adsorb the positively charged antibody from an aqueous phosphate buffered saline solution. This electrostatic adsorption allows bevacizumab to be concentrated by >100× (300 mg bevacziumab per gram of porous SiO2 when loaded from a 1 mg mL−1 solution of bevacziumab). Drug loading is monitored by optical interferometric measurements of the thin porous film. A two‐component Bruggeman effective medium model is employed to calculate percent porosity and film thickness, and is further used to determine the extent of drug loading into the porous SiO2 film. In vitro drug release profiles are characterized by an enzyme‐linked immunosorbent assay (ELISA), which confirms that the antibody is released in its active, VEGF‐binding form. The nanostructured delivery system described here provides a sustained release of the monoclonal antibody where approximately 98% of drug is released over a period of one month.
Self‐Assembling TiO2 Nanorods on Large Graphene Oxide Sheets at a Two‐Phase Interface and Their Anti‐Recombination in Photocatalytic Applications
Authors: Liu Jincheng , Bai Hongwei , Wang Yinjie , Liu Zhaoyang , Zhang Xiwang , Sun Darren Delai 
Published: September 2010

AbstractTiO2 nanorods are self‐assembled on the graphene oxide (GO) sheets at the water/toluene interface. The self‐assembled GO–TiO2 nanorod composites (GO–TiO2 NRCs) can be dispersed in water. The effective anchoring of TiO2 nanorods on the whole GO sheets is confirmed by transmission electron microscopy (TEM), X‐ray diffraction (XRD), Fourier transform IR spectroscopy (FTIR), and thermogravimetric analysis (TGA). The significant increase of photocatalytic activity is confirmed by the degradation of methylene blue (MB) under UV light irridiation. The large enhancement of photocatalytic activity is caused by the effective charge anti‐recombination and the effective absorption of MB on GO. The effective charge transfer from TiO2 to GO sheets is confirmed by the significant photoluminescence quenching of TiO2 nanorods, which can effectively prevent the charge recombination during photocatalytic process. The effective absorption of MB on GO is confirmed by the UV‐vis spectra. The degradation rate of MB in the second cycle is faster than that in the first cycle because of the reduction of GO under UV light irradiation.
An Organocatalytic Domino Thia‐Michael/Aldol Condensation Reaction: Highly Enantioselective Synthesis of Functionalized Dihydrothiophenes
Authors: Tang Jie , Xu Dan Qian , Xia Ai Bao , Wang Yi Feng , Jiang Jun Rong , Luo Shu Ping , Xu Zhen Yuan 
Published: September 2010

AbstractAn organocatalytic domino thia‐Michael/aldol condensation reaction of α, β‐unsaturated aldehydes with 1, 4‐dithiane‐2,5‐diol catalyzed by chiral diphenylprolinol TMS ether has been developed, which provides a new practical and direct route to chiral dihydrothiophenes with high yields (up to 90%) and excellent enantioselectivities (up to>99%ee). The catalytic mechanism of the domino reaction was further confirmed through the APCI‐MS detection of proposed reaction intermediates.
Efficient and Highly Chemoselective Direct Reductive Amination of Aldehydes using the System Silane/Oxorhenium Complexes
Authors: Sousa Sara C. A. , Fernandes Ana C. 
Published: September 2010

AbstractThis work reports a novel method for direct reductive amination of aldehydes with silanes catalyzed by several high‐valent oxorhenium(V) and oxorhenium(VII) complexes. The catalytic system PhSiH3/ReIO2(PPh3)2 (2.5 mol%) was very efficient for the synthesis of secondary amines and highly chemoselective, tolerating a wide range of functional groups such as NO2, CF3, SO2R, CO2R, F, Cl, Br, I, CN, OH, OCH3, SCH3, NCOR, and double bonds. This novel method was also employed in the synthesis of tertiary amines with moderate yields.
A Tripodal Peptidic Titanium Phosphonate as a Homochiral Porous Solid Medium for the Heterogeneous Enantioselective Hydration of Epoxides
Authors: Milo Anat , Neumann Ronny 
Published: September 2010

AbstractA porous, homochiral titanium‐phosphonate material based on a tripodal peptide scaffold was used as a heterogeneous reaction medium for the enantioselective hydration (>99%) of styrene oxide. This titanium‐phosphonate material, which was shown to contain confined chiral spaces, was prepared by polymerization of L‐leucine onto a tris(2‐aminoethyl)amine initiator, followed by capping with phosphonate groups and completed by non‐aqueous condensation with titanium isopropoxide. Circular dichroism confirmed that the peptide tethers yielded a secondary structure. X‐ray powder diffraction and transmission electron microscopy supported by a semi‐empirical model showed the likely formation of a porous, lamellar material that was quantified by nitrogen adsorption.
Macrocyclic Palladium(II) Complexes in CC Coupling Reactions: Efficient Catalysis by Controlled Temporary Release of Active Species
Authors: Röhlich Christoph , Köhler Klaus 
Published: September 2010

AbstractStabilization of palladium species against agglomeration is essential for reasonable catalytic activity in CC coupling reactions. In contrast to common methods of palladium(0) complex or particle stabilization, a new concept is introduced here: it is demonstrated that a controlled release of palladium from an inactive precatalyst provides stability, too, and leads to high catalytic activity. This paper presents surprising catalytic results for Heck and Suzuki reactions with aryl chlorides and bromides, using three highly stable macrocyclic palladium complexes as catalyst precursors. Three different behaviour patterns for the macrocyclic complexes can be deduced from the evaluation of catalytic activities, UV‐Vis spectroscopy, recycling studies of immobilized complexes, and ligand addition experiments. (i) Palladium tetraphenylporphyrin reversibly releases only extremely low amounts of palladium during the reactions, and low coupling activities are observed. (ii) Release of palladium from its phthalocyanine complex is irreversible; cumulative release of palladium into the reaction mixtures leads to high catalytic activity. (iii) Extraordinary results were obtained with a Robson‐type complex of palladium, which reversibly releases effectual amounts of palladium into solution under reaction conditions. This controlled release prevents the formation of inactive palladium agglomerates under harsh conditions and leads to high catalytic performances. Even strongly deactivated electron‐rich aryl chlorides (4‐chloroanisole) can be completely and selectively converted by the in situ formed anionic palladium halide complexes; the addition of typical stabilizing additives (TBAB) was found to be unnecessary. The bimetallic palladium complex is regenerated at the end of the reaction. These results contribute to the current understanding of the active species in CC coupling reactions of Heck and Suzuki types.
A Remarkable Titanium‐Catalyzed Asymmetric Strecker Reaction using Hydrogen Cyanide at Room Temperature
Authors: Ramalingam Balamurugan , Seayad Abdul Majeed , Chuanzhao Li , Garland Marc , Yoshinaga Kazuhiko , Wadamoto Manabu , Nagata Takushi , Chai Christina L. L. 
Published: September 2010

AbstractClose to perfect enantioselectivity (up to 98% ee) is obtained for the formation of amino nitriles using hydrogen cyanide (HCN) as the cyanide source at room temperature for the first time. In an operationally simple process, the catalyst generated from a partially hydrolyzed titanium alkoxide (PHTA) and (S)‐N‐salicyl‐β‐amino alcohol ligand, catalyzes the cyanation of imines in a short reaction time.
Synthesis of diblock and triblock copolymers from butyl acrylate and styrene by reverse iodine transfer polymerization
Authors: Enríquez‐Medrano Francisco J. , Guerrero‐Santos Ramiro , Hernández‐Valdez Martín , Lacroix‐Desmazes Patrick 
Published: September 2010

AbstractWell‐defined AB and BA diblock copolymers were obtained by a one‐pot two‐step sequential block copolymerization by reverse iodine transfer polymerization (RITP), A being a poly(styrene) block and B a poly(butyl acrylate) block. High monomer conversions during the formation of the first block avoided the purification steps before growing the second block. In a third sequential step, the diblock copolymers were further extended to synthesize ABA and BAB triblock copolymers. Furthermore, the synthesis of ABA and BAB copolymers in only two steps by RITP was investigated starting with the formation of the central block using 2,5‐di(2‐ethylhexanoylperoxy)‐2,5‐dimethylhexane as a difunctional initiator and then resuming the polymerization to grow the external blocks in a second step. The obtained copolymers were analyzed by size exclusion chromatography, transmission electron microscopy, and differential scanning calorimetry. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2011
Influence of chitosan posttreatment parameters on the fixation of pigment‐based inks on ink‐jet‐printed cotton fabrics
Authors: Momin Nasar H. , Padhye Rajiv , Khatri Awais 
Published: September 2010

AbstractCotton fabrics were digitally printed with pigment‐based black ink with an HP Desk‐Jet 880C printer. These ink‐jet‐printed fabrics were posttreated with chitosan samples for the fixation of the pigment‐based ink on the cotton. The influence of various parameters, including the molecular weight (MW), application method (pad–dry–cure vs pad–batch), concentration, and pH, on the degree of fixation (DF) of the pigment‐based inks was examined. The chitosan‐posttreated cotton samples were evaluated for their color strength, DF, color difference, and whiteness index values and their colorfastness properties. Chitosan samples with MWs of 150,000 and greater than 375,000 showed 100% (complete) fixation of the pigment‐based inks on the cotton fabrics. DF drastically decreased in the chitosan with an MW of less than 5000. Both the pad–dry–cure and pad–batch methods were found to be suitable for chitosan application onto ink‐jet‐printed fabrics. Chitosan with an MW of 150,000 showed 100% fixation at concentrations ranging from 0.3 to 1%. A further decrease in the concentration significantly decreased the fixation. High fixation values were achieved at acidic pH, whereas a neutral to alkaline pH resulted in poor fixation. The colorfastness properties for each parameter studied are also discussed. The posttreatment of the digitally printed cotton with chitosan was found to be very effective in fixing the pigment‐based inks. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2010
Constituents of cupuliferae, XIII: New and revised structures of acylated flavonoids from Quercus Suber L.
Authors: Romussi Giovanni , Bignardi Gaetano , Pizza Cosimo , De Tommasi Nunziatina 
Published: September 2010

AbstractFrom leaves of Quercus suber L. in addition to ten known glycosides, two new acylated flavonoids have been isolated and identified as 3‐O‐kaempferol 2‐O‐(trans‐p‐coumaroyl)‐β‐D‐glucopyranoside (1) and 3‐O‐kaempferol 2,3‐di‐O‐acetyl‐4‐O‐(cis‐p‐coumaroyl)‐6‐O‐(trans‐p‐coumaroyl)‐β‐D‐glucopyranoside (3). The structures of the previously described 3‐O‐kaempferol 2,4‐di‐O‐(trans‐p‐coumaroyl)‐β‐D‐glucopyranoside2) and 3‐O‐kaempferol 3,6‐di‐O‐acetyl‐2,4‐di‐O‐(trans‐p‐coumaroyl)‐β‐D‐glucopyranoside3) were revised to 3‐O‐kaempferol 2,6‐di‐O‐(trans‐p‐coumaroyl)‐β‐D‐glucopyranoside (4) and 3‐O‐kaempferol 3,4‐di‐O‐acetyl‐2,6‐di‐O‐(trans‐p‐coumaroyl)‐β‐D‐glu‐copyranoside (5).
Prodrugs nichtsteroidaler antirheumatika, 3. mitt.: Synthese und hydrolyse von acyloxy‐2‐oxopropanen
Authors: Schwenker Gerhard , Stiefvater Karlheinz 
Published: September 2010

AbstractSynthesis and Hydrolysis of Acyloxy‐2‐oxopropanes2‐Oxopropylesters are examined as potential prodrugs of acidic non‐steroidal anti‐inflammatory drugs. The esters are characterized by a high degree of chemical lability at pH 7.4 (37°C) while exhibiting a higher stability at pH < 7. The rate of the non‐enzymatic hydrolysis at pH 7.4 is dependent on steric and electronic effects which can be contributed to the particular acyloxy‐rest.
Antitumoraktive Platin(II)‐Komplexe Mit Substituierten 2‐Aminomethylpyridin‐Liganden
Authors: Brunner Henri , Nerl Georg , Angerer Erwin V. , Knebel Norbert 
Published: September 2010

AbstractDurch Umsetzung von K2P1CI4 mit den 2‐Aminomethylpyridinliganden 9, 14 und 22 sind die entspr. Dichloroplatin(II)‐Komplexe 3‐5 erhältlich. Die Verbindungen 3 und 22 zeigen beachtliche Bindungsaffinitäten zum Estrogenrezeptor. Gegen den hormonunabhängigen Tumor P388 der CD2F1‐Maus erwiesen sich die Platin(II)‐Komplexe 4 und 5 als schwach wirksam, Komplex 3 ist unwirksam. An der hormonunabhängigen MDA‐MB 231‐Zelllinie ist mit den Verbindungen 3‐5,9,14 und 22 keine signifikante Wirkung erkennbar. An der hormonabhängigen MCF‐7‐Zellinie zeigen die Verbindungen 3‐5,9,14 geringe Antitumorwirkung, der Ligand 22 dagegen hemmt stark.
Antikonvulsive 3‐Carbamoyl‐Isochinolinone: Synthese und Antikonvulsive Aktivität von 3‐Carbamoyl‐4‐Aryl‐Isochinolin‐1(2H)‐onen
Authors: Unverferth Klaus , Dörre Ronald , Körner Brunhild , Scheibe Heike , Morgenstem Eve 
Published: September 2010

AbstractDie Synthese von neunzehn 3‐Cabamoyl‐4‐aryl‐isochinolin‐1 (2H)‐onen wird beschrieben. Die Verbindungen wirken antikonvulsiv im maximalen Elektroschock‐Test (i.p.Gabe). Eine repräsentative Substanz ist 3‐Carbamoyl‐2‐isopropyl‐4‐(4‐chlorphenyl)‐isochinolin‐1(2H)‐on, ED50= 2.1 · 10−4mol/kg. Die Wirkungsstärke beträgt 20% von der des Phenytoins (ED50= 0.44 · 10−4mol/kg).
1,2‐dihydro‐3,1‐benzoxazin‐4‐one and 4H‐1,2‐dihydro‐pyrido‐[2,3‐d]‐[1,3]‐Oxazin‐4‐one derivatives as potential prodrugs part I: Synthesis
Authors: Schwenker Gerhard , Chen Jianbing 
Published: September 2010

Abstract1‐Mono‐ and previously unknown 1,2‐disubstituted 1,2‐dihydro‐3,1‐benzoxazin‐4‐ones 7 and 9, potential prodrugs of flufenamic acid (6) and mefenamic acid (8), and 4H‐1,2‐dihydro‐pyrido‐[2,3‐d]‐[1,3]‐oxazin‐4‐ones 11, potential prodrugs of niflumic acid (10), were prepared; the structures of all new compounds wereconfirmed by spectroscopic methods.
Release of ketoprofen from dermal bases in presence of cyclodextrins: Effect of the affinity constant determined in semisolid vehicles
Authors: Orienti I. , Zecchi V. , Bertasi V. , Fini A. 
Published: September 2010

AbstractWe describe a method to determine the affinity constant values between Ketoprofen and β‐cyclodextrin and hydroxypropyl‐β‐cyclodextrin in semisolid vehicles. The method is based on the diffusion of the drug, released from semisolid vehicles, through a lipidic non porous membrane. The affinity constants of Ketoprofen towards cyclodextrins as determined in semisolid media better represent the release of the drug from dermal bases than the corresponding values in aqueous systems.
Ring transformation with bridged 1,3‐dicarbonyl heteroanalogues, III 5‐(ω‐aminoalkyl)‐1,2,4‐oxadiazoles by ring‐transformations of 3‐methylthio‐2‐aza‐3‐propeniminium salts
Authors: Pätzel Michael , Liebscher JÜRgen 
Published: September 2010

Abstract3‐Methylthio‐2‐aza‐3‐propeniminium salts 5 react with hydroxylamine after ring transformation under formation of 5‐(ω‐aminoalkyl)‐1,2,4‐oxadiazole hydroiodides 4 HI, which show a remarkable antitussive activity.
Phenanthrylalkanoic acids, V: A useful access to α‐methylphenanthreneacetic acids
Authors: Balo Carmen , Fernández Franco , Gómez Generosa , González Carmen , López Carmen 
Published: September 2010

AbstractA very simple one‐pot monomethylation of phenanthreneacetic acids 2 or of their methyl esters 1 yields α‐methylphenanthreneacetic acids 3 in good yield. Altematively, the process may be extended to the preparation of the corresponding α‐arylisobutyric acids 4.
Synthesis and structure of quinoxaline‐substituted 1,4‐dihydropyridines
Authors: Stumm G. , Niclas H.‐J. , Winter G. , Reck G. 
Published: September 2010

AbstractThe preparation of a novel series of quinoxaline‐substituted 1,4‐dihydropyridines is described. Thus, the reaction of 1 with acetoacetates in the presence of ammonia leads to dialkyl 2,6‐dimethyl‐4‐(quinoxaline‐1,4‐dioxid‐2‐yl)‐1,4‐dihydropyridine‐3,5‐dicarboxylates 2a‐g. Compounds 4a‐c are obtained as by‐products. The asymmetrically substituted dihydropyridines 3a‐d are prepared from 1, acetoacetates, and 3‐aminocrotonates. The desoxygenated compounds 5a,b and 6a,b are obtained by reduction with ethanol/triethylamine or Na2S2O4. The results of the X‐ray structure analyses of 2b and 6a are discussed.
Peroxide Als Pflanzeninhaltsstoffe, 8. Mitt.: Guaianolid‐Peroxide Aus Der Schafgarbe, Achillea Millefolium L., Auslöser Der Schafgarbendermatitis
Authors: Rücker Gerhard , Manns Detlef , Breuer Judith 
Published: September 2010

AbstractAus dem Ether‐Extrakt der Blütenköpfchen der Schafgarbe (Achillea millefolium L.) wurden zwei Guaianolide (1,2) mit einer Peroxid‐Brücke im Cyclopentan‐Ring und einer α‐Methylen‐γ‐butyrolacton‐Struktur isoliert. Es werden die Bezeichnungen α‐Peroxyachifolid (1) und β‐Peroxyisoachifolid (2) vorgeschlagen. 1 ist u.a. verantwortlich für die Schafgarbendermatitis.
Alpha1‐antitrypsin deficiency–related alleles Z and S and the risk of Wegener's granulomatosis
Authors: Mahr Alfred D. , Edberg Jeffrey C. , Stone John H. , Hoffman Gary S. , St.Clair E. William , Specks Ulrich , Dellaripa Paul F. , Seo Philip , Spiera Robert F. , Rouhani Farshid N. , Brantly Mark L. , Merkel Peter A. ,   Wegener's Granulomatosis Genetic Repository Research Group
Published: September 2010

AbstractObjectiveDeficiency of α1‐antitrypsin (α1AT) may be a determinant of susceptibility to Wegener's granulomatosis (WG). Several previous, mainly small, case–control studies have shown that 5–27% of patients with WG carried the α1AT deficiency Z allele. It is not clear whether the S allele, the other major α1AT deficiency variant, is associated with WG. This study investigated the relationship of the α1AT deficiency Z and S alleles with the risk of developing WG in a large cohort.MethodsWe studied the distribution of the α1AT deficiency alleles Z and S in 433 unrelated Caucasian patients with WG and 421 ethnically matched controls. Genotyping was performed using an allele discrimination assay. Results were compared between cases and controls using exact statistical methods.ResultsAmong the patients with WG, the allele carriage frequencies of Z and S were 7.4% and 11.5%, respectively. The frequencies of the 6 possible genotypes differed in a statistically significant manner between cases and controls (P = 0.01). The general genetic 2‐parameter codominant model provided the best fit to the data. Compared with the normal MM genotype, the odds ratio (OR) for MZ or MS genotypes was 1.47 (95% confidence interval [95% CI] 0.98–2.22), and the OR for ZZ, SS, or SZ genotypes was 14.58 (95% CI 2.33–∞). ORs of similar direction and magnitude were observed within the restricted cohorts that excluded cases and controls carrying ≥1 Z or ≥1 S allele.ConclusionBoth Z and S alleles display associations with risk of WG in a codominant genetic pattern. These findings strengthen the evidence of a causal link between α1AT deficiency and susceptibility to WG.
Students as resurrectionists—A multimodal humanities project in anatomy putting ethics and professionalism in historical context
Authors: Hammer Rachel R. , Jones Trahern W. , Hussain Fareeda Taher Nazer , Bringe Kariline , Harvey Ronee E. , Person‐Rennell Nicole H. , Newman James S. 
Published: September 2010

AbstractBecause medical students have many different learning styles, the authors, medical students at Mayo Clinic, College of Medicine researched the history of anatomical specimen procurement, reviewing topic‐related film, academic literature, and novels, to write, direct, and perform a dramatization based on Robert Louis Stevenson'sThe Body‐Snatcher. Into this performance, they incorporated dance, painting, instrumental and vocal performance, and creative writing. In preparation for the performance, each actor researched an aspect of the history of anatomy. These micro‐research projects were presented in a lecture before the play. Not intended to be a research study, this descriptive article discusses how student research and ethics discussions became a theatrical production. This addition to classroom and laboratory learning addresses the deep emotional response experienced by some students and provides an avenue to understand and express these feelings. This enhanced multimodal approach to“holistic learning” could be applied to any topic in the medical school curriculum, thoroughly adding to the didactics with history, humanities, and team dynamics. Anat Sci Educ 3:244–248, 2010. © 2010 American Association of Anatomists.