Preparation and Inhibitory Effects of 20（S）-Ginsenoside Rh2 on Hep-A-22 Cells

<正>A modified method of preparing 20(S)-ginsenoside Rh_2(G-Rh_2) and the inhibitory effect of 20(S)-ginse-noside Rh_2 on Hep-A-22 cells were investigated.The total saponins and strong alkali were dissolved in glycerol at the atmospheric pressure,and the degradation was performed at a high temperature.After G-Rh_2 had been isolated and purified,MTT(methyl thiazolyl tetrazolium) assay was applied to evaluating the effect of 20(S)-ginsenoside Rh_2 on the cells viability and morphological changes were observed.It was shown that 20(S)-ginsenoside Rh_2 can reduce Hep-A-22 cells viability in dose-dependent manner and the cells took on cell shrinkage,membrane blebbing,chromosomal condensations,especially under the higher concentrations of it.In conclusion,20(S)-ginsenoside Rh_2 can be prepared effectively that not only decreases viability but also induces the apoptosis of Hep-A-22 cells.     

Expression and Emmprin Regulated Function of Aquaporinl in SMMC7221 Cells

<正>Herein lie the crosstalk and regulation between AQP1 and Emmprin in SMMC7221 cells by means of siRNA technology and deglycosylation method.Firstly,HAQP1,rather than hAQP3,was selectively upregulated in SMMC7221 cells by FBS,flollowed by the upregulated expression of Emmprin.Emmprin gene silencing caused a remarkable change in the expression of AQP1 gene,just like its downstream gene,MMP9,meanwhile the water permeability and cell migration were also descended prominently.Furthermore,when treated with tunicamycin, Emmprin was deglycosylated,which made the expression of AQP1 significantly declined,followed by remarkably decreased cell membrane water permeability and cell migration.Taken together,all the data indicates the expression level and the modification of Emmprin by glycosylation are the key factors in regulating the expression of AQP1.     

白血病感染的预防

白血病是一种恶性疾病．由于白血病人体内成熟的粒细胞减少或缺少，且经化疗、肾上腺皮质激素的应用，机体免疫功能减退，极易合并感染，感染是急性白血病患者最常见的并发症和最重要的死亡原因之一．为此，防治感染是提高白血病的缓解率、延长病人生命的重要环节［１］．我科１９９９年全年共收白血病１０７例，发生感染１２８例（表１），其中４例病人因感染控制无效而死亡．感染部位广泛，其中以呼吸道和口腔易发，二者占６６．４％，因此，对感染的预防应从多方面进行．１加强入院宣教，使病人心理上重视感染 白血病人初期往往一时无法…     

17α-羟化酶/C17,20-裂解酶(P45017α)抑制剂17-(取代吡唑、异唑基)雄烯衍生物的合成

在17-(3-吡唑基)和17-(5-异唑基)雄甾-4,16-二烯-3-酮的吡唑基的5-位和异唑基的3-位引入取代基, 设计并合成了11个17-(取代的吡唑基、异唑基)雄烯衍生物, 化合物的结构经1H NMR, IR, 元素分析或质谱确证.     

Experimental Verification of Left-Handed Metamaterials Composed of Coplanar Electric and Magnetic Resonators

We verified experimentally left-handed metamaterials （LHM） composed of coplanar electric and magnetic resonators. A typical LHM sample composed of coplanar resonator unit cells was fabricated, investigated and tested. The experimental results show that the tested sample has a left-handed band of width 1.4 GHz in the X band. The experimental results agree quite well with the simulation ones. Moreover, both the simulation and experimental results show that the LHM under study can automatically achieve good impedance-matching in the left-handed band.     

含有五个反馈权值的二维细胞神经网络可实现Mosaic模式

研究一类含有五个反馈权值二维细胞神经网络系统,以系统的输出反馈权值及阈值为参数构成参数空间,引入几何方法,将此空间分解分块成有限个区域,当输出反馈权值及阈值在某一区域上时,给出系统具有M osaic解所有可能的输出函数M osaic模式的充要条件.     

雷公藤内酯醇和缬沙坦对高糖诱导小鼠足细胞活性的影响

目的观察不同浓度高糖对小鼠足细胞活性的抑制作用,以及不同浓度雷公藤内酯醇（TP）和缬沙坦（Val）对高糖抑制后小鼠足细胞活性的影响,探讨高糖对足细胞的损伤作用,以及有效的药物干预浓度范围。方法将培养成熟的小鼠足细胞随机分为对照组（11.1mmol/L葡萄糖）和不同浓度高糖组（16.1、21.1、26.1、31.1、36.1mmol/L）,以上述浓度培养48h后采用CCK-8检测足细胞活性的变化。取活性变化最大的浓度为高糖诱导浓度,在此基础上随机分为不同浓度的TP组（4、8、16、32、64ng/ml）和Val组（2×10-8、2×10-7、2×10-6、2×10-5、2×10-4mol/L）,以上述浓度干预48h后,采用CCK-8检测足细胞活性的变化。结果（1）与对照组相比,除16.1mmol/L高糖组外,其余各高糖组的足细胞活性显著减少,其中以26.1mmol/L葡萄糖组减少最为明显（P＜0.01）。（2）与26.1mmol/L葡萄糖组相比,TP组（除4ng/ml组外）和Val组（除2×10-8mol/L组外）足细胞活性部分恢复,其中以16ng/mlTP组和2×10-5mol/LVal组足细胞活性恢复最为明显（P＜0.01）。结论一定浓度范围的TP和Val可部分恢复受高糖抑制的小鼠足细胞活性。     

补阳还五汤联合依达拉奉对脑缺血再灌注损伤后神经细胞凋亡的影响

目的研究补阳还五汤联合依达拉奉对小鼠脑缺血再灌注损伤后神经细胞凋亡及Bcl-2、Bax和Caspase-3表达的影响。方法将50只小鼠随机分为假手术组、模型组、补阳还五汤组、依达拉奉组和两药联用组,每组10只,其中缺血再灌注后1d和7d各5只。首先制备小鼠大脑中动脉缺血模型,TUNEL法观察神经细胞凋亡指数（AI）,免疫组化法观察小鼠大脑皮质神经元Bcl、Bax-2和Caspase-3表达阳性细胞数。结果与模型组比较,补阳还五汤组、依达拉奉组、两药联用组小鼠脑神经细胞AI值均明显降低（P＜0.05）,Bcl-2/Bax比值明显升高（P＜0.05）,Caspase-3表达阳性细胞数明显减少（P＜0.05）,其中又以两药联用组更为明显（P＜0.05）。结论两药联用能降低脑缺血再灌注损伤后神经细胞的凋亡,降低促凋亡基因Caspase-3的表达,协同发挥脑保护作用。     

Design and Synthesis of Tri-substituted Chiral Pyrrolidin-2-one Derivatives as CCR4 Antagonists

A series of tri-substituted chiral pyrrolidin-2-one derivatives have been designed and synthesized as CC chemokine receptor 4 （CCR4） antagonists. The structure of CCR4 was built by homology modeling. Asymmetric synthesis was applied to synthesize the R,R configuration chiral pyrrolidin-2-one scaffold. The stereoisomeric con- figurations of the compounds were identified by 2D I H-~H COSY spectroscopy and 1D NOESY spectroscopy. This method was more economical and convenient than traditional X-ray single crystal diffraction. In addition, the inter- actions between these compounds and the N-terminal extracellular tail of CCR4 were studied using capillary zone electrophoresis. The CCR4 chemotaxis inhibition effect was tested in CCR4-transfected HEK293 cells. Several compounds showed potent activities as CCR4 antagonists. Among these compounds, lc is the most active one. Its apparent binding constant of CZE experiment result is （1.569±0.11）× 10s L·mol ^-1, and its percentage inhibition of the HEK293/CCR4 cells migration with the concentration of I gmol·L ^-1 in DMSO is 59%. And compound If has slightly higher affinity to N-terminal of CCR4 according to its apparent binding constant than lb because of the in- troduced ester linkage. Further studies on the mechanism of these compounds are in progress.     

微流控芯片－质谱联用技术在细胞代谢与药物代谢中的研究进展

细胞代谢与药物代谢是新药筛选和研发的关键环节,在推动人类大健康发展进程中具有重要意义。通常情况下,细胞代谢和药物筛选以传统细胞培养测定研究为主,多为静态培养条件,无法很好地模拟体内细胞动态微环境。微流控芯片－质谱联用是近年发展起来的一种新型高通量分析技术。微流控芯片模块可高度模拟细胞体内动态微环境,与质谱联用可实时在线检测样品物质,具有高效、快速、简便、样品和试剂消耗低等特点,广泛应用于细胞代谢和药物代谢分析,有利于加速药物筛选研发进程。该文重点综述了微流控芯片－质谱联用技术及其在细胞代谢和药物代谢方面的应用概况,并对目前存在的局限性进行了讨论和展望,以期为微流控芯片－质谱联用技术在新药研发与细胞分析领域的发展提供参考。