主链型不饱和聚磷酸酯交联体系体外降解性能

研究了主链重复结构单元中含富马酸酯的不饱和聚磷酸酯（UPPE）与N-乙烯基吡咯烷酮（NVP）交联体系的体外降解过程,采用扫描电镜观察了降解一定时间后试样断面的形态结构．结果表明：交联体系试样是按照先表层、后中心。由外至内的规律进行降解,降解过程包括表层扩散溶出和基体降解两部分．在表层扩散溶出占主导阶段。交联试样中聚乙烯基吡咯烷酮（PVP）和NVP快速溶出,试样失重明显,试样吸水率、长度、直径也迅速增大;在基体降解占主导阶段,试样降解比较缓慢,试样失重、吸水率、长度和直径变化较小．     

The Biological Fate of Pharmaceutical Excipient β-Cyclodextrin: Pharmacokinetics,Tissue Distribution,Excretion, and Metabolism of β-Cyclodextrin in Rats

β-cyclodextrin has a unique annular hollow ultrastructure that allows encapsulation of various poorly water-soluble drugs in the resulting cavity, thereby increasing drug stability. As a bioactive molecule, the metabolism of β-cyclodextrin is mainly completed by the flora in the colon, which can interact with API. In this study, understanding the in vivo fate of β-cyclodextrin, a LC-MS/MS method was developed to facilitate simultaneous quantitative analysis of pharmaceutical excipient β-cyclodextrin and API dextromethorphan hydrobromide. The established method had been effectively used to study the pharmacokinetics, tissue distribution, excretion, and metabolism of β-cyclodextrin after oral administration in rats. Results showed that β-cyclodextrin was almost wholly removed from rat plasma within 36 h, and high concentrations of β-cyclodextrin distributed hastily to organs with increased blood flow velocities such as the spleen, liver, and kidney after administration. The excretion of intact β-cyclodextrin to urine and feces was lower than the administration dose. It can be speculated that β-cyclodextrin metabolized to maltodextrin, which was further metabolized, absorbed, and eventually discharged in the form of CO₂ and H₂O. Results proved that β-cyclodextrin, with relative low accumulation in the body, had good safety. The results will assist further study of the design and safety evaluation of adjuvant β-cyclodextrin and promote its clinical development.     

红鳍东方鲀中华拟德氏吸虫病的组织病理学观察

通过对感染了中华拟德氏吸虫的红鳍东方鲀的解剖取样,显微镜观察,用组织连续切片法对被感染的病鱼内脏器官组织进行病理学观察．发现该虫在养殖的红鳍东方纯循环系统中寄生,明确了虫体、虫卵在体内各器官组织中的分布情况以及主要器官组织的病变情况．探讨了该病的病理变化和虫体、虫卵在体内的发育过程以及该虫的传染途径．     

菠萝蜜嫩茎离体培养的研究

在成龄的菠萝蜜树茎干上取徒长的嫩茎为外植体,研究了菠萝蜜嫩茎离体培养的条件.结果表明:外植体芽萌发的最适培养基为MS 6-BA 2.0 mg.L-1 KT 1.0 mg.L-1 NAA 0.5mg.L-1;暗培养有助于芽的萌发;芽增殖的较适宜培养基为MS 6-BA 2.0 mg.L-1 KT 1.0mg.L-1 NAA 0.1 mg.L-1,连续培养7代后,其芽的平均增殖系数为4.3;本试验中增殖芽的诱导生根较难,还有待进一步地研究.     

促红细胞生成素B螺旋表面肽的代谢稳定性结构修饰：设计、合成及其提高的肾保护作用

肾脏缺血缺氧以及再灌注过程都将导致肾小管上皮细胞凋亡,使肾功能严重受损.肾脏的缺血再灌注损伤是移植肾功能延迟恢复的主要原因并能诱导急慢性排斥,影响肾存活率.近年来发现,衍生于促红细胞生成素（EPO）的B螺旋亚基亲水表面序列的肽链（HBSP）,对肾脏缺血再灌注损伤具有显著的保护作用,但其在体内极短的半衰期（约2min）极大地限制了它的临床应用.因此,本研究采用构象约束、全D-构型氨基酸替换和N-端封闭策略,设计了3种类型的EPOB螺旋表面肽衍生物,旨在提高其代谢稳定性环肽的设计采用了对氧化还原稳定的硫醚键和相对刚性的亚砜键两种环合方式.在多肽的合成上,采用微波辅助多肽自动合成和手工合成两种模式有机结合;优化了硫醚环合工艺,应用微波加热进行硫醚环肽的合成,大大提高了产率和效率;利用圆二色（CD）谱确定了亚砜环肽的相对构型.活性实验表明,相对于线性母肽HBSP,本文设计合成的代谢稳定衍生肽对大/小鼠肾脏缺血再灌注损伤均有显著提高的保护作用,且硫醚和R-构型亚砜环肽的肾脏保护活性强于S-构型亚砜环肽.而且,环化确实提高了功能肽的血浆稳定性.因此,本文合成的硫醚环肽一周一次注射剂量等效于线性肽HBSP一日三次剂量对小鼠肾损伤的保护作用.     

NUMERICAL SIMULATION OF FIBROBLAST DUROTAXIS MIGRATION INDUCED BY STIFFNESS GRADIENT OF SUBSTRATE1)

建立了一种细胞趋硬性迁移的理论模型和有限元分析框架,为连续变刚度人工基质的试验设计提供理论依据。考虑了细胞体的黏弹性属性,以及细胞与基质间的配受体动态反应过程,并以配受体合成时间为时间步长,将细胞运动方程化为静力学形式进行求解。对有限元过程提出一种动约束,便于消除其结构矩阵的奇异性。结果表明,模型能够模拟黏着斑内部力的快速波动现象,细胞的运动速度与观测数据一致,可有效模拟20,h以上的长时程问题。     

Pharmacokinetics and tissue distribution study of clevidipine and its primary metabolite H152/81 in rats

This present study was designed to investigate the pharmacokinetic profiles and tissue distribution characteristics of clevidipine and its primary metabolite H152/81 in rats following a single intravenous administration of clevidipine butyrate injectable emulsion. For this study, a sensitive and selective liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was established and validated for the simultaneous quantitation of clevidipine and H152/81 in rat whole blood and various tissues. A Hedera ODS‐2 column with two gradient elution programs was employed for the troubleshooting of matrix effect on the detection of analytes among different biological samples. The experimental data showed that clevidipine represented quick elimination from blood with a half‐life of about 4.3 min and rapid distribution in all of the investigated tissues after administration; the highest concentration of clevidipine was found in the heart whereas the lowest concentration was detected in the liver. In addition, clevidipine was almost undetectable in most tissues except for heart and brain at 90 min post‐dosing, suggesting that there was no apparent long‐term accumulation in rat tissues. For H152/81, the peak concentration of 3714 ± 319 ng/mL occurred at 0.129 ± 0.048 h, the half‐life was 10.08 ± 1.45 h and area under the concentration–time curve was 42091 ± 3812 ng h/mL after drug administration. In addition, H152/81 was found at significant concentration levels in all tissues, in descending order of lung, kidney, heart, liver, spleen and brain at each time point. The results of current study offer useful clues for better understanding the distribution and metabolism of clevidipine butyrate injectable emulsion in vivo.     

高强度复合式训练对健美操选手体脂及组织损伤的影响研究

目的:探讨高强度训练(HIT)与高负荷训练(HVT),对健美操运动员组织损伤的影响.方法:针对健美操选手进行为期12周高强度复合式训练,并于运动前、训练中、训练后对受试者血清肌肉损伤的生化指标、体脂率等进行监测.结果:(1)高强度复合式训练能显著降低受试者体质量、体脂、甘油三酯、总胆固醇及尿素氮浓度;(2)提升血液葡萄糖、乳酸、肌酸酐浓度,增强天门冬胺酸转胺酶及肌酸激酶活性;(3)血液中的肌肉损伤指标值的提升与体脂下降率呈负相关,这暗示高强度复合式训练有利于肌肉再生,从而促使脂肪组织下降.结论:12周高强度复合式训练使健美操选手体脂明显减少、血液中肌肉损伤指标值提升,表明该训练方式可以促使肌肉再生,吸引全身含碳资源重新分配,使脂肪组织下降、肌肉组织增加,强度越高,碳资源重新分配效果越好.     

Variations in T(2)* and fat content of murine brown and white adipose tissues by chemical-shift MRI

Purpose

The purpose was to compare T₂* relaxation times and proton density fat-fraction (PDFF) values between brown (BAT) and white (WAT) adipose tissue in lean and ob/ob mice.

Materials and Methods

A group of lean male mice (n=6) and two groups of ob/ob male mice placed on similar 4-week (n=6) and 8-week (n=8) ad libitum diets were utilized. The animals were imaged at 3 T using a T₂*-corrected chemical-shift-based water–fat magnetic resonance imaging (MRI) method that provides simultaneous estimation of T₂* and PDFF on a voxel-wise basis. Regions of interest were drawn within the interscapular BAT and gonadal WAT depots on co-registered T₂* and PDFF maps. Measurements were assessed using analysis of variance, Bonferroni-adjusted t test for multigroup comparisons and the Tukey post hoc test.

Results

Significant differences (P<.01) in BAT T₂* and PDFF were observed between the lean and ob/ob groups. The ob/ob animals exhibited longer BAT T₂* and greater PDFF than lean animals. However, only BAT PDFF was significantly different (P<.01) between the two ob/ob groups. When comparing BAT to WAT within each group, T₂* and PDFF values were consistently lower in BAT than WAT (P<.01). The difference was most prominent in the lean animals. In both ob/ob groups, BAT exhibited very WAT-like appearances and properties on the MRI images.

Conclusion

T₂* and PDFF are lower in BAT than WAT. This is likely due to variations in tissue composition. The values were consistently lower in lean mice than in ob/ob mice, suggestive of the former's greater demand for BAT thermogenesis and reflective of leptin hormone deficiencies and diminished BAT metabolic activity in the latter.     

A review on electrospun nanofibers for multiple biomedical applications

Electrospinning is a well-known technique since 1544 to fabricate nanofibers using different materials like polymers, metals oxides, proteins, and many more. In recent years, electrospinning has become the most popular technique for manufacturing nanofibers due to its ease of use and economic viability. Nanofibers have remarkable properties like high surface-to-volume ratio, variable pore size distribution (10–100 nm), high porosity, low density, and are suitable for surface functionalization. Therefore, electrospun nanofibers have been utilized for numerous applications in the pharmaceutical and biomedical field like tissue engineering, scaffolds, grafts, drug delivery, and so on. In this review article, we will be focusing on the versatility, current scenario, and future endeavors of electrospun nanofibers for various biomedical applications. This review discusses the properties of nanofibers, the background of the electrospinning technique, and its emergence in chronological order. It also covers the various types of electrospinning methods and their mechanism, further elaborating the factors affecting the properties of nanofibers, and applications in tissue engineering, drug delivery, nanofibers as biosensor, skin cancer treatment, and magnetic nanofibers.