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P-glycoprotein (P-gp), an ATP binding cassette protein, plays a major role in efflux transport of drugs and xenobiotics due to its abundant expression on several barriers. This study aimed to investigate the potential role of PKC/NF-κB-PXR signaling pathway in modulation of P-gp gene expression in human colon adenocarcinoma LS174T. The effect of PMA on MDR1 luciferase activity was investigated by PXR-MDR1 dual luciferase reporter gene assay. Real-time qPCR assay and Western blot analysis were used to study the gene expression of P-gp and NF-κB, respectively. Compared to the vehicle-treated group, PMA statistically decreased P-gp luciferase activity, mRNA expression and protein expression. Moreover, PMA treatment yielded a significant and dose-dependent increase in RelA/p65 translocation to nucleus. Meanwhile, a remarkable increase of the pho-IκBα status was observed in LS174T cells after treatment with PMA (1-100 nmol·L(-1)). In addition, knockdown of PKCα, NF-κB or PXR can significantly attenuate PMA-induced P-gp suppression. These results suggested that PKC/NF-κB-PXR signaling pathway might play crucial roles in modulation of P-gp gene expression.

Multi-robot System (MRS) for intelligent creel consists of automatic winder, transferring, transiting and supplying robot and provides the possibilities of the flexibility and automation of textile industry workshop. Based on the principle of centralized management and distributed control the system and designs distributed control system (DCS) of Multi-robot for intelligent creel based on CAN bus. Layered architecture is established consisting of main control layer, communication layer, synchronous coordination layer and execution layer. According to the complex characteristics of the system, a synchronous controller is designed to allocate and coordinate task,improving the intelligence of the system. Coordination controller also realizes function of CAN Bridge.

In order to solve the revolutionary labor cost, carpet loom yarn waste and production efficiency problem, the author puts forward a kind of new intelligent creel which is based on coreless package storage device. This paper summarizes the automatic winding system of intelligent creel and originally proposes the concept coreless package. The automatic winding unit is responsible for coreless package winding and auxiliary industrial robot finishes gripping, clipping and getting the yarn on. The system designs distributed control system (DCS) of Multi-robot for Intelligent creel based on CAN bus.

The computer control software is becoming complicate, to simplify the development of software, this paper proposes: the background control module of the control software is built automatically by a compiler according to a text descripting the nodes movement sequence, then the background control module and the interface are linked by shared variables. The method proposed is achieved by LabVIEW in the end.

Al + BaO2 + Fe2O3 + sucrose and O2 as reaction system and feeding gas, respectively, are used to prepare hollow multiphase ceramic microspheres (HMCMs) absorbent based on self-reactive quenching technology. The morphologies, particle size distribution, hollow structure and phase compositions were characterized by scanning electron microscope (SEM), X-ray diffraction (XRD) and size analysis. The results show that the quenching products possess high sphere-forming rate, and most of them are hollow structures. Owing to the self-burst, the particle size is between 40 and 70 μm. The phase compositions contain Al2O3, Fe3O4, Fe2O3, Ba2Fe14O22, BaO2 and BaFe4O7. The microwave absorbing tests show that the lowest reflectivity of HMCMs is −19 dB. The frequency bands less than −10 dB are from 13.0 to 15.8 GHz. The reasons for HMCMs possessing good microwave absorbing properties may be their magnetic and electrical properties as well as special hollow structure.

Under informationization, with the development of the technology, equipment becomes more and more complex, which has placed an increasing demand on the innovation of the design theory and methods to equipment support training. However, the methodology to develop the equipment support training is still in the traditional way. There is a lack of the general design on the training system and the systematic analysis of the training requirements. Based on the ISD process, using the IDEF0 modeling technique, a design theory framework for the design of equipment support training is proposed. The theory framework provides a basis for the further study on the establishment of the effective, cost efficient equipment support training system.

To accumulate human resources and strengthen the core competitiveness in an company, the assessment method of maintenance training effectiveness based on cloud models is provided. This method blends together the subjective and objective information. At the same time, the method integrates the fuzzy and random completely, achieves the mutual conversion of qualitative and quantitative assessment, and deals with the uncertainty of the system assessment indexes effectively. On the other hand, the final results of the assessment can provide explicit improvement suggestions to ensure the continuous improvement of the training. Combined with an example, the method is validated finally.

The study was designed to explore the drug-drug interactions mechanisms mediated by OATP1B1 between traditional Chinese medicine Danshensu and rosuvastatin. First, the changes of rosuvastatin pharmacokinetics were investigated in presence of Danshensu in rats. Then, the primary rat hepatocytes model was established to explore the effects of Danshensu on the uptake of rosuvastatin by hepatocytes. Finally, HEK293T cells with overexpression of OATP1B1*a and OATP1B1*5 were established using a lentiviral delivery system to explore the effects of Danshensu on the uptake of rosuvastatin. Rosuvastatin pharmacokinetic parameters of C(max0, AUCO(0-t), AUC(0-∞) were increased about 123%, 194% and 195%, by Danshensu in rats, while the CL z/F value was decreased by 60%. Uptake of rosuvastatin in the primary rat hepatocytes was decreased by 3.13%, 41.15% and 74.62%, respectively in the presence of 20, 40 and 80 μmol x L(-1) Danshensu. The IC50 parameters was (53.04 ± 2.43) μmol x L(-1). The inhibitory effect of Danshensu on OATP1B1 mediated transport of rosuvastatin was related to the OATP1B1 gene type. In OATP1B1*5-HEK293T mutant cells, transport of rosuvastatin were reduced by (39.11 ± 4.94)% and (63.61 ± 3.94)%, respectively, by Danshensu at 1 and 10 μmol x L(-1). While transport of rosuvastatin was reduced by (8.22 ± 2.40)% and (11.56 ± 3.04)% and in OATP1B1*1a cells, respectively. Danshensu significantly altered the pharmacokinetics of rosuvastatin in rats, which was related to competitive inhibition of transport by OATPJBI. Danshensu exhibited a significant activity in the inhibition of rosuvastatin transport by OATP1B1*5-HEK293T, but not by OATP1B1*1a, suggesting a dependence on OATP1B1 sequence.

Liquid chromatography–electrospray ionization mass spectrometry has been used for rapid, selective, and sensitive quantitative analysis of mitiglinide in human plasma. Sample pretreatment involved solid-phase extraction from plasma with gliclazide as internal standard. Separation was performed on a C18 column (150 × 2.0 mm) with 71:29 (v/v) acetonitrile–water (containing 0.1% formic acid and 0.2 mmol L−1 ammonium acetate) as mobile phase at a flow rate of 0.2 mL min−1. The method was validated then successfully applied to a clinical bioequivalence study of mitiglinide in 20 healthy volunteers after oral administration.

Based on the SEM observation on cracks in lined ceramics of the composite pipes, the stress fields in lined ceramics were analyzed. The results indicated that there are the compressive field and heat stress field in lined ceramics, resulting in the existence of radial cracks and net cracks; besides being influenced by wall thickness of ceramic layer, the strength of compressive stress field is also dependent on bonding strength between metal and ceramics, and the strength of heat stress field is dependent on temperature gradient in lined ceramics during cooling of the ceramics.

There is an ongoing debate on the safety of digoxin use in patients with atrial fibrillation (AF). To address this issue, the investigators assembled a synthesis of the available evidence on the relation between digoxin and all-cause mortality in patients with AF. PubMed and the Embase database were systematically searched to identify all eligible studies examining the association between digoxin use and the mortality risk in AF. Overall hazard ratios and 95% confidence intervals were calculated using the random-effects model. Eleven observational studies were identified that met the inclusion criteria, 5 of which additionally used propensity score matching for statistical adjustment. In total, 318,191 patients were followed up for a mean of 2.8 years. Overall, digoxin use was associated with a 21% increased risk for mortality (hazard ratio 1.21, 95% confidence interval 1.12 to 1.30). Sensitivity analyses found the results to be robust. In the propensity score–matched AF patients, digoxin use was associated with a 17% greater risk for mortality (hazard ratio 1.17, 95% confidence interval 1.13 to 1.22). When the AF cohort was grouped into patients with and without heart failure, the use of digoxin was associated with an increase in mortality in patients with and those without heart failure, and no significant heterogeneity was seen between the groups (p >0.10). In conclusion, the results suggest that digoxin use was associated with a greater risk for mortality in patients with AF, regardless of concomitant heart failure. A well-powered randomized trial is necessary to reveal the true effect of digoxin.

This study is to report the effect of OATP1B1 gene mutation in the 521T --C in Chinese human on the pharmacokinetics of rosuvastatin and guide the reasonable clinical application of rosuvastatin by the feature of genetic polymorphism of OATP1B1. Plasma samples were determined with LC-MS: the analyte and internal standard pitavastatin were both analyzed by MS in the ESI, m/z was 480.0 for rosuvastatin and 420.0 for the IS, separately. Genotyping of OATP1B1 was determined with the method of polymerase chain reaction--amplification refractory mutation system targeted at 40 healthy volunteers and showed that there were 7 subjects with 521T --C mutant, accounting to 17.5% of total and wild type homozygote accounted to 82.5%. It was found that there were significant differences between OATP1B1 mutation in the 521T --C and wild type homozygote for rosuvastatin pharmacokinetic process in Chinese human. In contrast to OATP1B1 wild type group, OATP1B1 mutation group's absorption degree increased, elimination process decreased. The OATP1B1 mutation should be noted for guiding the reasonable application of rosuvastatin during its clinical use.

A rapid and sensitive liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI/ MS) method for quantification of pentoxyverine citrate in human plasma has been developed and applied for the bioequivalence and pharmacokinetics study. After extracted from plasma samples with ethyl acetate, analysis was performed in selected ion monitoring (SIM) mode with a positive electrospray ionization (ESI) interface with a mobile phase consisted of methanol and water (0.4% glacial acetic acid and 4 mmol x L(-1) ammonium acetate, 43 : 57, v/v). The linear concentration range of the calibration curves was 1.0-160.0 ng x mL(-1) for pentoxyverine citrate, inter- and intra-precision (RSD) was less than 12.5%, accuracy (RE) was in +/- 13.5% and absolute recovery was more than 80%. The method was proved simple, rapid, sensitive, specific and suitable for pharmacokinetic and bioequivalence study of Yufenweilin capsule containing pentoxyverine citrate.

The aim of this study was to explore potential herb–drug interaction between danshensu or ursolic acid and rosuvastatin. Compared to the control group given rosuvastatin alone, the concurrent use of danshensu (46 mg/kg) or ursolic acid (80 mg/kg) prior to the oral administration of rosuvastatin (100 mg/kg) increased the systemic exposure of rosuvastatin more than twofold. The plasma clearance of rosuvastatin was reduced to more than 57% in the presence of danshensu or ursolic acid. Rosuvastatin is minimally metabolized in the CYP2C9 isoenzyme pathway and to an even lesser extent in the CYP2C19 isoenzyme pathway. Rosuvastatin is a substrate of drug transporters such as human OATP1B1, OATP 1B3, OATP 1A2, BCRP and NTCP. Therefore, the present results suggested that the potential drug interaction between danshensu or ursolic acid and rosuvastatin may be mediated by one or more transporters (OATP1B1, OATP 1B3, OATP 1A2, BCRP and NTCP) and/or CYPs.

To investigate the occurrence of supernumerary upper incisor teeth in Pax6-/- mouse fetuses and to provide a model to explore the role of Pax6 in the upper incisor development and the mechanism of supernumerary teeth involving Pax6.Twenty Pax6-/- mouse fetuses of strain DEBA were isolated on E18.5 (embryonic day). The fetuses were sectioned serially in coronal plane and stained with haematoxylin and erosion, then the presence of supernumerary teeth in the upper anterior area was examined histologically, and also the number, morphology and structure of lower incisor germs and the first and second molar germs in the maxilla and mandible were observed histologically. Eighteen E18.5 mouse fetuses of strain DEBA with Pax6+/+ genotype were used as control.Of the 20 Pax6-/- fetuses examined, four possessed a single supernumerary tooth in the upper incisors' region. No supernumerary upper incisor teeth were observed in any of the 18 Pax6+/+ fetuses examined. In the regions of lower incisors and the first and second molars of the maxilla and mandible, no significant difference was observed between Pax6-/- and Pax6+/+ fetuses regarding the number, morphology and structure of tooth germs.The results suggest that Pax6 played an important role in the development of upper incisor teeth in mice.

Desulfurization of dibenzothiophene (DBT) by a combination of both chemical oxidation and solvent extraction was investigated. Me3NCH2C6H5Cl·2ZnCl2 ionic liquid was prepared from cheap starting materials and used as extractant for oxidative desulfurization of DBT in n-octane. DBT in oil phase was extracted into ionic liquid phase and then oxidized to its corresponding sulfone by H2O2 and equal volume of acetic acid. The desulfurization yield of DBT in n-octane was 94% at 30 min under the conditions of H2O2/DBT molar ratio at 6 and V (ionic liquid) : V (n-octane) = 1 : 5, which was remarkably higher than that by mere extraction with ionic liquid (28.9%). The Me3NCH2C6H5Cl·2ZnCl2 ionic liquid could be recycled six times without a significant decrease in activity. Kinetics of oxidative desulfurization of DBT by H2O2 and acetic acid was first-order with an apparent rate constant of 0.0842 min−1 and half-time of 8.23 min.