生物黏附辅料对葛根总黄酮类化合物在Caco-2细胞模型中转运的影响

目的:葛根总黄酮（PTF）可治疗心脑血管疾病，但膜通透性差，口服生物利用度低。一些辅料如卡波姆、壳聚糖和羟丙基甲基纤维素可以提高口服生物利用度。传统的体外评价技术，包括大鼠肠灌流和细胞模型，不能评价PTF整体的吸收机制。方法:本研究评价辅料的黏附性及对PTF在Caco-2细胞单层模型中转运的影响。采用cDNA微阵列测定PTF和PTF+辅料给药后的Caco-2细胞的基因表达变化，从基因水平揭示辅料对PTF整体吸收的影响机制。结果:体外黏附和Caco-2细胞转运实验表明，与单独PTF相比，加入辅料后对胃黏膜具有更高的黏附性，且在Caco-2细胞模型中的转运效率更高。PTF与辅料的相互作用显著改变了某些基因的表达，可能影响PTF的吸收效率。结论:不同的生物黏附聚合物能提高PTF的肠道吸收，可能与ATP结合盒(ABC)和溶质载体转运体(SLC)的表达基因有关。     

结核分枝杆菌检测技术研究进展

结核是由结核分枝杆菌引起的一种世界性疾病,为最受关注的公共卫生问题之一。虽然近年来结核病的发病率呈下降趋势,但其对人类健康造成的危害仍十分严峻。患者的及时上报是结核病防控的重要环节之一,报告率的上升有助于提高结核的治愈率以及卫生机构对结核患者的管理强度。快速、准确的诊断方法直接影响结核病的报告率,影响疾病传播和患者管理,是控制结核发病的基础。近年来,分子诊断技术发展迅速,为结核病的快速诊断提供了新的思路。分子诊断技术检测速度快,灵敏度、特异度、准确率高,绝大多数技术成本低廉,可同时对多个样本进行检测,实用性较强,具有较好的发展前景。本文对现阶段临床上实际应用的结核诊断技术与近年来出现的新型分子诊断技术进行简要概述。     

功能磁共振技术在推拿科学研究中的应用进展

功能磁共振成像（fMRI）技术出现于20世纪90年代，它集合了神经活动与高分辨率磁共振成像技术，为学者们研究人及动物的脑或脊髓提供了巨大的技术支持。同时，也已成为揭示针灸、推拿等中医疗法发挥全身调节作用、研究针灸推拿在疾病治疗方面的大脑中枢机制提供了重要研究手段。文章通过搜集检索近年来国内外发表与fMRI相关的推拿手法文献，分类整理运用fMRI技术开展的相关研究内容，进一步阐释推拿中枢作用机制的研究进展，就fMRI技术在推拿研究领域的应用作一综述。     

The Influence of In Vivo Metabolic Modifications on ADMET Properties of Green Tea Catechins–In Silico Analysis

The health effects of green tea are associated with catechins: (?)-epigallocatechin-3-O-gallate (EGCG), (?)-epigallocatechin, (?)-epicatechin-3-O-gallate, and (?)-epicatechin. An understanding of compound absorption, distribution, metabolism, excretion, and toxicity characteristics is essential for explaining its biological activities. Herein, absorption, distribution, metabolism, excretion, and toxicity properties of in vivo detected metabolites of green tea catechins (GTCs) have been analyzed in silico. The influence of metabolic transformations on absorption, distribution, metabolism, and excretion profiles of GTCs corresponds to the effects of size, charge, and lipophilicity, as already observed for other small molecules. Mutagenic, carcinogenic, or liver toxic effects were predicted only for a few metabolites. Similar to galloylated GTCs EGCG and (--)-epicatechin-3-O-gallate, the sulfo-conjugates were predicted to bind at the warfarin binding site. The low free plasma concentration of these derivatives may be consequential to their serum albumin binding. The activity cliff detected for methylated conjugates of EGCG indicates that GTCs' pro-oxidative activity in bound state comes primarily from free hydroxyl groups of the pyrogallol ring B.     

Radioiodination and bioevaluation of rolipram as a tracer for brain imaging: In silico study,molecular modeling and gamma scintigraphy

Brain imaging is considered one of the most fruitful applications of radioisotope scanning. Rolipram, a selective phospodiesterase‐4 inhibitor, has been labeled using [¹²⁵I] with chloramine‐T (Ch‐T) as an oxidizing agent. Factors, such as the amount of substrate, pH, the amount of oxidizing agent, temperature, and the reaction time, have been systematically studied to optimize the iodination process. In addition, bio‐distribution studies have indicated that the brain uptake of [¹²⁵I]iodorolipram is 7.6 ± 0.33 injected dose/g organ at 10 minutes post‐injection, which cleared from the brain with time until it reaches 1.30 ± 0.17% at 1 hour post‐injection. Therefore, iodorolipram could be considered as a potential, new selective radiotracer for brain imaging.     

化学消毒剂对污水处理系统中游离细菌表面zeta电位的影响

为了解化学消毒剂对污水处理系统中游离细菌表面电位的影响,以探讨化学消毒剂对污泥中细菌杀灭机理,采用细胞表面电位测定方法,对活性污泥中常见游离菌的表面zeta电位进行了检测。结果,甲醛、戊二醛和高锰酸钾可使活性污泥中葡萄球菌、螺旋菌、杆菌、双球菌、荚膜细球菌和微球菌等6种游离细菌表面zeta电位增加;过氧化氢则使此6种游离菌表面zeta电位先增加后降低。细菌表面zeta电位增大,反映此类消毒剂与细菌胞壁肽聚糖结构中肽链上亚氨基和自由氨基发生酰化作用,从而致死细菌。细菌表面zeta电位减小,反映细胞壁的磷壁酸和脂多糖成份中的脂质基被氧化成过氧链,因此破坏了细胞壁的致密结构,改变了菌体代谢致细菌死亡。结论,通过测定细菌表面zeta电位变化,可了解消毒剂对污泥中游离菌初步杀菌机理。     

Homoisoflavanones with estrogenic activity from the rhizomes of Polygonatum sibiricum

A new homoisoflavanone, (3R)-5-hydroxy-7-methoxyl-3-(2′-hydroxy-4′- methoxybenzyl)-chroman-4-one (1), together with six known analogs, were isolated from the rhizomes of Polygonatum sibiricum. Their structures were elucidated on the basis of extensive spectroscopic analysis. All compounds were tested for their estrogenic activity using the MCF-7 estrogenresponsive human breast cancer cell lines. At a dose of 0.1 μmol/L, compounds 1–7 exhibited significant proliferative effects on MCF-7 cells compared with E₂. The molecular docking study results indicated that the activity of compounds 3, 5, 6, and 7 may be the binding with ERR.     

人参皂苷Rg3立体异构体差异抑制糖尿病调控基因蛋白-PXR机制的分子动力学研究

目的：为进一步了解Rg3对映体的立体化学选择性,对PXR配体结合结构域（PXR ligand-binding domain,PXR-LBD）中20（R/S）-Rg3的结合模式进行建模。方法：使用计算对接,分子动力学（molecular dynamics,MD）和基本动力学分析（essential dynamics analysis,EDA）等技术手段进行建模。结果：PXR中20（S）-Rg3的MM / PB-SA估计结合能大于20（R）-Rg3。两种配合物的RMSFs表明,20（S）-Rg3结合的LBD的迁移率比20（R）型对映体的迁移率降低得多。EDA预测和两个复合物的叠加三维结构都表明20（S）-Rg3在PXR中的结合比20（R）-Rg3更可能与生物学结果一致。结论：以上结果表明,基于目前的模拟结果,PXR中20（S）-Rg3的结合模式比20（R）-Rg3更有可能与生物实验结果吻合。     

Drug‐induced immune haemolytic anaemias

It has been more than 50 years since the first reports of penicillin‐ and methyldopa‐induced haemolytic anaemias emerged. Since these initial observations in 1966, that high‐dose intravenous penicillin can result in a penicillin‐antibody‐dependent immune haemolytic anaemia and patients receiving α‐methyldopa developed haemolytic anaemia similar to warm autoimmune haemolytic anaemia, cases of patients having a drug‐induced haemolysis has expanded greatly to include a myriad of different drugs. Indeed, there are now well over 100 drugs that have been described as causing immune‐mediated haemolysis. The history of drug‐induced immune haemolytic anaemia's can be subdivided into two different chapters: (1) The penicillin and methyldopa chapter and (2) the cephalothins and cefotetan chapter. In this review, these two chapters in the history of drug‐induced immune haemolytic anaemias will be dissected, including the different mechanisms of haemolysis that have been proposed. These include so‐called hapten, immune‐complex, drug adsorption and autoimmune mechanisms. The biochemical and immunological mechanisms of drug‐induced immune haemolytic anaemias will be discussed as well as important considerations in the approach to the laboratory investigation of these conditions in the blood bank and reference laboratories. An approach to the use of drug metabolites as well as a hypothesis as to how ‘non‐specific’ drug adsorption occurs and how it can be prevented will be presented. The objective of this review will be to provide an up‐to‐date understanding of the types of drug‐induced immune haemolytic anaemias, their differentiation in the laboratory and the biochemistry and immunology underlying these conditions.