Synthesis of 3′,4′-difluoro-3′-deoxyribonucleosides and its evaluation of the biological activities: Discovery of a novel type of anti-HCV agent 3′,4′-difluorocordycepin

Upon reacting 3′,4′-unsaturated cytosine (8 and 9) and adenine nucleosides (13 and 14) with XeF₂/BF₃·OEt₂, the respective novel 3′,4′-difluoro-3′-deoxyribofuranosyl nucleosides (10–12 and 15–18) could be obtained. Formation of anti-adducts (11, 16 and 18) revealed that the fluorination involved oxonium ions as incipient intermediates. TBDMS-protected 3′,4′-unsaturated adenosine provided the β-face adducts as sole stereoisomers whereas α-face-selectivity was observed with the TBDPS-protected adenosine 14. The evaluation of the novel 3′-deoxy-3′,4′-difluororibofuranosylcytosine-(19–21) and adenine nucleosides (22–25) against antitumor and antiviral activities revealed that 3′,4′-difluorocordycepin (24) was found to possess anti-HCV activity. The SI of 24 was comparable to that of the anti-HCV drug ribavirin. However, sofosbuvir, FDA-approved novel anti-HCV drug, showed better SI value. Our finding revealed that the introduction of the fluoro-substituent into the 4′-position of cordycepin derivatives decreased the cytotoxicity to the host cell with retention of the antiviral activity.     

Does transpiration have an essential function in long-distance ion transport in plants?

Abstract. Long-term effects of transpiration on growth and on long-distance ion transport were investigated in maize over a whole growth cycle. Maize plants were grown with nutrients supplied at adequate levels in hydroculture or in soil at 50–60% and at >95% relative humidity. Although the amount of water lost by the plants under these conditions differed by a factor 2 to 3, there was neither a decrease in growth (fresh weight and dry weight) nor in ash content of the 'humid'plants. This was also found when the upper part of the shoot (70–150 cm) was tested separately. It is suggested that transpiration is not essential for long-distance transport of mineral elements in plants. Alternatives are discussed.     

Somatic polyploidy in extraembryonic membranes of the snake,Elaphe guttata

Summary Video-densitometric DNA measurements of Feulgenstained tissues of 42 day old eggs of the corn snake,Elaphe g. guttata (Columbridae, Serpentes), revealed a basic DNA content of 2C=2.17 pg, with somatic polyploidy in the allantois, the chorioallontois, the yolk sac, and other extraembryonic membranes. The maximum value determined was 128C (in binucleate cells 2×128C) at the distal pole of the egg. This is the first report of somatic polyploidy in a snake, and one of the first in reptiles in general.     

Biochemical composition of the parasitic amphipod Hyperia galba in relation to age and starvation

Summary Hyperia galba was collected in the waters around Helgoland and in the Weser-Elbe-estuary during autumn. Its mode of life is a temporary but obligatory parasitism. The basal biochemical composition of the adults was analyzed in detail and related to the fresh, dry, and ash-free dry weight as well as sex and body length. Hyperia galba (males/females) consists of 85/86% water; the dry matter contains approximately 64/61% protein, 10/11% lipid, 1.2/1.5% carbohydrate, 10/8% chitin, and 23/23% ash. The analyses of basal elemental composition yielded approximately 38% C, 9% N and 6% H. Under natural conditions, individuals may encounter at least two periods of food shortage during their lives. Therefore, the analyses were carried out on individuals of different developmental stages also under food deprivation. The data are discussed with respect to the special mode of life of the species and compared with those found by other authors in several related crustacean species.Abbreviations AFDW ash-free dry weight - BL body length - DW dry weight - SD standard deviation - WW wet weight     

Arg-Gly-Asp (RGD) sequence conjugated in a synthetic copolymer bearing a sugar moiety for improved culture of parenchymal cells (hepatocytes)

A copolymer, including a Gly-Arg-Gly-Asp-Ser (GRGDS) sequence and sugar moieties, was synthesized for the culturing of parenchymal cells (hepatocytes). Hepatocyte cells attached to poly[N-p-vinylbenzyl-d-maltonamide-co-6-(p-vinylbenzamido)-hexanoic acid-GRGDS] [poly(VMA-co-VBRGD)]-coated dishes grew approximately 60% better than on other polymer-coated surface for 12 h. Also, about 80% greater albumin secretion (0.38 pg ml^–1) and about 70% greater urea synthesis (0.495 pg ml^–1) from hepatocytes were produced in this matrix as compared with unstimulated cells. The behaviour of hepatocytes on poly(VMA-co-VBGRGDS)-coated dishes was not distinct from those attached to a collagen. The conjugation of the adhesion molecules of the RGD peptide in the poly(VMA-co-VBGRGDS) copolymer therefore specifically interacts with integrin families on the hepatocyte cell membrane.     

喜树叶、枝水溶性糖提取的研究

用正交实验结果作方差分析表明：溶剂用量对试验结果有较显著的影响（a=0.10)，提取温度对试验结果也有较大的影响，而提取时间对试验结果的影响不显著。喜树叶中水溶性糖的提取最优方案是A3C2B3，即溶剂用量为60ml，提取温度80℃，提取时间60min；喜树叶水溶性糖的提取最优方案是A2C2B1，即溶剂用量为40ml，提取温度80℃，提取时间20min。通过对喜树叶与枝的成对比较分析，叶与枝的水溶性糖含量无显著差异。     

Chorologische phänomene in Wasserpflanzengesellschaften Mitteleuropas

On the basis of three selected examples chorological phenomena in waterplant communities of central, east and southern Europe are represented. Species of the Atlantic-oceanic floral element of the order Juncetalia bulbosi, like Pilularia globulifera, Eleocharis multicaulis and Deschampsia setacea are growing in markedly secondary sites near their eastern border, i.e. in the Lusatian district of central Europe, especially in sand, gravel and clay pits as well as in residue lakes of opencast mines. As a result of intensive recent human activities numerous new sites are being established now causing an expansion of their distribution area. With decreasing oceanity from the central part to the eastern border of the area a change in the floristic-sociological structure of the relevant plant communities and in the hydrochemical composition of the respective water bodies takes place. In western Europe the species grow in soft water poor in minerals, in the eastern part (central Europe) in mineral-rich, hard water with calcium and sulphate.At present Ceratophyllum submersum has a high frequency in the northeastern area in Mecklenburg. The sites are morainic lakes (kettle holes) and small waters and ponds near settlements, which are enriched in minerals and nitrales in consequence of the intensive agricultural use of inorganic fertilizers. Moreover the waters are alkaline and rich in minerals, especially bicarbonate and possess a high range of total hardness. The example of eight different sites of Aldrovanda vesiculosa illustrates a striking change of its diagnostic value in its disjunct north-south distribution. In the northern part of central Europe Aldrovanda is found in the communities of the Utricularietea intermedio-minoris, both in waters with a low acidity rich in sulphate and in alkaline waters rich in bicarbonate (Sphagno-Utricularion and Scorpidio-Utricularion respectively). In southern central Europe and in southeastern Europe Aldrovanda occurs in Lemnetea and Potametea communities. In northeastern Poland Aldrovanda is found together with Hydrilla verticillata, Chara mentosa, Myriophyllum verticillatum and Scorpidium scorpioides.

Die Sippennomenklatur richtet sich nach Rothmaler et al. (1970).     

Codon Usage in Pathogenic Entamoeba histolytica

Summary An analysis of 4680 codons expressed by pathogenic Entamoeba histolytica showed the A+U content of coding sequences to be 67%. The preference for A+U resulted in an unusual codon usage with an A+U content of 84% in the third codon position. The data show a remarkable similarity to those obtained for Plasmodium falciparum.     

Distinct feeding strategies of generalist and specialist spiders

1. Feeding behaviour of generalist and specialist predators is determined by a variety of trophic adaptations. Specialised prey‐capture adaptations allow specialists to catch relatively large prey on a regular basis. As a result, specialists might be adapted to exploit each item of prey more thoroughly than do generalists. 2. It was expected that obligatory specialist cursorial spiders would feed less frequently than generalists but for a longer time and, thus, that their foraging pause would be longer. First, the feeding frequencies of three generalist spider species (Cybaeodamus taim, Harpactea hombergi, Hersiliola sternbergsi) were compared with those three phylogenetically related specialist species: myrmecophagous Zodarion rubidum, and araneophagous Nops aff. variabilis and Palpimanus orientalis. 3. Generalists captured more prey, exploited each item of prey for a significantly shorter time, and had a shorter foraging pause than was the case for specialists. Generalists also gained significantly less relative amount of prey mass than did specialists. 4. Second, the study compared the prey DNA degradation rate in the gut of generalists and specialists by means of PCR. The degradation rate was not significantly different between specialists and generalists: the detectability half‐life was estimated to exist for 14.3 days after feeding. 5. This study shows that the feeding strategies of cursorial generalist and obligatory specialist spiders are different. Obligatory specialists have evolved a feeding strategy that is based on thorough exploitation of a few large prey, whereas generalists have evolved a strategy that is based on short exploitation of multiple small items of prey.