Enzymatic reductions for the regio- and stereoselective synthesis of hydroxy-keto esters and dihydroxy esters

Ketoreductases were utilized for the stereoselective synthesis of δ-hydroxy-β-keto esters, β-hydroxy-δ-keto esters, and β,δ-dihydroxy esters. Seven out of eight possible stereoisomers were obtained from the enzymatic reduction of the corresponding β,δ-diketo ester in high enantio- and diastereomeric excess.     

Singly resonant optical parametric oscillator based on adhesive-free-bonded periodically inverted KTiOPO4 plates: terahertz generation by mixing a pair of idler waves

We implemented a singly resonant optical parametric oscillator based on adhesive-free-bonded periodically inverted KTiOPO4 plates. It has major advantages such as walk-off compensation and oscillation at four wavelengths. The threshold of the oscillation was measured to be 8 MW/cm2, which is about a factor of 4 lower than that based in two separate KTiOPO4 crystals. By frequency-mixing the dual-wavelength output in GaP stacks, we generated the terahertz radiation at 2.54 THz. The tuning range of the terahertz output was demonstrated to be 2.19-2.77 THz.     

Design, synthesis and biological evaluation of non-natural modulators of quorum sensing in Pseudomonas aeruginosa

Many species of bacteria employ a mechanism of intercellular communication known as quorum sensing which is mediated by small diffusible signalling molecules termed autoinducers. The most common class of autoinducer used by Gram-negative bacteria are N-acylated-L-homoserine lactones (AHLs). Pseudomonas aeruginosa is a clinically important bacterium which is known to use AHL-mediated quorum sensing systems to regulate a variety of processes associated with virulence. Thus the selective disruption of AHL-based quorum sensing represents a strategy to attenuate the pathogenicity of this bacterium. Herein we describe the design, synthesis and biological evaluation of a collection of structurally novel AHL mimics. A number of new compounds capable of modulating the LasR-dependent quorum sensing system of P. aeruginosa were identified, which could have value as molecular tools to study and manipulate this signalling pathway. Worthy of particular note, this research has delivered novel potent quorum sensing antagonists, which strongly inhibit the production of virulence factors in a wild type strain of this pathogenic bacterium.     

One Step Reduction of Diaryl Ketones to Hydrocarbons by Etherated Boron Trifluoride-Triethylsilane System

A convenient one step reduction of diaryl ketones to hydrocarbons using etherated boron trifluoride-triethylsilane is described.     

Selective Reduction of Diaryl or Aryl Alkyl Alcohols in the Presence of Primary Hydroxyl or Ester Groups by Etherated Boron Trifluoride-Triethylsilane System

Diaryl or aryl alkyl carbinols bearing a second reducible functional group (such as hydroxyl or ester) are selectively deoxygenated in high yields by the action of etherated boron trifluoride and triethyl silane reducing system.     

Organic residue analysis of Neolithic pottery from North Greece

Organic residues associated with Neolithic pottery from two Late Neolithic sites, Paliambela and Makriyalos (Northern Greece), were analyzed by gas chromatography-mass spectrometry. The study aimed at identifying the origin of the tar used for waterproofing and gluing broken pots. Reference tars were prepared in laboratory conditions by pyrolysis of the bark from three tree species, namely from Betula pendula (silver birch), Ostrya carpinifolia (hop hornbeam) and Carpinus orientalis (Eastern hornbeam). The results suggest that mostly birch bark tar was used as glue for fixing broken pieces of the pots as well as for waterproofing close-shaped vessels. None of the archaeological tars derived from the two hornbeams. The analysis shows certain variability in the composition of birch bark tar, which is related to the production technique and to the re-use of tar. Of particular interest is the presence of characteristic diterpenoid biomarkers in several samples, which indicates that pine pitch was used for gluing and pine resin for waterproofing vessels for liquids. Correspondence: Sophia Mitkidou, Department of Science, School of Technological Applications, Technological Institute of Kavala, Greece     

Mechanically manipulating the DNA threading intercalation rate

The dumbbell shaped binuclear ruthenium complex DeltaDelta-P requires transiently melted DNA in order to thread through the DNA bases and intercalate DNA. Because such fluctuations are rare at room temperature, the binding rates are extremely low in bulk experiments. Here, single DNA molecule stretching is used to lower the barrier to DNA melting, resulting in direct mechanical manipulation of the barrier to DNA binding by the ligand. The rate of DNA threading depends exponentially on force, consistent with theoretical predictions. From the observed force dependence of the binding rate, we demonstrate that only one base pair must be transiently melted for DNA threading to occur.     

Novel Evidence-Based Combination of Plant Extracts with Multitarget Mechanisms of Action for the Elimination of Hot Flashes during Menopause

Hot flashes are considered the most bothersome complaint during menopause. Although hormone therapy is an effective option to relieve hot flashes, it has been associated with significant side effects. The aim of our study is to suggest a novel combination of different plant extracts with distinct mechanisms of action against hot flashes. We selected the rhizome of Glycyrrhiza glabra L. (Fabaceae), the rhizome of Actaea racemosa L. (Ranunculaceae), the aerial parts of Hypericum perforatum L. (Hypericaceae) to produce extracts rich in bioactive phytochemicals and the seed oil of Oenothera biennis L. (Onagraceae). We investigated their estrogenic and antioxidant potential and their inhibitory effect against prostaglandin D2 receptor 1 (DP1) as a novel mechanistic pathway for vasodilation in hot flashes, alone or in combination. The phytochemical footprint of the extracts was analyzed using HPLC-PDA and UPLC-HRMS. We observed that the tested extracts possess different mechanisms of action. A. racemosa exerts a beneficial activation of the estrogen receptor, H. perforatum possesses the highest antioxidant capacity and the seed oil of O. biennis inhibits the DP1 receptor. The triple combination in the optimal doses pertains to efficacy against all three mechanisms of action, serves as a multitarget plant-based therapy and could serve as a novel strategy for the alleviation of hot flashes in postmenopausal women.