Pterocaryquinone, a Novel Naphthoquinone Derivative from Pterocarya tonkinesis

Pterocaryquinone,a novel 1,4-naphthoquinone derivative,was isolated from Pterocarya tonkinesis and itsstructure was elucidated by spectroscopic methods.Pterocaryquinone is a new dimeric 1,4-naphthoquinone deriva-tive having a pentacyclic skeleton with two five-membered carbon rings,which provided a novel structural skeletonfor 1,4-naphthoquinone derivatives and showed apoptosis-inducing activity toward mouse cancer tsFT210 cells.     

硒化壳聚糖诱导NB4细胞凋亡及周期阻断作用

为研究硒化壳聚糖对NB4细胞的凋亡及周期阻断作用,用流式细胞法观察了药物对细胞的诱导凋亡及周期阻断作用。结果表明,硒化壳聚糖作用NB4细胞24 h,可剂量依赖性地诱导细胞凋亡并使G0—G1期细胞增多。提示硒化壳聚糖可诱导细胞凋亡,并对NB4细胞周期有特异性阻断作用。     

二甲胺四环素在蛛网膜下腔出血中保护作用的研究

Objective To investigate the effect of minocycline on early brain injury (EBI) following subarachnoid hemorrhage(SAH) in rats. Methods SAH was induced by the filament perforation model in male Sprague Dawley rats. SD rats(n=77) were randomly assigned to sham (n=22), SAH+vehicle (n=28), and SAH+minocycline (n=27) groups. Minocycline (135mg/kg) or equal volume of vehicle was administered 1 h after SAH induction. Mortality, neurological scores, brain edema were evaluated 24 h after SAH. Cell apoptosis were examined by TUNEL staining, and the expression of caspase-3 and Bcl-2 was assayed by Western blot at the same time point. Results The mortality was 21.4% in SAH+vehicle group, 18.5% in the SAH+minocycline group, while no death was observed in sham-operated rats; there was no significant difference in mortality between SAH+vehicle and SAH+minocycline groups (P＞0.05), but the mortality in these two groups was much higher than that in shamgroup(P＜0.05). The water content of brain was significantly increased in the SAH+vehicle group (80.00±0.16)% compared with that in sham group [(79.13±0.08)%, P＜0.05]. Minocycline treatment markedly reduced brain water content (79.36±0.07)% compared with that in SAH+vehicle group (P＜0.05). Caspase-3 levels were markedly increased in SAH+vehicle group (1.53±0.24) compared with sham group (1.00±0.21). Minocycline treatment significantly reduced caspase-3 levels, compared to SAH+vehicle group (1.11±0.18, P＜0.05). A significant decrease in Bcl-2 expression was observed in SAH+vehicle group(0.65±0.03) compared with the sham group (1.00±0.12). The treatment of minocycline upregulated the expression of Bcl-2,compared to SAH+vehicle group (0.93±0.13, P＜0.05). TUNEL-positive cells were increased in the cortex of SAH+vehicle rats,compared to sham group [(31.50±3.70)%, P＜0.05]. Minocycline treatment significantly reduced the number of TUNEL positive cells, compared to SAH+vehicle group [(14.25±2.50)%, P＜0.05]. Conclusion Minocycline may reduce early brain injury after subarachnoid hemorrhage in rats by inhibiting cell apoptosis, which is associated with down-regulation of caspase-3 and up-regulation of Bcl-2.     

纳米Eu2O3和Eu3+对人肝细胞HL-7702生长的影响

稀土化合物的生物效应研究已引起人们的大量关注,但纳米稀土氧化物对细胞产生的生物效应报道较少.为了研究纳米稀土氧化物和稀土离子对正常细胞作用后的影响差异,采用MTT比色实验,形态观察和流式细胞术等方法探讨了纳米Eu2O3和Eu3+对体外培养的人肝细胞HL-7702生长的影响.结果发现,较低浓度的纳米Eu2O3对细胞生长没有明显影响,较高浓度(≥800μg·ml-1)的纳米Eu2O3作用肝细胞后,具有明显的毒性作用,出现了凋亡特征;而Eu3+在较低含量,即≤100 μmol·L-1时诱导肝细胞S期细胞比率上升,对肝细胞增殖有较弱的促进作用.     

咔咯铁(Ⅲ)配合物与DNA的作用及其抗肿瘤活性

本文合成了10-(4-吩噻嗪苯基)-5,15-二(五氟苯基)铁咔咯配合物(2-Fe)。 在H₂O₂存在下,配合物2-Fe能有效抑制人肺癌细胞(A549)增殖。 流式细胞术检测结果显示在H₂O₂和2-Fe共同作用下,A549细胞生长被阻滞在S期和G2期,且有63.76%发生细胞凋亡。 Hoechst-33342细胞核染色实验观察到A549细胞核呈典型的凋亡形态学变化,同时细胞线粒体膜电势发生明显下降。 2-Fe与小牛胸腺DNA(ct-DNA)以外部模式相结合,且能有效催化氧化断裂DNA,此过程中涉及的活性氧物种可能是单线态氧。     

4-(2-羟基-3-氯)苯基-2,2'':6'',2"-三联吡啶Cu(Ⅱ)配合物的合成、结构表征及抗肿瘤活性

以4-(2-羟基-3-氯)苯基-2,2′∶6′,2″-三联吡啶(HL)为配体,合成了一种新的铜(Ⅱ)配合物[Cu2(μ-L-κO,O)2Cl2](1),并通过红外光谱、电喷雾质谱、元素分析及单晶X射线衍射分析等方法对配合物1进行结构表征。配合物1为双核结构,中心铜(Ⅱ)离子为五配位扭曲四方锥几何构型,每个铜离子与1个Cl-以及来自配体(L-)的2个N原子和2个羟基O原子配位,2个铜(Ⅱ)离子通过羟基的桥联形成双核结构。MTT实验结果表明:配合物1对所选5种癌细胞株表现出不同的抑制活性,尤其是对MGC80-3细胞的抑制作用最明显,抑制率高达(84.30±1.28)%,其IC50值为(3.36±0.43)μmol·L-1。流式细胞术分析结果显示:配合物1能诱导MGC80-3细胞凋亡。在配合物1浓度为4.5μmol·L-1时,MGC80-3的凋亡百分数为41.4%。此外,配合物1将MGC80-3细胞阻滞于G1期,从而抑制肿瘤细胞的生长。     

近紫外光辅助4-硫脱氧胸苷抗癌作用的研究

4-硫脱氧胸苷（4-thiothymidine, STdR）作为硫代类核苷类似物的典型代表,其具有较强的亲脂特性和强的紫外长波长（315～400 nm,UVA）吸收。这些特性使得4-硫脱氧胸苷能够靶向进入肿瘤细胞并以核苷酸的形式嵌入DNA链中,在近紫外UVA的辅助下发生光化学反应,损伤肿瘤细胞DNA,诱导细胞走向凋亡途径,达到抗癌的目的。本文系统地介绍和评述了长波紫外光/含硫脱氧胸苷（UVA/thiothymidine）的抗癌疗法及原理,探讨4-硫脱氧胸苷与人血清蛋白间的相互作用,为这种新型光化学疗法在今后的癌症治疗中提供基础的理论依据。     

内质网应激对碳离子辐照宫颈癌HeLa 细胞的影响

利用不同剂量的碳离子辐照二硫苏糖醇(2.5 mmol/L) 预处理的HeLa 细胞,探讨了内质网应激反应对碳离子辐照宫颈癌HeLa 细胞的影响。实验发现:与单独辐照组相比,二硫苏糖醇联合碳离子辐照后细胞的存活率下降,而凋亡率增加;二硫苏糖醇联合碳离子辐照加重了碳离子辐照引起的细胞周期阻滞;且联合辐照组的自噬被明显激活。结果表明,持续的内质网应激可改变宫颈癌HeLa 细胞对碳离子辐照反应,且二硫苏糖醇可能通过影响HeLa 细胞的自噬性细胞死亡通路发挥作用。To investigate the effect of endoplasmic reticulum stress on HeLa cells to 12C6+ ion irradiation,HeLa cells were pretreated with 2.5 mmol/L dithiothreitol and irradiated by 12C6+ ions with different doses.The results showed that, compared with IR alone, dithiothreitol combined with carbon ion irradiation caused HeLa cell survival decreased, and the apoptosis increased. Moreover, dithiothreitol and carbon ion radiation combination treatment led to a significant increase of G2/M phase, and autophagy was activated obviously in combination treatment group. The results imply that continuous endoplasmic reticulum stress can change the response of HeLa cells to 12C6+ irradiation, and dithiothreitol may affect HeLa cells through the autophagy cell death pathway.     

利用拉曼光谱分析顺铂诱导的胃癌细胞凋亡

利用激光拉曼光谱对顺铂诱导的胃癌细胞凋亡进行分析,胃癌细胞SGC7901经10 μg·mL-1顺铂处理24, 48, 72 h后,一部分用于荧光染色,另一部分用扫描方式收集细胞的拉曼光谱。光谱结果依次经背景扣除、平滑、归一化、基线校正、峰拟合等方法预处理。荧光染色结果显示对照组细胞核染色均匀,而药物处理72 h后,核碎裂,呈致密浓染。拉曼光谱结果显示顺铂处理24, 48, 72 h后,与核酸及蛋白质相关的峰均有降低,其中783, 1 002, 1 343 cm-1峰72 h后依次降低为初始值的52%,64%,76%,表明顺铂能够诱导胃癌细胞凋亡,凋亡细胞内核酸和蛋白质含量降低。以上结果说明,拉曼光谱能提供生物细胞内物质变化的丰富信息,是实时检测细胞凋亡过程的有效手段。     

利用三通道实时荧光成像方法研究单个活细胞凋亡与胞浆pH值变化的关系

利用双波长分光器(Dual-View)和自制滤光片滑块,在基于像增强型电荷耦合器件(ICCD)的实时/快速荧光成像系统基础上,建立了一种基于单个ICCD的三通道实时荧光成像方法,同时发展了相应的图像校准处理方法用于消除光谱串扰的影响,并将该方法应用于单个活细胞的研究。利用Annexin V-FITC和SNARF-1两种荧光探针进行双标记,在单细胞水平上对亚硝基谷胱甘肽(GSNO)诱导小鼠胸腺细胞凋亡与其胞浆pH值变化的关系进行实时研究。结果揭示了GSNO诱导的细胞凋亡与细胞发生自发凋亡时胞浆pH值有不同的变化规律,为这种三通道实时荧光成像方法在生物医学领域的应用展示了广阔的前景。