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As a nutrient-rich multigrain crop, buckwheat is a typical "medicinal food homology" crop that is rich in flavonoids, including rutin and various vitamins. It has positive anti-oxidant and anti-tumour properties and lowers blood pressure. However, due to strict self-crossing characteristics, slow progress has been made in Tartary buckwheat (TB) cross-breeding, resulting in the slow breeding of new varieties of new TB varieties, which has limited the improvement of yield and quality. Therefore, mutant breeding is a rapid and effective technique for broadening and innovating TB breeding. In recent years, improving qualities related to yield, lodging resistance, and stability have become key points in TB breeding. Based on the above findings, excellent, potentially valuable TB lines with rich phenotypes were obtained for the TB mutation library via ethyl methanesulfonate (EMS), laying a foundation for creating new TB germplasms. In this study, we systematically investigated more than 10 agronomic traits of JQ2 and JQ4 mutants, including plant type, leaf colour, grain type, grain colour, grain number per plant, grain length, grain width, grain weight per plant, and 1000-grain weight. The results show that the maximum number of grains per plant was 1956, the weight was 32.84 g, and the 1000-grain weight was 30.89 g. The maximum number of grains per JQ4 plant was 2308, and the weight was 44.82 g. The maximum 1000-grain weight was 24.7 g. Among the 295 JQ2 mutants and 153 JQ4 mutants, 10 flavonoids (orientin, morin, quercetin, kaempferol, luteolin, naringin, hesperetin, myricetin, hesperidin, and rutin) were detected with near infrared spectroscopy (NIR). The mutants were divided into five groups according to the flavonoid content of the JQ2 mutants, of which the first group included 31 individual lines. and the second to fifth groups included 70, 69, 72, and 53 lines, respectively. The JQ4 mutants were divided into four classes, of which 41, 50, 32, and 30 were individual lines, respectively, with the highest rutin content being 82.06 mg/g. In summary, through systematic analysis and screening of the agronomic traits and flavonoid contents of JQ2 and JQ4 mutant seeds, we obtained three lines with a high 1000-grain weight, including two JQ2 mutant lines (30.89 g) and one JQ4 mutant line, which reached 24.70 g and ten lines with high grain weight per plant. This included 8 JQ2 mutants and 2 JQ4 mutants, as well as 72 high-rutin mutants (including 31 lines from JQ2 and 41 lines from JQ4 mutants). These elite lines provide the material basis for creating TB germplasms with excellent qualities and cultivation characteristics. [ABSTRACT FROM AUTHOR]

Imine‐linked covalent organic frameworks (COFs) have been extensively studied in photocatalysis because of their easy synthesis and excellent crystallinity. The effect of imine‐bond orientation on the photocatalytic properties of COFs, however, is still rarely studied. Herein, we report two novel COFs with different orientations of imine bonds using oligo(phenylenevinylene) moieties. The COFs showed similar structures but great differences in their photoelectric properties. COF‐932 demonstrated a superior hydrogen evolution performance compared to COF‐923 when triethanolamine was used as the sacrificial agent. Interestingly, the use of ascorbic acid led to the protonation of the COFs, further altering the direction of electron transfer. The photocatalytic performances were increased to 23.4 and 0.73 mmol g−1 h−1 for protonated COF‐923 and COF‐932, respectively. This study provides a clear strategy for the design of imine‐linked COF‐based photocatalysts and advances the development of COFs. [ABSTRACT FROM AUTHOR]

Imine‐linked covalent organic frameworks (COFs) have been extensively studied in photocatalysis because of their easy synthesis and excellent crystallinity. The effect of imine‐bond orientation on the photocatalytic properties of COFs, however, is still rarely studied. Herein, we report two novel COFs with different orientations of imine bonds using oligo(phenylenevinylene) moieties. The COFs showed similar structures but great differences in their photoelectric properties. COF‐932 demonstrated a superior hydrogen evolution performance compared to COF‐923 when triethanolamine was used as the sacrificial agent. Interestingly, the use of ascorbic acid led to the protonation of the COFs, further altering the direction of electron transfer. The photocatalytic performances were increased to 23.4 and 0.73 mmol g−1 h−1 for protonated COF‐923 and COF‐932, respectively. This study provides a clear strategy for the design of imine‐linked COF‐based photocatalysts and advances the development of COFs. [ABSTRACT FROM AUTHOR]

Highlights • A new UPLC-MS/MS method was developed for determining tebipenem in human plasma. • The method was validated according to the guidelines of European Medicines Agency. • High throughput, sensitivity, and reliability were achieved. • The method was applied to a pharmacokinetic study of tebipenem in human volunteers. Abstract A rapid and sensitive ultra-high-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated for determining tebipenem (TBPM) in human plasma. Plasma samples were prepared following a single-step protein precipitation method using acetonitrile and 3-morpholinopropanesulfonic acid (MOPS, pH 7.0, 50 mM) which equal volume of plasma samples were added for stabilizing the analyte. Separation was achieved using an ACQUITY UPLC BEH C18 (1.7 μm, 2.1 × 50 mm) column. A repeated gradient program was employed for reducing the carryover effect, and the total chromatographic run time was 3.0 min. Method validation results showed TBPM was linear in its analytical range i.e. between 0.1–20 μg/mL (r2>0.99), and the lower limit of quantification (LLOQ) was 0.1 μg/mL. The intra-run and inter-run precision (coefficient of variation, CV) was within 3.81%, and the accuracy (relative error, RE) was within ± 8.56%. The carryover was restricted below 8.1%. Matrix effects were minimal, and recovery of TBPM was 90.19–95.74%. The stability of TBPM in plasma sample stored at room temperature (25 °C) for 4 h, at −20 °C for 3 days, at −80 °C for 30 days, five freeze-thaw cycles at −80 °C and processed samples at auto sampler vials (8 °C) for 24 h were within 91.11–106.33%. Finally, the validated method was successfully applied to a pharmacokinetic study of TBPM in healthy volunteers after oral administration of tebipenem pivoxil (TBPM-PI). [ABSTRACT FROM AUTHOR]

Oxaliplatin is a platinum compound that is frequently prescribed for the chemotherapeutic treatment of colorectal cancer. In tumor cells, cellular uptake is the first step of oxaliplatin action. Cellular accumulation of oxaliplatin is considered to play an important role in anti-cancer efficacy. However, limited information about cellular accumulation of intact oxaliplatin is available. In this study, a sensitive hydrophilic interaction liquid chromatography-tandem mass spectrometry (HILIC-MS/MS) approach for the quantification of oxaliplatin in cells was developed and validated. The method allowed for a rapid and simple determination of intact oxaliplatin in cell lysate. The retention time of oxaliplatin was 3.04 min, which was achieved by applying a chromatographic gradient elution of 5 min. The lower limit of quantification (LLOQ) was 2 ng/mL and the analytical range of oxaliplatin was linear between 2–200 ng/mL. The intra-day precision and inter-day precision (RSD (relative standard deviation)) ranged from 0.52 to 7.89%, and the accuracy (RE (relative error)) was within ± 4.5%. Matrix effects and recovery were acceptable. The method was successfully used for the determination of intact oxaliplatin uptake by HCT-116 colon cancer cells. Thus, our findings may prospectively support a celluar pharmacokinetic study and low concentration measurement of intact oxaliplatin in the clinic. [ABSTRACT FROM AUTHOR]

In this paper, a piecewise map with singularity of the power (-1/2) is introduced. For this piecewise map, there is an infinite discontinuous gap on the origin. The conditions of nonsmooth border-collision bifurcation and smooth fold or flip bifurcation are analytically derived. For period-1 fixed point, two-parameter-plane can be divided into seven ranges according to different bifurcation structures. For period-n orbits, codimension-2 bifurcation point may lead to different period-increment sequence, and a peculiar feature is found that there are two different period-increment sequences in the same bifurcation diagram. [ABSTRACT FROM AUTHOR]

Oroxylin A is a flavonoid monomer extracted from Scutellaria baicalensis Georgi with neuroprotective, anti-tumor activity and many other biological functions. However, the interaction between Oroxylin A and the drug transporters has not been clearly reported. The purpose of this study is to investigate the interaction between Oroxylin A and the solute carrier transporters (OATP1B1, OATP1B3, OAT1, OAT3, OCT2, MATE1, and MATE2K), and ATP-binding cassette transporters (BCRP, MDR1). The HEK293 cell lines (HEK293-OATP1B1, HEK293-OATP1B3, HEK293-OAT1, HEK293-OAT3, HEK293-OCT2, HEK293-MATE1, and HEK293-MATE2K) that stably expressing previous listed human-derived transporters were employed to evaluate the solute carrier transporters. Vesicles expressing human BCRP and MDR1 transporters was employed to research ATP-binding cassette transporters. Our work suggested that Oroxylin A was a substrate of OATP1B1, OATP1B3, but not a substrate of the other transporters in the concentration range of our study. Oroxylin A shows concentration-dependent inhibition of OATP1B1, OAT1, OAT3 and BCRP transportation with the half-inhibitory concentration (IC50) of 7.03, 0.961, 0.112 μM, and 0.477 μM, respectively. No inhibitory effects on the transport activities of other transporters were observed for Oroxylin A. Drug transporters profile of Oroxylin A was first confirmed by our work, which provides important information for its pharmacokinetics, pharmacodynamics, and drug-drug interactions studies. Image 1 • Drug transporters profile for Oroxylin A was researched. • Oroxylin A is a substrate for OATP1B1 and OATP1B3. • Oroxylin A was found to inhibit OATP1B1, OAT1, OAT3 and BCRP. [ABSTRACT FROM AUTHOR]

The ability of the projectile to strike accurately in the air depends on the accurate measurement of its flight distance. Due to the influence of the external environment, it is very difficult to measure the distance of high-speed projectiles in real time with ranging equipment such as radar and laser. Based on this, a real-time measurement model of the horizontal flight distance of the projectile was designed, which combines trajectory equation and discrete acceleration. First, the angle of inclination of the projectile at each position was calculated according to the six-degree-of-freedom rigid outer trajectory model. Then, two kinds of distance measurement models based on discrete acceleration integration were introduced, and the accuracy simulation was carried out. Simulation results show that the Simpson integral method is more accurate. The flight arc length of the projectile was calculated by the Simpson integral method. Finally, the horizontal flight distance of the projectile was obtained by combining the flight arc length and inclination angle of the projectile. Finally, the flight distance measurement model was simulated, and the simulation results show that the model has high accuracy. The simulation results show that the horizontal flight distance of the projectile can be measured by the trajectory equation and discrete acceleration according to the set conditions. This method can be used to measure the distance of the projectile by carrying the sensor and is less affected by the external environment. It can provide a theoretical basis and reference for the measurement of the horizontal distance of the projectile. [ABSTRACT FROM AUTHOR]

Floating ring bearing has the advantages of simple structure and high operating speed and is widely used in turbocharger and aero-engine. However, many harsh working conditions cause the floating ring bearing to produce starved lubrication and failures. Here, we investigated the starved lubrication characteristics of floating ring bearing via theoretical modeling and numerical simulation. We first established a theoretical model of starved-boundary lubrication based on the Reynolds equation for floating ring bearing. And meanwhile, an oil-film ratio coefficient is introduced into the theoretical model to reflect the degree of starved lubrication. We then analyzed the influence of inlet-boundary conditions (flow rate, oil-film thickness) on the starved-lubrication performance of floating ring bearings. The results showed that the flow rate obviously affects the bearing area of inside and outside oil film, and the oil-film ratio coefficient inside the bearing. When the oil supply is lower than 10 mL/min, the floating ring bearing is in a serious starved-lubrication state, and the oil-film area of bearing is reduced by 30%. The favorable oil supply flow rate can obviously improve the lubrication conditions, and also can predict the starved state of inner oil-film. Our study provides a theoretical basis for the fault detection of floating ring bearing. • Studied the mechanism of oil-starved lubrication on floating ring bearing. • Established model of oil-starved lubrication to calculate lubrication characteristics for floating ring bearing. • Calculated lubrication characteristics under different lubrication conditions. • Analyzed the influence of oil supply on bearing lubrication characteristics. [ABSTRACT FROM AUTHOR]

Planetary gear transmission system is an important transmission part of large machinery and is prone to failure. Aiming at the problem of how to extract fault information from vibration signals of nonlinear and nonstationary planetary gearboxes, a performance degradation evaluation index of planetary gearboxes based on improved distributed compressed sensing and modified multiscale symbolic dynamic entropy (DCSMDE) is proposed. DCSMDE combines distributed compression sensing with modified multiscale symbol dynamic entropy and solves the problem of strong nonlinearity and strong vibration signal coupling of the planetary transmission system from the homologous signals of multiple sensors. A distributed compression sensing parameter optimization algorithm based on Rényi entropy is proposed, which uses improved distributed compression sensing technology to simultaneously sample, compress, and denoise the multisource vibration data of rotating machinery. DCSMDE is used to calculate the reconstructed signal, extract the features with higher recognition characteristics, and use the change trend of the DCSMDE value to judge the working status of the planetary gearbox. Experimental results show that DCSMDE can be applied to dynamic evolution and fault identification of mechanical systems and accurately classify actual fault signals. It provides a new idea for the classification of planetary gear faults and the recognition of performance degradation. [ABSTRACT FROM AUTHOR]

1. Afatinib is an oral, selective tyrosine kinase inhibitor (TKI) primarily transported by P-glycoprotein (MDR1, gene code ABCB1) and breast cancer resistance protein (BCRP, gene code ABCG2). In the present study, the effects of ABCB1 and ABCG2 genetic polymorphisms on the pharmacokinetics of afatinib in healthy Chinese were investigated. 2. Blood samples from 24 healthy participants who received afatinib were used for genotyping ABCB1 (1236C>T, 2677G > T/A, 3435C>T) and ABCG2 (34G>A, 421C>A) polymorphisms. Subsequently, the association between afatinib plasma concentrations and target single-nucleotide polymorphisms (SNPs) was analyzed. 3. Among the five polymorphisms, plasma concentrations of afatinib in healthy subjects with ABCB1 1236CC–3435CC were remarkably higher than in other genotype subjects. No significant differences of afatinib exposure were found between the ABCG2 wild-type and heterozygous groups. 4. The ABCB1 genetic polymorphism influenced the plasma exposure of afatinib, and gene testing before drug administration may be useful for clinically individualized use of afatinib. Our data suggest the usefulness of afatinib pharmacogenetics in treatment optimization. [ABSTRACT FROM AUTHOR]

PEGylation techniques have been increasingly employed in drug delivery system and chemical modification of compounds with low aqueous solubility. Triacontanol (TA) is a natural product with several pharmacological activities, but its low aqueous solubility significantly limited its application. PEGylated triacontanol (PEG-TA) was designed as the prodrug to improve the aqueous solubility and pharmacokinetic properties of TA. On the basis of salting-out assisted liquid-liquid extraction (SALLE) and saponification sample preparation procedure, a reliable gas chromatography tandem mass spectrometric (GC–MS/MS) method was developed and validated for the quantification of PEG-TA and its metabolite TA in rat plasma after separation and transformation. Acetonitrile-methanol (9:1, v/v) and ammonium acetate (10 M) were utilized to separate PEG-TA and TA (including conjugated TA with fatty acid). Saponification facilitated the complete conversion of PEG-TA into TA, so PEG-TA could be indirectly quantified. The results revealed that the GC–MS/MS method had excellent selectivity, accuracy and linearity. Calibration curves were linear (R 2 >0.99) within the range of 20.0–1000.0 ng/mL for TA and 100.0–10,000.0 ng/mL for PEG-TA. The intra- and inter-day precision of quality control samples were within 15%, and their accuracy values varied from 93.54% to 113.38%. This analytical method has been successfully applied to pharmacokinetic study of PEG-TA. This study can facilitate the further exploration and quantification of PEGylated prodrugs. [ABSTRACT FROM AUTHOR]