Billingen (Lower Arenig/Lower Ordovician) acritarchs from the East European Platform and their palaeobiogeographic significance

Billingen (Lower Arenig/Lower Ordovician) sediments of the St. Petersburg region, northwest Russia and the Leba area, northern Poland of the East European Craton yield acritarch assemblages, which are largely homogenous though displaying minor compositional differences that probably reflect a gradient from inner to outer shelf environments. Comparison with coeval acritarch microflora from the Yangtze Platform, South China, shows an overall similarity between Baltoscandian and South Chinese phytoplankton. The widespread uniformity in the fossil microphytoplankton may be related to the extensive global 'evae' sea-level transgression, which characterized the Billingen time. This suggests that during the Tremadoc through early Arenig times, acritarch assemblages displayed essentially an undifferentiated cold-water and oceanic character along the whole margin of Perigondwana in the South, as well as on the South Chinese and Baltic platforms, at middle latitudes (Mediterranean oceanic Realm). Despite this overall similarity, however, some typical taxa of the high-latitude Mediterranean Province (Arbusculidium, Coryphidium and Striatotheca) occur in South China, but are absent in Baltica. This discrepancy is explained as caused by differences in climatic and physiographic conditions that prevailed at the two palaeocontinents at this time. The inferred pattern of oceanic circulation during the Lower Ordovician is consistent with the palynological evidence of a prevailing warmer climate in Baltica than in South China, although the two palaeocontinents occupied the same palaeolatitudinal position.     

Cyrtocrinids (Echinodermata,Crinoidea) from Upper Jurassic Štramberk‐type limestones in southern Poland

Abstract: A systematic account of highly diverse cyrtocrinid faunules from Upper Jurassic strata of ?tramberk type (Oxfordian–Tithonian) in southern Poland (Polish Carpathians) is presented. Fourteen taxa (Phyllocrinus malbosianus, Ph. stellaris, Ph. sp., Psalidocrinus armatus, Sclerocrinus compressus, S. polonicus sp. nov., Hemicrinus aff. kabanovi, Ancepsicrinus parvus gen. et sp. nov., Tetracrinus baumilleri sp. nov., Eugeniacrinites alexandrowiczi, E. cf. moravicus, E. sp., Eudesicrinus gluchowskii sp. nov. and Hemibrachiocrinus tithonicus sp. nov. are described and illustrated. Representatives of the genus Eudesicrinus, previously recorded only from the Lower Jurassic, are here shown to extend into the uppermost Jurassic. Other cyrtocrinids considered are common in Jurassic/Cretaceous strata across Europe. In the present faunules, isocrinid (Isocrinida), comatulid (Comatulida) and roveacrinid (Roveacrinida sensu Rasmussen, inclusive of Saccocoma) crinoids are associated.     

Binding site of ABC transporter homology models confirmed by ABCB1 crystal structure

The human ATP-binding cassette (ABC) transporters ABCB1, ABCC4 and ABCC5 are involved in resistance to chemotherapeutic agents. Here we present molecular models of ABCB1, ABCC4 and ABCC5 by homology based on a wide open inward-facing conformation of Escherichia coli MsbA, which were constructed in order to elucidate differences in the electrostatic and molecular features of their drug recognition conformations. As a quality assurance of the methodology, the ABCB1 model was compared to an ABCB1 X-ray crystal structure, and with published cross-linking and site directed mutagenesis data of ABCB1. Amino acids Ile306 (TMH5), Ile340 (TMH6), Phe343 (TMH6), Phe728 (TMH7), and Val982 (TMH12), form a putative substrate recognition site in the ABCB1 model, which is confirmed by both the ABCB1 X-ray crystal structure and the site-directed mutagenesis studies. The ABCB1, ABCC4 and ABCC5 models display distinct differences in the electrostatic properties of their drug recognition sites.     

Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516

(±)-2-Fluoro-2-(2-methyl-4-(((4-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-5-yl)methyl)thio)phenoxy)acetic acid (2a) has been prepared and subjected to biological testing against all three subtypes of the PPARs. This compound exhibited agonist effects with EC(50) values of 560 and 55 nM against PPARα and PPARδ, respectively, in a luciferase assay. Moreover, compound (±)-2a also exhibited potent ability to induce oleic acid oxidation in a human myotube cell assay with EC(50)=3.7 nM. Compound (±)-2a can be classified as a dual PPARα/δ agonist with a 10-fold higher potency against the PPARδ receptor than against the PPARα receptor. Molecular modeling studies revealed that both enantiomers of 2a bind to the PPARδ receptor with similar binding energies.     

Selective predation of the pike Esox lucius: comparison of lateral plates and some metric features of the three-spined stickleback Gasterosteus aculeatus

Selective predation of Esox lucius on Gasterosteus aculeatus in a natural assemblage of fish of a stream in Central Poland is described and analysed. The number of lateral plates, the standard length and four size-dependent traits were significantly smaller for sticklebacks from stomach samples than for those from population samples. Thc remaining three metric traits were not significantly different among the samples. The regressions of five metric features (out of seven) on the standard length were significantly different between the sample of caten sticklebacks and that from the free-living population. This supports the supposition that the selectivity of pikc predation with respect to metric traits is not attributable to selection on body size of the prey. Thus, it is reasonable to claim that the sample of caten sticklebacks is selectively taken from the natural population. It justifies the selective predation assumption of some hypotheses of the causes of the pattern of geographic variation in the three-spined stickleback.     

Haemoglobin concentration and body condition of nestling Great Tits Parus major : a comparison of first and second broods in two contrasting seasons

The physiological condition of nestling altricial birds depends on the quantity and quality of food delivered to them by parents. One indicator of the condition of Great Tit Parus major nestlings is the haemoglobin concentration in their blood. The present study demonstrates the influence of weather conditions (temperature and rainfall) on nestling haemoglobin concentrations during two consecutive breeding seasons in two different habitat types (parkland vs. woodland) in the city of Łódź in Central Poland. This influence probably results from the effects of weather on the trophic base of the Tits. Dry, hot weather strongly affected bush and herbal foliage later in the breeding season (mid-June to mid-July) in 2006, presumably by interfering with the development of herbivorous arthropod populations. This in turn caused food shortages for second broods of Great Tits, which resulted in nestlings having low haemoglobin levels. In the following year, temperature was on average lower, and rainfall was regular but not very heavy. These conditions enabled the development of arthropod assemblages, and the trophic base for birds was much richer. Haemoglobin concentrations in the blood of nestlings from second broods were significantly higher than those of first broods and, unexpectedly, second-brood nestlings in 2007 were on average in better physiological state than first-brood nestlings in 2006 in both habitats. The relationship between haemoglobin concentration, brood category and year was very similar to that for nestling body mass. However, it was independent of both body mass and brood size. In some years and under certain conditions, second broods can be more successful than first broods.     

Putative drug binding conformations of monoamine transporters

Structural information about monoamine transporters and their interactions with psychotropic drugs is important for understanding their molecular mechanisms of action and for drug development. The crystal structure of a Major Facilitator Superfamily (MFS) transporter, the lactose permease symporter (lac permease), has provided insight into the three-dimensional structure and mechanisms of secondary transporters. Based on the hypothesis that the 12 transmembrane alpha-helix (TMH) secondary transporters belong to a common folding class, the lac permease structure was used for molecular modeling of the serotonin transporter (SERT), the dopamine transporter (DAT), and the noradrenaline transporter (NET). The molecular modeling methods used included amino acid sequence alignment, homology modeling, and molecular mechanical energy calculations. The lac permease crystal structure has an inward-facing conformation, and construction of outward-facing SERT, DAT, and NET conformations allowing ligand binding was the most challenging step of the modeling procedure. The psychomotor stimulants cocaine and S-amphetamine, and the selective serotonin reuptake inhibitor (SSRI) S-citalopram, were docked into putative binding sites on the transporters to examine their molecular binding mechanisms. In the inward-facing conformation of SERT the translocation pore was closed towards the extracellular side by hydrophobic interactions between the conserved amino acids Phe105, Pro106, Phe117, and Ala372. An unconserved amino acid, Asp499 in TMH10 in NET, may contribute to the low affinity of S-citalopram to NET.