bluuebunny/crossref_metadata_2025_split huggingface dataset:
Cytotoxic and Nitric Oxide Production‐Inhibitory Activities of Limonoids and Other Compounds from the Leaves and Bark of Melia azedarach
Authors: Pan Xin , Matsumoto Masahiro , Nishimoto Yuki , Ogihara Eri , Zhang Jie , Ukiya Motohiko , Tokuda Harukuni , Koike Kazuo , Akihisa Momoko , Akihisa Toshihiro 
Published: August 2014

AbstractNine limonoids, 1–9, one apocarotenoid, 11, one alkaloid, 12, and one steroid, 13, from the leaf extract; and one triterpenoid, 10, five steroids, 14–18, and two flavonoids, 19 and 20, from the bark extract of Melia azedarach L. (Chinaberry tree; Meliaceae) were isolated. Among these compounds, three compounds, 4–6, were new, and their structures were established as 3‐deacetyl‐28‐oxosalannolactone, 3‐deacetyl‐28‐oxosalanninolide, and 3‐deacetyl‐17‐defurano‐17,28‐dioxosalannin, respectively, on the basis of extensive spectroscopic analyses and comparison with literature data. All of the isolated compounds were evaluated for their cytotoxic activities against leukemia (HL60), lung (A549), stomach (AZ521), and breast (SK‐BR‐3) cancer cell lines. 3‐Deacetyl‐4′‐demethyl‐28‐oxosalannin (3) against HL60 and AZ521 cells, and methyl kulonate (10) against HL60 cells exhibited potent cytotoxicities with IC50 values in the range of 2.8–5.8 μM. In addition, upon evaluation of compounds 1–13 against production of nitric oxide (NO) in mouse macrophage RAW 264.7 cells induced by lipopolysaccharide (LPS), seven, i.e., trichilinin B (1), 4, ohchinin (7), 23‐hydroxyohchininolide (8), 21‐hydroxyisoohchininolide (9), 10, and methyl indole 3‐carboxylate (12), inhibited production of NO with IC50 values in the range of 4.6–87.3 μM with no, or almost no, toxicity to the cells (IC50 93.2–100 μM). Western blot analysis revealed that compound 7 reduced the expression levels of the inducible NO synthase (iNOS) and COX‐2 proteins in a concentration‐dependent manner. Furthermore, compounds 5, 6, 13, and 18–20 exhibited potent inhibitory effects (IC50 299–381 molar ratio/32 pmol TPA) against EpsteinBarr virus early antigen (EBV‐EA) activation induced by 12‐O‐tetradecanoylphorbol‐13‐acetate (TPA) in Raji cell line.
Synthesis of Cholesterol Analogues Bearing BODIPY Fluorophores by Suzuki or Liebeskind–Srogl Cross‐Coupling and Evaluation of Their Potential for Visualization of Cholesterol Pools
Authors: Liu Zheng , Thacker Seth G , Fernandez‐Castillejo Sara , Neufeld Edward B. , Remaley Alan T. , Bittman Robert 
Published: August 2014

AbstractWe report a synthetic route to BODIPY–cholesterol conjugates in which the key steps were Suzuki or Liebeskind–Srogl cross‐coupling of cholesterol phenyl moieties with structurally diverse BODIPY scaffolds. All conjugates feature single‐bonded and hydrophobic linkages between the fluorophore and sterol that are devoid of heteroatoms. Using HeLa cells, we show that these BODIPY–cholesterol analogues can be used simultaneously with the parent BODIPY–cholesterol for cell imaging and flow cytometry. The BODIPY–cholesterol analogues exhibit similar cellular localization in HeLa cells and show similar cholesterol efflux properties from THP‐1 cells to HDL acceptors. These results demonstrate that the red‐shifted BODIPY–cholesterol analogues behave in a manner similar to unlabeled cholesterol and are useful probes for simultaneous visualization of intracellular cholesterol pools and for monitoring cholesterol efflux from cells to extracellular acceptors.
Traceless Semisynthesis of a Set of Histone 3 Species Bearing Specific Lysine Methylation Marks
Authors: Chen Zhonglei , Grzybowski Adrian T. , Ruthenburg Alexander J. 
Published: August 2014

AbstractConsiderable mechanistic insight into the function of histone post‐translational modifications and the enzymes that install and remove them derives from in vitro experiments with modified histones, often embedded in nucleosomes. We report the first semisyntheses of native‐like histone 3 (H3) bearing tri‐ and dimethyllysines at position 79 and trimethyllysine at position 36, as well as more facile and traceless semisyntheses of K9 and K27 trimethylated species. These semisyntheses are practical on a multi‐milligram scale and can also generate H3 with combinations of marks. Each of these modifications has distinct functional consequences, although the pathways by which H3K36me3 and H3K79me2/3 act have not been entirely mapped. To this end, we demonstrated that our semisynthetic histones, when reconstituted into nucleosomes, are valuable affinity reagents for unbiased binding partner discovery and compare them to their methyllysine analogue (MLA) counterparts at the nucleosome level.
Synthesis and Characterization of Supported Cobalt–Manganese Nanoparticles as Model Catalysts for Fischer–Tropsch Synthesis
Authors: Werner Sebastian , Johnson Gregory R. , Bell Alexis T. 
Published: August 2014

AbstractSupported Co is an effective catalyst for the Fischer–Tropsch synthesis of various hydrocarbon products that can be converted to diesel. Recent studies have shown that the formation of methane can be suppressed and the formation of C5+ products enhanced by promoting Co with Mn. Because the activity and product selectivity of Co‐based catalysts are dependent on the size of Co nanoparticles and the extent of Co promotion by Mn, it is desirable to understand these effects by investigating the performance of Co nanoparticles with well‐defined size and elemental composition. The present study was undertaken with the aim of producing well‐defined nanoparticles of Co and Co–Mn and then supporting them on silica. Co and Co–Mn particles were synthesized through the polyol reduction of Co and Mn acetylacetonates. By controlling synthesis conditions, Co particles with diameters of 7–10 nm and similarly sized Co–Mn (Mn/Co=0.1) particles were prepared. XRD and elemental mapping with scanning TEM‐energy‐dispersive X‐ray spectroscopy and scanning TEM‐electron energy loss spectroscopy studies suggested that most of the Mn species was associated with the Co particles. Ex situ prepared Co and Co–Mn nanoparticles were first supported on silica and then investigated for the catalytic activity for the Fischer–Tropsch synthesis. The turnover frequencies and product distributions obtained with silica‐supported Co and Co–Mn nanoparticles were similar to those obtained with catalysts prepared by using the conventional incipient wetness impregnation method. However, the rate of CO consumption per mass of Co was much lower for the catalysts produced by supporting ex situ prepared nanoparticles. This effect was attributed to the sintering of the nanoparticles during their calcination and reduction. Magnetic interactions among nanoparticles during their immobilization and thermal pretreatment were identified as the primary cause of sintering.
Stereoselective CH Borylations of Cyclopropanes and Cyclobutanes with Silica‐Supported Monophosphane–Ir Catalysts
Authors: Murakami Ryo , Tsunoda Kiyoshi , Iwai Tomohiro , Sawamura Masaya 
Published: August 2014

AbstractHeteroatom‐directed CH borylation of cyclopropanes and cyclobutanes was achieved with silica‐supported monophosphane–Ir catalysts. Borylation occurred at the CH bonds located γ to the directing N or O atoms with exceptional cis stereoselectivity relative to the directing groups. This protocol was applied to the borylation of a tertiary CH bond of a ring‐fused cyclopropane.
Randomized phase 2 study of bone‐targeted therapy containing strontium‐89 in advanced castrate‐sensitive prostate cancer
Authors: Bilen Mehmet Asim , Johnson Marcella M. , Mathew Paul , Pagliaro Lance C. , Araujo John C. , Aparicio Ana , Corn Paul G. , Tannir Nizar M. , Wong Franklin C. , Fisch Michael J. , Logothetis Christopher J. , Tu Shi‐Ming 
Published: August 2014

BACKGROUNDRadiopharmaceutical use may improve the survival time of patients with castrate‐resistant prostate cancer and bone metastases. Whether androgen‐deprivation therapy (ADT) combined with bone‐targeted therapy provides a clinical benefit to patients with advanced castrate‐sensitive prostate cancer has not been investigated.METHODSEighty male patients were enrolled, and 79 were randomized: 40 to the control arm and 39 to the strontium‐89 (Sr‐89) arm. After randomization, patients in both study arms received ADT, doxorubicin, and zoledronic acid. Kaplan‐Meier methodology was used to evaluate the progression‐free survival (PFS) time. Multivariate Cox proportional hazards regression was used to evaluate the effects of Sr‐89 after controlling for the number of bone metastases.RESULTSThe median follow‐up time for the 29 patients alive at the last follow‐up was 76.9 months (range, 0.07‐103.4 months). The median PFS time was 18.5 months (95% confidence interval, 9.7‐49.4 months) for the control arm and 12.9 months (95% confidence interval, 8.9‐72.5 months) for the Sr‐89 arm (P = .86). No patient developed myelodysplastic syndrome or a hematologic malignancy. An unplanned subgroup analysis suggested increased efficacy of bone‐targeted therapy with a greater extent of bone involvement (ie, >6 bone metastases vs ≤6 bone metastases on the bone scan).CONCLUSIONSThe data showed that bone‐targeted therapy using 1 dose of Sr‐89 combined with chemohormonal ablation therapy did not favorably affect the PFS of patients with castrate‐sensitive prostate cancer. The combined therapy was feasible and safe. Whether such bone‐targeted therapy provides a favorable outcome for those patients with a greater tumor burden in the bone warrants further investigation. Cancer 2015;121:69–76. © 2014 American Cancer Society.
No evidence for induction or selection of mutant sodium channel expression in the copepod Acartia husdsonica challenged with the toxic dinoflagellate Alexandrium fundyense
Authors: Finiguerra Michael , Avery David E. , Dam Hans G. 
Published: August 2014

AbstractSome species in the dinoflagellate genus Alexandrium spp. produce a suite of neurotoxins that block sodium channels, known as paralytic shellfish toxins (PST), which have deleterious effects on grazers. Populations of the ubiquitous copepod grazer Acartia hudsonica that have co‐occurred with toxic Alexandrium spp. are better adapted than naïve populations. The mechanism of adaptation is currently unknown. We hypothesized that a mutation in the sodium channel could account for the grazer adaptation. We tested two hypotheses: (1) Expression of the mutant sodium channel could be induced by exposure to toxic Alexandrium fundyense; (2) in the absence of induction, selection exerted by toxic A. fundyense would favor copepods that predominantly express the mutant isoform. In the copepod A. hudsonica, both isoforms are expressed in all individuals in varying proportions. Thus, in addition to comparing expression ratios of wild‐type to mutant isoforms for individual copepods, we also partitioned copepods into three groups: those that predominantly express the mutant (PMI) isoform, the wild‐type (PWI) isoform, or both isoforms approximately equally (EI). There were no differences in isoform expression between individuals that were fed toxic and nontoxic food after three and 6 days; induction of mutant isoform expression did not occur. Furthermore, the hypothesis that mutant isoform expression responds to toxic food was also rejected. That is, no consistent evidence showed that the wild‐type to mutant isoform ratios decreased, or that the relative proportion of PMI individuals increased, due to the consumption of toxic food over four generations. However, in the selected line that was continuously exposed to toxic food sources, egg production rate increased, which suggested that adaptation occurred but was unrelated to sodium channel isoform expression.
International Legal: Detecting Foreign Corrupt Practices Crucial to Due Diligence in Acquisitions
Authors: Leibe Brandt 
Published: August 2014

AbstractDue diligence in corporate transactions can be a major project undertaken with significant time constraints. Acquiring companies will ordinarily conduct detailed reviews of target companies' finances and contracts. Depending on the size and significance of the acquisition, there may be dozens of other issues delved into during the due diligence process. As part of this process, acquiring companies must not overlook an assessment of whether the target company has knowingly made corrupt payments to foreign officials to obtain or retain business that would constitute violations of the Foreign Corrupt Practices Act (FCPA).
Litigation—Environment: EPA Reinforces Standards to Use “Representative Data” After Sierra Club
Authors: Sanderson James W. , Lofland Samuel Lee 
Published: August 2014

AbstractOn January 22, 2013, in Sierra Club v. EPA, the US Court of Appeals for the District of Columbia issued an opinion that addressed some Prevention of Significant Deterioration (PSD) permitting program issues. Following this case, on March 4, 2013, the EPA issued guidance entitled “Draft Guidance for PM2.5 Permit Modeling,” and on May 20, 2014, issued its final “Guidance for PM2.5 Permit Modeling.” Sierra Club held that the Environmental Protection Agency lacked the legal authority to create an exemption to the PSD preconstruction data‐gathering requirement through the use of Significant Monitoring Concentrations (SMCs).
NERC and Enforcement Issues: NERC Provides New Definition of Bulk Electric System
Authors: Carpentier Deborah 
Published: August 2014

AbstractSection 215 of the Federal Power Act (FPA) broadly defines the Bulk‐Power System (BPS) as “(A) facilities and control systems necessary for operating an interconnected electric energy transmission network (or any portion thereof); and (B) electric energy from generating facilities needed to maintain transmission system reliability.” Defining the extent of the BPS is important because the Federal Energy Regulatory Commission (FERC) requires each user, owner, and operator of the BPS to register with the North American Electric Reliability Corporation (NERC), and it is this registration that dictates the reliability standards with which the entity must comply.
Examining the association between late‐life depressive symptoms, cognitive function, and brain volumes in the context of cognitive reserve
Authors: O'Shea Deirdre M. , Fieo Robert A. , Hamilton Jamie L. , Zahodne Laura B. , Manly Jennifer J. , Stern Yaakov 
Published: August 2014

ObjectiveThe present study aimed to investigate whether cognitive reserve moderated the association between depressive symptoms and cognition, as well as brain volumes in a sample of older adults.MethodsNon‐demented participants (n = 3484) were selected from the Washington Heights/Hamilton Heights Inwood Columbia Aging Project (Northern Manhattan). A subsample of these participants without dementia (n = 703), who had brain imaging data, was also selected for a separate analysis. Depressive symptomatology was assessed with the 10‐item Center for Epidemiologic Studies Depression Scale. Reading level and years of education were used as measures of cognitive reserve. Four distinct cognitive composite scores were calculated: executive function, memory, visual–spatial, and language.ResultsMultiple regression analysis revealed interaction effects between both measures of cognitive reserve and depressive symptoms on all the cognitive outcome measures except for visual–spatial ability. Those with greater reserve showed greater cognitive decrements than those with lower levels of reserve as depressive symptoms increased. A borderline interaction effect was revealed between reading level and depressive symptoms on total brain volumes. Those with lower reading scores showed greater volume loss as depressive symptoms increased than those with higher reading scores.ConclusionsOur findings indicate that the association between late‐life depressive symptoms and core aspects of cognition varies depending on one's level of cognitive reserve. Those that had greater levels of education and/or reading ability showed a greater decrease in memory, executive, and language performances as depressive symptoms increased than those with lower years of education and reading ability. Copyright © 2014 John Wiley & Sons, Ltd.
First Diastereoselective PasseriniSmiles and UgiSmiles Reactions Using Chiral Aldehydes
Authors: Radha Krishna Palakodety , Dayaker Gandrath , Venkata Ramana D. , Kunde Ramesh 
Published: August 2014

AbstractA diastereoselective O/N‐arylative Passerini/Ugi reaction of chiral aldehydes with commercially available isocyanides affording O‐aryl amides and N‐aryl amides, respectively, as products in moderate to good yields, together with de values, is reported.
Ethenolate Transfer Reactions: A Facile Synthesis of Vinyl Esters
Authors: Kaliyaperumal Appaye Srinivasan , Pandurang Nikumbh Satish , Reddy Govindapur Rajeshwar , Banerjee Shyamapada , Bhalerao Dinesh S. , Syam Kumar Unniaran K. 
Published: August 2014

AbstractA simple and efficient metal‐free ethenolate transfer reaction has been elaborated in moderate‐to‐high yields from vinyl acetate. This reaction was accomplished by generation of potassium ethenolate, which was then reacted with homo and mixed anhydrides of aliphatic, aryl and heteroaryl acids, to yield the corresponding vinyl esters. The utility of thus generated vinyl esters was then probed by carrying out intramolecular Heck reactions to give isobenzofuran‐1(3H)‐one derivatives in excellent yields.
A New Megastigmane Glucoside and Three New Flavonoid Glycosides from Spiraea prunifolia var. simpliciflora
Authors: Hye Yean Min , Sun Kim Ju , Sik Kang Sam , Shik Kim Yeong 
Published: August 2014

AbstractA new megastigmane glucoside, simplicifloranoside (1), and three new flavonol glycosides, prunifolianosides A–C (2–4, resp.), were isolated from the aerial parts of Spiraea prunifolia var. simpliciflora. In addition, fifteen known compounds, including five phenolic acids, three lignans, four flavonoids, one eugenol glycoside, and two alkyl‐primeverosides, were also identified. Their structures were elucidated on the basis of detailed spectroscopic analyses and acid hydrolysis.
Labdane Diterpenoids from the Roots of Amomum maximum and Their Cytotoxic Evaluation
Authors: Luo Jian‐Guang , Yin Hong , Fan Bo‐Yi , Kong Ling‐Yi 
Published: August 2014

AbstractA rare labdane diterpene γ‐lactam, 1, and two new labdane diterpenoids, 2 and 3, along with two known diterpenes, 4 and 5, were isolated from the roots of Amomum maximum. Their structures were established on the basis of spectroscopic data. All of the isolates were evaluated for their cytotoxic activities, and compound 3 was found to exhibit an inhibitory activity against MG‐63 cell lines with an IC50 value of 3.3±0.8 μg/ml.
Synthesis of 3‐(ω‐Hydroxyalkoxy)isobenzofuran‐1(3H)‐ones by Trifluoroacetic Acid‐Mediated Lactonization of tert‐Butyl 2‐(1,3‐Dioxol‐2‐yl)‐ or 2‐(1,3‐Dioxan‐2‐yl)benzoates
Authors: Kobayashi Kazuhiro , Kuroda Minami 
Published: August 2014

AbstractAn efficient two‐step method for the preparation of 3‐(2‐hydroxyethoxy)‐ or 3‐(3‐hydroxypropoxy)isobenzofuran‐1(3H)‐ones 3 has been developed. Thus, the reaction of 1‐(1,3‐dioxol‐2‐yl)‐ or 1‐(1,3‐dioxan‐2‐yl)‐2‐lithiobenzenes, generated in situ by the treatment of 1‐bromo‐2‐(1,3‐dioxol‐2‐yl)‐ or 1‐bromo‐2‐(1,3‐dioxan‐2‐yl)benzenes 1 with BuLi in THF at −78°, with (Boc)2O afforded tert‐butyl 2‐(1,3‐dioxol‐2‐yl)‐ or 2‐(1,3‐dioxan‐2‐yl)benzoates 2, which can subsequently undergo facile lactonization on treatment with CF3COOH (TFA) in CH2Cl2 at 0° to give the desired products in reasonable yields.
Dye‐Labeled Cα‐Tetrasubstituted α‐Amino Acids
Authors: Dobmeier Michael , Maity Prantik , König Burkhard 
Published: August 2014

AbstractWe report the synthesis of pyrene‐ and carboxyfluorescein labeled Cα‐tetrasubstituted amino acids (TAAs). The fluorescent dye can be coupled to the TAA before or after its incorporation into a peptide sequence using a Suzuki‐type CC bond formation.
Oligonucleotide Analogues with Integrated Bases and Backbone (ONIB). Part 31
Authors: Schulze‐Adams Martina , Touboul David , Bernet Bruno , Vasella Andrea 
Published: August 2014

AbstractThe self‐complementary guanosine‐ and cytidine‐derived aminomethylene‐linked C*[n]G dinucleoside 9 was synthesized by reductive amination of aldehyde 3 with an iminophosphorane derived from azide 7. Deacylation of 9 gave the isopropylidene‐protected dinucleoside 10. The sequence‐isomeric G*[n]C dinucleoside 11 was similarly prepared from aldehyde 8 and azide 5, and deacylated to 12. The association of 10 and 12 in CHCl3 or in CHCl3/DMSO mixtures, and the structure of the associates were studied by 1H‐NMR, ESI‐MS, CD, and vapor pressure osmometry (VPO). Broad 1H‐NMR signals of dinucleosides 10 and 12 evidence an equilibrium between duplexes and quadruplexes (Hoogsteen base pairing between the WatsonCrick base‐paired duplexes). The quadruplex dominates for the G*[n]C dinucleoside 12 between −50° and room temperature. The sequence‐isomeric C*[n]G 10 forms mostly only a cyclic duplex in CDCl3 and in CDCl3/(D6)DMSO 9 : 1.
Methylation of Bone SOST, Its mRNA, and Serum Sclerostin Levels Correlate Strongly With Fracture Risk in Postmenopausal Women
Authors: Reppe Sjur , Noer Agate , Grimholt Runa M , Halldórsson Bjarni V , Medina-Gomez Carolina , Gautvik Vigdis T , Olstad Ole Kristoffer , Berg Jens Petter , Datta Harish , Estrada Karol , Hofman Albert , Uitterlinden André G , Rivadeneira Fernando , Lyle Robert , Collas Philippe , Gautvik Kaare M 
Published: August 2014

ABSTRACT

Inhibition of sclerostin, a glycoprotein secreted by osteocytes, offers a new therapeutic paradigm for treatment of osteoporosis (OP) through its critical role as Wnt/catenin signaling regulator. This study describes the epigenetic regulation of SOST expression in bone biopsies of postmenopausal women. We correlated serum sclerostin to bone mineral density (BMD), fractures, and bone remodeling parameters, and related these findings to epigenetic and genetic disease mechanisms. Serum sclerostin and bone remodeling biomarkers were measured in two postmenopausal groups: healthy (BMD T-score &gt; –1) and established OP (BMD T-score &lt; –2.5, with at least one low-energy fracture). Bone specimens were used to analyze SOST mRNAs, single nucleotide polymorphisms (SNPs), and DNA methylation changes. The SOST gene promoter region showed increased CpG methylation in OP patients (n = 4) compared to age and body mass index (BMI) balanced controls (n = 4) (80.5% versus 63.2%, p = 0.0001) with replication in independent cohorts (n = 27 and n = 36, respectively). Serum sclerostin and bone SOST mRNA expression correlated positively with age-adjusted and BMI-adjusted total hip BMD (r = 0.47 and r = 0.43, respectively; both p &lt; 0.0005), and inversely to serum bone turnover markers. Five SNPs, one of which replicates in an independent population-based genomewide association study (GWAS), showed association with serum sclerostin or SOST mRNA levels under an additive model (p = 0.0016 to 0.0079). Genetic and epigenetic changes in SOST influence its bone mRNA expression and serum sclerostin levels in postmenopausal women. The observations suggest that increased SOST promoter methylation seen in OP is a compensatory counteracting mechanism, which lowers serum sclerostin concentrations and reduces inhibition of Wnt signaling in an attempt to promote bone formation. © 2014 American Society for Bone and Mineral Research.
Semiframes with Block Size Three and Odd Group Size
Authors: Cao H. , Fan J. , Xu D. 
Published: August 2014

AbstractA ‐semiframe of type is a ‐GDD of type , , in which the collection of blocks can be written as a disjoint union where is partitioned into parallel classes of and is partitioned into holey parallel classes, each holey parallel class being a partition of for some . A ‐SF is a ‐semiframe of type in which there are p parallel classes in and d holey parallel classes with respect to . In this paper, we shall show that there exists a (3, 1)‐SF for any if and only if , , , and .