Metabolism studies on prim‐O‐glucosylcimifugin and cimifugin in human liver microsomes by ultra‐performance liquid chromatography quadrupole time‐of‐flight mass spectrometry

Prim‐O‐glucosylcimifugin (PGCN) and cimifugin (CN) are major constituents of Radix Saposhnikoviae that have antipyretic, analgesic and anti‐inflammatory pharmacological activities. However, there were few reports with respect to the metabolism of PGCN and CN in vitro. In this paper, we describe a strategy using ultra‐performance liquid chromatography quadrupole time‐of‐flight mass spectrometry (UPLC‐Q‐TOF‐MS) for fast analysis of the metabolic profile of PGCN and CN in human liver microsomes. In total, five phase I metabolites of PGCN, seven phase I metabolites and two phase II metabolites of CN were identified in the incubation of human liver microsomes. The results revealed that the main phase I metabolic pathways of PGCN were hydroxylation and hydrolysis reactions. The phase I metabolic pathways of CN were found to be hydroxylation, demethylation and dehydrogenation. Meanwhile, the results indicated that O‐glucuronidation was the major metabolic pathway of CN in phase II metabolism. The specific UDP‐glucuronosyltransferase (UGT) enzymes responsible for CN glucuronidation metabolites were identified using recombinant UGT enzymes. The results indicated that UGT1A1, UGT1A9, UGT2B4 and UGT2B7 might play major roles in the glucuronidation of CN. Overall, this study may be useful for the investigation of metabolic mechanism of PGCN and CN, and it can provide reference and evidence for further pharmacodynamic experiments. Copyright © 2016 John Wiley & Sons, Ltd.     

Tungsten doped mesoporous SBA‐16 as novel heterogeneous catalysts for oxidation of cyclopentene to glutaric acid

Novel heterogeneous tungsten species in mesoporous silica SBA‐16 catalysts based on ship‐in‐a‐bottle methodology are originally reported for oxidizing cyclopentene (CPE) to glutaric acid (GAC) using hydrogen peroxide (H₂O₂). For all W‐SBA‐16 catalysts, isolated tungsten species and octahedrally coordinated tungsten oxide species are observed while WO₃ crystallites are detected for the W‐SBA‐16 catalysts with Si/ W = 5, 10, and 20. The specific surface areas and the corresponding total pore volumes decrease significantly as increasing amounts of tungsten incorporated into the pores of SBA‐16. Using tungsten‐substituted mesoporous SBA‐16 heterogeneous catalysts, high yield of GAC (55%) is achieved with low tungsten loading (for Si/W = 30, ~13 wt%) for oxidation of CPE. The W‐SBA‐16 catalysts with Si/W = 30 can be reused five times without dramatic deactivation. In fact, low catalytic activity provided by bulk WO₃ implies that the highly distributed tungsten species in SBA‐16 and the steric confinement effect of SBA‐16 are key elements for the outstanding catalytic performance.     

Studies on pharmacokinetics,body distribution,plasma protein binding rate,and excretion of 1-methyl hydantoin in rats in vivo

In this paper, plasma concentration, plasma protein binding rate, body distribution, and excretion of both oral and intravenous administration of rats were determined by high performance liquid chromatography (HPLC) combining with UV detector. The blood drug concentration of oral and intravenous administration was summarized. The bioavailability of T_1/2 was approximately 0.75?hr. At the meanwhile, the bioavailability was about 18.84?±?2.21%. The plasma protein binding rate of 1-methyl hydantoin was about 24.36?±?0.93%, belonging to low protein binding drug. The result shows that 1-methyl hydantoin can be rapidly distributed in various organs and tissues and quickly eliminated within 6?hr without accumulation in the organs. Its discharge from the urine and feces was 16.58?±?4.48% and 3.37?±?0.71%, respectively. All of the results showed that the recovery rate, liner relationship, specificity, stability, and precision of the method were good. The study also proved that 1-methyl hydantoin has been eliminated quite faster in rats.     

面向客户群的服务方案配置规则挖掘方法

产品/服务配置规则获取的主要方式是用数据挖掘技术从设计实例数据库中提取.客户化服务方案配置规则为服务功能需求和方案特征间的关联规则.考虑到常用关联规则挖掘算法Apriori具有运算复杂的缺点,提出基于PIETM(Principle of Inclusion—Exclusion and Transaction Mapping)算法的配置规则挖掘方法,考虑置信度和有趣度指标,提取强关联规则.针对配置实例数据库数据量较大时,配置规则挖掘的效率会降低且会产生大量冗余规则的问题,采用二元语义模型表达定性的服务功能需求,将同类客户群的功能需求进行合并,替换多样化的功能需求,减少规则的冗余.最后以一工程机械制造企业服务方案配置规则挖掘为例,验证了所提方法的有效性.     

A Novel Fission Process in Mini-emulsion RAFT Polymerization: Shell Crosslinked Nanoparticles as a Model

Shell crosslinked nanoparticles, prepared from copolymerization of styrene and disulfide crosslinker, using poly(2-(dimethylamino)ethyl methacrylate) (PDMAEMA) as stabilizer and macroinitiator, exhibited a special fission behavior during the mini-emulsion RAFT polymerization process.     

Thermal Properties of Copoly(L‐lactic acid/glycolic acid) by Direct Melt Polycondensation

Poly(L‐lactic acid‐co‐glycolic acid) (PLGA) was prepared from hydroxy‐acids with melt polymerization. In this way, the copoly(L‐LA/GA) (PLGA) was synthesized directly using a binary catalyst (tin chloride dihydrate/p‐toluenesulfonic acid). The thermal properties of PLGA were studied by differential scanning calorimetry (DSC) and nuclear magnetic resonance (NMR). The results show that the melting point of PLGA decreases with increasing mole fraction of GA units in the copolymer. In addition, the melting point of polymer also decreases with increasing degree of racemization of the polymer.