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Introduction: Numerous studies have found that expert players anticipate better than novices. If more accurate prediction represents performance monitoring of experts, what are the advantages of elite basketball players in identifying and processing available cues? There is still a lack of sufficient evidence. This study examined the visual search in basketball players and explored the performance monitoring of action anticipation, adopting an expert–novice paradigm and eye‐movement technology. Methods: Forty basketball players were recruited in this study: 20 in the expert group and 20 in the novice group. Participants were asked to predict the outcome of videotaped basketball throws and their accuracy and eye‐movement characteristics were record. Results: The accuracy of the expert was significantly higher than that of the novice. The experts were able to instantly search and identify important cues in anticipation, and the gaze area of the experts was concentrated on the area of interest of the body. Additionally, the expert group showed long, repetitive, and rapid visual search of vital information, and improved their performance of the task. Conclusion: The experts could monitor the performance of prediction by grabbing vital shooting information (such as the body of a player). The results suggest the athletes and coaches that if they want to improve the ability of prediction, it may be useful to shift their focus of attention from ball trajectory to body action. [ABSTRACT FROM AUTHOR]

Despite widespread use of the deuterium isotope effect, selective deuterium labeling of chemical molecules remains a major challenge. Herein, a facile and general electrochemically driven, organic mediator enabled deuteration of styrenes with deuterium oxide (D2O) as the economical deuterium source was reported. Importantly, this transformation could be suitable for various electron rich styrenes mediated by triphenylphosphine (TPP). The reaction proceeded under mild conditions without transition‐metal catalysts, affording the desired products in good yields with excellent D‐incorporation (D‐inc, up to >99 %). Mechanistic investigations by means of isotope labeling experiments and cyclic voltammetry tests provided sufficient support for this transformation. Notably, this method proved to be a powerful tool for late‐stage deuteration of biorelevant compounds. [ABSTRACT FROM AUTHOR]

Despite widespread use of the deuterium isotope effect, selective deuterium labeling of chemical molecules remains a major challenge. Herein, a facile and general electrochemically driven, organic mediator enabled deuteration of styrenes with deuterium oxide (D2O) as the economical deuterium source was reported. Importantly, this transformation could be suitable for various electron rich styrenes mediated by triphenylphosphine (TPP). The reaction proceeded under mild conditions without transition‐metal catalysts, affording the desired products in good yields with excellent D‐incorporation (D‐inc, up to >99 %). Mechanistic investigations by means of isotope labeling experiments and cyclic voltammetry tests provided sufficient support for this transformation. Notably, this method proved to be a powerful tool for late‐stage deuteration of biorelevant compounds. [ABSTRACT FROM AUTHOR]

Forming high‐temperature α‐Al2O3 phase under soft sparking is an intriguing phenomenon in plasma electrolytic oxidation (PEO) of Al alloys, which contradicts the low energy input of the process. In this study, α‐Al2O3 doped with black CuO is formed beneath an amorphous white outer layer on Al–Cu–Li alloy by PEO in a dilute silicate electrolyte under soft sparking. In comparison, reddish coatings with dominating γ‐Al2O3 are formed under the conventional plasma discharges, although blackish inner layer with α‐Al2O3 can also be exposed by heavily polishing the samples. In order to know the underlying mechanism, temperatures at the coating surface and the underlying substrate have been monitored by a thermocouple under the conventional and soft sparking PEO regimes, respectively. Interestingly, high temperatures are detected in the case of soft sparking rather than PEO with strong discharges. The formation of CuO, quartz, and cristobalite within the soft sparking coating also supports the existence of high temperature. Hence, the formation of α‐Al2O3 under soft sparking can be resolved to the conventional thermal activation mechanism, without the need of seeking other plausible explanations. Thermal condition evaluation for soft sparking PEO suggests that values of the effective thermal conductivity during PEO process for the outer layer and the barrier layer at the coating/substrate interface might be lower than ∼0.05 and ∼0.0017 W m−1 K−1, respectively. It is believed that the amorphous structure of the outer and barrier layers effectively blocks the heat dissipation, facilitating the formation of a highly wear‐resistant inner layer with α‐Al2O3, CuO, and the other high‐temperature species under soft sparking. [ABSTRACT FROM AUTHOR]

This paper constructs a local classical solution of degenerate hyperbolic problem for the two‐dimensional nonlinear wave system. To deal with the parabolic degeneracy, we introduce a new set of coordinates to transform the nonlinear wave system to a new system that has explicitly singularity‐regularity structures. By constructing a weighted metric space, we establish the existence of solution for the new system. Returning the solution to the original variables, we obtain the existence of the classical solution for the nonlinear wave system with degenerate boundary value problem. [ABSTRACT FROM AUTHOR]

Carbon dioxide (CO2) is an abundant, inexpensive, renewable C1 resource and the main component of greenhouse gas, thereby the research for its sustainable and efficient conversion has received notable attention in recent years. Electrochemical organic synthesis, as a green and efficient synthetic method, is convinced to be an ideal approach for CO2 utilization. In this review, recent advances in electrocarboxylation with CO2 were summarized through different reaction types, which would disclose the great potential of electrocarboxylation in green organic synthesis. [ABSTRACT FROM AUTHOR]

Herein, we disclose a straightforward, robust, and simple route to access β‐substituted desaturated cyclic amines via an electrochemically driven desaturative β‐functionalization of cyclic amines. This transformation is based on multiple single‐electron oxidation processes using catalytic amounts of ferrocene. The reaction proceeds in the absence of stoichiometric amounts of electrolyte under mild conditions, affording the desired products with high chemo‐ and regioselectivity. The reaction was tolerant of a broad range of substrates and also enables late‐stage β‐C(sp3)−H acylation of potentially valuable products. Preliminary mechanistic studies using cyclic voltammetry reveal the key role of ferrocene as a redox mediator in the reaction. [ABSTRACT FROM AUTHOR]

Herein, we disclose a straightforward, robust, and simple route to access β‐substituted desaturated cyclic amines via an electrochemically driven desaturative β‐functionalization of cyclic amines. This transformation is based on multiple single‐electron oxidation processes using catalytic amounts of ferrocene. The reaction proceeds in the absence of stoichiometric amounts of electrolyte under mild conditions, affording the desired products with high chemo‐ and regioselectivity. The reaction was tolerant of a broad range of substrates and also enables late‐stage β‐C(sp3)−H acylation of potentially valuable products. Preliminary mechanistic studies using cyclic voltammetry reveal the key role of ferrocene as a redox mediator in the reaction. [ABSTRACT FROM AUTHOR]

A variety of climatological indices have been established to illustrate the impact of climate change on air pollution in China, but major facts for causing variations of air pollution attributed to climate change are still unclear. Here, using in‐situ PM2.5 (particles with the aerodynamic diameter less than 2.5 μm) measurement, atmospheric reanalysis data and a chemical transport model, we show that meridional distribution of PM2.5 loadings is strongly modulated by the intensity of East Asian winter monsoon (EAWM). The EAWM drives the heavily polluted zone in eastern China to migrate southward, i.e., under stronger EAWM, more southward migration of air pollution occurs. We expect that the migration will likely re‐distribute carbon sources‐ and sinks‐related ecosystem, posing a new challenge for the Chinese government, who needs to implement region‐different emission reduction plans in the future, to mitigate air pollution and to go carbon neutral. Plain Language Summary: The relationship between the severe air pollution in China and climate has drawn much attention from scientific community, which still remains unclear. In this study, we present that air pollution with high PM2.5 loadings in winter, China is significantly modulated by East Asian winter monsoon (EAWM) based on ambient PM2.5 measurements, atmospheric reanalysis data and the GEOS‐Chem model. We find that the change in EAWM intensity dominates the location of heavily polluted zone and its meridional distribution. Stronger EAWM generally drives the zone to migrate more southward in eastern China, highlighting the predominant role of EAWM in redistributing air pollution of China during wintertime. Under climate change, the inter‐annual variability and decadal oscillation of EAWM projected by CMIP5 and CMIP6 models indicate a southward migration of the heavily polluted zone in next decades, probably approaching the Yangtze River Delta. This result may pose new challenges in air pollution control for local governments in different regions regarding climatic influence. Key Points: East Asian winter monsoon strongly modulates PM2.5 levels meridionally in eastern ChinaUnder climate change, the heavily polluted zone will likely move southward to Yangtze River Delta in the next decadesChina needs to implement regional‐different emission reduction measures regarding to the influence of climate change [ABSTRACT FROM AUTHOR]

A series of new alkali-metal-based coordination polymers, [Li(H2IMDC)(H2O)]n (1), [Na2(H2IMDC)2(H3IMDC)2(H2O)4]n (2), and [K(H2IMDC)(H2O)]n (3), have been constructed under solvothermal conditions by using imidazole-4,5-dicarboxylic acid (H3IMDC) as ligand. The structure of the complexes has been determined by single-crystal X-ray diffraction and further characterized by elemental analyses, IR spectra, powder X-ray diffraction and thermogravimetric analyses. The single crystal Xray structural studies showed that their structural dimensionalities varying from 1-D zigzag chain, 2-D 44-sql network to 3-D 4,6-connected coordination framework are strongly governed by the ionic radii and coordination geometries of the metal cations. For the first time, the alkali-metal-based coordination polymers were demonstrated to be effective catalysts for the solvent-free ring-opening polymerization (ROP) of ɛ-caprolactone. The catalytic activity of complexes 1–3 depends on the metal cations, increasing in the order Li+ < Na+ < K+. [ABSTRACT FROM AUTHOR]

Boar sperm are susceptible to oxidative damage caused by reactive oxygen species (ROS) during storage. Adenosine monophosphate (AMP)‐activated protein kinase (AMPK) is an important therapeutic target, because it is a cellular metabolism energy sensor and key signalling kinase in spermatozoa. We evaluated the effects of rosmarinic acid (RA), an antioxidant, on boar sperm during liquid storage to determine whether it protects boar sperm via AMPK activation. Boar ejaculates were diluted with Modena extender with different concentrations of RA and stored at 17°C for 9 days. Sperm quality parameters, antioxidant capacity, energy metabolism, AMPK phosphorylation and fertility were analysed. Compared with the control, 40 μmol/L significantly improved sperm motility, plasma membrane integrity and acrosome integrity (p <.05). The effective storage time of boar sperm was up to 9 days. On the third and seventh days, the sperm with RA exhibited increased total antioxidant capacity (T‐AOC), superoxide dismutase (SOD) activity, adenosine triphosphate (ATP) content, mitochondrial membrane potential (ΔΨm) and glyceraldehyde‐3‐phosphate dehydrogenase (GAPDH) activity, whereas malondialdehyde (MDA) content was significantly decreased (p <.05). Western blot showed that RA, as well as AICAR (AMPK activator), promoted AMPK phosphorylation, whereas Compound C (AMPK inhibitor) inhibited this effect. The sperm–zona pellucida binding experiment showed that 40 μmol/L RA increased the number of sperm attached to the zona pellucida (p <.05). These findings suggest meaningful methods for improved preservation of boar sperm in vitro and provide new insights into the mechanism by which RA protects sperm cells from oxidative damage via AMPK activation. [ABSTRACT FROM AUTHOR]

An important manifestation of the background or coseismic deformation surrounding megathrust earthquakes is the offshore microseismicity, which are difficult to be directly detected by land‐based seismic instruments. Here, we improve the capability of detecting offshore events by combining two popular techniques: backprojection (BP) imaging and matched‐filter (MF) detection. The BP method is effective in retrieving offshore seismicity (Mw > 4.5) buried in the coda wave of large earthquakes. The capability of the MF method depends on the availability of the template pool; therefore, the BP‐inferred events can be used as additional templates to expand the MF detections (BP‐MF). We performed the BP‐MF approach in the period within 600 days after the 2011 Mw 9.0 Tohoku earthquake. We find overall 44.2% more offshore events than those listed in the Japan Meteorological Agency (JMA) catalog. In the near‐trench area, we detect 213% more events. Among the newly detected Mw > 4 events, the BP template contributions are twice more than those matched by the JMA templates. Based on the spatial consistency between aftershock‐depleted zones and large coseismic slip, we identify a possible large coseismic slip zone in the near‐trench region offshore Fukushima. Large b values (≥1.2) are found close to large aftershocks, possibly indicating localized pockets of small differential stresses. At several locations close to the trench, p values (0.93–1.11) are higher than those in the inland area (0.64–0.85). This may be due to the larger coseismic slip and hence larger stress drop of the outer‐rise normal‐faulting events compared to the deeper thrust‐faulting events. Key Points: We improve the capability of detecting offshore events by combining backprojection imaging and matched‐filter detection (BP‐MF)The BP‐MF approach detects twice more events in the near‐trench region than those of the JMA catalogWe identify a possible large‐slip zone in the near‐trench region offshore Fukushima based on aftershock‐depleted zones [ABSTRACT FROM AUTHOR]

As a high‐efficient photocatalyst, g‐C3N4/TiO2 (PCN) was successfully prepared by thermal polymerization. In addition, the structure and morphological characteristics of the as‐prepared samples were investigated by XRD, BET, XPS, SEM, TEM, and UV‐vis DRS. The results revealed that in the presence of g‐C3N4, the physicochemical properties of the catalyst and the band gap of PCN decreased from 3.09 eV to 2.98 eV, clearly indicative of the enhanced photocatalytic performance relative to pure P25 or g‐C3N4 under sunlight. Furthermore, the photocatalytic properties of PCN were examined by the degradation of pyridine and other nitrogen heterocyclic pollutants under sunlight irradiation. Next, the main factors affecting the photocatalytic activity were investigated in detail, including the initial concentration of the pollutant, the mass of the photocatalyst, the initial pH of the solution, and the doping amount of g‐C3N4, as well as different free‐radical scavengers. On the other hand, the reusability of PCN demonstrated that photocatalysts exhibit outstanding photocatalytic stability after 10 cycles. Hence, high efficiency photocatalysts demonstrate potential for industrial applications such as sewage treatment. [ABSTRACT FROM AUTHOR]

The aim of this study was to characterize the effects of upadacitinib, a Janus kinase 1 inhibitor, on in vivo activity of different cytochrome P450 (CYP) enzymes using a cocktail approach. Healthy subjects (n = 20) received single oral doses of the modified Cooperstown 5+1 cocktail drugs (midazolam [CYP3A], caffeine [CYP1A2], warfarin + vitamin K [CYP2C9], omeprazole [CYP2C19], and dextromethorphan [CYP2D6]) without upadacitinib and on day 11 (midazolam) or 12 (all other probes) of a 15‐day regimen of upadacitinib 30 mg once daily (extended‐release formulation). Serial blood samples and 12‐hour urine samples were collected for assays of the probe substrates and select metabolites. The ratio (90%CI) of area under the plasma concentration‐time curve from time 0 to infinity (AUCinf) central values when the cocktail drugs were administered with upadacitinib relative to when administered alone were 0.74 (0.68‐0.80) for midazolam, 1.22 (1.15‐1.29) for caffeine, 1.11 (1.07‐1.15) for S‐warfarin, 1.07 (0.95‐1.22) for dextromethorphan, and 0.82 (0.72‐0.94) for omeprazole. The ratio (90%CI) was 1.09 (1.00‐1.19) for 5‐hydroxy‐omeprazole to omeprazole AUCinf ratio and 1.17 (0.97‐1.41) for dextromethorphan to dextrorphan 12‐hour molar urinary ratio. Upadacitinib 30 mg once daily (a dose that is twice the optimal dose in rheumatoid arthritis based on phase 3 results) has a limited effect on CYP3A activity (26% decrease in exposure of midazolam, a sensitive CYP3A substrate) and no relevant effects on CYP1A2, CYP2C9, CYP2C19, or CYP2D6 activity in vivo. No clinically relevant changes in plasma exposures are expected for drugs that are substrates for the evaluated CYP enzymes when coadministered with upadacitinib. [ABSTRACT FROM AUTHOR]

Sulfanilamide (SA) is an effective broad‐spectrum antibacterial agent in human and veterinary medicine. The purpose of this study was to evaluate the effects of SA on boar sperm quality during liquid storage at 17°C and determine the optimal concentration of SA and its effects on bacterial growth, microbial composition, and maternal fertility. Boar ejaculates were diluted with a basic extender, containing different concentrations of SA, and stored in a 17°C incubator for 6 days. The sperm motility, plasma membrane integrity, and acrosome integrity were measured daily. The results showed that when the concentration of SA was 0.02 g/L, the sperm quality parameters were significantly higher than those of all other treatment groups (p < .05). We also monitored the bacterial growth and compared the differences in the microbial species between the 0.02 g/L SA group and the control by 16S rDNA sequencing. The results revealed that some bacteria, such as Staphylococcus and Pseudomonas, were considerably lower in the 0.02 g/L SA group than in the control group (p < .05). In addition, preserved semen was used for artificial insemination, and results showed that 0.02 g/L SA group had a higher litter size, and its pregnancy rate was 92.5%. [ABSTRACT FROM AUTHOR]

The asymmetrical growth of a single‐wall carbon nanotube (SWCNT) by introducing a change of a local atomic structure, is usually inevitable and supposed to have a profound effect on the chirality control and property tailor. However, the breaking of the symmetry during SWCNT growth remains unexplored and its origins at the atomic‐scale are elusive. Here, environmental transmission electron microscopy is used to capture the process of breaking the symmetry of a growing SWCNT from a sub‐2‐nm platinum catalyst nanoparticle in real‐time, demonstrating that topological defects formed on the side of a SWCNT can serve as a buffer for stress release and inherently break its axis‐symmetrical growth. Atomic‐level details reveal the importance of the tube‐catalyst interface and how the atom rearrangement of the solid‐state platinum catalyst around the interface influences the final tubular structure. The active sites responsible for trapping carbon dimers and providing enough driving force for carbon incorporation and asymmetric growth are shown to be low‐coordination step edges, as confirmed by theoretical simulations. [ABSTRACT FROM AUTHOR]

A novel synthesis of cyclobutanol‐fused 2‐nitronaphthalen‐1‐ols and nitrocyclobutane‐fused naphthalene‐1,2‐diones through cascade reactions of benzene‐linked allenynes with tert‐butyl nitrite is presented. The formation of the title compounds involves a tandem process including allenyne [2+2] cycloaddition, radical addition onto the in situ formed cyclobutenyl moiety followed by radical coupling/oxidation. Interestingly, different kinds of functionalized naphthalene derivatives could be obtained selectively from the same substrates, and the selectivity was easily controlled by finely tuning the reaction conditions. [ABSTRACT FROM AUTHOR]

Herein, an electrochemically driven NiH‐catalyzed reductive coupling of alkyl halides and alkyl alkenes for the construction of Csp3−Csp3 bonds is firstly reported. Notably, alkyl halides serve dual function as coupling substrates and as hydrogen sources to generate NiH species under electrochemical conditions. The tunable nature of this reaction is realized by introducing an intramolecular coordinating group to the substrate, where the product can be easily adjusted to give the desired branched products. The method proceeds under mild conditions, exhibits a broad substrate scope, and affords moderate to excellent yields with over 70 examples, including late‐stage modification of natural products and drug derivatives. Mechanistic insights offer evidence for an electrochemically driven coupling process. The sp3‐carbon‐halogen bonds can be activated through single electron transfer (SET) by the nickel catalyst in its low valence state, generated by cathodic reduction, and the generation of NiH species from alkyl halides is pivotal to this transformation. [ABSTRACT FROM AUTHOR]

Herein, an electrochemically driven NiH‐catalyzed reductive coupling of alkyl halides and alkyl alkenes for the construction of Csp3−Csp3 bonds is firstly reported. Notably, alkyl halides serve dual function as coupling substrates and as hydrogen sources to generate NiH species under electrochemical conditions. The tunable nature of this reaction is realized by introducing an intramolecular coordinating group to the substrate, where the product can be easily adjusted to give the desired branched products. The method proceeds under mild conditions, exhibits a broad substrate scope, and affords moderate to excellent yields with over 70 examples, including late‐stage modification of natural products and drug derivatives. Mechanistic insights offer evidence for an electrochemically driven coupling process. The sp3‐carbon‐halogen bonds can be activated through single electron transfer (SET) by the nickel catalyst in its low valence state, generated by cathodic reduction, and the generation of NiH species from alkyl halides is pivotal to this transformation. [ABSTRACT FROM AUTHOR]

Electrochemistry. An electrochemical desaturative α‐acylation of cyclic N‐aryl amines to access α‐substituted enamines is reported in the Communication by Youai Qiu et al. (e202115178). [ABSTRACT FROM AUTHOR]

Frontispiece: Electrochemical Desaturative -Acylation of Cyclic N-Aryl Amines Keywords: -Acylation; Desaturation; Electrochemistry; Ferrocene mediator; Selectivity EN -Acylation Desaturation Electrochemistry Ferrocene mediator Selectivity 1 1 1 01/28/22 20220201 NES 220201 B Electrochemistry b . An electrochemical desaturative -acylation of cyclic N-aryl amines to access -substituted enamines is reported in the Communication by Youai Qiu et al. (e202115178). [Extracted from the article]

Elektrochemie. Die elektrochemische desaturierende α‐Acylierung von cyclischen N‐Arylaminen zu α‐substituierten Enaminen wird in der Zuschrift von Youai Qiu et al. vorgestellt (e202115178). [ABSTRACT FROM AUTHOR]

-Acylation, Desaturation, Electrochemistry, Ferrocene mediator, Selectivity Keywords: -Acylation; Desaturation; Electrochemistry; Ferrocene mediator; Selectivity EN -Acylation Desaturation Electrochemistry Ferrocene mediator Selectivity 1 1 1 01/28/22 20220201 NES 220201 B Elektrochemie b . Frontispiz: Electrochemical Desaturative -Acylation of Cyclic N-Aryl Amines. [Extracted from the article]

To determine the epigenetic events associated with NMDA receptor-mediated activation of brain-derived neurotrophic factor gene ( Bdnf) promoter 1 by hippocampal neurons in culture, we screened 12 loci across 4.5 kb of genomic DNA 5′ of the transcription start site (TSS) of rat Bdnf for specific changes in histone modification and transcription factor binding following NMDA receptor stimulation. Chromatin immunoprecipitation (ChIP) assays showed that NMDA receptor stimulation produced a durable, time-dependent decrease in histone H3 at lysine 9 dimethylation (H3K9me2), within 3 h after NMDA treatment across multiple loci. Concomitant increases in H3K4me2 and H3K9/14 acetylation (H3AcK9/14) were associated with transcriptional activation, but occurred at fewer sites within the promoter. The decrease in H3K9me2 was associated with release of HDAC1, MBD1, MeCP2, and REST from specific locations within promoter 1, although with different kinetics. In addition, occupancy of sites proximal to and distal to the TSS by the transcription factors NF-κB, CREB-binding protein (CBP), and cAMP-response element-binding protein were correlated with increased occupancy of RNA polymerase II at two loci proximal to the TSS following NMDA receptor stimulation. These temporal changes in promoter occupancy could occur thousands of base pairs 5′ of the TSS, suggesting a mechanism that produces waves of Bdnf transcription. [ABSTRACT FROM AUTHOR]

The neuroprotective effect and molecular mechanisms underlying preconditioning with N-methyl-D-aspartate (NMDA) in cultured hippocampal neurons have not been described. Pre-incubation with subtoxic concentrations of the endogenous neurotransmitter glutamate protects vulnerable neurons against NMDA receptor-mediated excitotoxicity. As a result of physiological preconditioning, NMDA significantly antagonizes the neurotoxicity resulting from subsequent exposure to an excitotoxic concentration of glutamate. The protective effect of glutamate or NMDA is time- and concentration-dependent, suggesting that sufficient agonist and time are required to establish an intracellular neuroprotective state. In these cells, the TrkB ligand, brain-derived neurotrophic factor (BDNF) attenuates glutamate toxicity. Therefore, we tested the hypothesis that NMDA protects neurons via a BDNF-dependent mechanism. Exposure of hippocampal cultures to a neuroprotective concentration of NMDA (50 μ m) evoked the release of BDNF within 2 min without attendant changes in BDNF protein or gene expression. The accumulated increase of BDNF in the medium is followed by an increase in the phosphorylation (activation) of TrkB receptors and a later increase in exon 4-specific BDNF mRNA. The neuroprotective effect of NMDA was attenuated by pre-incubation with a BDNF-blocking antibody and TrkB-IgG, a fusion protein known to inhibit the activity of extracellular BDNF, suggesting that BDNF plays a major role in NMDA-mediated survival. These results demonstrate that low level stimulation of NMDA receptors protect neurons against glutamate excitotoxicity via a BDNF autocrine loop in hippocampal neurons and suggest that activation of neurotrophin signaling pathways plays a key role in the neuroprotection of NMDA. [ABSTRACT FROM AUTHOR]

This phase 1, 2‐part, 2‐period, open‐label, drug‐drug interaction study evaluated the potential for pharmacokinetic interactions between upadacitinib and rosuvastatin, an organic anion transporting polypeptide (OATP) 1B1 and breast cancer resistance protein substrate, or atorvastatin, a cytochrome P450 3A, OATP1B1, and OATP1B3 substrate, in 36 healthy volunteers. During period 1, a single dose of rosuvastatin (5 mg; part 1) or atorvastatin (10 mg; part 2) was administered on day 1, followed by a washout period of 5 days. During period 2, once‐daily doses of upadacitinib extended‐release (30 mg) were administered on days 1 to 10, and a single dose of rosuvastatin (5 mg; part 1) or atorvastatin (10 mg; part 2) was administered 1 hour after the upadacitinib dose on day 7. Serial blood samples were collected for assays of drug concentrations. In Part 1, rosuvastatin maximum observed plasma concentration (Cmax) and area under the plasma concentration–time curve from time 0 to infinity (AUCinf) were 23% and 33% lower, respectively, when administered with upadacitinib relative to when administered alone. In part 2, atorvastatin Cmax and AUCinf was 11% and 23% lower, respectively, when administered with upadacitinib relative to when administered alone. The Cmax and AUCinf of the active metabolite ortho‐hydroxyatorvastatin remained unchanged. Administration of a single 5‐mg dose of rosuvastatin or a single 10‐mg dose of atorvastatin had no relevant effect on upadacitinib Cmax or area under the plasma concentration–time curve. These results demonstrated that upadacitinib has no clinically relevant effect on the pharmacokinetics of rosuvastatin and atorvastatin or on substrates transported by OATP1B or breast cancer resistance protein. [ABSTRACT FROM AUTHOR]

Typical ground‐motion prediction equations (GMPEs) measure source‐to‐site distances relative to the closest point on the rupture plane (Rrup). However, for megathrust earthquakes (Mw > 8), the oversimplification of the earthquake source characteristics in distance metrics results in significant bias. Recent studies suggest that the high‐frequency (HF) and low‐frequency (LF) energy tend to emanate from different portions of the megathrusts. This phenomenon motivates an alternative distance metric based on the array backprojection imaging technique that effectively captures regions releasing HF energy. Herein, we define an HF distance metric (Rhf) as the distance from the site to the high‐frequency radiation zone. We study five Mw > 7.2 megathrust earthquakes in Japan and Chile and find that Rhf outperforms Rrup in predicting the ground shaking intensity between 0.5 and 4 Hz. We consider Rhf as a complementary measure to conventional GMPE distance metrics and a more accurate ground‐motion predictor in many cases. Plain Language Summary: Traditional distance metrics for GMPEs are frequency‐independent, which perform reasonably well in predicting the shaking intensity of small earthquakes. However, the frequency dependence of source distances becomes more significant for large subduction‐zone earthquakes. Our paper proposes a new frequency‐dependent distance metric based on backprojection imaging technique. It improves the accuracy of GMPE prediction for the large megathrust earthquakes, especially for the high‐frequency ground motion. We study five large subduction zone earthquakes in Japan and Chile: 2011 Mw 9.0 Tohoku, 2003 Mw 8.0 Tokachi, 2005 Mw 7.2 off‐Miyagi earthquakes, 2014 Mw 8.1 Iquique earthquake, and 2015 Mw 8.3 Illapel earthquake. In these five earthquakes, our frequency‐dependent distance metric outperforms traditional distance metrics. Key Points: We propose a new frequency‐dependent distance metric Rhf for use in ground‐motion prediction equations (GMPEs)Rhf improves the accuracy of high‐frequency (0.5–4 Hz) ground‐motion prediction for the megathrust earthquakesGMPEs utilizing Rhf can potentially provide rapid ground‐motion intensity estimation for megathrust earthquakes [ABSTRACT FROM AUTHOR]

GSTP1 has been considered to be a marker for malignancy in many tissues. However, the existing GST fluorescent probes are unfavorable for in vivo imaging because of the limited emission wavelength or insufficient fluorescence enhancement (six‐fold). The limited fluorescence enhancement of GST fluorescent probes is mainly ascribed to the high background signals resulting from the spontaneous reaction between GSH and the probes. In this work, a highly specific GST probe with NIR emission has been successfully developed through optimization of the essential unit of the probe to repress the spontaneous reaction. The novel GST probe exhibits over 100‐fold fluorescence enhancement upon incubation with GSTP1/GSH and high selectivity over other potential interference. In addition, the probe has been proved to be capable of tracking endogenous GST in A549 cells. Finally, the in vivo imaging results demonstrate that the probe can be used for effective imaging of endogenous GST activity in subcutaneous tumor mouse with high contrast. [ABSTRACT FROM AUTHOR]

Upadacitinib is a selective Janus kinase 1 inhibitor being developed for the treatment of several inflammatory autoimmune diseases, including rheumatoid arthritis. Upadacitinib is a nonsensitive substrate for metabolism by cytochrome P450 3A enzymes. This open‐label, single‐dose, multicenter study assessed the pharmacokinetics of upadacitinib following oral administration of a single 15‐mg dose of the upadacitinib extended‐release formulation in subjects with mild (n = 6) and moderate (n = 6) hepatic impairment relative to demographically matched healthy subjects (n = 6). Subjects were assigned to 1 of the 3 groups according to the Child‐Pugh classification. Relative to subjects with normal hepatic function, the ratios (90% confidence intervals) of upadacitinib area under the plasma concentration‐versus‐time profile from time 0 to infinity (AUCinf) for subjects with mild and moderate hepatic impairment were 1.28 (0.91‐1.79) and 1.24 (0.87‐1.76), respectively. The central ratios of upadacitinib maximum observed concentration (Cmax) were 1.04 (0.77‐1.39) and 1.43 (1.05‐1.95) in subjects with mild and moderate hepatic impairment, respectively, compared with subjects with normal hepatic function. No clinically significant changes in vital signs or hematology measurements were observed, and no new safety events were identified in this study. These results indicate that mild and moderate hepatic impairment has no clinically relevant effect on upadacitinib pharmacokinetics. [ABSTRACT FROM AUTHOR]

Upadacitinib is a novel selective Janus kinase 1 inhibitor developed for treatment of rheumatoid arthritis and other autoimmune diseases. The objective of this study was to assess the pharmacokinetics and safety of a single upadacitinib dose in subjects with normal renal function and in subjects with renal impairment. A total of 24 subjects between the ages of 18 and 75 years were assigned to 1 of 4 renal function groups based on estimated glomerular filtration rate (normal, mild, moderate, severe; N = 6/group). A single 15‐mg dose of upadacitinib extended‐release formulation was administered under fasting conditions. Serial plasma and urine samples were assayed to evaluate the effect of renal impairment on upadacitinib exposure through regression analysis and analysis of covariance. The primary analysis was the regression analysis of upadacitinib exposures versus estimated glomerular filtration rate. The point estimates for upadacitinib plasma exposure ratios (90% confidence interval [CI]) in subjects with mild, moderate, and severe renal impairment were 1.18 (90%CI, 1.06–1.32), 1.33 (90%CI, 1.11–1.59), and 1.44 (90%CI, 1.14–1.82) for area under the plasma concentration–time curve and 1.06 (90%CI, 0.92–1.23), 1.11 (90%CI, 0.88–1.40), and 1.14 (90%CI, 0.84–1.56) for maximum observed plasma concentration, respectively, relative to subjects with normal renal function based on the regression analysis. The analysis of covariance categorical analysis provided consistent results. Upadacitinib was well tolerated by all subjects, and no safety issues were identified in subjects with renal impairment. Renal impairment has a limited effect on upadacitinib pharmacokinetics. This is in agreement with the known limited role of urinary excretion in upadacitinib elimination. Based on the limited impact on exposure, no dose adjustment is necessary for upadacitinib in subjects with impaired renal function. [ABSTRACT FROM AUTHOR]

Upadacitinib is a novel selective oral Janus kinase 1 (JAK) inhibitor being developed for treatment of several inflammatory diseases. Oral contraceptives are anticipated to be a common concomitant medication in the target patient populations. This study was designed to evaluate the effect of multiple doses of upadacitinib on the pharmacokinetics of ethinylestradiol and levonorgestrel in healthy female subjects. This phase I, single‐center, open‐label, 2‐period crossover study evaluated the effect of multiple doses of 30 mg once daily extended‐release upadacitinib on the pharmacokinetics of a single oral dose of ethinylestradiol/levonorgestrel (0.03/0.15 mg; administered alone in period 1 and on day 12 of a 14‐day regimen of upadacitinib in period 2) in 22 healthy female subjects. The ratios (90% confidence intervals) for maximum plasma concentration and area under the plasma drug concentration–time curve from time zero to infinity following administration of ethinylestradiol/levonorgestrel with upadacitinib compared with administration of ethinylestradiol/ levonorgestrel alone were 0.96 (0.89–1.02) and 1.1 (1.04–1.19), respectively, for ethinylestradiol, and 0.96 (0.87–1.06) and 0.96 (0.85–1.07), respectively, for levonorgestrel. The harmonic mean terminal half‐life for ethinylestradiol (7.7 vs 7.0 hours) and levonorgestrel (37.1 vs 33.1 hours) was similar in the presence and absence of upadacitinib. Ethinylestradiol and levonorgestrel were bioequivalent in the presence and absence of upadacitinib. Therefore, upadacitinib can be administered concomitantly with oral contraceptives containing ethinylestradiol or levonorgestrel. [ABSTRACT FROM AUTHOR]

2-Hydroxybenzohydrazides are efficiently applied as ligands in the copper-catalyzed coupling of aryl iodides and bromides with a variety of N-heterocycles as well as aniline and benzylamine (X). [ABSTRACT FROM AUTHOR]

The novel catalytic system allows the N-arylation of imidazole and pyrrole with aryl iodides and bromides in water as the solvent without the need for an inert atmosphere. [ABSTRACT FROM AUTHOR]

The article presents chemical equations related to the article "Tetrazole-1-acetic Acid as a Ligand for Copper-Catalyzed N-Arylation of Imidazoles with Aryl Iodides under Mild Conditions" by Feng-Tian Wu, B. Dai and others, published in the journal "Chinese Chemical Letters" in 2013.

Determination of the orientation of microfibrils within ultra-high molecular weight polyethylene (UHMWPE) fibers is considered to be an important method in evaluating the mechanical properties of the fibers. Four commonly used orientation evaluation methods are summarized and used to evaluate UHMWPE fibers at different drawing stages in the industrial line, and the results exhibit certain limitations. To overcome these limitations, a new evaluation method for quantitive characterization of UHMWPE fiber properties is proposed. Meanwhile, in situ small-angle X-ray scattering data of an UHMWPE fiber drawn at 100 °C were used to perform a Pearson correlation coefficient test, and the results show a very strong correlation between the strain ratio and the evaluated coefficient. [ABSTRACT FROM AUTHOR]

The method is limited to aryl/heteroaryl methyl ketones, and cyclic or acyclic amines. [ABSTRACT FROM AUTHOR]

This phase 1 study characterized the effect of multiple doses of upadacitinib, an oral Janus kinase 1 selective inhibitor, on the pharmacokinetics of the cytochrome P450 (CYP) 2B6 substrate bupropion. Healthy subjects (n = 22) received a single oral dose of bupropion 150 mg alone (study period 1) and on day 12 of a 16‐day regimen of upadacitinib 30 mg once daily (study period 2). Serial blood samples for measurement of bupropion and hydroxybupropion plasma concentrations were collected in each study period. The central values (90% confidence intervals) for the ratios of change were 0.87 (0.79‐0.96) for bupropion maximum plasma concentration (Cmax), 0.92 (0.87‐0.98) for bupropion area under the plasma‐concentration time curve from time 0 to infinity (AUCinf), 0.78 (0.72‐0.85) for hydroxybupropion Cmax, and 0.72 (0.67‐0.78) for hydroxybupropion AUCinf when administered with, relative to when administered without, upadacitinib. After multiple‐dose administration of upadacitinib 30 mg once daily, upadacitinib mean ± SD AUC0‐24 was 641 ± 177 ng·h/mL, and Cmax was 83.3 ± 30.7 ng/mL. These results confirm that upadacitinib has no relevant effect on pharmacokinetics of substrates metabolized by CYP2B6. [ABSTRACT FROM AUTHOR]

In this study, the Dynamical‐Statistical‐Analog Ensemble Forecast model for landfall typhoon precipitation (the DSAEF_LTP model), which has been developed by Ren et al., in 2020, is applied to precipitation simulations for super‐typhoon Lekima (2019), a tropical cyclone (TC) that produced heavy rainfall over eastern China. A new variable, TC intensity, is introduced into the generalized initial value (GIV) of the DSAEF_LTP model. Two different groups of simulation experiments, one group including the new TC intensity variable in the GIV and the other group excluding it, have been conducted. Results show that, with TC intensity, the ability of the DSAEF_LTP model to forecast heavy rainfall (i.e. accumulated precipitation exceeding thresholds of 250 and 100 mm) for Lekima is improved. Its threat score (TS) ranks the second compared with that of three numerical weather prediction models (i.e. ECMWF, GRAPES and GFS). Further study shows that three factors prevent the DSAEF_LTP model from achieving more satisfactory results for Lekima: the historically rare occurrence of extreme precipitation in northern China during Lekima, the increase of forecast track error when Lekima moved northwards, and the calculation of similarity between tracks of Lekima and historical TCs within an improper region (i.e. similarity region). To solve the third problem, new similarity region schemes are adopted that produce higher TS, in which case TS of precipitation greater than 100 mm (TS100) ranks first and TS of precipitation greater than 250 mm (TS250) gets closer to the first place. [ABSTRACT FROM AUTHOR]

Adding a certain amount of antioxidants to semen extender has been shown to improve semen quality. The aim of present study was to elucidate whether the supplementation of melatonin to the Tris‐based extender (CTR) could enhance the quality of ram spermatozoa during storage at 4°C. Ram semen samples were collected and diluted with CTR extender containing different concentrations (0, 0.05 (M 0.05), 0.1 (M 0.1), 0.2 (M 0.2) or 0.4 (M 0.4) mM) of melatonin. Sperm routine indicators, mitochondrial activity, total antioxidant capacity (T‐AOC) and malondialdehyde (MDA) content were analysed in control and melatonin treatment groups. The higher per cent of motility, plasma membrane integrity, mitochondrial activity and T‐AOC activity was observed in M 0.05, M 0.1 and M 0.2 groups compared to control group at 5 days of storage (p < 0.05), while lower percentage of MDA content was observed among these groups (p < 0.05). In addition, there were no significant differences in acrosome integrity among the control and M 0.05, M 0.1 and M 0.2 groups during the experiment. The above results show that the addition of 0.05, 0.1, 0.2 mM of melatonin is beneficial to the preservation of ram semen during liquid storage at 4°C mainly through antioxidative stress. [ABSTRACT FROM AUTHOR]

Background and Aims Recent genome-wide association studies have shown associations between variants in loci (4q28.1, 6p21.32, 6p21.1, 6q16.1, 10q22.1 and 10q22.3) and chronic obstructive pulmonary disease (COPD) or smoking behaviors. The objective of this study was to look for associations between 16 single nucleotide polymorphisms (SNP) at these six loci and COPD susceptibility in Hainan region. Methods A case-control cohort was composed of 200 COPD cases and 401 controls that were genotyped and analyzed statistically. Odds ratios (OR) and 95% confidence intervals (CIs) were computed by chi-square (χ2) test and genetic models by unconditional logistic regression. Results After Hardy-Weinberg equilibrium (HWE) P value screening, we excluded the SNP rs12220777 with P < 0.001. By χ2 test only rs9296092 which located on 6p21.32 was provided the strongest evidence of an increasing risk of COPD with an OR of 3.28 (95% CI = 1.03 - 2.32; P = 0.003) between cases and controls. By genetic models analysis, we not only found rs9296092 increased COPD risk, but also found in the over-dominant model the genotype 'C/T' (OR = 0.55; 95% CI = 0.33 - 0.93; P = 0.023) of rs950063 was proved to be associated with decreased COPD risk. Conclusions This study is the first to provide evidence of importance of rs9296092 and rs950063 for risk of COPD in Hainan Province. Further studies are needed to characterize the functional sequences that cause COPD. [ABSTRACT FROM AUTHOR]

CRM197 is a naturally nontoxic diphtheria toxin mutant that binds and inhibits heparin-binding epidermal growth factor-like growth factor. CRM197 serves as carrier protein for vaccine and other therapeutic agents. CRM197 also inhibits the growth, migration, invasion, and induces apoptosis in various tumors. Vascular cell adhesion molecule-1 (VCAM-1) is an important cell surface adhesion molecule associated with malignancy of gliomas. In this work, we aimed to investigate the role and mechanism of CRM197 combined with shRNA interference of VCAM-1 (shRNA-VCAM-1) on the migration, invasion, and apoptosis of glioblastoma cells. U87 and U251 human glioblastoma cells were treated with CRM197 (10 µg/ml) and shRNA interfering technology was employed to silence VCAM-1 expression. Cell viability, migration, invasiveness, and apoptosis were assessed with CCK8, Transwell and Annexin V-PE/7-AAD staining. Activation of cleaved caspase-3, 8, and 9, activity of matrix metalloproteinase-2/9 (MMP-2/9), and expression of phosphorylated Akt (p-Akt) were also checked. Results showed that CRM197 and shRNA-VCAM-1 not only significantly inhibited the cell proliferation, migration, invasion, but also promoted the apoptosis of U87 and U251 cells. Combined treatment of both displayed enhanced inhibitory effects on the malignant biological behavior of glioma cells. The activation of cleaved caspase-3, 8, 9 was promoted, activity of MMP-2 and MMP-9 and expression of p-Akt were inhibited significantly by the treatment of CRM197 and shRNA-VCAM-1 alone or in combination, indicating that the combination of CRM197 with shRNA-VCAM-1 additively inhibited the malignant behavior of human glioblastoma cells via activating caspase-3, 8, 9 as well as inhibiting MMP-2, MMP-9, and Akt pathway. J. Cell. Physiol. 230: 1713-1728, 2015. © 2014 Wiley Periodicals, Inc. [ABSTRACT FROM AUTHOR]

The article presents chemical equations for an article related to iron-catalyzed synthesis of alkenyl halides via coupling reactions of alcohols and alkynes with aqueous HX as exogenous halide sources by Y.-R. Yang and others, published in the periodical "Tetrahedron" in 2015.

Background and aims: Great interest persists in useful therapeutic targets in glioblastoma (GBM). Deregulation of microRNAs (miRNAs) expression has been associated with cancer formation through alterations in gene targets. In this study, we reported the role of miR-101 in human glioblastoma stem cells (GSCs) and the potential mechanisms. Methods and results: Quantitative real-time PCR showed that miR-101 expression was decreased in GSCs. Overexpression of miR-101 reduced the proliferation, migration, invasion, and promoted apoptosis of GSCs. One direct target of miR-101, the transcription factor Kruppel-like factor 6 (KLF6), was identified using the Dual-Luciferase Reporter Assay System, which mediated the tumor suppressor activity of miR-101. This process was coincided with the reduced expression of Chitinase-3-like protein 1 (CHI3L1) whose promoter could be bound with and be promoted by KLF6 demonstrated by luciferase assays and chromatin immunoprecipitation assays. The downregulation of CHI3L1 led to the inactivation of MEK1/2 and PI3K signal pathways. Furthermore, nude mice carrying the tumors of overexpressed miR- 101 combined with knockdown of KLF6 produced the smallest tumors and showed the highest survival rate. Conclusions: Our findings provided a comprehensive analysis of miR-101 and further defining it as a potential therapeutic candidate for GBM. [ABSTRACT FROM AUTHOR]

Aim The aim of this study was to determine the psychometric properties, content range, and measurement precision of a lower extremity physical functioning and mobility skills item bank (LE85) in children with cerebral palsy (CP). Method Lower extremity functioning and mobility skill items were administered to 308 parents of children (169 males, 139 females; mean age 10y 8mo, SD 4y) with spastic CP (145 diplegia, 73 hemiplegia, 89 quadriplegia; [for one person type of CP was unknown]) classified using the Gross Motor Function Classification System (75 level I, 91 level II, 79 level III, 37 level IV, 26 level V). Additional legacy measures were administered to assess concurrent validity. Psychometric characteristics, differential item functioning, content range, and score precision were examined. Results The LE85 had acceptable psychometric properties. Content range matched the ability range of the sample population and exceeded legacy measures with minimal differential item functioning. The LE85 had good correlation with the Paediatric Outcomes Data Collection Instrument, Functional Independence Measure for Children, Gillette Functional Assessment Questionnaire, and Paediatric Quality of Life Inventory – CP module (range r=0.63–0.86). Precision of the LE85 and 10-item simulated computer adaptive test scores outperformed legacy measures. Interpretation The LE85 appears to be suitable to administer as a computer adaptive test to measure lower extremity physical functioning and mobility in children with CP. [ABSTRACT FROM AUTHOR]

The aims of the study were to compare (i) the effects of transcatheter arterial embolization on initial hemostasis and the control of rebleeding in the treatment of hemorrhage due to hepatic artery injury; and (ii) the outcomes of embolization by different locations.Subjects were 32 patients with suspected hepatic artery injury who were transferred to Chi-Mei Foundation Medical Center for hepatic angiography and embolization. The causes of arterial injury included liver trauma (n = 15) and iatrogenic injury (n = 17). The sites of embolization were classified into four groups: group 1 (n = 8) was classified as‘combined outlet, target and inlet control’ with embolization of the vascular lesion (target) and hepatic artery distal (outlet) and proximal (inlet) to the vascular lesion simultaneously; group 2 (n = 11) as‘combined target and inlet control’; group 3 (n = 8) as‘combined outlet and inlet control’; group 4 (n = 5) as‘inlet control’ only.Successful initial hemostasis was achieved in 30 of the 32 patients (93.8%), with two failures, both of which were caused by liver injury and occurred in subjects in group 4. Rebleeding was seen in three patients who had successful initial hemostasis: two of them in group 4 (66.7%) and one in group 1 (12.5%). All rebleedings were successfully managed by repeat embolization. Abscess formation was found in two group 1 patients, and both were successfully managed by percutaneous drainage.Transcatheter arterial embolization is an effective method for hemostasis in hepatic artery hemorrhage for both patients with liver trauma and patients with iatrogenic injuries to the hepatic artery. Based on this experience, embolization of the vascular lesion and/or the arterial lumen distal to the vascular lesion combined with inlet control is recommended for preventing recurrent hemorrhage, but studies with larger sample sizes will be required to validate this conclusion. [ABSTRACT FROM AUTHOR]

The article presents a study of using airborne hyperspectral remote sensing data in mineral resource prospecting in China's Gansu and Qinghai Regions. Alteration minerals and surface mineralization are checked through field verification which is noted to confirm prospecting indicators. Airborne hyperspectral data is found to have an accurate and fast identification of mineralized alteration zones in the regions.

An abstract of the article "Copper-Catalyzed Direct Oxyphosphorylation of Alkynes with H-Phosphine Oxides and Dioxygen: A Convenient Approach to ß-Ketophosphine Oxides" by authors including W.-W. Zhong, Hideaki Yazawa, and Shigeru Shimada.

An abstract of the article "Copper-Catalyzed Direct Oxyphosphorylation of Alkynes with H-Phosphine Oxides and Dioxygen: A Convenient Approach to β-Ketophosphine Oxides" by W. W. Zhong and colleagues is presented.