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Development and validation of an LC-MS/MS method for tyrphostin A9

Journal of Pharmaceutical Analysis 2019年第3期9卷 163-169页

作者： Lyndsey F.meyer Dhaval K.Shah Department of Pharmaceutical Sciences School of Pharmacy and Pharmaceutical SciencesThe State University of New York at Buffalo

Here we have presented a sensitive and selective LC-MS/MS method for the quantification of tyrphostin A9, which is a selective inhibitor for platelet derived growth factor receptor tyrosine kinase and has been investigated in vitro as a potent oxidative phosphorylation uncoupler. The murine analytical method was developed for three biological matrices: cell culture media, 3T3-L1 cell lysate, and murine plasma. For each matrix the limit of detection and the limit of quantification were found to be 0.5 ng/ml and 1.0 ng/ ml, respectively. The range of standard curve for each matrix was 1.0-100 ng/ml, linearity was >0.99, and the precision and accuracy were within 20%. 3-(3,5-di-tert-butyl-4-hydroxyphenyl) propanoic acid was found to be the most suitable internal standard. The validated LC-MS/MS method was used to investigate stability and in vitro pharmacokinetics of tyrphostin A9. It was found that tyrphostin A9 is susceptible to hydrolysis, and the degradation product was identified as 3,5-di-tert-butyl-4- hydroxybenzaldehyde. Tyrphostin A9 was not stable in biological matrices, and the rate of its degradation in murine plasma was faster than that in cell culture media. In vitro pharmacokinetic studies revealed that tyrphostin A9 concentrations in the cell culture media declined in a bi-exponential manner and the concentrations inside the adipocytes remained constant, suggesting tyrphostin A9 has an intracellular binding site and is retained within the cell. The LC-MS/MS method presented here paves the way for further quantitative investigations involving tyrphostin A9.

关键词： Tyrphostin 9/ A9/AG-9/Malonoben/SF6847 LC-MS/MS Stability Pharmacokinetics Tyrosine kinase inhibitor

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Thermal and Mechanical Properties of Isotactic Polypropylene/TiO_2 Particulate Composites

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应用化学 2001年第5期18卷 275-279页

作者： CASCONE，E DILORENIO，ml 等 IstitutodiRicercaeTecnologiadelleMateriePlastiche（C.N.R.） VIaToiano680072ArcoFelice（NA）Italy

Particulate composites based on isotactic polypropylene(iPP) and titanium dioxide(TiO 2) have been prepared and their morphology and thermal behavior investigated by scanning electron microscopy(SEM), differential scanning calorimetry(DSC) and thermogravimetric analysis(TGA). Tensile tests were performed to assess the influence of TiO 2 on the mechanical properties of the iPP.

关键词：等规立构聚丙烯二氧化钛颗粒复合材料机械性质

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Comparison of Two Methods in Determining the Composition Distribution of SBS Copolymers

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Chinese Chemical Letters 1998年第2期9卷 173-175页

作者： Xu, J Shi, LH Ye, ml Wu, JS Liu, Q Chinese Acad Sci Inst Chem Polymer Phys Lab Beijing 100080 Peoples R China Yanshan Petrochem Corp Res Inst SINOPEC Beijing 102500 Peoples R China

The comparison of the determination of chemical composition distributions of butadiene-styrene copolymers, obtained by the formula method and experimental method of GPC, is given in this paper. The relative error of average composition was shown to be less than 5%. The formula method was found to be a more convenient and time-saving approach in the characterization of the copolymer composition distribution.

关键词： GPC chemical composition distribution butadiene-styrene copolymer

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Methods for the Efficient Energy Management in a Smart Mini Greenhouse

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Computers, Materials & Continua 2022年第2期70卷 3169-3187页

作者： Vasyl Teslyuk Ivan Tsmots Michal Gregus ml. Taras Teslyuk Iryna Kazymyra Department of Automated Control Systems Lviv Polytechnic National UniversityLviv79013Ukraine Faculty of Management Comenius University in BratislavaBratislava2582005Slovakia Department of Information Systems and Networks Lviv Polytechnic National UniversityLviv79013Ukraine

To solve the problem of energy efficiency of modern enterprise it is necessary to reduce energy *** of the possible ways is proposed in this research.A multi-level hierarchical system for energy efficiency management of the enterprise is designed,it is based on the modular principle providing rapid *** novelty of the work is the development of new and improvement of the existing methods and models,in particular:1)models for dynamic analysis of IT tools for data acquisition and processing(DAAP)in multilevel energy management systems,which are based on Petri nets;2)method of synthesis of DAAP tools in energy efficiency management information systems(EEMIS)of the enterprise which provides a reduction in hardware and time costs from 10%to 40%;3)method of conflict-free data exchange determining the minimum memory speed for the synthesis of realtime exchanges,it reduces the cost and energy consumption;4)method of calculating the signal of postsynaptic excitation of neural elements decreases the processing time of technological data two or more *** proposed methods,models and tools have been tested while implementing the EEMIS of the intelligent mini-greenhouse,as a result,energy efficiency has increased by 12%-25%(depending on season and peculiarities of growing plants).

关键词： Energy efficiency management information system(EEMIS) data acquisition and processing(DAAP) industry 4.0 Petri nets smart mini greenhouse

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Lattice Effects of Surface Cell:ml-MCTDH Study on Surface Scattering of CO/Cu（100）

Lattice Effects of Surface Cell:ML-MCTDH Study on Surface Sc...

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第十五届全国化学动力学会议

作者：孟庆勇 Hans-Dieter meyer Department of Applied Chemistry Northwestern Polytechnical University Theoretische Chemie Physikalisch-Chemisches InstitutRuprecht-Karls Universitat

To study the scattering of CO on a movable Cu（100） surface,multilayer multiconfiguration time-dependent Hartree（ml-MCTDH） calculations were performed based on the SAP potential energy surface（PES） in conjunction with a recently developed expansion model for including lattice *** surface potential was constructed by a sum of Morse potentials where the parameters were determined through comparing the MCTDH vibration energies with the experimental *** flux analysis of the ml-MCTDH propagated wave packets,we calculated the sticking probabilities for a series of models as shown in the following Figure *** these sticking probabilities,the 6 D +5 D/15 D calculations predict a slower decrease of sticking with increasing energy as compared to the sticking of the6 D + 0 D/3 D *** is because the translational energy of CO is more easily transfered to surface vibrations,when the vibrational dimensionality of the surface is enlarged.

关键词： ml-MCTDH Molecule-surface coupling Lattice motion CO/Cu(100)

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Osteoinductivity assay of the variability of repeated extractions of bone morphogenetic proteins from bovine bone at different times

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Chinese Journal of Traumatology 2004年第5期7卷 301-307页

作者：胡侦明 Sean AF Peel Cameron ml Clokie ClokieOrthobiologics Laboratory Department of Oral Maxillofacial Surgery Faculty of Dentistry University of Toronto Canada The Affiliated Second Hospital Kunming Medical College 1 Mayuan Kunming Yunnan 650101 China ClokieOrthobiologics Laboratory Department of Oral Maxillofacial Surgery Faculty of Dentistry University of Toronto Canada

Objective: To observe the activity of repeated extracts of bone matrix and the production of purified bone morphogenetic proteins (BMPs). Methods: BMPs were extracted 1- 4 times from fresh bovine cortical bone by the modified Urist’s method, with each collected precipitate separated and lyophilized as partially purified BMPs. Another fresh bovine bone was extracted three times and the precipitates were mixed and lyophilized. Meanwhile,the alkaline phosphatase (ALP) activity was measured by an in vitro assay employing cultured C2C12 mouse myoblast cells through the osteoinductivity of bovine BMPs extracted four times at days 1, 4, 7, and 14, and the correlation between BMPs quantities and costing during extraction processes was ***: The BMPs purified and the cost showed a positive correlation (r=(0.969)). To separate and lyophilize each collected precipitate as partially purified BMPs raised the cost, and mixed precipitates also cost much. ALP activities of the 1st and mixed extractions of BMPs were shown to be highly osteoinductive and keep a significantly high level (P<(0.05)-(0.01)) 4 days after culturing, compared with the 2nd, 3rd and 4th extractions, especially the control group. However, the more times the extraction was done, the less activity of BMPs was shown and more costing was. The x-ray and histological analysis also showed that the 1st extraction of BMPs induced more ossicles and new bone ***: The results indicated that BMPs enhanced the abilities of osteoinductivity in C2C12 culture in vitro. The first extraction of BMPs from bone is fitfull, the second extraction should be enough, while, the 3rd and 4th extractions are unnecessary for they cost more and waste more time, say nothing of mixed extractions.

关键词： Bone morphogenetic proteins Extraction

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The mutation induced by space conditions in Escherichia coli

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World Journal of Gastroenterology 1999年第5期5卷 445-447页

作者： Weng ml Li JG Gao F Zhang XY Wang PS Jiang XC Chinese Acad Sci Genet Inst Beijing 100101 Peoples R China

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Effect of exogenous fibrolytic enzymes on performance and blood profile in early and mid-lactation Holstein cows

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Animal Nutrition 2015年第3期1卷 229-238页

作者： Anja Peters Ulrich meyer Sven Danicke Institute of Animal Nutrition Friedrich-Loeffler-Institute(FLI)Federal Research Institute for Animal Health

The supplementation of exogenous fibrolytic enzymes(EFE) to dairy cows diets could be a strategy to improve fiber degradation in the rumen which is especially important for the early lactating cows characterized by a high milk energy output and an insufficient energy intake. The objective of this study was to examine the effects of a fibrolytic enzyme product(Roxazyme G2 Liquid, 3.8 and 3.9 ml/kg total mixed ration [TMR] DM) supplemented to a TMR on production performance and blood parameters of dairy cows during early(trial 1) and mid-lactation(trail 2). In addition, rumination activity was measured in trial 2. The nutrient digestibility of the experimental TMR was obtained by using wethers. In the digestibility trial, EFE was supplemented at a rate of 4.4 m L/kg Roxazyme G2 Liquid TMR-DM. The TMR contained 60% forage and 40% concentrate(DM basis). Twenty eight 50 ± 16 days in milk(DIM)and twenty six 136 ± 26 DIM Holstein cows were used in two 8-wk completely randomized trails,stratified by parity and milk yield level. One milliliter of the enzyme product contained primarily cellulase and xylanase activities(8,000 units endo-1,4-? glucanase, 18,000 units endo-1,3(4)-? glucanase and 26,000 units 1,4-? xylanase). No differences in digestibility of DM, OM, CP, NDF and ADF were observed(P >0.05) between the control and the EFE supplemented TMR. Addition of EFE to the TMR fed to early(trial 1) and mid-lactation cows(trial 2) did not affect daily dry matter intake(DMI), milk yield,4% fat-corrected milk, energy-corrected milk(ECM), concentration of milk fat, protein, fat-protein-quotients, somatic cell score, energy balance, and gross feed efficiency of early and mid-lactation cows(P >0.05). Mid-lactation cows(trial 2) fed with TMR enzyme showed a tendency of a slightly higher ECM yield(P = 0.09). The tested blood parameters were not affected by treatment in trials 1 and 2(P >0.05).Exogenous fibrolytic enzymes supplementation did not alter daily time spent ruminating in t

关键词： Fibrolytic enzymes Dairy cows Milk yield Feed efficiency

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Prospective validation of %p2PSA and the Prostate Health Index, in prostate cancer detection in initial prostate biopsies of Asian men, with total PSA 4-10 ng ml-1

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Asian Journal of Andrology 2017年第3期19卷 286-290页

作者： Lincoln GL Tan Yung Khan Tan Bee Choo Tai Karen ml Tan Vineet Gauhar Ho Yee Tiong Robert CW Hawkins Thomas P Thamboo Felicia SK Hong Edmund Chiong Department of Urology National University Hospital National University Health System Singapore Department of Urology Tan Tock Seng Hospital Singapore Saw Swee Hock School of Public Health National University of Singapore Singapore Department of Laboratory Medicine National University Hospital Singapore Department of Urology Alexandra Hospital Jurong Health Singapore Department of Laboratory Medicine Tan Teck Seng Hospital Singapore Department of Pathology National University Hospital Singapore.

Despite its widespread use for prostate cancer screening, low specificity makes PSA a suboptimal biomarker, especially in the diagnostic ＂gray zone＂ of 4-10 ng ml-1, False-positives lead to unnecessary biopsies with attendant morbidities. This is the first prospective validation study of %p2PSA and the Prostate Health Index （PHI） in Asian men presenting with a total PSA between 4.0 and 10 ng m1-1. We studied 157 Asian men between 50 and 75 years old, with normal per rectal prostate examinations, undergoing their first prostate biopsy, using a standardized biopsy protocol, for PSA levels of 4-10 ng ml-1, Thirty （19.1%） were found to have prostate cancer on biopsy. Statistically significant differences between patients with and without prostate cancer were found for total PSA, p2PSA, %p2PSA, and PHh The areas under the curve of the receiver operating characteristic curve for total PSA, %fPSA, %p2PSA, and PHI were 0.479, 0.420, 0.695, and 0.794, respectively. PHI predicts prostatic biopsies results best. At a sensitivity of 90%, the specificity （95% CI） of PHI was 58.3%, more than triple the specificity of total PSA at 17.3%, potentially avoiding 77 （49%） unnecessary biopsies. Similar to studies in mainly Caucasian populations, we have prospectively shown that %p2PSA and PHI greatly outperform total and free to total PSA ratio, in the detection of prostate cancer at first biopsy. Higher PHi levels also correspond to increasing the risk of detecting GS ≥7 cancers. We have validated the use of PHI to aid decision-making regarding prostate biopsies in Asian men with serum PSA between 4 and 10 ng *** its widespread use for prostate cancer screening, low specificity makes PSA a suboptimal biomarker, especially in the diagnostic ＂gray zone＂ of 4-10 ng m1-1, False-positives lead to unnecessary biopsies with attendant morbidities. This is the first prospective validation study of %p2PSA and the Prostate Health Index （PHI） in Asian men presenting with a total PSA betwe

关键词： biological markers prostate specific antigen prostatic neoplasms

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Adverse reactions of Amiodarone

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Journal of Geriatric Cardiology 2019年第7期16卷 552-566页

作者： Ruben ml Colunga Biancatelli Viviana Congedo Leonardo Calvosa Marco Ciacciarelli Alessandro Polidoro Luigi Iuliano UOC of Internal Medicine Sapienza University of Rome and ICOT HospitalLatinaItaly Vascular Biology&Mass Spectrometry Laboratory Department of Medico-Surgical Sciences and BiotechnologiesSapienza University of Rome and ICOT HospitalLatinaItaly

Adverse drug reaction is defined by the World Health Organization as any response to a drug that is noxious and unintended and occurs at a dose normally used in *** people are at elevated risk of adverse drug reactions—because of changes in pharmacodynamics,concurrent use of multiple medications and the related drug ***,adverse drug reactions are significantly underestimated in the elderly population that is also exposed to inappropriate *** is an antiarrhythmic drug used commonly for the treatment of atrial fibrillation and is increasingly prescribed in older *** amiodarone is an efficient drug for rhythm control,it’s a carrier of different adverse reactions,and pro and cons must be carefully evaluated before its use especially in older people.

关键词： Amiodarone Atrial fibrillation Drug-adverse reaction Drug toxicity

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