螺环季酮酸的羧酸酯衍生物的合成及其杀螨活性

采用类同合成、活性亚结构拼接方法,对螺环季酮酸类杀虫杀螨剂Spirodiclofen进行设计修饰,合成了18种螺环季酮酸羧酸酯的新衍生物,结构经1H NMR、IR和元素分析确证,并用X射线单晶衍射测定了化合物6d的晶体结构。 通过其生物活性测试,探讨了其构效关系。     

CdTe QDs-based prostate-specific antigen probe for human prostate cancer cell imaging

l-glutathione (GSH) stabilized CdTe quantum dots (QDs) were directly prepared in aqueous solution. The as-prepared QDs were linked to prostate-specific antigen (PSA) for the direct labeling and linked to immunoglobulin G (IgG) for the indirect labeling of fixed prostate cancer cells. The results indicated that QD-based probes were ideal fluorescent markers with excellent spectral properties and photostability and much better than organic dyes making them very suitable in target detection. Meanwhile, the indirect labeling showed much better specificity than the direct labeling. Furthermore, the prepared CdTe QDs did not show detectable effect on cell growth after having cultured for three days, which suggested that the l-glutathione capped CdTe had scarcely cytotoxicity.     

量子点的荧光共振能量转移在生物分析中的应用

量子点良好的光谱特性和自身优点,使其可以作为生物荧光探针,而替代传统荧光染料。近年来这方面的研究已经取得了一定的进展。目前,量子点在共振能量转移方面的研究,进一步扩展了它在生物分析中的应用。介绍了量子点基于共振能量转移原理在生物分析中的应用,即利用量子点设计的两种类的蛋白-蛋白特异性结合分析和3种生物传感器的模型设计。     

纳米金生物探针及其应用

纳米技术与生物技术的融合,使纳米生物技术获得了很多重要的进展.纳米金作为研究较早的一种纳米材料,其在纳米生物探针方面的应用是最近几年较为活跃的研究方向.本文评述了近年来纳米金探针在生物分析中的应用及进展,阐述了纳米金与生物大分子作用的机理,介绍了纳米金探针在核酸分析、免疫分析、单细胞分析和靶向药物载体4个方面应用的最新进展,并对其未来的发展方向进行了展望.     

Tumor microenvironment-oriented adaptive nanodrugs based on peptide self-assembly

The aberrant metabolism of tumor cells creates an inimitable microenvironment featuring acidic pH, high glutathione (GSH) levels, and overexpression of certain enzymes, which benefits the overwhelming progress of a tumor. Peptide self-assembly, emerging as a biofriendly and versatile fabrication strategy, harnesses multiple noncovalent interactions to obtain a variety of nanostructures tailored on demand. Orchestrating the reversible nature of noncovalent interactions and abnormal physiological parameters in the tumor microenvironment enables peptide-based nanodrugs to be targetable or switchable, thereby improving the drugs’ bioavailability and optimizing the treatment outcome. This review will focus on peptide-modulated self-assembly of photosensitizers, chemotherapeutic drugs, immunoactive agents for tumor microenvironment-oriented adaptive phototherapy, chemotherapy, immunotherapy and combinatorial therapy. We will emphasize the building block design, the intermolecular interaction principle, adaptive structural transformation in the tumor microenvironment and corresponding therapeutic efficacy, and aim to elucidate the critical role of peptide-modulated, tumor microenvironment-oriented adaptive assemblies in improving the therapeutic index. Challenges and opportunities will be covered as well to advance the development and clinical application of tumor therapies based on peptide self-assembly materials and techniques.

The tumor microenvironment is of significance to promote release or reorganization of peptide-modulated nanodrugs, optimizing drug bioavailability and therapeutic outcome.     

取代喹喔啉-1,4-二氧化物合成方法的改进

苯并呋咱-1-氧化物(1)分别与1,3-二酮、β-酮酯(2a～c)在氢氧化钾(钠)的醇溶液中反应,合成了取代喹喔啉-1,4-二氧化物(3a～c),产率较高。将本方法与在有机胺中合成这些化合物的Beirut反应作了比较,并且讨论了溶剂和反应温度对产物的影响。     

Synthesis and biological evaluation of novel isopropanolamine derivatives as non-peptide human immunodeficiency virus protease inhibitors

Novel potential human immunodeficiency virus (HIV) protease inhibitors were designed by a combination of nelfinavir and amprenavir motifs. The designed compounds were prepared by a facile synthetic route and their stereochemistry was further confirmed by a stereospecific synthesis from commercially available (S)-2-oxiranylmethyl m-nitrobenzenesulfonate. All compounds were tested for their ability in inhibiting HIV type 1 protease activity with the published method of reference 19. Derivatives 1a--u exhibited moderate to significant inhibitory activities in preliminary bioassay. The best compound 1a has IC50 value of 0.02 microM, comparable to that of amprenavir. A docking study on compounds 1a--u was performed using the published X-ray crystal structure of HIV type 1 protease, all compounds bound to the HIV type 1 protease in an extended conformation and the scaffoldings of the binding conformations could be aligned quite well. Comparative molecular field analysis (CoMFA) study was performed to explore the specific contributions of electrostatic and steric effects in the binding of these new compounds to HIV type 1 protease and a predictive CoMFA model was built with thirteen compounds as training set. Test analysis of other five compounds as test set demonstrated that the CoMFA model has strong predictive ability to this series of compounds. It will be very useful to further optimize the designed inhibitors.     

Synthesis and electrochemical characterization of β-tetra-(2-isopropyl-5-methylphenoxylphthalocyaninato)titanium(IV) Oxide

A β-4-(2-isopropyl-5-methylphenoxylphthalocyaninato)titanium(IV) oxide (TiOPc) was prepared and characterized by MS, ¹H NMR, and elemental analysis. Cyclic voltammograms show that this TiOPc has two quasi-reversible reduction couples and two quasi-reversible to irreversible oxidations processes. The first reductions are two-electron processes, confirmed by spectroelectrochemistry to be due to Ti^IVPc²⁻/Ti^IIIPc³⁻ redox processes. The second reductions are two-electron processes during which Ti^IIIPc³⁻ was reduced to Ti^IIIPc⁵⁻ species. Spectroelectrochemistry showed that oxidation occurs at the ring during the first oxidation. However, spectroelectrochemistry also showed that upon the second oxidation, the molecule decomposes. Chronocoulometry confirmed transfer of two electrons at the first and second reduction steps. Published in Elektrokhimiya in Russian, 2008, Vol. 44, No. 12, pp. 1466–1472. The text was submitted by author in English.     

Oligomerization and Polymerization of Ethylene Initiated by a Novel Ni(Ⅱ)-Based Acetyliminopyridine Complexes as Single-Site Catalysts

Novel Ni(Ⅱ)-based acetyliminopyridine complexes 1b, 2b, 3b (1-3b), which are synthesized from ligands 1a, 2a, 3a (1-3a) and [NiCl2(DME)], are suitable precursors for the catalysts that are necessary for ethylene oligomerization and polymerization reactions, activated by methylaluminoxane (MAO).The MAO-treated 1-3b presents an active catalytic center, which may oligomerize and polymerize ethylene to produce linear α-olefins and polyethylene, respectively. The molecular weight distributions of oligomers that are obtained are in good agreement with the Schulz-Flory rules for oligomers＞C4. The activity of oligomers show significant reliance on the structures of catalyst precursors.