Me

Richter综合征
  • 文章类型: Journal Article
    这项研究的目的是确定回肠可消化能(IDE),我,和米饭,碎米,还有米糠.在孵化后,从第0天至第14天饲喂鸟类标准起始饮食,从第15天至第21天饲喂实验饮食。总共336只鸟按BW分组,并分配给7种饮食,每个饮食包括8个重复,每个重复6只鸟。饮食包括参考饮食(RD)和6种测试饮食(TD)。TD包含2级大米,碎米或米糠,以120或240克/千克(大米和碎米)或150或300克/千克(米糠)部分替代RD中的能源。向RD中添加大米或碎米线性增加(P<0.01)DM的回肠消化率,能源,以及DM的全道代谢性,能源,和TD中的N校正能量。TD中包含的米糠线性降低了测试日粮中的能量消化率和利用率(P<0.01)。水稻相关的回归,碎米相关,或米糠相关的IDE,我,或者MEn对大米的千卡摄入量,碎米,或米糠的摄入量如下:IDE=Y=2(6)3,185(73)×大米3,199(72)×碎米2,562(61)×米糠,r2=0.98;ME=Y=8(6)+3,103(72)×大米+3,190(71)×碎米+2,709(60)×米糠,r2=0.98;MEn=Y=4(5)+3,014(68)×大米+3,092(101)×碎米+2,624(57)×米糠,r2=0.98;根据回归方程,IDE,我,大米的MEn值(kcal/kgDM)分别为3,185、3,103和3,014,而对于碎米,分别为3199,3190,3092,米糠,数值分别为2,562,2,709和2,624.
    The objective of this study was to determine the ileal digestible energy (IDE), ME, and MEn of rice, broken rice, and rice bran. The birds were fed a standard starter diet from day 0 to 14 and experimental diets from day 15 to 21 after hatching. A total of 336 birds were grouped by BW and assigned to 7 diets, each diet comprised 8 replicates with 6 birds per replicate. The diets comprised a reference diet (RD) and 6 test diets (TD). The TD contained 2 levels of rice, broken rice or rice bran that partly replaced the energy sources in the RD at 120 or 240 g/kg (rice and broken rice) or 150 or 300 g/kg (rice bran). Addition of rice or broken rice to RD linearly increased (P < 0.01) ileal digestibility of DM, energy, as well as total tract metabolizability of DM, energy, and N-corrected energy in the TD. The inclusion of rice bran in the TD linearly decreased (P < 0.01) energy digestibility and utilization in the test diet. Regressions of rice-associated, broken rice-associated, or rice bran-associated IDE, ME, or MEn intake in kcal against rice, broken rice, or rice bran intake were as follows: IDE = Y = 2 (6) + 3,185 (73) × Rice + 3,199 (72) × Broken Rice + 2,562 (61) × Rice Bran, r2 = 0.98; ME = Y = 8 (6) + 3,103 (72) × Rice + 3,190 (71) × Broken Rice + 2,709 (60) × Rice Bran, r2 = 0.98; MEn = Y = 4 (5) + 3,014 (68) × Rice + 3,092 (101) × Broken Rice + 2,624 (57) × Rice Bran, r2 = 0.98; Based on the regression equations, the IDE, ME, MEn values (kcal/kg of DM) of rice were 3,185, 3,103 and 3,014, respectively, while for broken rice, the values were 3,199, 3,190, and 3,092 and for rice bran, the values were 2,562, 2,709, and 2,624, respectively.
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  • 文章类型: Journal Article
    A stable and sensitive method has been developed for use in food and livestock product safety for the detection of mycotoxins. This newly developed method allows for the determination of T-2 toxin, HT-2 toxin and diacetoxyscirpenol (DAS) in heart, liver, spleen, lung, kidney, Glandular stomach, muscular stomach, small intestine, muscle, bone and brain samples from broilers using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). The samples were initially extracted with ethyl acetate before being filtered through a 0.22μm nylon syringe filter and subjected to chromatographic separation on a reversed-phase C18 (50×2.1mm, 3μm) column. A mobile phase composed of 0.1% acetic acid and 10mM ammonium acetate in methanol and water was used in an assay of the levels of T-2 toxin, HT-2 toxin and DAS. For the analysis of the target compounds, the mass spectrometer was operated under positive electrospray ionization conditions in the selected reaction monitoring mode. The limit of detection was in the range of 0.02-0.05ng/g, whereas the limit of quantification was in the range of 0.08-0.15ng/g. The extraction recoveries of spiked samples from the high, intermediate and low levels ranged from 58.5% to 110.5%, and the relative standard deviation (RSD (%)) values were less than 17.0%. The results of inter- and intra-day precision (RSD (%)) were within 14.7%. The results revealed that the present method could be successfully applied to the analysis of T-2 toxin, HT-2 toxin and DAS in the real samples.
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  • 文章类型: Journal Article
    背景:血清素转运蛋白(SERT)的体内正电子发射断层扫描(PET)成像是药物开发和监测血清素能功能改变的脑部疾病的有价值的工具。我们已经开发了两步标记反应,用于制备高5-羟色胺亲和配体[(18)F]FPBM([(18)F]2-(2'-((二甲基氨基)甲基)-4'-(3-氟丙氧基)苯硫基)苯胺,1).
    方法:为了改进和自动化[(18)F]FPBM的放射性标记,1、中间、[(18)F]3-氟丙基甲苯磺酸酯,[(18)F]4,首先准备好了,然后与苯酚前体(4-(2-氨基苯硫基)-3-((二甲基氨基)甲基)苯酚反应,3)提供[(18)F]FPBM,1.要优化标签,该O-烷基化反应在不同温度下进行评价,使用不同的碱和不同量的前体3.在固相萃取(SPE)纯化后获得所需产物。
    结果:这种两步放射性标记反应成功地产生了所需的[(18)F]FPBM,1,具有优异的放射化学纯度(>95%,n=8)。放射化学产率在31%和39%之间(衰变校正,标签的总时间:70分钟,n=8)。SPE纯化不能完全去除[(18)F]FPBM最终剂量中的假载体,1.通过UV-HPLC测量主要假载体的浓度(前体3,O-羟丙基和O-烯丙氧基衍生物的476-676、68-95和50-71μg,分别为5和6)。为了研究这些假载体的SERT结合的潜在抑制作用,我们进行了体外竞争实验,通过放射自显影评估。已知数量的\'标准\'FPBM,1,在伪载波中,将5和6加入到HPLC纯化的[(18)F]1剂量中。“标准”FPBM的抑制,1,与SERT结合位点结合,用猴子的大脑切片,测量(EC50=13、46、7.1和8.3nM,分别为1,前体3,O-羟丙基和O-烯丙氧基衍生物3)。
    结论:通过SPE纯化制备[(18)F]FPBM的改进的放射性标记方法,1、开发。结果表明,使用该标记方法制备[(18)F]FPBM是可行的,1,不影响体内SERT结合。
    BACKGROUND: In vivo positron emission tomography (PET) imaging of the serotonin transporter (SERT) is a valuable tool in drug development and in monitoring brain diseases with altered serotonergic function. We have developed a two-step labeling reaction for the preparation of the high serotonin affinity ligand [(18)F]FPBM ([(18)F]2-(2\'-((dimethylamino)methyl)-4\'-(3-fluoropropoxy)phenylthio)benzenamine, 1).
    METHODS: To improve and automate the radiolabeling of [(18)F]FPBM, 1, an intermediate, [(18)F]3-fluoropropyltosylate, [(18)F]4, was prepared first, and then it was reacted with the phenol precursor (4-(2-aminophenylthio)-3-((dimethylamino)methyl)phenol, 3) to afford [(18)F]FPBM, 1. To optimize the labeling, this O-alkylation reaction was evaluated under different temperatures, using different bases and varying amounts of precursor 3. The desired product was obtained after a solid phase extraction (SPE) purification.
    RESULTS: This two-step radiolabeling reaction successfully produced the desired [(18)F]FPBM, 1, with an excellent radiochemical purity (>95%, n = 8). Radiochemical yields were between 31% and 39% (decay corrected, total time of labeling: 70 min, n = 8). The SPE purification cannot completely remove pseudo-carriers in the final dose of [(18)F]FPBM, 1. The concentrations of major pseudo-carriers were measured by UV-HPLC (476-676, 68-95 and 50-71 μg for precursor 3, O-hydroxypropyl and O-allyloxy derivatives, 5 and 6, respectively). To investigate the potential inhibition of SERT binding of these pseudo-carriers, we performed in vitro competition experiments evaluated by autoradiography. Known amounts of \'standard\' FPBM, 1, of the pseudo-carriers, 5 and 6, were added to the HPLC-purified [(18)F]1 dose. The inhibition of \'standard\' FPBM, 1, binding to the SERT binding sites, using monkey brain sections, were measured (EC50=13, 46, 7.1 and 8.3 nM, respectively for 1, precursor 3, O-hydroxypropyl and O-allyloxy derivative of 3).
    CONCLUSIONS: An improved radiolabeling method by a SPE purification for preparation of [(18)F]FPBM, 1, was developed. The results suggest that it is feasible to use this labeling method to prepare [(18)F]FPBM, 1, without affecting in vivo SERT binding.
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  • 文章类型: Journal Article
    A rapid, sensitive, and enantioselective method was developed and validated for determination of ornidazole enantiomers in human plasma by liquid chromatography-tandem mass spectrometry. Ornidazole enantiomers were extracted from 100μl of plasma using ethyl acetate. Baseline chiral separation (Rs=2.0) was obtained within 7.5min on a Chiral-AGP column (150mm×4.0mm, 5μm) using an isocratic mobile phase of 10mM ammonium acetate/acetic acid (100/0.01, v/v). Stable isotopically labeled R-(+)-d5-ornidazole and S-(-)-d5-ornidazole were synthesized as internal standards. Acquisition of mass spectrometric data was performed in multiple reaction monitoring mode via positive electrospray ionization, using the transitions of m/z 220→128 for ornidazole enantiomers, and m/z 225→128 for d5-ornidazole enantiomers. The method was linear in the concentration range of 0.030-10.0μg/ml for each enantiomer. The lower limit of quantification for each enantiomer was 0.030μg/ml. The relative standard deviation values of intra- and inter-day precision were 1.8-6.2% and 1.5-10.2% for R-(+)-ornidazole and S-(-)-ornidazole, respectively. The relative error values of accuracy ranged from -4.5% to 1.2% for R-(+)-ornidazole and from -5.4% to -0.8% for S-(-)-ornidazole. The validated method was successfully applied to a stereoselective pharmacokinetic study of ornidazole after oral administration of 1000mg racemic ornidazole.
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  • 文章类型: Journal Article
    Two series of novel C-9 chloro- and bromo-substituted mansonone E derivatives with triazole moieties at the C-3 position were prepared by using copper-catalysed azide-alkyne cycloaddition click chemistry. These compounds were found as potent inhibitors of topoisomerase II (Topo II) and topoisomerase I (Topo I). The Topo II-mediated pBR322 DNA relaxation and cleavage assay showed that the derivatives might act as catalytic inhibitors. Their cytotoxic activities against A549, HL-60, K562 and HeLa cells were evaluated, indicating that these compounds were potent antitumour agents. Their structure activity relationships and molecular docking study revealed that the substituents of the triazole were particularly important for cytotoxicity.
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  • 文章类型: Journal Article
    随着全球石油的枯竭及其价格的上涨,生物柴油已成为全球燃料市场最有前途的生物燃料之一。研究人员利用含油微生物生产生物柴油,因为它们的生命周期短,需要更少的劳动力,减少了对场地的感情,更容易扩大规模。许多含油微生物可以积累脂质,尤其是三酰基甘油(TAG),是生产生物柴油的主要原料。本文综述了不同产油微生物的相关研究,比如酵母,霉菌,细菌和微藻,这可能成为未来生物柴油生产的潜在石油原料,表明含油微生物生物柴油在生物质能源开发中具有广阔的前景。微生物油的生物合成过程包括脂肪酸合成方法和TAG合成方法。此外,通过代谢工程技术增加脂质积累的策略,涉及脂肪酸合成方法的增强,TAG合成方法的增强,相关TAG生物合成旁路方法的调节,阻断竞争途径和多基因方法,详细讨论。提示DGAT和ME是最有希望的基因转化靶标,观察到降低PEPC活性有利于脂质生产。
    With the depletion of global petroleum and its increasing price, biodiesel has been becoming one of the most promising biofuels for global fuels market. Researchers exploit oleaginous microorganisms for biodiesel production due to their short life cycle, less labor required, less affection by venue, and easier to scale up. Many oleaginous microorganisms can accumulate lipids, especially triacylglycerols (TAGs), which are the main materials for biodiesel production. This review is covering the related researches on different oleaginous microorganisms, such as yeast, mold, bacteria and microalgae, which might become the potential oil feedstocks for biodiesel production in the future, showing that biodiesel from oleaginous microorganisms has a great prospect in the development of biomass energy. Microbial oils biosynthesis process includes fatty acid synthesis approach and TAG synthesis approach. In addition, the strategies to increase lipids accumulation via metabolic engineering technology, involving the enhancement of fatty acid synthesis approach, the enhancement of TAG synthesis approach, the regulation of related TAG biosynthesis bypass approaches, the blocking of competing pathways and the multi-gene approach, are discussed in detail. It is suggested that DGAT and ME are the most promising targets for gene transformation, and reducing PEPC activity is observed to be beneficial for lipid production.
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