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Sinapic acid (SA) is renowned for its many pharmacological activities as a polyphenolic compound. The cause of polycystic ovary syndrome (PCOS), a commonly encountered array of metabolic and hormonal abnormalities in females, has yet to be determined. The present experiment was performed to evaluate the antifibrotic properties of SA in rats with letrozole‐induced PCOS‐related ovarian fibrosis. SA treatment successfully mitigated the changes induced by letrozole in body weight (BW) (p <.01) and relative ovary weight (p <.05). Histological observation revealed that SA reduced the number of atretic and cystic follicles (AFs) and (CFs) (p <.01), as well as ovarian fibrosis, in PCOS rats. Additionally, SA treatment impacted the serum levels of sex hormones in PCOS rats. Luteinizing hormone (LH) and testosterone (T) levels were decreased (p <.01, p <.05), and follicle‐stimulating hormone (FSH) levels were increased (p <.05). SA administration also decreased triglyceride (TG) (p <.01) and total cholesterol (TC) levels (p <.05) and increased high‐density lipoprotein cholesterol (HDL‐C) levels (p <.01), thereby alleviating letrozole‐induced metabolic dysfunction in PCOS rats. Furthermore, SA treatment targeted insulin resistance (IR) and increased the messenger RNA (mRNA) levels of antioxidant enzymes in the ovaries of PCOS rats. Finally, SA treatment enhanced the activity of peroxisome proliferator‐activated receptor‐γ (PPAR‐γ), reduced the activation of transforming growth factor‐β1 (TGF‐β1)/Smads, and decreased collagen I, α‐smooth muscle actin (α‐SMA), and connective tissue growth factor (CTGF) levels in the ovaries of PCOS rats. These observations suggest that SA significantly ameliorates metabolic dysfunction and oxidative stress and ultimately reduces ovarian fibrosis in rats with letrozole‐induced PCOS. [ABSTRACT FROM AUTHOR]

The current study aimed to explore the pharmacokinetics of danofloxacin in non‐laying hens after a single oral (PO) and intravenous (IV) dose, both at 5 mg/kg body weight (BW). Eighteen 13‐week‐old healthy hens were equally and randomly divided into two groups. After both doses, blood samples (approximately 1 ml) were collected at different time points. Danofloxacin concentrations were quantified by a validated high‐performance liquid chromatography (HPLC) method followed by a non‐compartmental analysis using the software of WinNonLin. The elimination half‐lives (t1/2λzs) after PO and IV routes were determined as 8.15 ± 3.37 and 7.69 ± 3.40 h, respectively. After IV administration, danofloxacin had an initial concentration (C0) of 3.62 μg/ml, a volume of distribution at steady state (VSS) of 3579.72 ± 454.29 ml/kg, and a total body clearance (Cl) of 0.49 ml/h/g. After PO administration, the absolute bioavailability and absorption half‐life (t1/2ka) were calculated as 100.99% ± 23.10% and 0.82 ± 0.58 h, respectively. Based on the calculated ratio values of AUC/MIC and Cmax/MIC, an oral dose of 5 mg/kg danofloxacin would be expected to successfully treat hens infected with strains with MIC values ≤0.1 μg/ml. [ABSTRACT FROM AUTHOR]

The objective of this study was to determine the pharmacokinetics of meloxicam after a single intravenous (IV), intramuscular (IM), and oral (PO) dose at 1 mg/kg body weight in Jing Hong laying hens. Blood samples were collected at predetermined time points. Plasma meloxicam concentrations were determined using a validated high‐performance liquid chromatography (HPLC) assay method and then subjected to a non‐compartmental analysis. After IV administration, meloxicam had a mean (±SD) volume of distribution at steady‐state (Vdss) of 206.50 ± 25.23 ml/kg, a terminal half‐life (t1/2λ) of 5.45 ± 0.53 h, and a total body clearance (Cl) of 26.48 ± 4.13 ml/h/kg. After PO and IM administration, meloxicam was absorbed relatively rapidly: the peak concentrations (Cmaxs) of 3.04 ± 0.56 and 8.94 ± 2.31 μg/ml were observed at 3.08 and 0.80 h, respectively. After PO and IM administration, the absolute bioavailability (F) was determined as 70.13% and 125.50%, respectively. Assuming that hens shared the same analgesic threshold of meloxicam (0.5 μg/ml) with humans, the plasma concentrations after three different routes (PO, IM, and IV) of administration were above this value for 16.7, 19.2, and 14.9 h, respectively. [ABSTRACT FROM AUTHOR]

A flow‐limited physiologically based pharmacokinetic (PBPK) model consisting of seven compartments was established for orbifloxacin in crucian carp to predict drug concentrations after intravenous or intramuscular injections. Physiological and anatomical parameters, including tissue weights and blood flow through different tissues, were obtained from previous literature. The tissue/plasma partition coefficients for orbifloxacin were calculated using the area method or parameter optimization. In addition, their values were 0.9326, 1.1204, 1.1644, 1.3514, and 2.0057 in the liver, skin, muscle, kidney, and the rest of the body compartment, respectively. Based on the current PBPK model, orbifloxacin concentrations were predicted and compared with those previously reported for further validation. In addition, the mean absolute percentage error (MAPE) values were also calculated, with values ranging from 10.21% in plasma to 42.37% in kidneys, indicating acceptable predictions for all tissues and plasma. A local sensitivity analysis was performed, which showed that the parameters related to elimination and distribution were most influential on orbifloxacin concentrations in muscle. This model was finally used to predict plasma and tissue concentrations after multiple intramuscular dosing. The current PBPK model provided a valuable tool for predicting the tissue residues of orbifloxacin in crucian carp following intramuscular injection. [ABSTRACT FROM AUTHOR]

As a fluoroquinolone antimicrobial agent, danofloxacin is mainly used to treat avian bacterial and mycoplasma infections. The pharmacokinetic characteristics of danofloxacin are usually explored in healthy animals, while those in endotoxemic broilers are still rare. This study aimed to investigate the pharmacokinetics of danofloxacin in endotoxemic broilers induced by Escherichia coli (E. coli) lipopolysaccharide (LPS) after single oral administration. Ten healthy 5‐week‐old Arbor Acres (AA) broilers with similar body weight (BW) were randomly and equally divided into LPS and control groups. The LPS group was intravenously injected with an LPS of E. coli O55: B5 at 2.5 mg/kg BW, and the control group was intravenously injected with the same volume of sterile saline. Danofloxacin was administered orally at a dose of 5 mg/kg BW immediately 1 h after the intravenous injection of LPS or sterile saline. Rectal temperature was measured at predetermined times points in all broilers, and plasma and serum samples were taken. The interleukin‐6 (IL‐6) levels in serum samples were detected by the enzyme‐linked immunosorbent assay (ELISA) kits, and danofloxacin concentrations in plasma were detected through the high‐performance liquid chromatography (HPLC) method and subjected to a compartmental analysis using Phoenix software. The LPS challenge led to biphasic adaptive changes in broiler body temperature and increased the levels of IL‐6. Compared with the control group, LPS treatment significantly prolonged the time to the peak concentration (LPS: 8.75 ± 3.88 h; Control: 3.20 ± 2.20 h). However, there were no significant differences in the other pharmacokinetic parameters between both groups. [ABSTRACT FROM AUTHOR]

Enantiomers of 2, 6‐diaminotriptycene (R, R‐1 and S, S‐1) are split by chiral‐phase HPLC and their absolute configurations are identified by single‐crystal X‐ray diffraction technology. Using the enantiomers as monomers, a couple of chiral porous polyimides (R‐FTPI and S‐FTPI) are prepared by polycondensation reactions and display good heat stability, high BET surface area and good solubility in organic solvents. Moreover, both of R‐FTPI and S‐FTPI can be cast into robust, free‐standing films suitable for enantioselective separation with symmetrical chiral selectivity. [ABSTRACT FROM AUTHOR]

The present study aimed to determine the pharmacokinetic profiles of ceftiofur (as measured by ceftiofur and its active metabolites concentrations) in a small‐size dog breed, Peekapoo, following a single intravenous or subcutaneous injection of ceftiofur sodium. The study population comprised of five clinically healthy Peekapoo dogs with an average body weight (BW) of 3.4 kg. Each dog received either intravenous or subcutaneous injection, both at 5 mg/kg BW (calculated as pure ceftiofur). Plasma samples were collected at different time points after the administration. Ceftiofur and its active metabolites were extracted from plasma samples, derivatized, and further quantified by high‐performance liquid chromatography. The concentrations versus time data were subjected to noncompartmental analysis to obtain the pharmacokinetic parameters. The terminal half‐life (t1/2λz) was calculated as 7.40 ± 0.79 and 7.91 ± 1.53 hr following intravenous and subcutaneous injections, respectively. After intravenous treatment, the total body clearance (Cl) and volume of distribution at steady‐state (VSS) were determined as 39.91 ± 4.04 ml hr−1 kg−1 and 345.71 ± 28.66 ml/kg, respectively. After subcutaneous injection, the peak concentration (Cmax; 10.50 ± 0.22 μg/ml) was observed at 3.2 ± 1.1 hr, and the absorption half‐life (t1/2ka) and absolute bioavailability (F) were calculated as 0.74 ± 0.23 hr and 91.70%±7.34%, respectively. The pharmacokinetic profiles of ceftiofur and its related metabolites demonstrated their quick and excellent absorption after subcutaneous administration, in addition to poor distribution and slow elimination in Peekapoo dogs. Based on the time of concentration above minimum inhibitory concentration (T > MIC) values calculated here, an intravenous or subcutaneous dose at 5 mg/kg of ceftiofur sodium once every 12 hr is predicted to be effective for treating canine bacteria with a MIC value of ≤4.0 μg/ml. [ABSTRACT FROM AUTHOR]

ABSTRACT The stability of hydroxyl polyacrylate emulsion was studied from two aspects of the structure of latex particles and polymerization conditions. Waterborne polyacrylate was prepared through seeded semicontinuous emulsion polymerization method with pre-emulsification process. HEMA was used to provide a high content of hydroxyl group, and the reactive emulsifier SE-10 was introduced to substitute for the traditional emulsifier. The best conditions including polymerization process and temperature, monomer types and dropping time were determined, and the effects of emulsifier content and addition method, HEMA content, chain transfer agent content, and soft/hard monomer ratio on the properties of emulsion were investigated. Through the optimization of polymerization conditions and the control of the structure of particles, we have successfully synthesized the core-shell structure of polyacrylate emulsion with a good appearance, low viscosity and a solid content of 46.5%. The hydroxyl polyacrylate exhibits good performance, which has great potential in development and application. © 2017 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2017, 134, 44844. [ABSTRACT FROM AUTHOR]

Gastric cancer remains one of the most prevalent and lethal malignancies in the world. Despite new advances in treatment and diagnosis, patients with advanced gastric cancer are still difficult to cure resulting in a high mortality rate and poor prognosis. Signal transducer and activator of transcription 3 (Stat3) is observed aberrant in multiple tumours, including gastric cancer. Stat3 overexpression was confirmed performing a vital role in tumorigenesis. In the present study, we constructed a pSi-Stat3 plasmid to silence Stat3 and investigated the effect of pSi-Stat3 on cell proliferation, apoptosis and cell cycle progression in gastric cancer cell line SGC-7901 and mice xenograft model. Downstream proteins of Stat3, including Cyclin-D1, Survivin and Bcl-2, were detected as well for the underlying mechanism exploration. It showed that pSi-Stat3 can effectively silence the expression of Stat3 and inhibits the growth of gastric tumour both in vitro and in vivo significantly via cell apoptosis and cell cycle shift induction. The findings suggest that Stat3 signal pathway might be a promising therapeutic target for tumour treatment, including gastric cancer. Copyright © 2015 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

Tropical cyclone Tembin (2012) passed twice and made landfall over south tip of Taiwan in August 2012. During its passage, an unusual sea surface warming was generated at 22.5°N, 117°E in the coastal region of northern South China Sea. Subsequently, Tembin passed over this extreme warming region and its intensity was enhanced drastically and suddenly from Category 1 to Category 3 within less than 1-day time interval. This unusual warming seems to largely prompt the intensification of Tembin. Next, the relationship between this extreme warming and rapid intensification of Tembin is identified by atmospheric model Weather Research and Forecast (WRF) with updated time-varying lower boundary condition. In addition, given the tight relationship between generation of unusual warming in the shore region and following possible TC intensification, a series of numerical experiments based on oceanic model Regional Oceanic Modeling System (ROMS) were designed and executed to resolve the possible generated mechanism of the extreme warming. The results indicate that a distinct positive short-wave radiation influx anomaly may dominate the generation of the unusual warming in the shore region during Tembin's passage. This result is validated by the distributions of free cloudy coverage shown in satellite infrared images. [ABSTRACT FROM AUTHOR]

A series of sphere-rod shape amphiphiles, in which a [60]fullerene (C60) sphere was connected to the center of an oligofluorene (OF) rod through a rigid linkage (OF-C60), were designed and synthesized. Alkyl chains of various lengths were attached onto the OFs on both sides of the C60 spheres. These compounds, denoted as alkyl-OF-C60, were fully characterized by 1H NMR, 13C NMR, and FTIR spectroscopy and by MALDI-TOF mass spectrometry. The morphologies and structures of their crystals were elucidated by wide-angle X-ray diffraction (WAXD) and by electron diffraction in transmission electron microscopy (TEM). Butyl-OF-C60 forms a monoclinic unit cell ( a=1.86, b=3.96, c=2.24 nm; α= γ=90°, β=68°; space group P2), octyl-OF-C60 also forms a monoclinic unit cell ( a=2.21, b=4.06, c=1.81 nm; α= γ=90°, β=75.5°; space group C2m), and dodecanyl-OF-C60 forms a triclinic structure ( a=1.82, b=4.35, c=2.26 nm; α=93.1°, β=94.5°, γ=92.7°; space group P1). The inequivalent spheres and rods were found to pack into an alternating layered structure of C60 and OF in the crystals, thus resembling a 'double-cable' structure. UV/Vis absorption spectroscopy revealed an electron perturbation between the two individual chromophores (C60 and OF) in their ground states. Fluorescence spectroscopy exhibited complete fluorescence quenching of their solutions in toluene, thus suggesting an effective energy transfer from OF to C60. Cyclic voltammetry indicated that the energy-level profiles of C60 and OF remained essentially unchanged. This work has broad implications in terms of understanding the self-assembly and molecular packing of conjugated materials in crystals and has potential applications in organic field-effect transistors and bulk heterojunction solar cells. [ABSTRACT FROM AUTHOR]

A novel perylene bisimide dye bearing carboxylphenylene substituents on the imide N atoms was synthesized and four conjugated copolymers containing different contents of perylene bisimide dye were synthesized via PPA/P2O5 copolymerization method. The structures of the four copolymers were characterized by FTIR, elementary analysis, 1H-NMR and XRD. The copolymers showed good thermal stabilities but poor solubilities due to the high rigidity of the backbone. The photophysical characteristics of the copolymers were investigated by UV-Vis and PL spectra in solutions and films. Because of the conformational change of perylene bisimide chromophore, the absorptions of perylene bisimide core in copolymers showed a large blue-shift (56 nm) compared to that of the perylene monomer. In PL experiments, when exciting the benzoxazole, an obvious fluorescent quenching was observed in all copolymers, which can be attributed to the energy transfer from benzoxazole units to perylene bisimide fragments and fluorescence quenching. With increasing perylene content, the copolymers turned to layered and friable. The XRD test showed that the interchain distances increased slightly with increasing perylene content. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2010 [ABSTRACT FROM AUTHOR]

The polymerization‐induced phase‐separation behavior of a thermoplastic [poly(ether sulfone) (PES)]‐ modified thermosetting bismaleimide resin during isothermal curing was investigated with differential scanning calorimetry, time‐resolved light scattering, and scanning electron microscopy with various contents and molecular weights of PES. The results suggested that the phase structure changed from a dispersed structure to a bicontinuous structure to phase inversion with an increase in the PES content. Three kinds of PES with different molecular weights were used to study the effects of the molecular weight on the phase structure and mechanical properties of modified systems. With higher molecular weight PES, a phase‐inversion morphology could be obtained at lower PES contents. The curing conversion of bismaleimide was affected by the composition of the blend. The curing rate decreased with an increase in the PES content. A blend with 15 wt % PES of a suitable molecular weight had a higher tensile strength and elongation at break than that without PES. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci 2007 [ABSTRACT FROM AUTHOR]