Rhodium(III)-Catalyzed C−H/N−H Functionalization with Hydrogen Evolution

A rhodium(III)-catalyzed C−H/N−H bond functionalization of benzimidates with α-chloroaldehydes to afford isoquinolin-3-ol derivatives is reported. No external oxidants are needed in this process, and interestingly, evolution of hydrogen gas is observed.     

金色梦想，一触即发——化学专业校外实践教学基地建设与思考

高等教育要适应世界潮流和时代变化,本科教育须进一步提高实践教学的比重,加强理论教学与实践教学相结合,完善协同育人机制。结合学科发展和企业发展需求,中山大学化学学院与金发科技股份有限公司(简称金发科技)共同建设大学生实践教学基地。本文以中山大学-金发科技本科实践教学基地为例,探讨大学生校外实践基地建设过程中遇到的问题以及实践基地的建设内容与成果体会。     

Regulation of shear stress on rolling behaviors of HL-60 cells on P-selectin

Circulating leukocytes in trafficking to the inflammatory sites, will be first tether to, and then roll on the vascular surface. This event is mediated through specific interaction of P-selectin and P-selectin glycoprotein ligand-1(PSGL-1), and regulated by hemodynamics. Poor data were reported in understanding P-selectin-mediated rolling. With the flow chamber technique, we herein observed HL-60 cell rolling on P-selectin with or without 3% Ficoll at various wall shear stresses from 0.05 to 0.4 dyn/cm2. The results demonstrated that force rather than transport regulated the rolling, similar to rolling on L- and E-selectin. The rolling was accelerated quickly by an increasing force below the optimal shear threshold of 0.15 dyn/cm2 first and then followed by a slowly decelerating phase starting at the optimum, showing a catch-slip transition and serving as a mechanism for the rolling. The catch-slip transition was completely reflected to the tether lifetime and other rolling parameters, such as the mean and fractional stop time. The narrow catch bond regime stabilized the rolling quickly, through steeply increasing fractional stop time to a plateau of about 0.85. Data presented here suggest that the low shear stress threshold serves as a mechanism for most cell rolling events through P-selectin.     

Preferential magnetic nanoparticle uptake by bone marrow derived macrophages sub-populations: effect of surface coating on polarization,toxicity, and in vivo MRI detection

For the first time, we report the successful application of inhouse synthesized CdS quantum dots (QDs) with particle sizes between 1 and 7 nm exhibiting excellent fungicidal activity based on the interactions with Saccharomyces cerevisiae and Candida utilis. The growth curves and the growth rates of both fungi were established in the presence of three varying concentrations of CdS QDs. It was observed that the CdS QDs were highly inhibitory even at the lowest concentration of 10 mg/L used in this study, while the untreated control cells followed a normal growth pattern in the cases of both Saccharomyces and Candida. MALDI-MS was applied to substantiate the observations obtained by direct cell count method. It was observed that the trend observed in the case of Saccharomyces and Candida was well-represented in the MALDI-MS spectra. This study proposes a mechanism for the first time based on MALDI-MS results, that the CdS QDs interact with the extracellular polymeric substances (EPS) and remove small molecules from EPS layer; on the other hand, it was observed that CdS QDs at all concentrations lead to enrichment of protein signals in MALDI-MS. We have substantiated these results by quantifying the EPS in the control and treated cells and also using TEM to further confirm the results.     

电子信息类卓越工程师培养模式探讨

根据国家培养卓越工程师的要求,探讨了电子信息类卓越工程师的培养标准与内容,提出了校企深度合作培养卓越工程师的模式.从低年级学生中选拔有学习激情、自学能力强、善于思考的优秀本科生组成卓越工程师班,在信息学科校企卓越工程师培养教学指导委员会指导下,制定拔尖人才培养方案,加强学生的实践和创新能力培养,采用"3+1"的校企培养模式并通过学科竞赛等手段,使学生在保证学科基础理论学习的同时,突出工程师实践能力的培养,充分发挥学生的主观能动性,培养学生创新能力和独立分析问题、解决问题的能力,从而达到学以致用并完成卓越工程师的基本训练.     

Synthesis and characterization of a tetranuclear copper(Ⅱ) complex with a chiral Schiff base ligand

The title complex l-[Cu^Ⅱ₄（Hvap）₂（vap）₂（MeOH）₂]（CIO₄）₂ 1 has been synthesized and characterized by EA. IR,TGA,solid-state CD spectra and X-ray single-crystal analyses（l-H₂vap’.a Schiff base ligand derived from the condensation of o-vanillin and l-2-amino-3-phenyl-l-propanol）.Complex 1 crystallizes in monoclinic system,chiral space group P2₁ with a =10.4257（18）.b = 21.695（4）,c = 15.721（3）A,β= 94.443（3）.V= 3545.1（11） ³,Z=2,Cu₄C₇₀H₇₈N₄O₂₂Cl₂.Mr= 1652.42,D_c= 1.548 g/cm³, F（000）= 1704 andμ（MoKα） = 1.338 mm^-1.The final R = 0.0682 and wR = 0.1420 for 6170 observed reflections with I > 2σ（I） and R = 0.1775 and wR = 0.1830 for all data.The structure of complex 1 contains a boat-shaped(Cu₄O₄} motif.The solid-state CD spectra confirm the chiral nature of complex 1.     

靶向抑制拓扑异构酶和端粒酶的钌配合物研究进展

金属配合物抗肿瘤研究,尤其是铂类药物,已取得了相对令人瞩目的成功,但同时也面临着包括耐药性和毒副作用等诸多问题。近年来钌配合物作为新的抗癌药物引起了人们的注意。在非铂系药物中,金钌配合物;拓扑异构酶;G-四链体;端粒酶属钌配合物是最有前途的抗癌药物之一,国际上普遍认为钌和钌的配合物属于低毒性,容易吸收并在体内很快排泄。本文将着重介绍钌配合物与DNA结合后进一步引发的细胞内核酶活性抑制研究,从新的角度来诠释钌配合物的抗肿瘤研究最新进展。     

化学基元组学与药物创新

化学基元组学（chemomics）是与化学信息学、生物信息学、合成化学等学科相关的交叉学科．生物系统从内源性小分子（天然砌块）出发,通过酶催化的化学反应序列制造天然产物．生物系统通过化学反应和天然砌块向目标天然产物“砌入”一组原子,这样的一组原子称为化学基元（chemoyl）．化学基元组（chemome）是生物组织中所含有的化学基元的全体．化学基元组学研究各种化学基元的结构、组装与演化的基本规律．在生存压力和繁衍需求的驱动下,生物系统已经进化出有效手段来合成天然产物以应付环境的变化,并产生了丰富多彩的生物和化学多样性．近年来,人们意识到药物创新的瓶颈之一是药物筛选资源的日益枯竭．化学基元组学可以解决这个瓶颈问题,它通过揭示生物系统制备化学多样性的规律,发展仿生合成方法制备类天然化合物库（quasi natural product libraries）以供药物筛选．本文综述了化学基元组学的主要研究内容及其在药物创新各领域中的潜在应用．