Green tea flavonoid epigallocatechin-3-gallate (EGCG) inhibits cardiac hERG potassium channels

The catechin EGCG is the main flavonoid compound of green tea and has received enormous pharmacological attention because of its putative beneficial health effects. This study investigated for the first time the effect of EGCG on hERG channels, the main pharmacological target of drugs that cause acquired long QT syndrome.Cloned hERG channels were expressed in Xenopus oocytes and in HEK293 cells. Heterologous hERG currents were inhibited by EGCG with an IC₅₀ of 6.0 μmol/l in HEK293 cells and an IC₅₀ of 20.5 μmol/l in Xenopus laevis oocytes. Onset of effect was slow and only little recovery from inhibition was observed upon washout. In X. laevis oocytes EGCG inhibited hERG channels in the open and inactivated states, but not in the closed states. The half-maximal activation voltage of hERG currents was shifted by EGCG towards more positive potentials.In conclusion, EGCG is a low-affinity inhibitor of hERG sharing major electrophysiological features with pharmaceutical hERG antagonists.     

QTL analysis of flower and fruit traits in sour cherry

The map locations and effects of quantitative trait loci (QTLs) were estimated for eight flower and fruit traits in sour cherry (Prunus cerasus L.) using a restriction fragment length polymorphism (RFLP) genetic linkage map constructed from a double pseudo-testcross. The mapping population consisted of 86 progeny from the cross between two sour cherry cultivars, Rheinische Schattenmorelle (RS)×Erdi Botermo (EB). The genetic linkage maps for RS and EB were 398.2 cM and 222.2 cM, respectively, with an average interval length of 9.8 cM. The RS/EB linkage map that was generated with shared segregating markers consisted of 17 linkage groups covering 272.9 cM with an average interval length of 4.8 cM. Eleven putatively significant QTLs (LOD >2.4) were detected for six characters (bloom time, ripening time, % pistil death, % pollen germination, fruit weight, and soluble solids concentration). The percentage of phenotypic variation explained by a single QTL ranged from 12.9% to 25.9%. Of the QTLs identified for the traits in which the two parents differed significantly, 50% had allelic effects opposite to those predicted from the parental phenotype. Three QTLs affecting flower traits (bloom time, % pistil death, and % pollen germination) mapped to a single linkage group, EB 1. The RFLP closest to the bloom time QTL on EB 1 was detected by a sweet cherry cDNA clone pS141 whose partial amino acid sequence was 81% identical to that of a Japanese pear stylar RNase. Received: 4 March 1999 / Accepted: 27 August 1999     

Verification of a benthic boxcosm system with potential for extrapolating experimental results to the field

A marine mesocosm system (boxcosm system) was developed for ecological and/or ecotoxicological studies of sediment community function and structure. The system consists of continuous flow-through incubations of intact sediment samples, each with a surface area of 0.25 m². The experimental setup enables repeated non-destructive measurements of benthic fluxes, such as of nutrients, oxygen and dissolved inorganic carbon, over the sediment-water interface. The benthic fluxes reflect the function of the sediment community, integrating over the chemical, biological and physical activities in the sediment. The suitability of the boxcosm system for controlled, highly ecologically relevant studies of intact sediment communities was evaluated in two experiments of six weeks and five months duration respectively, where the functional and structural development over time was compared to the development of the sampling site. The function of the sediment was measured as nutrient and oxygen fluxes, and the structural component consisted of microbial functional diversity and meio- and macrofauna composition. Differences between the boxcosm and the sampling site were detected especially in nitrate fluxes and meiofauna diversity and abundance, but all differences fell within seasonal and inter-annual variability at the sampling site. The cause of the differences could be referred to differences in oxygen availability, supply of organic matter particles, and recruitment of larvae. These factors can however be compensated for within the present setup. The study shows that the boxcosms are suitable tools for ecologically relevant studies generating comparable conditions to the natural environment.     

The vegetation of road verges in the coastal dunes of the Netherlands

The vegetation of road verges in the coastal dune area of the Netherlands was surveyed phytosociologically. Nine plant communities have been distinguished. They belong to theAmmophiletea, Koelerio-Corynephoretea, Molinio-Arrhenatheretea, Plantaginetea majoris andArtemisietea vulgaris. Most plant communities appear to be, fragmentarily developed and have thus been described by the so-called deductive method. Vegetation in road verges often appears to be heterogeneous. Species composition is influenced by man, distance from the sea, fertility and moisture content of the soil. It is clearly correlated with total nitrogen, magnesium and organic matter. Therophytes are preponderant; these and sclerophytes indicate the dry environment. The majority of the species are apophytes.     

Conformational stability of antamanide and analogs. Crystal structure of perhydrosymmetric antamanide, cyclic (-Val-Pro-Pro-Cha-Cha-Val-Pro-Pro-Cha-Cha-)

The synthetic perhydrogenated symmetric analog of the cyclic decapeptide antamanide is biologically inactive, although the conformation of the molecule and the crystal packing are very similar to that of the active symmetric analog of antamanide. In fact, the same conformation for the molecule has now been found in six polymorphs of uncomplexed antamanide and its analogs. The differences between the active and inactive antamanide analogs are displayed dramatically in the conformations of their metal ion (Na+ or Li+) complexes, thus suggesting strongly that for physiological activity antamanide is not in the conformation assumed by the uncomplexed molecule, but rather in the conformation assumed by the complexed state of natural antamanide. The present structure crystallizes in space group P2(1)2(1)2(1) with a = 20.515(14) A, b = 21.316(16) A, c = 17.128(16) A and four peptide molecules in the unit cell. There are three cocrystallized water molecules at full occupancy intrinsic to the peptide, and several more water molecules or other solvent molecules at partial occupancy. The formula of the peptide is C66H106N10O10.4-H2O.2X.     

Role of Molecular Electronic Properties of Some Novel Antimalarial Cyclic Peroxy Ketals in Relation to Potency and Potential Toxicity

Calculated molecular electronicproperties of 20 recently reported cyclic peroxy ketals have been rationalized with their in vitro antimalarial activity with the overall goal to guide the design for safer and effective peroxide-containing antimalarial agents. Stereoelectronicproperties were calculated on the optimized geometry of each compound using the ab initio 3-21G* quantum chemical basis set. Potency appears to be related to electronic properties rather than structural properties such as bond lengths and bond angles though an aliphatic cyclic ring seems to be a structural requirement for potent activity. Electronic properties such as differences in molecular polarity, in electrostatic potential profiles about the peroxide bond and the aromatic ring, in peroxide bond strength, and in the LUMO orbital energy of the molecules are all associated with potency. The three-dimensionalisopotential profile beyondthe van der Waals surface at –10 kcal/mol for the more potent analogs has a distinct large negative potential region by the aromatic ring extending to the methoxy moiety, suggesting a site for initial recognition interaction with the receptor away from the peroxide bond. The HOMO and LUMO isodensity surfaces for all molecules are located on the aromatic ring. The peroxide bond strength of the compounds is around 100 kcal/mol greater than the peroxide-containing clinically used antimalarial artemisinin compounds. In addition, density of the peroxy ketals also appears related to potent activity. The above features of the cyclic peroxy ketals are consistent with these compounds being less potent than the artemisinin compounds, but at the same time are less likely to be as neurotoxic as the artemisinins.     

Variability in the backbone conformation of cyclic pentapeptides. Crystal structure of cyclic(Gly-L-Pro-D-Phe-Gly-L-Ala)

All the peptide bonds in cyclic(Gly-L-Pro-D-Phe-Gly-L-Ala) are in the trans conformation; however, the peptide bond C'5-N1 is twisted by 19 degrees from planarity (omega 5 = -161 degrees). A Type II beta-turn encompasses the L-Pro-D-Phe residues. Carbonyl oxygens O2, O4 and O5 are directed to the same side of the average plane through the backbone ring and they form hydrogen bonds with N3, N5 and N1, respectively, in adjacent molecules in a stacked column where the adjacent molecules are related by one translational unit. The conformation of the backbone is different from that established in other molecules with the DLDDL chirality sequence. The P21 cell contains two molecules of C21H26N5O5 with a = 4.836(2) A, b = 18.346(8) A, c = 12.464(5) A and beta = 100.05(4) degrees. The R factor for 1382 data with [F0[ greater than 1 sigma is 7.0%.     

Insights into the Role of Gasotransmitters Mediating Salt Stress Responses in Plants

Salinity stress is one of the most significant global issues that negatively affect plant growth and development. Modern agricultural practices have expanded the destructive effects of salinity stress, affecting plants through immediate osmotic stress, followed by a slow onset of ionic or hyper-osmotic stress. Plants alteration and resistance to salinity stress involve complex physiological, biochemical, and molecular systems to maintain homeostasis. As of late, the investigation of gaseous molecules in plants has attained much consideration, particularly for abiotic stress. Abiotic stresses generally initiate gasotransmitter (GT) generation in plants. In the interim, these GTs enhance the accumulation and activities of few antioxidant molecules, check the destructiveness of reactive oxygen species (ROS), and improve plant resilience under different stress conditions. The current review presented the role of gaseous molecules in plants under salinity stress, which include nitric oxide (·NO), hydrogen sulfide (H₂S), hydrogen gas (H₂), carbon monoxide (CO), methane (CH₄), and the only gaseous phytohormone ethylene. Further, we highlighted the underlying molecular mechanisms of the gasotransmitter signaling and cross-talks in salinity stress. Also, we presented a general update on the inclusion of GT in salt stress response, including the research gaps and its applications in the advancement of salinity-resistant plants.