bluuebunny/crossref_metadata_2025_split huggingface dataset:
Semisynthetic Ursolic Acid Fluorolactone Derivatives Inhibit Growth with Induction of p21waf1 and Induce Apoptosis with Upregulation of NOXA and Downregulation of c‐FLIP in Cancer Cells
Authors: Leal Ana S. , Wang Rui , Salvador Jorge A. R. , Jing Yongkui 
Published: July 2012

AbstractA series of ursolic acid ((1S,2R,4aS,6aR,6aS,6bR,8aR,10S,12aR,14bS)‐10‐hydroxy‐1,2,6a,6b,9,9,12a‐heptamethyl‐2,3,4,5,6,6a,7,8,8a,10,11,12,13,14b‐tetradecahydro‐1H‐picene‐4a‐carboxylic acid) derivatives with a 12‐fluoro‐13,28β‐lactone moiety were synthesized using the electrophilic fluorination reagent Selectfluor. The antiproliferative effects of these novel compounds were evaluated in AsPC‐1 pancreatic cancer cells, and the structure–activity relationships (SARs) were evaluated. Of the compounds synthesized, ursolic acid derivatives carrying a heterocyclic ring, such as imidazole or methylimidazole, and cyanoenones were among the more potent inhibitors of AsPC‐1 pancreatic cancer cell growth. 2‐Cyano‐3‐oxo‐12α‐fluoro‐urs‐1‐en‐13,28β‐olide, compound 20, was the most effective inhibitor with IC50 values of 0.7, 0.9 and 1.8 μM in pancreatic cancer cell lines AsPC‐1, MIA PaCa‐2 and PANC‐1, respectively. This compound also exhibited better antiproliferative activities against breast (MCF7), prostate (PC‐3), hepatocellular (Hep G2) and lung (A549) cancer cell lines, with IC50 values lower than 1 μM. The mechanism of action by which these compounds exert their biological effect was evaluated in AsPC‐1 cells using the most potent inhibitor synthesized, compound 20. At 1 μM, the cell cycle arrested at the G1 phase with upregulation of p21waf1. Apoptosis was induced at an inhibitor concentration of 8 μM with upregulation of NOXA and downregulation of c‐FLIP. These data indicate that fluorolactone derivatives of ursolic acid have improved antiproliferative activity, acting through arrest of the cell cycle and induction of apoptosis.
Pericyte coverage of differentiated vessels inside tumor vasculature is an independent unfavorable prognostic factor for patients with clear cell renal cell carcinoma
Authors: Cao Yun , Zhang Zhi‐Ling , Zhou Ming , Elson Paul , Rini Brian , Aydin Hakan , Feenstra Kristin , Tan Min‐Han , Berghuis Bree , Tabbey Rebeka , Resau James H. , Zhou Fang‐Jian , Teh Bin Tean , Qian Chao‐Nan 
Published: July 2012

AbstractBACKGROUND.The objective of this study was to evaluate the effect of pericyte coverage (PC) of differentiated tumor microvessels on the prognosis of patients with clear cell renal cell carcinoma (CCRCC).METHODS.Samples from 2 cohorts of patients with CCRCC (101 Asian patients and 524 US patients) were prepared using 2 different histologic approaches: routine sectioning versus tissue microarray. Then, the samples were immunohistochemically doubled‐stained for a pericyte marker (alpha smooth muscle actin [α‐SMA]) and a differentiated vessel marker (cluster of differentiation 34 [CD34]), followed by multispectral image capturing and computerized image analyses to quantify the microvessel density (MVD) and the PC of differentiated vessels. The correlations of PC and the MVD:PC ratio with clinicopathologic characteristics were analyzed.RESULTS.There was an inverse correlation between differentiated MVD and PC. Higher PC correlated with more aggressive clinicopathologic characteristics of CCRCC in both cohorts, including more advanced T‐classification, higher pathologic grades, and the occurrence of tumor necrosis. The MVD:PC ratio was an independent favorable prognostic factor for overall and recurrence‐free survival in the Asian cohort and for recurrence‐free survival in the US cohort. PC also was an independent prognostic factor, with higher PC predicting a poorer outcome. The combination of PC and MVD was better at distinguishing the outcome of patients with CCRCC. PC combined with differentiated MVD or with the MVD:PC ratio provided additional, independent prognostic information to the Leibovich risk model, and that information was used to generate improved risk models.CONCLUSIONS.The authors consistently observed that higher PC was correlated with more aggressive clinicopathologic characteristics. PC was an independent unfavorable prognostic factor. The authors concluded that pericytes should be considered for therapeutic targeting. Cancer 2013. © 2012 American Cancer Society.
Adjuvant chemotherapy for stage III colon cancer in the oldest old
Authors: Abraham Anasooya , Habermann Elizabeth B. , Rothenberger David A. , Kwaan Mary , Weinberg Armin D. , Parsons Helen M. , Gupta Pankaj , Al‐Refaie Waddah B. 
Published: July 2012

AbstractBACKGROUND:Randomized trials demonstrating the benefits of chemotherapy in patients with American Joint Committee on Cancer stage III colon cancer underrepresent persons aged ≥ 75 years. The generalizability of these studies to a growing elderly population remains unknown.METHODS:Using the California Cancer Registry for 1994 through 2008, the authors conducted a population‐based study of postcolectomy patients aged 50 years to 94 years with stage III (N1M0) colon adenocarcinoma. A 2‐sided chi‐square test and Cochran‐Armitage test for trend were used to compare patient and tumor characteristics associated with receipt of chemotherapy across age groups. Multivariate regression was used to assess the association between older age and receipt of chemotherapy. Kaplan‐Meier methods and Cox proportional hazards modeling were used to evaluate the association between chemotherapy and mortality, with propensity score adjustment.RESULTS:Approximately 44% (12,382 patients) of the study cohort was aged ≥ 75 years. Persons aged ≥ 75 years were found to be less likely to have received adjuvant chemotherapy than those aged < 75 years (30% vs 68% in patients aged 50 years‐74 years; P < .0001). On multivariate analysis, patients aged 75 years to 84 years were 13 times less likely, and those aged 85 years to 94 years were 24 times less likely, to have received chemotherapy as patients aged 50 years to 64 years. Nevertheless, age‐stratified multivariate survival analyses indicated that chemotherapy provided comparable mortality reduction across age groups.CONCLUSIONS:The percentage of persons aged ≥ 75 years receiving adjuvant chemotherapy remains low despite demonstrated survival benefits. These findings deserve attention within the context of a patient's life expectancy, underlying comorbidities, and performance status, as well as clinician bias. The results of the current study support the call for phase II/III studies assessing the toxicities and benefits of adjuvant chemotherapy for the treatment of stage III colon cancer in the elderly. Cancer 2013. © 2012 American Cancer Society
From Molecular Gallium and Indium Siloxide Precursors to Amorphous Semiconducting Transparent Oxide Layers for Applications in Thin‐Film Field‐Effect Transistors
Authors: Samedov Kerim , Aksu Yilmaz , Driess Matthias 
Published: July 2012

AbstractThe syntheses, structural characterization, and thermal degradation of a series of the new indium and gallium siloxide dimers [{Me2In(OSiEt3)}2] (1), [{Me2Ga(OSiEt3)}2] (2), [{Me2In(OSi(OtBu)3)}2] (3), [{Me2Ga(OSi(OtBu)3)}2] (4), and In[OSi(OtBu)3)] (5) is reported. Compounds 1–4 are readily accessible by facile Brönsted reaction of InMe3 or GaMe3 with the corresponding silanols Et3SiOH and (tBuO)3SiOH, respectively. Compound 5 could be obtained by analogous protolysis of [In{N(SiMe3)2}3] with an excess amount of (tBuO)3SiOH. The suitability of 1–5 to serve as molecular precursors for low‐temperature synthesis of amorphous indium and gallium oxide for electronic applications was probed. Thus their thermal degradation was studied by Thermogravimetric/differential thermogravimetry analysis (TGA/DTG). Compounds 1–4 were decomposed under dry synthetic air (20 % O2, 80 % N2) at low temperature to yield amorphous indium oxide and gallium oxide particles, respectively. In contrast, thermal degradation of 5 affords amorphous indium silicate. All of these products were analyzed by multiple techniques including powder X‐ray diffraction analysis (PXRD), transmission electron microscopy (TEM), and energy dispersive X‐ray spectroscopy (EDX). Thin‐film field‐effect transistors (FETs) could be fabricated through spin‐coating of silicon‐wafers with solutions of 1 in toluene and subsequent calcination under dry synthetic air at 350 °C. These films exhibit very good FET performance with a field‐effect mobility of 3.0×10−1 cm2 V−1 s and an on/off current ratio of 108.
Functionalized Dithienylthiazolo[5,4‐d]thiazoles For Solution‐Processable Organic Field‐Effect Transistors
Authors: Van Mierloo Sarah , Vasseur Karolien , Van den Brande Niko , Boyukbayram Ayse E. , Ruttens Bart , Rodriguez Silvio D. , Botek Edith , Liégeois Vincent , D'Haen Jan , Adriaensens Peter J. , Heremans Paul , Champagne Benoît , Van Assche Guy , Lutsen Laurence , Vanderzande Dirk J. , Maes Wouter 
Published: July 2012

AbstractA series of 5′‐aryl‐substituted 2,5‐bis(3′‐hexylthiophen‐2′‐yl)thiazolo[5,4‐d]thiazole derivatives was synthesized and these expanded semiconductors were investigated as active materials for solution‐processable organic field‐effect transistors. Field‐effect mobilities of up to 10−3 cm2 V−1 s−1 were obtained, representing the first reasonable FET behavior for highly soluble thiazolo[5,4‐d]thiazole‐based small organic compounds suitable for printable electronics. Thermal and electrooptical material properties were studied by thermogravimetric analysis, differential scanning calorimetry, cyclic voltammetry, and UV/Vis spectroscopy. Trends in thermal and optical data were supported by (time‐dependent) density functional theory calculations. Additional X‐ray diffraction, atomic force microscopy, and scanning electron microscopy studies provided insight in the relationship between the molecular structures, film morphologies, and FET performances. The fibrillar microcrystalline structure observed for the best‐performing thienyl‐substituted material was linked to the high mobility.
Electrodes of Poly(N‐methyl pyrrole)/Au and Poly(m‐aminobenzene sulfonic acid)‐Functionalized Multiwalled Carbon Nanotubes for Supercapacitor Applications
Authors: Narsimha Reddy B. , Billa Naresh , Deepa Melepurath 
Published: July 2012

AbstractAn assembly of poly(N‐methyl pyrrole) (PMP) doped with poly(3‐styrene sulfonate) with embedded Au nanoparticles (PMP/Au) was grown by electropolymerization of the monomer (MP) followed by adsorption of a Au colloid. Multiwalled carbon nanotubes were functionalized with poly(m‐aminobenzene sulfonic acid) (MWCNT/PABS) and deposited electrophoretically over conducting substrates. X‐ray diffraction (XRD) and Raman studies confirmed the successful functionalization of the MWCNTs by PABS. A new asymmetric supercapacitor design incorporating PMP/Au and MWCNT/PABS as electrodes was implemented for the first time, and the cell delivered a reversible specific capacitance of 967 F g−1 and a maximum energy density of 174 Wh Kg−1, which was superior to a PMP‐MWCNT/PABS cell (167 F g−1) and higher than many reported capacitances of poly(pyrrole)‐based supercapacitors. The PMP/Au electrode outperformed pristine PMP, graphite, and MWCNT/PABS electrodes in a study of different symmetric and asymmetric cells employing these electrodes. Scanning spreading resistance microscopy (SSRM) and conducting atomic force microscopy (C‐AFM) showed a lower spreading resistance and a larger nanoscale electronic conductivity for the PMP/Au electrode than for the pristine PMP electrode; these attributes allow unhindered charge transport both in the radial direction and across the cross‐section of the PMP/Au electrode. The facile electron propagation in the PMP/Au electrode, enabled by the presence of localized conducting domains of Au nanoparticles implanted in the PMP electrode, effectively translates into an enhanced specific capacitance of PMP/Au‐based cells relative to PMP. The results demonstrate that asymmetrically designed cells offer an exciting way to boost the overall performance of supercapacitors.
Tol2 gene trap integrations in the zebrafish amyloid precursor protein genes appa and aplp2 reveal accumulation of secreted APP at the embryonic veins
Authors: Liao Hsin‐Kai , Wang Ying , Noack Watt Kristin E. , Wen Qin , Breitbach Justin , Kemmet Chelsy K. , Clark Karl J. , Ekker Stephen C. , Essner Jeffrey J. , McGrail Maura 
Published: July 2012

AbstractCOVER PHOTOGRAPH: Confocal image of live 36 hpf double transgenic appais22Gt; Tg(flk1:moesin‐gfp)is1 embryo. The image shows accumulation of appaRFP fusion proteins specifically at the veinous vessels in the head and anterior region of the trunk, including the midcerebral and common cardinal veins. Arteries and veins are visualized by expression of moesin:GFP throughout all endothelial cells of the vasculature. From Liao et al., Developmental Dynamics 241:415–425, 2012.
Mercury‐Sequestering Pseudopeptides with a Tris(cysteine) Environment in Water
Authors: Pujol Anaïs M. , Lebrun Colette , Gateau Christelle , Manceau Alain , Delangle Pascale 
Published: July 2012

AbstractThe three pseudopeptides L1–3 having three converging cysteine arms anchored on a nitrilotriacetic acid scaffold, are demonstrated to be efficient sulfur‐based HgII chelating agents. The three ligands differ by the nature of the carbonyl group of the cysteine moieties, ester, amide, and carboxylate for L1, L2, and L3, respectively. The coordination chemistry of the mercury thiolate complexes was characterized in water by acid–base titration and several spectroscopic methods, including UV, 1H, and 199Hg NMR spectroscopy and Hg‐LIII EXAFS. At alkaline pH, they form monometallic complexes with typical signatures of a trigonal HgS3 coordination site, which is uncommon, as HgII usually prefers a coordination number of two. The digonal HgS2 structure is formed at acidic pH, where one cysteine group is protonated (HgLH complex). EXAFS spectra at liquid He temperature and alkaline pH are nearly identical for the three HgL complexes. Their analysis reveals an asymmetrical HgS3 binding environment with three S atoms at 2.38, 2.51, and 2.67 Å. This suggests that the C3‐symmetrical species detected by 1H NMR spectroscopic analysis at 298 K are averages of nonsymmetrical complexes that rapidly equilibrate on the NMR time‐scale at ambient temperature. At acidic pH, HgII is coordinated in a linear configuration to the two sulfur atoms from the thiolate groups at a distance of 2.36 Å, and in a T‐shaped geometry to the third sulfur atoms from the protonated cysteine at 3.07 Å. The three pseudopeptides have high affinities for HgII and are interesting alternatives for the design of efficient water‐soluble mercury‐sequestering agents that favor an uncommon tris(thiolato)mercury environment.
Effective Palladium‐Catalyzed Synthesis of Triarylethene‐Based Molecules in Aqueous Solution
Authors: Zhu Yan , Sun Peng , Yang Hailong , Lu Linhua , Yan Hong , Creus Marc , Mao Jincheng 
Published: July 2012

AbstractHighly effective and selective Pd‐catalyzed coupling reactions of 1,1‐dibromo‐1‐alkenes with various arylboronic acids have been performed in aqueous solution under mild conditions. The method is simple, economic, and practical for the synthesis of triarylethene‐based compounds.
The First Total Synthesis of Solomonsterol B, a Marine Pregnane X Receptor Agonist
Authors: Sepe Valentina , Ummarino Raffaella , D'Auria Maria Valeria , Renga Barbara , Fiorucci Stefano , Zampella Angela 
Published: July 2012

AbstractA concise route to the pregnane X receptor (PXR) agonist solomonsterol B, a natural product isolated from the marine sponge Theonella swinhoei, has been developed starting from commercially available hyodeoxycholic acid. The synthesis features a one‐carbon side chain degradation and the refunctionalization of the A and B rings to install the desired trans junction and the two hydroxy groups at C2 and C3 in a trans relationship. The protocol proceeded with good yields (10 % over 13 steps), also allowing the preparation of a side chain‐modified derivative useful for a preliminary structure–activity relationship on PXR. The pharmacological characterization of solomonsterol B demonstrated that this compound was a PXR agonist in a transactivation assay, and when it was incubated with liver cells, it increased the expression of PXR‐regulated genes. These data support the development of sponge steroids as PXR ligands endowed with therapeutic potential.
Near‐source seismic hazard and design scenarios
Authors: Chioccarelli Eugenio , Iervolino Iunio 
Published: July 2012

SUMMARYEarthquakes damage engineering structures near, relatively to the rupture's size, to the source. In this region, the fault's dynamics affect ground motion propagation differently from site to site, resulting in systematic spatial variability known as directivity. Although a number of researches recommend that records with directivity‐related velocity pulses should be explicitly taken into account when defining design seismic action on structures, probabilistic seismic hazard analysis (PSHA), in its standard version, seems inadequate for the scope. In the study, it is critically reviewed why, from the structural engineering point of view, hazard assessment should account for near‐source effects (i.e., pulse‐like ground motions), and how this can be carried out adjusting PSHA analytically via introduction of specific terms and empirically calibrated models. Disaggregation analysis and design scenarios for near‐source PSHA are also formulated. The analytical procedures are then applied to develop examples of hazard estimates for sites close to strike–slip or dip–slip faults and to address differences with respect to the ordinary case, that is, when pulse‐like effects are not explicitly accounted for. Significant increase of hazard for selected spectral ordinates is found in all investigated cases; increments depend on the fault‐site configuration. Moreover, to address design scenarios for seismic actions on structures, disaggregation results are also discussed, along with limitations of current design spectra to highlight the pulse‐like effects of structural interest. Finally, an attempt to overcome these, by means of disaggregation‐based scenarios specific for the pulse occurrence case, is presented. Copyright © 2012 John Wiley & Sons, Ltd.
Numerical simulation of a single rising bubble by VOF with surface compression
Authors: Klostermann J. , Schaake K. , Schwarze R. 
Published: July 2012

SUMMARYThe capability of the direct volume of fluid method for describing the surface dynamics of a free two‐dimensional rising bubble is evaluated using quantities of a recently published benchmark. The model equations are implemented in the open source computational fluid dynamics library OpenFOAM®. Here, a main ingredient of the numerical method is the so‐called surface compression that corrects the fluxes near the interface between two phases. The application of this method with respect to two test cases of a benchmark is considered in the main part. The test cases differ in physical properties, thus in different surface tension effects. The quantities centre of mass position, circularity and rise velocity are tracked over time and compared with the ones given in the benchmark. For test case one, where surface tension effects are more pre‐eminent, deviations from the benchmark results become more obvious. However, the flow features are still within reasonable range. Nevertheless, for test case two, which has higher density and viscosity ratios and above all a lower influence of the surface tension force, good agreement compared with the benchmark reference results is achieved. This paper demonstrates the good capabilities of the direct volume of fluid method with surface compression with regard to the preservation of sharp interfaces, boundedness, mass conservation and low computational time. Some limitation regarding the occurrence of parasitic currents, bad pressure jump prediction and bad grid convergence have been observed. With these restrictions in mind, the method is suitable for the simulation of similar two‐phase flow configurations. Copyright © 2012 John Wiley & Sons, Ltd.
Elevated levels of 1‐hydroxypyrene and N′‐nitrosonornicotine in smokers with head and neck cancer: A matched control study
Authors: Khariwala Samir S. , Carmella Steven G. , Stepanov Irina , Fernandes Patricia , Lassig Amy Anne , Yueh Bevan , Hatsukami Dorothy , Hecht Stephen S. 
Published: July 2012

AbstractBackgroundHead and neck squamous cell carcinoma (HNSCC) is associated with tobacco use. Still, most smokers do not develop HNSCC. The mechanisms of varying susceptibility to HNSCC are poorly studied to date. Tobacco metabolite research provides insight regarding the innate metabolism and excretion of carcinogens.MethodsSmokers with HNSCC (cases) were compared with smokers without HNSCC (controls) in a matched cohort. The tobacco metabolites studied were: 1‐hydroxypyrene (1‐HOP), N′‐nitrosonornicotine (NNN), and 4‐(methylnitrosamino)‐1‐(3‐pyridyl)‐1‐butanol (NNAL).ResultsIn 33 subjects, mean 1‐HOP was 1.82 pmol/mg creatinine versus 1.08 pmol/mg creatinine (p = .004) and mean NNN was 0.10 pmol/mg creatinine versus 0.04 pmol/mg creatinine (p = .01) in cases and controls, respectively. NNAL did not differ between groups.ConclusionsSmokers with HNSCC have elevated urinary levels of 1‐HOP and total NNN compared with matched controls, suggesting an increased effective exposure to these carcinogens. Tobacco constituent metabolites may be useful in understanding tobacco‐related carcinogenesis in HNSCC. © 2012 Wiley Periodicals, Inc. Head Neck, 2013
Plumbagin inhibits tumorigenesis and angiogenesis of ovarian cancer cells in vivo
Authors: Sinha Sutapa , Pal Krishnendu , Elkhanany Ahmed , Dutta Shamit , Cao Ying , Mondal Gourish , Iyer Seethalakshmi , Somasundaram Veena , Couch Fergus J. , Shridhar Viji , Bhattacharya Resham , Mukhopadhyay Debabrata , Srinivas Priya 
Published: July 2012

AbstractAngiogenesis is a hallmark of tumor development and metastatic progression, and anti‐angiogenic drugs targeting the VEGF pathway have shown to decrease the disease progression in cancer patients. In this study, we have analyzed the anti‐proliferative and anti‐angiogenic property of plumbagin in cisplatin sensitive, BRCA2 deficient, PEO‐1 and cisplatin resistant, BRCA2 proficient PEO‐4 ovarian cancer cells. Both PEO‐1 and PEO‐4 ovarian cancer cells are sensitive to plumbagin irrespective of BRCA2 status in both normoxia and hypoxia. Importantly, plumbagin treatment effectively inhibits VEGF‐A and Glut‐1 in PEO‐1 and PEO‐4 ovarian cancer cells. We have also analyzed the p53 mutant, cisplatin resistant, and BRCA2 proficient OVCAR‐5 cells. Plumbagin challenge also restricts the VEGF induced pro‐angiogenic signaling in HUVECs and subsequently endothelial cell proliferation. In addition, we observe a significant effect on tumor regression among OVCAR‐5 tumor‐bearing mice treated with plumbagin, which is associated with significant inhibition of Ki67 and vWF expressions. Plumbagin also significantly reduces CD31 expression in an ear angiogenesis assay. Collectively, our studies indicate that plumbagin, as an anti‐cancer agent disrupts growth of ovarian cancer cells through the inhibition of proliferation as well as angiogenesis.
SIMPLIFIED OVERSHOT GATE CONSTRUCTED AND MAINTAINED BY IRRIGATION DISTRICTS
Authors: Stringam Blair L. , Gill Tom 
Published: July 2012

ABSTRACTAn overshot gate is designed so that it can be manufactured by local irrigation district personnel. This gate uses a linear actuator to provide the movement for the gate. All other components required for this device are off‐the‐shelf components. The gate has performed with few problems for more than four irrigation seasons. All of the components used in this application have functioned without failure except for a problem with the gate motor. Copyright © 2012 John Wiley & Sons, Ltd.