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This study aimed to evaluate the bioequivalence between test tablet dacomitinib and reference product Vizimpro® under fasting and fed conditions and assess their pharmacokinetic (PK) and safety profiles for gaining marketing approval of the new generic drug. A single‐center, randomized, open‐label, single‐dose, two‐treatment, two‐period, crossover bioequivalence study was conducted in healthy Chinese subjects. Eligible healthy subjects randomly received a single 45 mg dose of test or reference formulations with an administration sequence of test tablet (T), reference tablet (R), or (RT), under both fasting and fed conditions, and each single administration was followed by a 21‐day washout period. Plasma concentrations and corresponding non‐compartmental PK parameters of dacomitinib were determined. The 90% confidence intervals of the geometric mean ratio (GMR) (test/reference) for Cmax, AUC0–t, and AUC0–∞, respectively, were 97.75%–119.99%, 101.00%–115.09%, and 100.27%–113.90% under fasting conditions and 95.20%–104.94%, 97.24%–102.23%, and 97.27%–101.88% under fed conditions, which were within the limits of 80%–125%. Under fasting and fed conditions, the PK characteristics of the test dacomitinib tablet and reference Vizimpro® were comparable; the two formulations of dacomitinib were demonstrated to be bioequivalent and well‐tolerated in healthy Chinese volunteers. [ABSTRACT FROM AUTHOR]

Herein, nitrogen‐ and phosphorus‐doped carbon quantum dots (CQDs) are synthesized using a one‐step hydrothermal method that uses glucose and diammonium phosphate as the main raw material to improve bottleneck problems, such as low yield of fluorescent quantum, short‐emission wavelength, and the poor photoelectrical performance of CQDs. The optimal synthesis conditions are found to be a duration of 10 h, optimal synthesis temperature of 240 °C, and optimal raw material ratio of glucose: diammonium phosphate as 3:0.5. The shape, composition, optical properties, and electrochemical properties of the nitrogen‐ and phosphorus‐doped CQDs (N,P‐CQDs) are characterized and studied by means of instruments. The experimental results show that the N,P‐CQDs prepared following the hydrothermal method using glucose and diammonium phosphate as the main raw material produce a higher fluorescence quantum yield (41.7%), longer‐emission wavelength (470 nm), and better photoelectric properties, expanding the applicability of N,P‐CQDs in the field of life science. [ABSTRACT FROM AUTHOR]

Oomycetes represent a unique group of plant pathogens that are phylogenetically distant from true fungi and cause significant crop losses and environmental damage. Understanding of the genetic basis of host plant susceptibility facilitates the development of novel disease resistance strategies. In this study, we report the identification of an Arabidopsis thaliana T‐DNA mutant with enhanced resistance to Phytophthora parasitica with an insertion in the Raf‐like mitogen‐activated protein kinase kinase kinase gene Raf36. We generated additional raf36 mutants by CRISPR/Cas9 technology as well as Raf36 complementation and overexpression transformants, with consistent results of infection assays showing that Raf36 mediates Arabidopsis susceptibility to P. parasitica. Using a virus‐induced gene silencing assay, we silenced Raf36 homologous genes in Nicotiana benthamiana and demonstrated by infection assays the conserved immune function of Raf36. Mutagenesis analyses indicated that the kinase activity of Raf36 is important for its immune function and interaction with MKK2, a MAPK kinase. By generating and analysing mkk2 mutants and MKK2 complementation and overexpression transformants, we found that MKK2 is a positive immune regulator in the response to P. parasitica infection. Furthermore, infection assay on mkk2 raf36 double mutant plants indicated that MKK2 is required for the raf36‐conferred resistance to P. parasitica. Taken together, we identified a Raf‐like kinase Raf36 as a novel plant susceptibility factor that functions upstream of MKK2 and directly targets it to negatively regulate plant resistance to P. parasitica. [ABSTRACT FROM AUTHOR]

In this paper, we construct the individual stock sentiment indexes at daily, weekly and monthly frequencies. We empirically demonstrate the different effects of individual stock sentiment of three frequencies on the excess returns. The results show that the effect of individual stock sentiment on excess returns is a monotonous decreasing function of time term in China's stock market, which presents obvious term structure effect. Moreover, we find that sentiment factor can better explain the variation of excess returns than size factor and book‐to‐market factor do at the same frequency, and thus we should pay more attention to the individual effect of investor sentiment in the short‐term decision‐making. Our results shed new light on the short‐sighted behaviour of irrational investors and the micro‐mechanism of sentiment effect. [ABSTRACT FROM AUTHOR]

Growth differentiation factor 15 (GDF15), a member of the transforming growth factor β (TGF‐β) superfamily, is a prognostic biomarker of cervical cancer. In addition, GDF15 has been reported to enhance the migration of colorectal cancer cells and liver cancer stem‐like cells. However, the mechanism by which GDF15 promotes cervical cancer cell migration is not completely understood. Here, we report that GDF15 expression is enhanced in cervical cancer tissues, as well as in cultured cervical cancer cells. ShGDF15 transfection markedly inhibited expression of Vimentin, N‐cadherin and Snail1, and resulted in up‐regulation of E‐cadherin expression in HT‐3 and HeLa cells. Moreover, knockdown of GDF15 suppressed wound healing rate and reduced the number of invasive cells. Furthermore, knockdown of GDF15 significantly suppressed the expression of phosphorylated Smad2 and Smad3. The addition of TGF‐β1 partially abolished the inhibitory effects of GDF15 knockdown on the migration and invasion of cervical cancer cells. In summary, we report here that GDF15 knockdown inhibits migration and invasion of cervical cancer cells in vitro through the TGF‐β/Smad2/3/Snail1 pathway. [ABSTRACT FROM AUTHOR]

Phytophthora species are destructive plant pathogens that cause significant crop losses worldwide. To understand plant susceptibility to oomycete pathogens and to explore novel disease resistance strategies, we employed the Arabidopsis thaliana–Phytophthora parasitica model pathosystem and screened for A. thaliana T‐DNA insertion mutant lines resistant to P. parasitica. This led to the identification of the resistant mutant 267‐31, which carries two T‐DNA insertion sites in the promoter region of the ethylene‐responsive factor 19 gene (ERF019). Quantitative reverse transcription PCR (RT‐qPCR) assays showed that the expression of ERF019 was induced during P. parasitica infection in the wild type, which was suppressed in the 267‐31 mutant. Additional erf019 mutants were generated using CRISPR/Cas9 technology and were confirmed to have increased resistance to P. parasitica. In contrast, ERF019 overexpression lines were more susceptible. Transient overexpression assays in Nicotiana benthamiana showed that the nuclear localization of ERF019 is crucial for its susceptible function. RT‐qPCR analyses showed that the expression of marker genes for multiple defence pathways was significantly up‐regulated in the mutant compared with the wild type during infection. Flg22‐induced hydrogen peroxide accumulation and reactive oxygen species burst were impaired in ERF019 overexpression lines, and flg22‐induced MAPK activation was enhanced in erf019 mutants. Moreover, transient overexpression of ERF019 strongly suppressed INF‐triggered cell death in N. benthamiana. These results reveal the importance of ERF019 in mediating plant susceptibility to P. parasitica through suppression of pathogen‐associated molecular pattern‐triggered immunity. [ABSTRACT FROM AUTHOR]

BaSi2 O2 N2: Eu2+ phosphor was successfully synthesized by using a simple solid-state reaction method. Its properties were systematically investigated utilizing XRD, photoluminescence, excited state decay curve, afterglow emission spectra, and thermoluminescence ( TL) glow curve. With increasing temperature, its emission intensity decreases with the broadening full widths at half maximum. Particularly, its temperature-dependent afterglow emission spectra were investigated for the first time. Based on the information from TL glow curve, temperature-dependent afterglow decay curves, and afterglow emission spectra, a model was constructed to explain the mechanism of afterglow. This study provides a new perspective to use the temperature-dependent luminescence properties for studying the afterglow processes of long-lasting phosphorescence phosphors. [ABSTRACT FROM AUTHOR]

The antileishmanial activity of compounds inspired by naphthoquinone secondary metabolitesfrom Bignoniaceae is presented. Three structural series of compounds from a common biosyntheticpathway were evaluated against Leishmania major. Compound (15), an analog of the natural productpinnatal, was more active than amphotericin B against L. major. When tested against L. (Viannia) braziliensisand L. infantum, compound 15 showed similar activity to amphotericin B. Drug Dev Res 74 :237-241, 2013. [ABSTRACT FROM AUTHOR]

Oxynitride long-lasting phosphorescence ( LLP) phosphor SrSi2 O2 N2: Eu2+ was prepared by a new method using SrSi alloy as a precursor. Its properties were systematically investigated utilizing XRD, photoluminescence, excited-state decay curve, long-lasting phosphorescence, and thermoluminescence spectrum. This phosphor was found to be well-crystallized by calcinations of the Sr1− x Eu x Si alloy and the SiO2 mixture at 1400°C for 3 h. After irradiation under the 280 nm UV light, the afterglow emission of Eu2+ (4 f65 d1 → 4 f7) was obviously observed for at least 2 h in the limit of light perception of dark-adapted human eyes (0.32 mcd/m2). Furthermore, the possible mechanism for the LLP of SrSi2 O2 N2: Eu2+ phosphor is also discussed in this article. [ABSTRACT FROM AUTHOR]

The nitrides Ca2 Si5 N8:0.5% Eu2+, x% Tm3+( x = 0, 0.5, 1, 2, 4) ( CSN:0.5E, xT) phosphors were prepared via the high temperature solid-sintering method using CaH2 as calcium source. These phosphors exhibited strong orange long-lasting phosphorescence ( LLP) after turning off the activating light. Besides, the CSN:0.5E, 1T phosphor with an afterglow time of more than 200 min (0.32 mcd/m2). Furthermore, the temperature-dependent emission spectra of CSN:0.5E, 1T were investigated from temperature 80-500 K and an anti-quenching phenomenon that the emission intensities increased then decreased under excitation at increased temperature was found. Ultimate, the proposed mechanism on temperature dependence of luminescence was analyzed. This study provides a new perspective for the impact of temperature-dependent problem as a consequence of heating processes in luminescent materials. [ABSTRACT FROM AUTHOR]

BaSi2 O2 N2: Eu2+ phosphor was successfully synthesized by using a simple solid-state reaction method. Its properties were systematically investigated utilizing XRD, photoluminescence, excited state decay curve, afterglow emission spectra, and thermoluminescence ( TL) glow curve. With increasing temperature, its emission intensity decreases with the broadening full widths at half maximum. Particularly, its temperature-dependent afterglow emission spectra were investigated for the first time. Based on the information from TL glow curve, temperature-dependent afterglow decay curves, and afterglow emission spectra, a model was constructed to explain the mechanism of afterglow. This study provides a new perspective to use the temperature-dependent luminescence properties for studying the afterglow processes of long-lasting phosphorescence phosphors. [ABSTRACT FROM AUTHOR]