bluuebunny/crossref_metadata_2025_split huggingface dataset:
Identification of an Ene Reductase from Yeast Kluyveromyces Marxianus and Application in the Asymmetric Synthesis of (R)‐Profen Esters
Authors: Li Zhining , Wang Zexu , Meng Ge , Lu Hong , Huang Zedu , Chen Fener 
Published: January 2018

AbstractGiven their ability to reduce activated alkenes thereby generating up to two stereogenic centers, ene reductases from the old yellow enzyme (OYE) family have received much attention as effective biocatalysts. Through genome mining, a “classical” OYE, KYE2, was identified from Kluyveromyces marxianus CBS4857 and fully characterized in vitro. This NADPH‐dependent enzyme displayed a broad substrate spectrum for the bioreduction of activated alkenes. The highly stereoselective synthesis (>95 % ee) of various (R)‐profen methyl esters, including the synthesis of (R)‐flurbiprofen methyl ester on a semi‐preparative scale further demonstrates the potential of KYE2 to be developed as a general biocatalyst for chemical synthesis.
What have we been looking at? A call for consistency in studies of primate vigilance
Authors: Allan Andrew T.L. , Hill Russell A. 
Published: January 2018

AbstractVigilance functions to detect threats. In primates, these threats emerge from both predators and conspecifics, but a host of other social, demographic, and ecological factors have been shown to influence primate vigilance patterns. The primate vigilance literature is thus characterized by considerable variation in findings, with inconsistent or contradictory results reported not only across different species but also within species and populations across studies. Some of this variation could emerge from fundamental differences in the methods employed, making comparisons across species and groups challenging. Furthermore, identifying consistent behavioral markers for the state of vigilance appears to have proved challenging in primates, leading to a range of definitions being developed. Deviation at this level leads directly into concomitant variation at the level of sampling methodologies. As a result, the primate vigilance literature currently presents a diverse series of approaches to exploring subtly different behaviors and phenomena. This review calls for a greater consistency in studying vigilance, with the aim of encouraging future research to follow similar principles leading to more comparable results. Identifying whether an animal is in a vigilant state is challenging for most field researchers; identifying and recording a more general behavior of “looking” should though be more achievable. Experimental approaches could then be employed to understand the compatibility “looking” has with predator detection (and other threats) in individual study systems. The outcome of this approach will allow researchers to understand the key determinants of looking in their study groups and explore threat detection probabilities given an individual or group's relative level of looking.
Ossification Pattern in Forelimbs of the Siamese Crocodile (Crocodylus siamensis): Similarity in Ontogeny of Carpus Among Crocodylian Species
Authors: Gregorovičová Martina , Kvasilová Alena , Sedmera David 
Published: January 2018

ABSTRACTCrocodylians have highly derived elongated carpus, which is related to their use of forelimbs in many types of gaits as well as in burrowing. The objective of present study was to describe the ossification of the forelimb in five stages of Siamese crocodile (Crocodylus siamensis). The ossification begins approximately at stage 20 in arm and forearm bones moving sequentially to the metacarpal elements. The first carpal elements with ossification centers are radiale + intermedium and ulnare (stage 22–23), and their ossification mode is typical of long bones. Between stages 22 and 24 distal carpals 3, 4, and 5 fuse together to a single formation. In the stage 25, the ossification proceeds to the pisiform, which starts ossifying late during the embryogenesis. The phalangeal formula of the digits is 2,3,4,5,3. Although there are some interspecific differences, it appears that all crocodylians have similarly uniform skeletal pattern, the process of ossification, number of carpal elements and phalangeal formulas probably due to their similar lifestyles. Anat Rec, 301:1159–1168, 2018. © 2018 Wiley Periodicals, Inc.
Cardiac repolarization during fingolimod treatment in patients with relapsing–remitting multiple sclerosis
Authors: Laiho Aapo , Laitinen Tiina M. , Hartikainen Päivi , Hartikainen Juha E. K. , Laitinen Tomi P. , Simula Sakari 
Published: January 2018

AbstractBackgroundFingolimod is a sphingosine‐1‐phosphate receptor modulator for the treatment of relapsing–remitting multiple sclerosis (RRMS). Despite an established effect on heart rate, the effect of fingolimod on cardiac repolarization is not completely known.MethodsTwenty‐seven patients with RRMS underwent 24‐hr ambulatory ECG before fingolimod (baseline), at the day of fingolimod initiation (1D) and after three‐month treatment (3M). The mean values of RR‐interval as well as QT‐interval corrected by Bazzet's (QTcBaz) and Fridericia's (QTcFri) formula were compared between baseline, 1D, and 3M over 24‐hr period as well as at daytime and nighttime.ResultsQTcBaz over 24‐hr was shorter at 1D (414 ± 20 ms, p < .001) and at 3M (414 ± 20 ms, p < .001) than at baseline (418 ± 20 ms). In contrast, QTcFri over 24‐hr was longer at 1D (410 ± 19 ms, p < .001) but similar at 3M (406 ± 19 ms, p = .355) compared to baseline (407 ± 19 ms). Daytime QTcBaz was shorter at 1D (p < .001) and at 3M (p = .007), whereas daytime QTcFri was longer at 1D (p < .05) but similar at 3M (p = ns) compared to baseline. During the night, changes were observed neither in QTcBaz nor in QTcFri between baseline, 1D, and 3M.ConclusionsChanges in cardiac repolarization after fingolimod initiation were mild and occurred at daytime. Ambiguously, QTcBaz demonstrated shortening, whereas QTcFri showed prolongation in cardiac repolarization after fingolimod initiation. The formula applied for QT‐interval correction needs to be taken carefully into account as evaluating pharmacovigilance issues related to fingolimod.
The dilemma of environmental sustainability in a developing country: Environmental crimes in southern Brazil
Authors: Roque Patrícia Gonçalves , Severo Eliana Andréa , Dorion Eric Charles Henri , Roque Eliel de Souza , de Guimarães Julio Cesar Ferro 
Published: January 2018

AbstractIn a contemporary society, awareness of the importance of environmental causes is eminent; however, crimes against the Brazilian environment do occur at an unacceptable rate, because it concerns a developing country situation. This study aims to analyze the most incident environmental crimes that occurred in the State of Rio Grande do Sul, a meridional region of Brazil, in a territory that covers 239 municipalities. The study analyzes the environmental management dilemmas that occurred in the inspection carried out by the Third Environmental Battalion of the Military Brigade in the period of 2011 to 2016. The method was qualitative and exploratory considering that the research is the first of its kind in the region. The results highlight a lack of commitment with the Brazilian environmental legislation, from offenders acting in the criminal, administrative, and civil spheres. The 5 most serious environmental crimes refer to deforestation, unlicensed activities, captive animals, solid waste pollution, and effluents pollution. Furthermore, environmental sustainability is still not present as a strategic area in the Brazilian organizations, and the ones that do have some internal practices do it more in reaction to legal penalties than for awareness of the environmental causes. The research brings important environmental information on decision making related to actions and public policies that promote environmental sustainability in developing countries.
The differences on efficacy of oxaliplatin in locally advanced colon cancer between mucinous and nonmucinous adenocarcinoma
Authors: Yu Dehao , Gao Peng , Song Yongxi , Yang Yuchong , Chen Xiaowan , Sun Yu , Li Ailin , Wang Zhenning 
Published: January 2018

AbstractUntil now, it remains unclear how to best use the histological subtype in clinical practice. This study aimed to compare differences in the efficacy of postoperative chemotherapy among different histological subtypes of colon adenocarcinomas. Using the Surveillance, Epidemiology, and End Results‐Medicare database, 51,200 patients with stage II or III primary colon carcinomas who underwent resection for curative intent between 1992 and 2008 were included. The survival benefit was evaluated using a Cox proportional hazards model, interaction analyses, and propensity score‐matched techniques. There was no significant difference in survival for low‐risk stage II mucinous adenocarcinoma (MA) or nonmucinous adenocarcinoma (NMA) between 5‐FU and oxaliplatin‐treated groups (P = 0.387 for MA, P = 0.629 for NMA). Patients with high‐risk stage II NMA who received the oxaliplatin chemotherapy regimen had significantly improved cancer‐specific survival (CSS) compared with the 5‐FU group (P = 0.004), while those with MA saw no improvement (P = 0.690). For stage III tumors, patients with NMA who received the oxaliplatin chemotherapy regimen had significantly improved CSS compared with the 5‐FU group (P < 0.001), while those with MA saw no improvement (P = 0.300). There were significant interactions between chemotherapy regimen and histological subtype. For patients with resected colon cancer who received 5‐FU‐based postoperative chemotherapy, oxaliplatin chemotherapy prolongs CSS for stage III and high‐risk stage II NMA. Conversely, there was no similar improvement with addition of oxaliplatin for patients with stage III or stage II MA.
Selective Oxidative Carbonylation of Aniline to Diphenylurea with Ionic Liquids
Authors: Zahrtmann Nanette , Claver Carmen , Godard Cyril , Riisager Anders , Garcia‐Suarez Eduardo J. 
Published: January 2018

AbstractA catalytic system for the selective oxidative carbonylation of aniline to diphenylurea based on Pd complexes in combination with imidazolium ionic liquids is presented. Both oxidants, Pd complexes, and ionic liquids affect the activity of the reaction, and the choice of oxidant determines the selectivity of the reaction. Together they allow the reaction to proceed under comparatively mild conditions without a loss of activity. Examination of the reaction by use of in situ NMR spectroscopy allowed us to observe an intermediate suggested only previously, which supported the proposed mechanism.
Icosahedral Pt–Ni Nanocrystalline Electrocatalyst: Growth Mechanism and Oxygen Reduction Activity
Authors: Tian Renxiu , Shen Shuiyun , Zhu Fengjuan , Luo Liuxuan , Yan Xiaohui , Wei Guanghua , Zhang Junliang 
Published: January 2018

AbstractEngineering the structure of Pt alloy offers an effective way to the design of high performance electrocatalysts. Herein, we synthesize a sandwich‐structured, icosahedral Pt2.1Ni catalyst through a hot injection method. Its growth involves three steps: 1) burst nucleation of Pt atoms to form a Pt‐enriched core, 2) heterogeneous nucleation of Ni atoms onto the Pt core to form a Ni‐enriched interlayer, and 3) kinetic controlled growth of a Pt‐enriched shell. The Pt‐enriched core protects the nanostructure from collapse and mitigates the strain change caused by lattice mismatch, and thus enhances the stability of the structure. The Ni‐enriched interlayer induces the electronic modification of the outermost Pt shell, and in turn tunes the activity. The Pt‐enriched shell provides more active sites through the exposure of (1 1 1) facets and retards the dissolution of Ni atoms. As a result, this sandwich‐structure enables impressive electrocatalytic activity (0.91 mA cm−2 and 0.32 A
@ 0.9 V) and duability.
Ursolic acid derivatives as potential antidiabetic agents: In vitro, in vivo, and in silico studies
Authors: Guzmán‐Ávila Ricardo , Flores‐Morales Virginia , Paoli Paolo , Camici Guido , Ramírez‐Espinosa Juan José , Cerón‐Romero Litzia , Navarrete‐Vázquez Gabriel , Hidalgo‐Figueroa Sergio , Yolanda Rios Maria , Villalobos‐Molina Rafael , Estrada‐Soto Samuel 
Published: January 2018

Abstract

Hit, Lead & Candidate Discovery

Protein tyrosine phosphatase 1B (PTP‐1B) has attracted interest as a novel target for the treatment of type 2 diabetes, this because its role in the insulin‐signaling pathway as a negative regulator. Thus, the aim of current work was to obtain seven ursolic acid derivatives as potential antidiabetic agents with PTP‐1B inhibition as main mechanism of action. Furthermore, derivatives 1–7 were submitted in vitro to enzymatic PTP‐1B inhibition being 3, 5, and 7 the most active compounds (IC50 = 5.6, 4.7, and 4.6 μM, respectively). In addition, results were corroborated with in silico docking studies with PTP‐1B orthosteric site A and extended binding site B, showed that 3 had polar and Van der Waals interactions in both sites with Lys120, Tyr46, Ser216, Ala217, Ile219, Asp181, Phe182, Gln262, Val49, Met258, and Gly259, showing a docking score value of −7.48 Kcal/mol, being more specific for site A. Moreover, compound 7 showed polar interaction with Gln262 and Van der Waals interactions with Ala217, Phe182, Ile219, Arg45, Tyr46, Arg47, Asp48, and Val49 with a predictive docking score of −6.43 kcal/mol, suggesting that the potential binding site could be localized in the site B adjacent to the catalytic site A. Finally, derivatives 2 and 7 (50 mg/kg) were selected to establish their in vivo antidiabetic effect using a noninsulin‐dependent diabetes mice model, showing significant blood glucose lowering compared with control group (p < .05).
The potential of radiolabeled chemotherapeutics in tumor diagnosis: Preliminary investigations with 68Ga‐gemcitabine
Authors: Ghosh Subhajit , Das Tapas , D. Sarma Haladhar , Dash Ashutosh 
Published: January 2018

Abstract

Preclinical Research & Development

Gemcitabine, a nucleoside analog, is a well‐known chemotherapeutic drug that is used either alone or with other agents to treat a wide variety of cancers. The aim of the present work was to evaluate the potential of 68Ga‐labeled gemcitabine for its application in positron emission tomography (PET) imaging of tumorous lesions. Gemcitabine was coupled with p‐NCS‐benzyl‐DOTA in order to facilitate radiolabeling with 68Ga. The gemcitabine‐p‐NCS‐benzyl‐DOTA was radiolabeled with 68Ga, obtained from a 68Ge/68Ga radionuclide generator. The radiolabeled product was characterized by high performance liquid chromatography (HPLC) and its tumor specificity was evaluated by biodistribution studies in Swiss mice bearing fibrosarcoma tumors. Preliminary bioevaluation study showed good tumor uptake within 1 hr post‐administration [2.5% Injected Activity (IA) per g of tumor] with rapid renal clearance (>90% IA) and a high tumor to muscle ratio. 68Ga‐gemcitabine may have potential as a PET agent for tumor imaging.
A novel sperm adaptation to evolutionary constraints on reproduction: Pre‐ejaculatory sperm activation in the beach spawning capelin (Osmeridae)
Authors: Beirão José , Lewis Jason A. , Wringe Brendan F. , Purchase Craig F. 
Published: January 2018

AbstractReproduction of external fertilizing vertebrates is typically constrained to either fresh or salt water, not both. For all studied amphibians and fishes, this constraint includes immotile sperm that are activated after ejaculation only by the specific chemistry of the fertilizing medium in which the species evolved (fresh, brackish, or salt water). No amphibians can reproduce in the sea. Although diadromous fishes may migrate between salt and fresh water, they are shackled to their natal environment for spawning in part because of sperm activation. Here, we report for the first time among all documented external fertilizing vertebrates, that in the absence of any external media, sperm are motile at ejaculation in a marine spawning fish (Osmeridae, capelin, Mallotus villosus). To illuminate why, we evaluated sperm behavior at different salinities in M. villosus as well as the related freshwater spawning anadromous rainbow smelt (Osmerus mordax). Surprisingly, sperm performance was superior in fresh water for both species. M. villosus spend their entire life at sea but our results show that their sperm are deactivated by sea water, suggesting a freshwater ancestry. By circumventing constraining water chemistry, we interpret the unique pre‐ejaculatory sperm activation in this species as a novel adaptation that enables fertilization in the marine environment. These findings also contribute to understanding the persistence of anadromy, despite great energetic costs to adult fishes.
Sea ice meiofauna distribution on local to pan‐Arctic scales
Authors: Bluhm Bodil A. , Hop Haakon , Vihtakari Mikko , Gradinger Rolf , Iken Katrin , Melnikov Igor A. , Søreide Janne E. 
Published: January 2018

AbstractArctic sea ice provides microhabitats for biota that inhabit the liquid‐filled network of brine channels and the ice–water interface. We used meta‐analysis of 23 published and unpublished datasets comprising 721 ice cores to synthesize the variability in composition and abundance of sea ice meiofauna at spatial scales ranging from within a single ice core to pan‐Arctic and seasonal scales. Two‐thirds of meiofauna individuals occurred in the bottom 10 cm of the ice. Locally, replicate cores taken within meters of each other were broadly similar in meiofauna composition and abundance, while those a few km apart varied more; 75% of variation was explained by station. At the regional scale (Bering Sea first‐year ice), meiofauna abundance varied over two orders of magnitude. At the pan‐Arctic scale, the same phyla were found across the region, with taxa that have resting stages or tolerance to extreme conditions (e.g., nematodes and rotifers) dominating abundances. Meroplankton, however, was restricted to nearshore locations and landfast sea ice. Light availability, ice thickness, and distance from land were significant predictor variables for community composition on different scales. On a seasonal scale, abundances varied broadly for all taxa and in relation to the annual ice algal bloom cycle in both landfast and pack ice. Documentation of ice biota composition, abundance, and natural variability is critical for evaluating responses to decline in Arctic sea ice. Consistent methodology and protocols must be established for comparability of meiofauna monitoring across the Arctic. We recommend to (1) increase taxonomic resolution of sea ice meiofauna, (2) focus sampling on times of peak abundance when seasonal sampling is impossible, (3) include the bottom 30 cm of ice cores rather than only bottom 10 cm, (4) preserve specimens for molecular analysis to improve taxonomic resolution, and (5) formulate a trait‐based framework that relates to ecosystem functioning.
Mate choice decision rules: Trait synergisms and preference shifts
Authors: Burley Nancy Tyler , Hamedani Elnaz , Symanski Cole 
Published: January 2018

AbstractAn important and understudied question in sexual selection is how females evaluate information from multiple secondary sexual traits (SSTs), particularly when expression of traits is phenotypically uncorrelated. We performed mate choice experiments on zebra finches (Taeniopygia guttata castanotisGould) to evaluate two hypotheses: preference shifts (obstacles to choice using one trait increase chooser reliance on others) and trait synergisms (choice based on the sum/product of two or more independently varying traits). The first experiment, which employed males raised on diets that impactSSTexpression, supported the trait synergism hypothesis: overall, male pairing success was best predicted by synergisms involving beak color and cheek patch size. Results did not support the preference shift hypothesis. Results of a follow‐up experiment that included males reared on a single diet, and in which male beak color and cheek patch size were manipulated, were also consistent with the trait synergism hypothesis. Results have implications for understanding the long‐term persistence of multipleSSTs in populations and for the measurement of repeatability and heritability of mate preferences.
Multiple surveys employing a new sample‐processing protocol reveal the genetic diversity of placozoans in Japan
Authors: Miyazawa Hideyuki , Nakano Hiroaki 
Published: January 2018

AbstractPlacozoans, flat free‐living marine invertebrates, possess an extremely simple bauplan lacking neurons and muscle cells and represent one of the earliest‐branching metazoan phyla. They are widely distributed from temperate to tropical oceans. Based on mitochondrial 16S rRNA sequences, 19 haplotypes forming seven distinct clades have been reported in placozoans to date. In Japan, placozoans have been found at nine locations, but 16S genotyping has been performed at only two of these locations. Here, we propose a new processing protocol, “ethanol‐treated substrate sampling,” for collecting placozoans from natural environments. We also report the collection of placozoans from three new locations, the islands of Shikine‐jima, Chichi‐jima, and Haha‐jima, and we present the distribution of the 16S haplotypes of placozoans in Japan. Multiple surveys conducted at multiple locations yielded five haplotypes that were not reported previously, revealing high genetic diversity in Japan, especially at Shimoda and Shikine‐jima Island. The observed geographic distribution patterns were different among haplotypes; some were widely distributed, while others were sampled only from a single location. However, samplings conducted on different dates at the same sites yielded different haplotypes, suggesting that placozoans of a given haplotype do not inhabit the same site constantly throughout the year. Continued sampling efforts conducted during all seasons at multiple locations worldwide and the development of molecular markers within the haplotypes are needed to reveal the geographic distribution pattern and dispersal history of placozoans in greater detail.
Life history changes in Trogoderma variabile and T. inclusum due to mating delay with implications for mating disruption as a management tactic
Authors: Gerken Alison R. , Campbell James F. 
Published: January 2018

AbstractControlling postharvest pest species is a costly process with insecticide resistance and species‐specific control requiring multiple tactics. Mating disruption (MD) can be used to both decrease a female's access to males and delay timing of mating and decreases overall mating success in a population and population growth rate. Development of new commercially available MD products requires an understanding of life history parameters associated with mating delay. These can provide information for targeting proportions of reproducing individuals using MD. After delaying mating for females of two closely related beetle species, Trogoderma variabile and T. inclusum, we surveyed survivorship, number of eggs laid, and number of progeny emerged. With increases in mating age, total number of eggs laid and total number of progeny emerged significantly declined over time. T. inclusum typically had greater numbers of eggs laid and progeny emerged compared to T. variabile as female age at mating increased, suggesting that T. inclusum may be more resistant to long‐term delays in mating. Life span showed an increase as mating age increased but life span significantly decreased almost immediately following mating. Simulations depicting multiple distributions of mating within a population suggest that in a closed population, high levels of mating delay significantly reduced reproductive growth rates. Although reproductive growth rates were decreased with increased mating age, they are still large enough to maintain populations. This study highlights the differences in life history between two closely related species, suggesting that T. inclusum outperforms T. variabile over the course of a life span, but T. variabile has better reproductive capabilities early in life. MD may also be a viable component of a pest management system for these two species as it significantly decreased overall reproductive output and population growth.