Investigation on the accumulation of lead and other metals in plants caused by motor-traffic and smelting

The Pb and Br content of plants growing along roads has been determined. It has been stated that the Pb-content of rye grass is proportional to the level of public road traffic. The Pb-content of plants cannot be removed by washing. The Pb, Cu and Zn-concentration of plants grown in the vicinity of smeltery may reach the 10–1000 times value of the normal level.     

Biosynthesis of sulfated glycopeptide antibiotics by using the sulfotransferase StaL

The unique glycopeptide antibiotic A47934, produced by Streptomyces toyocaensis, possesses a nonglycosylated heptapeptide core that is sulfated on the phenolic hydroxyl of the N-terminal 4-hydroxy-L-phenylglycine residue. Genetic and biochemical experiments confirmed that StaL is a sulfotransferase capable of sulfating the predicted crosslinked heptapeptide substrate to produce A47934 both in vivo and in vitro. Incubation of purified His(6)-StaL with various substrates in vitro revealed substrate specificity and yielded two sulfo-glycopeptide antibiotics: sulfo-teicoplanin aglycone and sulfo-teicoplanin. Quantification of the antibacterial activity of desulfo-A47934, A47934, teicoplanin, and sulfo-teicoplanin demonstrated that sulfation slightly increased the minimum inhibitory concentration. This unique modification by sulfation expands glycopeptide diversity with potential application for the development of new antibiotics.     

An in vitro screen of bacterial lipopolysaccharide biosynthetic enzymes identifies an inhibitor of ADP-heptose biosynthesis

The lipopolysaccharide (LPS)-rich outer membrane of gram-negative bacteria provides a protective barrier that insulates these organisms from the action of numerous antibiotics. Breach of the LPS layer can therefore provide access to the cell interior to otherwise impermeant toxic molecules and can expose vulnerable binding sites for immune system components such as complement. Inhibition of LPS biosynthesis, leading to a truncated LPS molecule, is an alternative strategy for antibacterial drug development in which this vital cellular structure is weakened. A significant challenge for in vitro screens of small molecules for inhibition of LPS biosynthesis is the difficulty in accessing the complex carbohydrate substrates. We have optimized an assay of the enzymes required for LPS heptose biosynthesis that simultaneously surveys five enzyme activities by using commercially available substrates and report its use in a small-molecule screen that identifies an inhibitor of heptose synthesis.     

Chimeric streptogramin-tyrocidine antibiotics that overcome streptogramin resistance

Streptogramin antibiotics are comprised of two distinct chemical components: the type A polyketides and the type B cyclic depsipeptides. Clinical resistance to the type B streptogramins can occur via enzymatic degradation catalyzed by the lyase Vgb or by target modification through the action of Erm ribosomal RNA methyltransferases. We have prepared through chemical and chemo-enzymatic approaches a series of chimeric antibiotics composed of elements of type B streptogramins and the membrane-active antibiotic tyrocidine that evade these resistance mechanisms. These new compounds show broad antibiotic activity against gram-positive bacteria including a number of important pathogens, and chimeras appear to function by a mechanism that is distinct from their parent antibiotics. These results allow for the development of a brand new class of antibiotics with the ability to evade type B streptogramin-resistance mechanisms.     

Interaction of a polymer matrix and short reinforcing fibers

A model of a glass-reinforced plastic with short unidirectional fibers is proposed. The distribution of tensile stresses in the polymer matrix and the fibers and the shear stress distribution at the interface in uniaxial tension are investigated in the elastic formulation.Riga Polytechnic Institute. Translated from Mekhanika Polimerov, No. 6, pp. 1030–1035, November–December, 1971.     

pH-Sensitive Cyanine Dyes for Biological Applications

A series of functionalized, water-soluble, pH-sensitive pentamethine cyanine (Cy^TM5) dyes has been designed and synthesized. These probes are fluorescent in acidic media but are non-fluorescent in an alkaline environment. Subtle changes to the structure of these probes can lead to pronounced changes in the pKa of these probes. These probes have been utilized in a cellular environment to detect localized changes in pH using the IN Cell Analyzer, a confocal imager formatted for imaging of cell-based assays.     

Total Synthesis and Activity of the Metallo‐β‐lactamase Inhibitor Aspergillomarasmine A

Resistance to β‐lactam antibiotics is mediated primarily by enzymes that hydrolytically inactivate the drugs by one of two mechanisms: serine nucleophilic attack or metal‐dependent activation of a water molecule. Serine β‐lactamases are countered in the clinic by several codrugs that inhibit these enzymes, thereby rescuing antibiotic action. There are no equivalent inhibitors of metallo‐β‐lactamases in clinical use, but the fungal secondary metabolite aspergillomarasmine A has recently been identified as a potential candidate for such a codrug. Herein we report the synthesis of aspergillomarasmine A. The synthesis enabled confirmation of the stereochemical configuration of the compound and offers a route for the synthesis of derivatives in the future.     

Modeling of the mechanical characteristics of chaotically reinforced GRP

Experimental results on the mechanical properties under tension and compression of composites based on a phenol-formaldehyde binder reinforced with short glass fibers are reported. Unidirectional structures, in which the reinforcing elements had different orientations with respect to the external load, were studied, as well as chaotically reinforced composites. In addition, the mechanical properties of the polymer matrix and of the reinforcing elements as well as the bond strength between them were also determined. An analysis of the results obtained in the tension experiments is presented, based on a model in which the frictional mechanism of interaction between the polymer matrix and the reinforcing elements is utilized. The quantitative relationships deduced give results agreeing with those obtained experimentally.