鹿角短指软珊瑚Sinularia Cervicornis Tix-Dur 中的一个新糖甙-Cervicoside

珊瑚属腔肠动物门 ( Clelenterata) ,海鸡冠目 ( Alcyonacea) ,是一种热带与亚热带海洋中广泛分布Scheme 1　 Structure of cervicoside(1 )的低等海洋生物 .软珊瑚的次生代谢物中含有萜类和甾体类等各类生理活性物质[1～ 5] .我们在对鹿角短指软珊瑚的次生代谢产物研究中 ,分离到一个新三糖甙 ,命名为 Cervicoside( 1 ) ,结构见 Scheme 1 .该化合物具有较强的体外抗癌活性 .1　实验部分1 .1　样品　鹿角短指软珊瑚采自海南岛三亚海域 .样品储藏于中山大学化学与化学工程学院天然有机化学研究室 ,编号为 98- SY- 3.种属由中国科学院南海…     

具有植物激素活性的Schiff碱化合物的研究（Ⅱ）

合成了１１个新的含三氮唑环的Ｓｃｈｉｆｆ碱类化合物，ＵＶ、ＩＲ、ＨＮＭＲ谱和元素分析确定了它们的结构，生物活性测试表明，一些化合物具有明显的植物生长调节活性，其中化合物Ⅱｅ、Ⅰｂ、Ⅰｃ和Ⅰｃ具有良好的细胞分裂素活性，化合物Ⅱ、Ⅰ、Ⅰ、Ⅰ和Ⅰ具有优异的生根性能。     

Study of the interaction of Zn^2＋ with Aβ（10-21） by fluorescamine assay

Zinc may play a role as a co-factor in the pathogenesis of Alzheimer's disease(AD)through influencing the conformation and neurotoxicity of amyloidβ-protein(Aβ).Using the fluorescamine assay,we show for the first time that Zn~(2 )induced Aβ(10-21) aggregate in a concentration-dependent manner.These results indicate that Aβ(10-21)can be used as an in vitro model in Zn~(2 )- induced Aβaggregation and that the region 10-21 to be the minimal fragment of zinc-binding domain of full length Aβ(1-42).     

The Pharmacophore Hypothesis of Novel Inhibitors for Aurora A Kinase

A three-dimensional pharmacophore model was developed from a series of inhibitors of Aurora A kinase to discover new potent anti-cancer agents using the HypoGen module in the Catalyst software. The pharmacophore model was developed based on the structure of 20 currently available inhibitors, which were carefully selected from the literature. The best hypothesis （Hypo 1） was defined by four features： one hydrogen-bond donor and three hy- drophobic points, with the best correlation coefficient of 0.909, the lowest rms deviation of 1.563, and the highest cost difference of 99.075. The Hypo 1 was then validated by a test set consisting of 24 compounds and by a cross-validation of 95% confidence level through randomizing the data using the CatScramble program, which suggested that a predictive pharmacophore model had been successfully obtained.     

硅氧聚合度对细胞毒性的影响

本文采用家兔肺泡巨噬细胞(AM)存活率和细胞过氧化脂质(LPO)值为测定指标,研究了硅氧的聚合度对其细胞毒性的影响。结果表明:各种聚合度的硅氧都有一定的细胞毒性,聚合度愈大,细胞毒性也愈大。胶体SiO_2的粒径增大,其细胞毒性降低。十硅酸盐及粒径小于5nm的硅溶胶的细胞毒性大于α-石英。聚合度小于6的低聚硅酸及其盐、粒径18nm以上的硅溶胶以及硅胶H的毒性皆小于α-石英。本实验细胞存活率降低和过氧化脂质值升高的趋势基本一致,这表明硅氧可能主要与细胞表面膜作用,膜上磷脂等表面活性物质被氧化和变性,从而导致细胞损伤。     

Synthesis and Insulin—sensitizing Activity of a Series of 2—Benzyl—1,3—dicarbonyl Derivatives

A series of 2-benzyl-1,3-dicabonyl derivatives was synthesized.Their insulin-sensitizing activity was evaluated in 3T3-L1 preadipocyte cells.Compounds3,26 and 27 were found to possess strong insulin-sensitizing activity in vitro and were selected for further hypoglycemic evaluation in vivo.     

Zs－93硒剂对移植性小鼠S＿（180）肉瘤的抑制作用及其免疫活性

用硒与尿素化合，新生的由杂环有机硒所组成的Ｚｓ－９３硒剂治疗移植性Ｓ１８０肉瘤，有显著的抑瘤作用（Ｐ＜０．０１），其作用表现出一定的剂量效应，以５μｇ／只小鼠为最适，抑瘤率达６０．７６％，治疗组小鼠的Ｔ细胞、ＳＯＤ活性均有增强。     

Expression and Characterization of Catalytic Domain of T Cell Protein Tyrosine Phosphatase（△TC-PTP） —— Immunohistochemical Study of △TC-PTP Expression in Non-small Cell Lung Carcinomas

This study objective was to express and characterize the catalytic domain of the human T cell protein tyrosine phosphatase（△TC-PTP） and to study immunohistochemically the expression of △TC-PTP in human non-small cell lung cancers. △TC-PTP gene was PCR amplified with the cDNA of human TC-PTP as template, and cloned into the pT7 expression vector. The recombinant pT7-△TC-PTP was expressed in E. coli Rosetta （ DE3 ） host cells and puri- fied. The enzymatic characteristics of △TC-PTP including enzyme activity and kinetics assay were measured. The antiserum was prepared by immunizing rabbit with the purified recombinant △TC-PTP. Rabbit polyclonal antibody against △TC-PTP was purified by PVDF immobilized antigen affinity chromatography. Immunohistochemical staining of lung cancer tissues was performed with antibody against △TC-PTP protein. △TC-PTP gene was correctly cloned, expressed, and purified. The recombinant △TC-PTP had a highly catalytic activity of PTPase. Squamous cell lung carcinoma showed a significantly higher expression rate of △TC-PTP （76. 92%, 10/13 ） than adenocarcinoma （57.14%, 4/7） and normal lung tissue（20%, 1/5 ）. This study represents the first demonstration that △TC-PTP is highly expressed in human squamous cell lung carcinomas. In addition, this study provides an important basis for further studying the biological function of TC-PTP and its relationship with lung carcinomas and other diseases.     

PEO／PBHE共混体系X射线散射研究

在聚环氧乙烷(PEO)/聚双酚A羟基醚(PBHE)共混体系中PEO是一个强质子受体,而PBHE是一个强质子给体,两者极易形成氢键,十分有利于形成互容对。笔者研究了PEO/PBHE共混体系的相容性,等温及非等温结晶动力学,本文根据Vonk提出的一维电子密度相关函数,分析了PEO/PBHE的SAXS现象,求得了共混体系的结晶度,片晶层厚度,过渡层厚度及长周期等结构参数。     

A Novel Dihydroflavone from the Roots of Uvaria Macrophylla

A new dihydroflavone (1), named macrophyllol A, was isolated from the roots of Uvaria macrophylla. Its structure was elucidated on the basis of spectroscopic evidence.