Einflüsse von Triazolapplikationen auf Kornertrag und -qualität von Winterraps

Effects of Growth Substance Applications (Triazole) on Yield Formation and Grain Quality of Winter Rape Field trials have been conducted for two years (1986/87 and 1987/88) with cv. Lirabon (low erucic acid and low glucosinolate content). At several growth stages uptil beginning of flowering and at different rates the triazole RSW 0411 (Bayer) was applied. The problem was to investigate growth regulator effects on agronomically important traits, the utilization of yield potential and on seed quality. Applications during stem elongation reduced plant height phoma lingam infestation and lodging. Branching and numbers of pods/plant increased, partly on costs of pod filling. In 1986/87 grain yields/ha indicated (not significant) increases without any effects on grain quality. In 1987/88 grain yield/ha decreased significantly combined with increasing protein- and glucosinolate contents.     

Relations between anxiety sensitivity, distress tolerance, and fear reactivity to bodily sensations to coping and conformity marijuana use motives among young adult marijuana users.

The present investigation examines anxiety sensitivity, distress tolerance, and fear reactivity to bodily sensations in relation to Coping and Conformity marijuana use motives among a sample of young adult marijuana users (n = 135; 46.7% women; Mage = 20.45, SD = 5.0). After controlling for current marijuana use frequency (past 30 days), daily cigarette smoking rate, average volume of alcohol used over the past year, negative affectivity, and other marijuana use motives, anxiety sensitivity was significantly and uniquely associated with Coping and Conformity motives for marijuana use. Distress tolerance evidenced significant and unique incremental relations to Coping motives, whereas fear reactivity to bodily sensations was unrelated to any marijuana use motive. These results provide novel information related to the role of emotional sensitivity and tolerance factors as they pertain to specific types of motives for marijuana use among young adults. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Characterization of GPVI- or GPVI-CD39-Coated Nanoparticles and Their Impact on In Vitro Thrombus Formation

Traditional antithrombotic agents commonly share a therapy-limiting side effect, as they increase the overall systemic bleeding risk. A novel approach for targeted antithrombotic therapy is nanoparticles. In other therapeutic fields, nanoparticles have enabled site-specific delivery with low levels of toxicity and side effects. Here, we paired nanotechnology with an established dimeric glycoprotein VI-Fc (GPVI-Fc) and a GPVI-CD39 fusion protein, thereby combining site-specific delivery and new antithrombotic drugs. Poly(lactic-co-glycolic acid) (PLGA) nanoparticles, NP-BSA, NP-GPVI and NP-GPVI-CD39 were characterized through electron microscopy, atomic force measurements and flow cytometry. Light transmission aggregometry enabled analysis of platelet aggregation. Thrombus formation was observed through flow chamber experiments. NP-GPVI and NP-GPVI-CD39 displayed a characteristic surface coating pattern. Fluorescence properties were identical amongst all samples. NP-GPVI and NP-GPVI-CD39 significantly impaired platelet aggregation. Thrombus formation was significantly impaired by NP-GPVI and was particularly impaired by NP-GPVI-CD39. The receptor-coated nanoparticles NP-GPVI and the bifunctional molecule NP-GPVI-CD39 demonstrated significant inhibition of in vitro thrombus formation. Consequently, the nanoparticle-mediated antithrombotic effect of GPVI-Fc, as well as GPVI-CD39, and an additive impact of CD39 was confirmed. In conclusion, NP-GPVI and NP-GPVI-CD39 may serve as a promising foundation for a novel therapeutic approach regarding targeted antithrombotic therapy.     

Untersuchungen zur Synthese von Polyethern aus Anhydropolyolen

Studies on the Synthesis of Polyethers from Anhydropolyols . By reaction of 1,4:3,6-dianhydro-D-sorbitol with base and αω-dihaloalkanes mono and dialkyl derivatives are obtained. The use of trans-1,4-dichloro-2-butene leads to oligomers up to the heptamer which are isolated and structurally assigned. Polymerisations with super acids of substituted tetrahydrofuranes such as the 1,4-anhydro-2,3-di-O-alkyl-D-erythritols lead to functionalized poly(oxytetramethylenes). By detailed studies of reaction parameters optimized conditions are achieved, and by polymer analyses the linear structures of these polyethers are demonstrated.     

Structural and Functional Characterization of 4-Hydroxyphenylacetate 3-Hydroxylase from Escherichia coli

The hydroxylation of phenols into polyphenols, which are valuable chemicals and pharmaceutical products, is a challenging reaction. The search for green synthetic processes has led to considering microorganisms and pure hydroxylases as catalysts for phenol hydroxylation. Herein, we report the structural and functional characterization of the flavin adenine dinucleotide (FAD)-dependent 4-hydroxyphenylacetate 3-monooxygenase from Escherichia coli, named HpaB. It is shown that this enzyme enjoys a relatively broad substrate specificity, which allows the conversion of a number of non-natural phenolic compounds, such as tyrosol, hydroxymandelic acid, coumaric acid, hydroxybenzoic acid and its methyl ester, and phenol, into the corresponding catechols. The reaction can be performed by using a simple chemical assay based on formate as the electron donor and the organometallic complex [Rh(bpy)Cp*(H₂O)]²⁺ (Cp*: 1,2,3,4,5-pentamethylcyclopentadiene, bpy: 2,2′-bipyridyl) as the catalyst for FAD reduction. The availability of a crystal structure of HpaB in complex with FAD at 1.8 Å resolution opens up the possibility of the rational tuning of the substrate specificity and activity of this interesting class of phenol hydroxylases.     

Complete Photochemical Regulation of 8–17 DNAzyme Activity by Using Reversible DNA Photo-crosslinking

The regulation of DNAzyme activity is an important problem for its in vivo applications. We achieved photochemical regulation of DNAzyme activity by using reversible DNA photo-crosslinking of 3-cyanovinylcarbazole (^CNVK). The ODN containing ^CNVK photo-crosslinked to a pyrimidine base in the complementary strand after a few seconds of photoirradiation, and its photoadduct was split by photoirradiation of another wavelength. The activity of photo-crosslinked DNAzyme with ^CNVK was completely inhibited (OFF state). In contrast, after 312 nm irradiation, DNAzyme activity was recovered upon addition of a substrate strand (ON state). In addition, the photo-crosslinked DNAzyme is prone to enzymatic digestion by exonuclease. This photochemical OFF to ON switching with reversible DNA photo-crosslinking was regulated at the desired time and position; therefore, it might be possible to use it for in vivo application.     

Biosynthetic Plasticity Enables Production of Fluorinated Aurachins

Enzyme promiscuity has important implications in the field of biocatalysis. In some cases, structural analogues of simple metabolic building blocks can be processed through entire pathways to give natural product derivatives that are not readily accessible by chemical means. In this study, we explored the plasticity of the aurachin biosynthesis pathway with regard to using fluoro- and chloroanthranilic acids, which are not abundant in the bacterial producers of these quinolone antibiotics. The incorporation rates of the tested precursor molecules disclosed a regiopreference for halogen substitution as well as steric limitations of enzymatic substrate tolerance. Three previously undescribed fluorinated aurachin derivatives were produced in preparative amounts by fermentation and structurally characterized. Furthermore, their antibacterial activities were evaluated in comparison to their natural congener aurachin D.     

Rapid Discovery of Aspartyl Protease Inhibitors Using an Anchoring Approach

Pharmacophore searches that include anchors, fragments contributing above average to receptor binding, combined with one-step syntheses are a powerful approach for the fast discovery of novel bioactive molecules. Here, we are presenting a pipeline for the rapid and efficient discovery of aspartyl protease inhibitors. First, we hypothesized that hydrazine could be a multi-valent warhead to interact with the active site Asp carboxylic acids. We incorporated the hydrazine anchor in a multicomponent reaction and created a large virtual library of hydrazine derivatives synthetically accessible in one-step. Next, we performed anchor-based pharmacophore screening of the libraries and resynthesized top-ranked compounds. The inhibitory potency of the molecules was finally assessed by an enzyme activity assay and the binding mode confirmed by several soaked crystal structures supporting the validity of the hypothesis and approach. The herein reported pipeline of tools will be of general value for the rapid generation of receptor binders beyond Asp proteases.