Using bio-orthogonally catalyzed lethality strategy to generate mitochondria-targeting anti-tumor metallodrugs in vitro and in vivo

Synthetic lethality was proposed nearly a century ago by geneticists and recently applied to develop precision anti-cancer therapies. To exploit the synthetic lethality concept in the design of chemical anti-cancer agents, we developed a bio-orthogonally catalyzed lethality (BCL) strategy to generate targeting anti-tumor metallodrugs both in vitro and in vivo. Metallodrug Ru-rhein was generated from two non-toxic species Ru-N₃ and rhein-alkyne via exclusive endogenous copper-catalyzed azide alkyne cycloaddition (CuAAC) reaction without the need of an external copper catalyst. The non-toxic species Ru-arene complex Ru-N₃ and rhein-alkyne were designed to perform this strategy, and the mitochondrial targeting product Ru-rhein was generated in high yield (>83%) and showed high anti-tumor efficacy in vitro. This BCL strategy achieved a remarkable tumor suppression effect on the tumor-bearing mice models. It is interesting that the combination of metal-arene complexes with rhein via CuAAC reaction could transform two non-toxic species into a targeting anti-cancer metallodrug both in vitro and in vivo, while the product Ru-rhein was non-toxic towards normal cells. This is the first example that exclusive endogenous copper was used to generate metal-based anti-cancer drugs for cancer treatment. The anti-cancer mechanism of Ru-rhein was studied and autophagy was induced by increased reactive oxygen species and mitochondrial damage. The generality of this BCL strategy was also studied and it could be extended to other metal complexes such as Os-arene and Ir-arene complexes. Compared with the traditional methods for cancer treatment, this work presented a new approach to generating targeting metallodrugs in vivo via the BCL strategy from non-toxic species in metal-based chemotherapy.     

积分第二中值定理的一种改进

著名的第二积分中值定理在《数学分析》中占有十分重要的位置,并作为很多学科计算的一个重要工具,因此它得到了多种改进和推广。本文采用了一种引入参数的办法,又得到了第二积分中值定理的一种改进形式。     

香菇中麦角甾醇生成维生素D_2的光化反应实验设计

蘑菇中的麦角甾固醇经紫外线照射后可产生维生素D2,能被人体吸收利用,是天然维生素D的重要来源之一。为了增进本科生对脂溶性维生素代谢的认识和理解,设计了从香菇中提取麦角甾醇,再经光化反应将麦角甾醇转化为维生素D2的生物化学教学实验。为简化实验步骤、方便教学,试验筛选出了样品预处理、光反应及热反应的最佳条件,确定了不经皂化处理,提取物先后用254、365 nm的紫外光照射1 h后,置于85℃水浴下处理15 min实验流程。经高效液相色谱分析,测得产物收率为4.5%。     

论等级顺序理论对形态阻遏的阐释力

英语中存在多种阻遏现象,形态阻遏是其中的一种,它包括词项对派生词和曲折词缀生成词的阻遏。等级顺序理论认为在英语中派生和曲折过程是按等级顺序进行的,其顺序与形态构词过程有关。试用等级顺序理论来揭示形态阻遏是如何产生的,指出等级顺序理论对形态阻遏有一定的阐释力,并对该理论不足之处提出的修正。     

置换法测金属原子量实验的微型化

对置换法测金属原子量实验进行了微型化研究,改进了实验装置,实现了药品的微量化．与常量制备的方法相比较,具有节约药品、省时、装置简便、操作安全快速等优点．     

磁约束核聚变环境中流道插件的热变形分析

对国际热核聚变实验堆的双冷锂铅包层进行流固共轭传热的三维数值模拟,计算两端不同约束下流道插件FCI结构的热变形和热应力分布,分析对流换热系数和热导率对FCI结构热变形和热应力的影响规律.结果表明,若钢壁与外界的对流换热系数增大,则FCI温度降低,导致热变形和热应力减小;高热导率的FCI材料将使得FCI沿厚度方向温度梯度减小,导致结构的热应力减小.     

Effect of 6-weeks WBVT on the behaviour of the lower limb muscle fibres during vertical jumping

The purpose of the current study was to examine the effect of 6 weeks of whole body vibration training (WBVT) on body composition, muscle activity of the gastrocnemius and vastus lateralis, gastrocnemius muscle architecture (static and dynamic) and ground reaction forces (performance jump) during the take-off phase of a countermovement jump in young healthy adult males. A total of 33 men (23.31 ± 5.62 years) were randomly assigned to a whole body vibration group (experimental group, EG_WBVT: n = 17; 22.11 ± 4.97 years) or a control group (CG: n = 16; 24.5 ± 6.27 years). The total duration of the intervention phase (WBVT) was 6 weeks with a frequency of 3 sessions per week. Statistically significant differences were observed (P ≤ 0.05) between pre- and post-test in the power peak (Δ 1.91 W · kg^?1; P = 0.001), take-off velocity (0.1 cm · s^?1; P = 0.002) and jump height (Δ 0.4 cm; P = 0.002) for EG_WBVT. There were no statistically significant differences in any of the body composition and muscle architecture variables. Moreover, no significant differences were found between EG_WBVT and CG nor changes in muscle activity during take-off phase of the gastrocnemius and vastus lateralis pre- versus post-training. This study suggests that a 6-week WBVT programme with increasing intensity improves jump performance but does not alter muscle activity nor muscle architecture in healthy young men.     

对优秀自由式滑雪空中技巧运动员反应时与背力的研究

研究目的：自由式滑雪空中技巧运动属技能类难美项群的一个典型项目,对反应速度和肌肉力量都有很高的要求。通过对我国优秀自由式滑雪空中技巧运动员的反应时和背力的测量,并与体育学院大学生的进行对比,了解运动员的身体形态和机能特点,为今后我国优秀自由式滑雪空中技巧运动员的训练和选材提供一些参考。研究方法：以中国自由式滑雪空中技巧国家队的运动员16人作为研究组,体育学院04级社体大学生25人作为对照组,测量两组研究对象反应时和背力指标。研究结果：与对照组相比,运动员的背力较好,有统计学意义（P〈0.05）,反应时无统计学意义,但有存在差异的趋势;健将级运动员的背力和反应时与一般运动员相比,并无明显差异。研究结论：我国国家队的运动员已经拥有较好的背力,说明运动员在训练中已经加强了背力的训练;但反应时不理想,在今后的训练中有必要对此方面注意。     

影响篮球裁判员预判能力的因素分析

篮球裁判员预判能力好坏,对比赛能否顺利进行具有重要的意义。利用文献资料法从运动生理学、心理学角度出发,分析影响篮球裁判员预判能力的因素。通过对诸多因素分析,提出一些相关的具体训练方法,旨在提高篮球裁判员执裁水平。     

文言课刺激学生思维之我见

文言诗文教学是中学语文教学的重点,可是多数学生对文言课不感兴趣,文言教学索然无味,那么怎样激发学生学习文言的热情,给文言教学增添活力呢？笔者认为文言课一定要不停地刺激学生的思维,刺激学生的思维可采取情感法、幽默法、形象法、质疑法、反弹法、故事法等。