Studies on the Later Stage of the Biosynthesis of Pleuromutilin

Mutilin (4) and deoxy analogues 2 and 3 are biosynthetic precursors of pleuromutilin (1) in the later stage of biosynthesis. Precursors 2 and 3 are required for studies on the oxygenation steps in biosynthesis, and were synthesized from readily available 1 via 4 by deoxygenation of the hydroxy groups. Feeding experiments with the ²H-labeled precursors confirmed their microbial conversion into 1.     

Host-Guest Interactions as a Model for the Solvent Influence on the Conformational Populations in [2.2.2.2]Paracyclophane

The interaction of a number of small organic molecules with the two lowest energy minimum conformations of [2.2.2.2]paracyclophane (4°-PCP), 1 and 2, are studied by MMP2(87) force field calculations. Formations of nesting as well as inclusion complexes were identified on the potential energy surface. With CH₂Cl₂ and CHCl₃ used as guests, the nesting complexes are lower in energy than the inclusion ones with both conformations 1 and 2. Furthermore, the nesting complexes with 2 are found to be more stable than the nesting ones with 1. Formation of the double nesting complexes of CH₂Cl₂ and CHCl₃ with 1 and 2 raise the difference in complexation energy in favour of 2. The preference of 4°-PCP for the form 2 in solution is explained based on the above analysis, although 2 is calculated to be 0.2 kcal·mol^–1 higher in steric energy than 1 in the gas phase.Supplementary material to this paper is available in electronic form at http://dx.doi.org/10.1007/s0089490050218     

Two remarks on the mathematical biology of automobile driving

In connection with a series of previous papers by this author (Bulletin of Mathematical Biophysics,21, 299–308, 375–385;22, 257–262, 263–267;23, 19–29;24, 319–325) results obtained by A. Crawford (Economics 5, 417–428) on the effects of irrelevant lights on reaction times toward a given light stimulus are discussed. The conclusions from a previous paper of this author (Bulletin of Mathematical Biophysics,23, 19–29) are elaborated.     

Spectral responses and chromatic processing in the dragonfly lamina

The dragonfly Hemicordulia tau has five spectral classes of photoreceptor which drive five lamina monopolars, m1-m5. The monopolars encode spectral information. Here, spectral coding by m2, m4 and m5 are described. m2 is the most sensitive to dim light. m4 and m5 are less sensitive than m2, and so we call them photopic cells. The effects of selective adaptation of receptor inputs to m4 and m5 are unusual. For example, in m4 adaptation of the green receptor suppresses the UV input, but green sensitivity is unaffected, while green adaptation of m5 increases its green sensitivity. In m5 the dark adapted spectral tuning resembles the 520 nm receptor, but on adaptation to 430 nm light this narrows markedly. Adaptation either of green or of UV receptor input to m2 and m4 modifies the time course of responses both to green and to UV, implying that changes in the time courses of monopolar responses with adaptation state do not directly reflect receptor responses (Fig. 2). Finally, the antagonistic surround of m2 is UV sensitive, and of m4 green sensitive (Fig. 3).Abbreviations LMC large monopolar cell - LVF long visual fibre - rf receptive field - SVF short visual fibre     

A DNA fragment fromStreptomyces fradiae increases the production of a metalloprotease inStreptomyces lividans

Streptomyces fradiae produces several extracellular proteases and many of these are inducible. An 8.8 kb DNA fragment of Streptomyces fradiae cloned on pIJ699 caused increased protease activity in Streptomyces lividans.Clones carrying this recombinant plasmid showed a significant delay in sporulation. A protein of 18 kDa was purified from the extracellular proteins secreted by the host carrying the recombinant plasmid. Further characterization showed that this protease is a metalloprotease.     

A comparative study of the O-3 reactivity of isomeric N-dimethylmaleoyl-protected d-glucosamine and d-allosamine acceptors

Four isomeric N-dimethylmaleoyl 4,6-O-benzylidene-protected d-hexosamine acceptors (2, 3, 4, and 5) with all possible configurations at C-1 and C-3 (e.g., derived from d-glucosamine and d-allosamine) were prepared, and the assessment of their O-3 relative reactivity through competition experiments using the known per-O-acetylated d-galactopyranosyl trichloroacetimidate donor (15) was then carried out. The reactivities are in the order 4 ? 2 > 5 > 3. The analysis of the NMR spectra of 2–5 at different temperature and modeling experiments carried out on analogs of 2–5 (DFT) and on the acceptors themselves (MM) are coincident, and have helped to establish the stability of the different hydrogen bonds, and of the conformers which carry them. The whole results suggest that the electronic effects (hydrogen bonds) are required to explain the observed trend, in spite of the axial conformation of the most reactive hydroxyl group. The steric effects appear only when hydrogen bonds are weak.     

A new genus of the tribe Acratini from the continental Neotropical region (Coleoptera: Curculionoidea,Brentidae)

A group of 10 species belonging to the Neotropical tribe Acratini Alonso-Zarazaga, Lyal, Bartolozzi & Sforzi 1999, is shown to be monophyletic by a phylogenetic analysis based on 48 morphological characters. A new genus, Pertusius n. gen., is described, based on three derived characters of external and genital morphology: venter of prorostrum of males with fine median longitudinal carina, base of elytra with deep pit at the place of insertion on mesonotum, and proximal sclerite of endophallus more or less horseshoe-shaped. Eight species were previously known and, according to former authors, belonged to the genera Acratus Lacordaire 1865 [Pertusius apicalis (Sharp 1895), n. comb., P. errabundus (Kleine 1927), n. comb., P. extrarius (Kleine 1927), n. comb., P. fidus (Kleine 1927), n. comb. and P. telesi (Soares & Meyer 1959), n. comb.] and Proteramocerus Kleine 1921 [Pertusius chalcites (Perty 1832), n. comb., P. filum (Sharp 1895), n. comb., and P. laevis (Germar 1824), n. comb.]. Four new synonymies are proposed: Proteramocerus disparilis Soares & Dias 1971, n. syn. for Acratus apicalis Sharp 1895; Teramocerus laevigatus Boheman 1840, n. syn. for Arrhenodes chalcites Perty 1832; Acratus extraordinarius Kleine 1927, n. syn. for Acratus errabundus Kleine 1927; Proteramocerus diringshofeni Soares & Dias 1971, n. syn. for Acratus filum Sharp 1895. Two new species are described: Pertusius guyanensis n. sp. from French Guiana, and P. mexicanus n. sp. from Mexico (Yucatán Peninsula). Pertusius apicalis is newly cited from Bolivia and Peru, P. chalcites from Argentina and Paraguay, P. extrarius from Ecuador, P. fidus from Peru and P. telesi from Trinidad and Tobago and Venezuela. An identification key to species of the genus is provided.     

The movements of the Kittiwake

Capsule During winter songbirds were far more abundant in game cover crops than conventional agricultural habitats.

Aims To quantify game crop use during winter by farmland songbirds when compared with conventional farmland at a regional scale.

Methods Songbirds were counted on 20 farms in eastern Scotland. The number of songbirds using game crops was compared with a sample of nearby conventional crops – with particular emphasis on set-aside and cereal stubbles.

Results Game crops supported up to 100 times as many birds per hectare, of significantly more species, than the other two habitat categories. Many of these species were those currently causing concern because of their declining populations.

Conclusion Game crops could provide opportunities for increasing food resources to songbirds whose populations may be limited by food availability and possibly arrest population declines. At present, the only measures likely to facilitate this are the government's various agri-environment schemes.     

Heritability: the link between development and the microevolution of molar tooth form

Abstract

The developmental gene expression, morphogenesis, and population variation in mammalian molar teeth has become increasingly well understood, providing a model system for synthesizing evolution and developmental genetics. In this study, we estimated additive genetic covariances in molar shape (G) using parent-offspring regression in Cryptotis parva, the Least Shrew. We found that crown shape had an overall h² value of 0.34 (±0.08), with higher heritabilities in molar cusps than notches. We compared the genetic covariances to phenotypic (P) and environmental (E) covariances, and to the covariances in crown features expected from the enamel knot developmental cascade (D). We found that G and D were not strongly correlated and that major axes of G (evolutionary lines of least resistance) are better predictors of evolutionary divergences in soricines than is D. We conclude that the enamel knot cascade does impose constraints on the evolution of molar shape, but that it is so permissive that the divergences among soricines (whose last common ancestor lived about 14 million years ago) do not fully explore its confines. Over tens of millions of years, G will be a better predictor of the major axes of evolution in molar shape than D.     

Revision of the species of the Tychus rufus group (Coleoptera: Staphylinidae: Pselaphinae)

The species belonging to Tychus rufus group are revised. Eleven species are recognized, described and illustrated and a key to their identification is provided. Nine taxa are new to science: Tychus carpathius n. sp. from Karpathos island (Greece); T. torticornis n. sp. from Lesbos Island (Greece); T. pisidicus n. sp. and T. inermis n. sp. from southwestern Turkey; T. antiocheus n. sp. and T. effeminatus n. sp. from southeastern Turkey; T. artvinensis n. sp. from northeastern Turkey, and T. sidonicus n. sp. and T. libanus n. sp. from Lebanon.     

Segregation in the African wintering ranges of English and Swiss Swallow Hirundo rustica populations: a stable isotope study

Capsule Stable isotope analysis of Swallow feathers, grown in Africa, revealed significant differences between populations breeding in Switzerland and England.

Aims To investigate the extent to which Swallow populations breeding in Switzerland and England are separated on their African wintering grounds.

Methods Swallows were caught at breeding colonies, biometric measurements were taken and feathers, grown in Africa, were collected. Feathers were combusted in a Carlo Erba C/N/S analyser and the δ¹³C and δ¹⁵N signatures were measured using a mass spectrometer.

Results The δ¹³C signatures of Swiss birds were significantly more depleted than those of birds from England. The δ¹⁵N signatures did not differ between the two populations.

Conclusion Birds from Switzerland and England probably winter in geographically distinct parts of Africa. The Swiss birds probably feed on prey that are more reliant on C₃ vegetation, from woodlands, than the prey of English birds, which are more reliant on C₄ vegetation, from grasslands.     

Molecular phylogenetics and definition of the Acrapex minima Janse group (Lepidoptera,Noctuidae, Apameini,Sesamiina) with the description of four new species from the Afrotropics

Five morphologically similar species of Acrapex Hampson (Lepidoptera, Noctuidae, Noctuinae, Apameini), from sub-Saharan Africa are reviewed, including four new species that are described: Acrapex mondogeneta Le Ru n. sp., A. mubale Le Ru n. sp., A. robe Le Ru n. sp. and A. rubona Le Ru n. sp. These five species belong to a species complex that we hereby define as the Acrapex minima group. Host plants of three species are recorded; Acrapex minima is recorded for the first time on a host plant, Digitaria natalensis Stent; A. mondogeneta on Hyparrhenia hirta (L.) Stapf and A. rubona on Imperata cylindrica (L.) P. Beauv. We also conducted molecular phylogenetics (using both Bayesian inference and maximum likelihood) and molecular species delimitation analyses (Poisson tree processes) on a six gene multi-marker dataset (four mitochondrial and two nuclear gene fragments; 4582 nucleotides in length) of 42 specimens and 22 species, including 23 specimens from the Acrapex minima group. The results of the corresponding analyses support the monophyly of the group and the species status of the newly described taxa.     

一株海洋真菌Aspergillus jensenii LW128的次级代谢产物及其抗菌活性研究

【目的】研究一株西北太平洋深海沉积物来源真菌Aspergillus jensenii LW128的次级代谢产物及其抗菌活性。【方法】利用硅胶柱色谱(silica gel column chromatography)、凝胶柱色谱(Sephadex LH-20 column chromatography)和反相高效液相色谱(reversed-phase high-performance liquid chromatography, RP-HPLC)等方法对菌株的发酵粗提物进行分离纯化得到单体化合物;将核磁共振波谱(nuclear magnetic resonance, NMR)、质谱(mass spectrometry, MS)数据与相关文献报道数据进行比对后确定化合物结构;采用肉汤微量稀释法测定化合物的抗菌活性。【结果】从海洋真菌Aspergillus jensenii LW128中分离并鉴定了10个已知化合物,分别为diorcinol D(1)、diorcinol K(2)、diorcinol I(3)、(+)-(7S)-7-O-methylsydonic acid (4)、(+)-s...     

Investigation of the effects of some sulfonamide derivatives on the activities of glucose-6-phosphate dehydrogenase, 6-phospho gluconate dehydrogenase and glutathione reductase from human erythrocytes

In this study, the in vitro effects of some sulfonamide derivatives, which are carbonic anhydrase inhibitors, on the enzymes activities of glucose-6-phosphate dehydrogenase, 6-phospho gluconate dehydrogenase and glutathione reductase were investigated. For this purpose, these three enzymes were purified from human erythrocytes. Purification procedure composed of four steps; preparation of the hemolysate, ammonium sulfate precipitation, 2′,5′-ADP Sepharose 4B affinity chromatography, and gel filtration chromatography on Sephadex G-200. 5-(3α-Hydroxy-5-β-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (1), 5-(3α,12α-Dihydroxy-5-β-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (2), 5-(3α,7α,12α-Trihydroxy-5-β-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (3), 5-(3α,Acetoxy-5-β-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (4), 5-(3α,7α,12α-Triacetoxy-5-β-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (5), 5-(3,7,12-Trioxo-5-β-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (6), acetazolamide, and dorzolamide were tested in this experiment. Compounds 3, 5, and dorzolamide showed inhibitory effects on the activity of 6-phosphogluconate dehydrogenase, and I₅₀ values and K_i constants were calculated as 0.0601 mM, 0.00253 mM, and 1.41 mM and 0.0878 ± 0.0274 mM, 0.0042 ± 0.0009 mM, and 3.1446 ± 0.2081 mM, respectively. Glutathione reductase was also inhibited by 1 and 2. I₅₀ values and K_i constants were 0.0471 mM and 0.0723 ± 0.0388 mM for 1 and 0.0045 mM and 0.0061 ± 0.0014 mM, for 2. If these sulfonamide derivatives are proposed as drugs, some of which are being used in glaucoma treatment such as acetazolamide and dorzolamide, these results should be taken into consideration concerning via these enzymes.     

Production of NO and N2O by the Heterotrophic Nitrifier Alcaligenes faecalis parafaecalis under Varying Conditions of Oxygen Saturation

Production of NO and N ₂ O by the heterotrophic nitrifier Alcaligenes faecalis subsp. parafaecalis was studied during growth in batch and continuous culture on peptone-meat extract medium. Depending on oxygen saturation level, medium redox status and amount of substrate supplied, the microorganisms produced 0.002–0.25 mg NO-N h^{- 1} (g protein)^{- 1} and 0.16–2.4 mg N ₂ O-N h^{- 1} (g protein)^{- 1} . Maximum rates of nitrogen oxides production were observed during peak events initiated by sudden changes of oxygen supply in the medium and were due to combined nitrification/denitrification taking place simultaneously within the cells. Based on model simulations of enzymatic kinetics of denitrification, possible mechanisms of increased nitrogen oxides production during periods of changes in oxygen supply are suggested.     

基层医疗卫生机构的基本医疗服务范围研究 ——基于常见病、多发病的视角

目的 基于常见病、多发病的视角界定基层医疗卫生机构的基本医疗服务范围。方法 以广东省A市为例,根据该市基本医疗保险参保人的微观数据,统计分析了该市的常见病、多发病,并对该市128个医疗机构进行问卷调查。结果 分别确定了社区卫生服务中心104个病种、乡镇卫生院101个病种、社区卫生服务站38个病种和村卫生室34个病种作为四类基层医疗卫生机构的基本医疗服务范围。结论 应依据四类基层医疗卫生机构的基本医疗服务范围从诊疗项目、药品目录、基层首诊制等方面进行政策调整与完善。