杯[6]芳烃-双金属卟啉仿P-450酶模型的研究Ⅳ.对异丙苯氧化的催化行为

研究了杯[6]芳烃-双金属卟啉在氧化异丙苯中的催化行为，结果表明杯[6]芳烃-双金属卟啉比之相应的金属卟啉具有更高的催化活性，并表现同样的选择性，生成苯乙酮和醇组份。此一结果同通常酞菁或其它如西弗碱大分子金属络合物催化下生成丙酮和酚不同。还考察了温度、轴向配体、催化剂用量及金属离子种类等对反应的影响，仔细地通过测定反应速度比较了反应的活性。     

Structure-Activity Relationship, Cytotoxicity and Mode of Action of 2-Ester-substituted 1,5-Benzothiazepines as Potent Antifungal Agents

Our studies examined the structural features responsible for the antifungal activity of 2-ethoxycarbonyl-1,5- benzothiazepine （7a）. Three series of 1,5-benzothiazepine derivatives were synthesized and screened for their antifungal activity. The results suggested that the ethoxycarbonyl group at the 2 position and the imine moiety on the seven-membered ring are essential for activity. The most potent of the synthesized analogues （7a, 7b） were further studied by evaluating their cytotoxicity and mode of action （for 7a）. The results showed that compounds 7a and 7b were relatively safe for BV2 cells, but compound 7a interfered with Cryptococcus neoformans cell wall integrity by increasing the chitinase activity. Therefore, compound 7a was considered safe as an antifungal agent for animal cells.     

β-环糊精聚轮烷的合成及其细胞摄取行为的研究

以聚丙二醇-双[3,4,5-三(炔丙氧基)苯甲酰胺]为轴,以小体积的2-叠氮乙醇为封端剂通过水相炔-叠氮点击化学反应(Cu AAC)生成的多个三氮唑进行封端,合成了新型的β-环糊精聚轮烷.利用核磁氢谱和旋转坐标系欧沃豪斯增益谱对所合成的β-环糊精聚轮烷进行了结构表征.进一步通过聚轮烷上的羟基,在聚轮烷上依次共价连接了水溶性聚合物聚乙二醇和荧光分子FITC,对聚轮烷进行了亲水化改性和荧光标记,研究了改性后的聚轮烷的细胞毒性和细胞摄取行为,结果表明,改性后的聚轮烷具有良好的细胞相容性,并可通过胞吞的方式被细胞摄取.     

急性髓细胞白血病基因筛选模型的贝叶斯分析

基因表达数据蕴含着大量的生物信息,在生物基因信息研究中,筛选表达水平发生显著变化的差异基因是认识疾病形成机理和辅助靶点药物研究的关键问题.根据急性髓细胞白血病(AML)的基因表达数据,构造基因均值差序列,建立贝叶斯分层混合模型,并为模型的参数赋予具有基因生物特征的先验信息.采用马尔可夫链蒙特卡洛(MCMC)算法对模型参数进行估计,并筛选出急性髓细胞白血病差异表达基因.在实际数据分析中,从美国生物信息中心(NCBI)的高通量基因表达数据库中获取急性髓细胞白血病基因数据集,从经过非特异滤波预处理的14688个急性髓细胞白血病基因中筛选出711个差异表达基因,差异表达基因数仅占急性髓细胞白血病基因总数的4.84%,这一结果与基因差异表达的生物学原理相吻合.     

一类具Rotenberg模型解的存在性

迁移方程是研究物质中的粒子运动所产生的微观效应综合所致的宏观迁移现象规律的一种模型,研究这类迁移方程对数学基础理论的发展有着非常重要的意义.在L_1空间中,运用线性算子理论,研究了种群细胞增生中具Rotenberg模型的迁移方程,采用所谓的豫解算子等法证明了种群细胞增生中具Rotenberg模型解的存在性.     

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.     

高交联大孔吸附剂对海洛因依赖者的临床应用试验

采用高交联大孔吸附剂充填制成了"一次性使用血液灌流器",并对海洛因依赖者进行血液灌流临床治疗实验,观察海洛因的清除率、血液生化各项指标及血液相容性,实验结果表明,该高交联大孔吸附剂充填制成的"一次性使用血液灌流器"具有安全、有效和实用等特点。     

谢晓亮院士研发出单细胞测序新技术

人类、草莓、蜜蜂、鸡和大鼠等许多生物体都已经进行过DNA测序。如果说测序个别物种具有挑战性,那么测序单个细胞的DNA无疑更难。为了获得足够的DNA进行测序,通常需要数以千计或甚至数以百万计的细胞。而找出哪种突变存在于哪种细胞     

一种安来霉素A与B分离方法

公开号:CN103232530A公开日:2013.08.07申请人:南京工业大学摘要本发明公开了一种安来霉素A与B的分离方法。主要包括菌丝体的珠磨破碎、超滤浓缩、大孔树脂柱的吸附洗脱、浓缩干燥等。本方法通过加入有机溶剂进行珠磨,将细胞破碎与萃取集成到一步完成,同时选择了合适的大孔