Double-Headed Cationic Lipopeptides: An Emerging Class of Antimicrobials

Antimicrobial peptides (AMPs) constitute a promising tool in the development of novel therapeutic agents useful in a wide range of bacterial and fungal infections. Among the modifications improving pharmacokinetic and pharmacodynamic characteristics of natural AMPs, an important role is played by lipidation. This study focuses on the newly designed and synthesized lipopeptides containing multiple Lys residues or their shorter homologues with palmitic acid (C₁₆) attached to the side chain of a residue located in the center of the peptide sequence. The approach resulted in the development of lipopeptides representing a model of surfactants with two polar headgroups. The aim of this study is to explain how variations in the length of the peptide chain or the hydrocarbon side chain of an amino acid residue modified with C₁₆, affect biological functions of lipopeptides, their self-assembling propensity, and their mode of action.     

层状双氢氧化物和蒙脱石的剥离及其自组装

以钙基蒙脱石为原料,氟化钠为钠化剂,十六烷基三甲基溴化铵为有机改性剂采用离子交换法制备了有机蒙脱石(CTA-MMT);以硝酸镁、硝酸铝、氢氧化钠和十二烷基磺酸钠为原料,采用水热法制备了有机型镁铝层状双氢氧化物(Mg Al-SDS-LDH);以氯仿为剥离介质,采用超声法剥离CTA-MMT和MgAl-SDS-LDH,分别获得了两种剥离型矿物溶胶,将其混合自组装制备了蒙脱石/层状双氢氧化物(MMT/LDH)组装材料。用XRD和AFM表征了CTA-MMT和MgAl-SDS-LDH及其剥离产物,并分析了组装材料的热稳定性。结果表明,CTA-MMT和MgAl-SDS-LDH在氯仿介质中剥离仅需20 min,剥离型CTA-MMT和MgAl-SDS-LDH片层平均厚度分别约为9和8 nm。MMT/LDH由剥离型CTA-MMT和MgAl-SDS-LDH片层有序组装而成,组装材料结构与MgAl-SDS-LDH和CTA-MMT的含量有关,其结构单元层间距2.59 nm(CTA-MMT含量较低时)随着组装材料中CTA-MMT含量的升高而转变为1.82 nm。MMT/LDH组装材料具有较单一的CTA-MMT或MgAl-SDS-LDH更高的热稳定性。     

自组装法合成介孔铝酸锌尖晶石陶瓷纳米粉

采用硝酸铝和硝酸锌为无机原料,以嵌段聚合物P123为表面活性剂,自组装法合成了介孔结构的铝酸锌尖晶石纳米粉体。利用X射线衍射、透射电镜、氮气吸附-脱附比表面测定仪对铝酸锌样品进行表征,样品为单一尖晶石相,而且具有介孔结构,500℃焙烧的铝酸锌样品比表面积最大,比表面积为98.4m2·g-1。     

CRITICAL SELF-ASSEMBLY CONCENTRATION OF AN IONIC-COMPLEMENTARY PEPTIDE EAK16-I

Understanding the process of self-assembly of peptides has been important in various biomedical engineering applications. This work focuses on the effect of peptide concentration on the molecular self-assembly of an ionic-complementary peptide, EAK16-I (AEAKAEAKAEAKAEAK), in aqueous solution. The surface tension and self-assembled nanostructures were determined for a wide range of peptide concentrations using axisymmetric drop shape analysis-profile (ADSA-P) and atomic force microscopy (AFM), respectively. Surface tension measurements revealed a critical self-assembly concentration of 0.3 mg peptide/ml water, below which the surface tension decreased rapidly with increasing peptide concentration, and above which the surface tension remained at a constant, plateau value. There were two structural transitions observed with increasing peptide concentration: the first was from globular nanostructures to fibrils, and the second from the fibrils to relatively thick fibers. The second structural transition occurred at the critical self-assembly concentration as determined by the surface tension measurements. The nanostructural behavior of EAK16-I was compared with that of EAK16-II, which has the same amino acid composition but a different charge distribution. Salt effects were also examined by adding NaCl to the peptide solution. The salt addition facilitated the formation of peptide fibrils at low peptide concentrations but increased the critical self-assembly concentration, which occurred at 0.8 mg peptide/ml water in the presence of 20 mM NaCl. The structural transitions involved in the self-assembly of EAK16-I resemble those from protofibrils to fibrils observed with numerous naturally occurring peptides. An understanding of this structural transition may have relevance in the analysis and treatment of peptide/protein conformational diseases and have application in the production of self-assembled protein nanostructures.     

耐溶剂复合纳滤膜的研究进展

耐溶剂纳滤是一种新型的膜分离技术,用于有机混合物的分离。商品耐溶剂纳滤膜大多是采用相转化法制备的整体皮层非对称膜,膜皮层较厚,通量较低。耐溶剂复合纳滤膜由基膜和分离层组成,具有薄皮层、高溶剂通量和高溶质截留率的优点。耐溶剂复合纳滤膜的制备与改性也因此成为近年来的研究热点。本文从界面聚合、表面涂覆、层层自组装、原位生长、有机-无机杂化和表面改性六个方面介绍耐溶剂复合纳滤膜的研究进展,最后对其发展前景进行展望。     

矿质离子螯合肽自组装递送体系研究进展

钙、铁、锌、硒、铜、铬等矿质元素与人体生长、发育、繁殖、代谢等生命活动密切相关,多肽与矿质离子间可自发组织或聚集成具有稳定结构的有机螯合物,这一类新型补充剂在稳定性、促吸收、生理活性等方面比以往的金属离子补充剂更具优势。该文阐述了多肽-矿质离子螯合物来源及制备、自组装模式、促生物利用度,并对多肽-矿质离子螯合物及其多元超分子自组装递送体系前景进行了展望。     

光子晶体及其自组装制备

自从理论计算指出金刚石结构具有完全光子带隙以来，三维光子晶体的理论研究和实验制作一直受到高度重视。光子晶体的制备方法总体上可分为两大类：微制作法和自组装法。前者适合于制备微波、远红外及近红外波段的光子晶体，后者制备近红外、可见或更短波段的光子晶体具有独特的优势。简述了光子晶体的概念和基本特征，并对三维光子晶体的自组装制备方法进行了综述。     

离子自组装成膜技术制备TiO2／SiO2薄膜光波导

采用离子自组装(ISA)成膜技术制备了TiO2／SiO2复合薄膜光波导，研究了光波导的波导特性。结果表明，随着TiO2含量的增大，光波导的折射率增加，但同时光波导传输损耗增大。一般TiO2占10wt％，此时，光波导中的光损耗较低。在更高的含量范围内，必须使TiO2分散。     

A novel design for stable self-assembly cubosome precursor-microparticles enhancing dissolution of insoluble drugs

Cubosomes have been presented to enhance dissolution of insoluble drugs, but their applications are limited by the practical hurdles associated with both preparation and storage instability, resulting in drug delivery failure. In the present study, an innovative cubosome precursor-microparticles (CPMs) spray dried from an aqua-free precursor solution was developed to improve cubosome stability during both preparation and storage as well as to enhance the dissolution of insoluble drugs. These CPMs spontaneously self-assembled in situ forming homogeneous cubosome dispersion by hydration and disintegration after exposure to the aqueous medium. The stable cubosome dispersion was obtained from self-assembly (SA) of CPMs after administration instead of fragmentation of bulk cubic phase gel into cubosomes, which settled the preparation instability due to avoidance of high energy fragmentation (e.g. ultrasonic effect, high speed shear and high pressure homogenization). Also, the subsequent storage instability issue can be excluded as the CPMs were stored in a solid stable form. The CPMs disintegration and cubosome SA were demonstrated by the notable morphology variation and the distinct microparticle size decrease from CPMs (10–20?μm) to SA-cubosomes (150–200?nm). The cumulative release of docetaxel (DTX, model insoluble drug) incorporated in CPMs increased to 96.4% within 120?minutes compared with only 75.2% for blank CPMs and DTX physical mixture, demonstrating that CPMs significantly enhanced the dissolution extent of insoluble drug. The SA-cubosomes possessed quite high drug entrapment efficiency (>95%) and an integrated drug dissolution content, which significantly increased the drug utilization rate.     

Synthesis and Self-Organization of Fluorene-Conjugated Bisimidazolylporphyrin and Its Optical Properties

A conjugated-bisimidazolylporphyrin bridged by bis(ethynylfluorene) was synthesized and organized into linear polymer through self-coordination having mean molecular weights, M_w and M_n, of ~2.1 × 10⁵ Da and ~1.6 × 10⁵ Da, respectively. A large two-photon absorption cross section value of 3.4 × 10⁵ GM (per dimer unit) was observed. This value was comparable to that of the previously reported self-assembled linear polymer consisting of butadiyne-bridged imidazolylporphyrins. The two-photon absorption properties could be controlled by tuning the wavelength and absorption intensity of the one-photon absorption.