Modular synthesis of diphospholipid oligosaccharide fragments of the bacterial cell wall and their use to study the mechanism of moenomycin and other antibiotics

We present a flexible, modular route to GlcNAc-MurNAc-oligosaccharides that can be readily converted into peptidoglycan (PG) fragments to serve as reagents for the study of bacterial enzymes that are targets for antibiotics. Demonstrating the utility of these synthetic PG substrates, we show that the tetrasaccharide substrate lipid IV (3), but not the disaccharide substrate lipid II (2), significantly increases the concentration of moenomycin A required to inhibit a prototypical PG-glycosyltransferase (PGT). These results imply that lipid IV and moenomycin A bind to the same site on the enzyme. We also show the moenomycin A inhibits the formation of elongated polysaccharide product but does not affect length distribution. We conclude that moenomycin A blocks PG-strand initiation rather than elongation or chain termination. Synthetic access to diphospholipid oligosaccharides will enable further studies of bacterial cell wall synthesis with the long-term goal of identifying novel antibiotics.     

β-Na（Y_（1.5-x-y）Na_（0.5））F_6：Yb_xTm_y纳米颗粒的合成及其上转换发光性质

本文采用水热合成法制备了β-Na（Y1.5-x-yNa0.5）F6：YbxTmy（x=0.2~1.0,y=0.001~0.008）纳米颗粒,并利用X射线粉末衍射仪、透射电子显微镜和F-4600荧光分光光度计表征了其样品的物相、形貌和发光性质.结果表明样品物相为六角相,颗粒平均直径约22nm,并探讨了Yb3＋和Tm3＋掺杂浓度对样品的上转换发光性质的影响,结果表明敏化剂Yb3＋的最佳掺杂浓度为60%,而激活剂Tm3＋的最佳掺杂浓度为0.6%.     

Thermal conductivity of open‐cell polyolefin foams

The thermal conductivity and the cellular structure of novel open‐cell polyolefin foams produced by compression molding and based on blends of an ethylene‐vinyl acetate copolymer (EVA) and a low‐density polyethylene (LDPE) have been studied in the temperature range between 24 and 50 °C. The experimental results have shown that the cellular structure of the analyzed materials has interconnected cells because of the presence of large and small holes in the cell walls, this structure being clearly different to the typical structure of open‐cell polyurethane foams. It has been found that at low temperatures the materials have a slightly higher thermal conductivity than closed‐cell polyolefin foams of similar densities. The different mechanisms of heat flow, conduction, convection, and radiation have been analyzed by using experimental measurements and a theoretical model. It has been proved that, in spite of having an open‐cell structure, the convention mechanism is negligible, being the radiation mechanism the one which made different the conductivity of materials with varying cellular structures. © 2007 Wiley Periodicals, Inc. J Polym Sci Part B: Polym Phys 46: 212–221, 2008     

Relaxation Limit for Aw-Rascle System

We study the relaxation limit for the Aw-Rascle system of traffic flow. For this we apply the theory of invariant regions and the compensated compactness method to get global existence of Cauchy problem for a particular Aw-Rascle system with source, where the source is the relaxation term, and we show the convergence of this solutions to the equilibrium state.     

Absolutely isolated singularities of a differential equation

In this paper we solve the problemof desingularization of an absolutely isolatedsingularity of a differential equation, including thedicritical case. As an application, we prove thefiniteness of the number of dicritical points in theblowing up tree of an absolutely isolated singularity.     

Decarboxylative Cyclization of Allylic Cyclic Carbamates: Mechanism Studies and Applications to the Synthesis of Natural Products

The mechanism of decarboxylative cyclization of allylic cyclic carbamates 1 leading to 2-substituted △~3-piperidines and-pyrrolidines, as well as its applications to the total synthesis of (--)codonopsine, are described.     

藏药"西藏猫乳"的色谱指纹谱研究

用75%乙醇回流法提取出藏药"西藏猫乳(生等)"的有效成分并浓缩精制后,采用HPLC梯度洗脱法,在选定的色谱条件{DuPont ZORBAX ODS C18色谱柱(4.6 mm×25 cm),用甲醇(A)-甲酸铵水溶液(pH=3.5,1.0 mL·min-1,B)进行梯度洗脱(甲醇浓度0～10 min,20%～25%;10～20 min,25%～40%;20～55 min,40%～55%;55～75 min,55%～75%;75～85 min,75%～90%),检测波长为290 am}下,对藏药"生等"的提取液进行了有效的分离与检测,并建立了"生等"药材的数字化色谱指纹谱(DFPS).所建立的方法能对藏药的产地归属进行有效的分辨.     

Nine enzymes are required for assembly of the pacidamycin group of peptidyl nucleoside antibiotics

Pacidamycins are a family of uridyl peptide antibiotics that inhibit the translocase MraY, an essential enzyme in bacterial cell wall biosynthesis that to date has not been clinically targeted. The pacidamycin structural skeleton contains a doubly inverted peptidyl chain with a β-peptide and a ureido linkage as well as a 3'-deoxyuridine nucleoside attached to DABA(3) of the peptidyl chain via an enamide linkage. Although the biosynthetic gene cluster for pacidamycins was identified recently, the assembly line of this group of peptidyl nucleoside antibiotics remained poorly understood because of the highly dissociated nature of the encoded nonribosomal peptide synthetase (NRPS) domains and modules. This work has identified a minimum set of enzymes needed for generation of the pacidamycin scaffold from amino acid and nucleoside monomers, highlighting a freestanding thiolation (T) domain (PacH) as a key carrier component in the peptidyl chain assembly as well as a freestanding condensation (C) domain (PacI) catalyzing the release of the assembled peptide by a nucleoside moiety. On the basis of the substrate promiscuity of this enzymatic assembly line, several pacidamycin analogues were produced using in vitro total biosynthesis.