Synthesis and biological evaluation of 3-(azolylmethyl)-1H-indoles and 3-(α-azolylbenzyl)-1H-indoles as selective aromatase inhibitors

This present study identifies a number of azolyl-substituted indoles as potent inhibitors of aromatase. In the sub-series of 3-(azolylmethyl)-1H-indoles, four imidazole derivatives and their triazole analogues were tested. Imidazole derivatives 11 and 14 in which the benzyl moiety was substituted by 2-chloro and 4-cyano groups, respectively, were the most active, with IC₅₀ values ranging between 0.054 and 0.050 μM. In the other sub-series, eight 3-(α-azolylbenzyl)-1H-indoles were prepared and tested. Compound 30, the N-ethyl imidazole derivative, proved to be an aromatase inhibitor, showing an IC₅₀ value of 0.052 μM. All target compounds were further evaluated against 17α-hydroxylase/C17,20-lyase to determine their selectivity profile.     

House mouse dispersal in Iron Age Spain: a geometric morphometrics appraisal

During the Iron Age, sea trade in the Mediterranean increased, particularly with the expansion of Phoenician and Greek colonies in the Western Mediterranean. A side effect of these human movements was the involuntary dispersion of commensal species, such as the house mouse (Mus musculus domesticus). One archaeological layer dated from the 4th Century BC, coming from an Iberian village located in the Mediterranean coast of Spain, contained a large and reliable accumulation of small mammals. The presence of the house mouse was highly suspected within this layer. To assess its abundance quantitatively, we used a geometric morphometrics approach of the first lower molar contour using elliptical Fourier analysis. We also increased the power of the discrimination between the Algerian mouse (Mus spretus) and the house mouse by combining a dimension reduction approach together with different validation procedures. The relative importance of age, sex, and geographical origin onto the shape and form of the lower molar contour was also investigated. The results obtained demonstrate the presence and the dominance of the house mouse in the landscape surrounding the Iberian village in the 1st Millennium BC, only a few centuries after its arrival in the Western Mediterranean Basin. A cross‐validated linear discriminant function considering different Mediterranean populations suggest Morocco and France as the most probable geographical origins for the Algerian mouse, and Tunisia for the origin of house mice in North‐Eastern Spain. © 2011 The Linnean Society of London, Biological Journal of the Linnean Society, 2011, 102 , 483–497.     

The Mechanism of Temperature Dependent Sex Determination in Crocodilians: A Hypothesis

Incubation of alligator eggs at 30°C produces 100% females,at 33°C 100% males; temperatures in between produce varyingsex ratios. Wild nests of Alligator mississippiensis show similareffects and the populations are biased towards females. Theincidence and patterns of temperature dependent sex determination(TSD) in other crocodilians are reviewed. Temperature also affectshatchling size and pigmentation patterns, post-hatching growthrates and thermoregulation by juvenile crocodilians. The significanceof temperature sensitive periods defined by temperature shiftexperiments is questioned in relation to a hypothesis to explainthe mechanism of TSD in crocodilians. It is postulated thatthere is an initial sex differentiation mechanism which involvesa quantum period of time and a threshold for a dose of a maledetermining factor. The conditions for induction of males areprecise but exhibit variation between individuals within thepopulation. Females develop by default. The hypothalamus mayhave an important role in a later sex differentiation mechanism.The hypothesis is used to explain the late temperature sensitiveperiods defined by high to low temperature shift experiments,why cooler temperatures are more effective at determining sex,how intermediate temperatures can produce both sexes, the differencesin the pattern between turtles and crocodilians and geographicalsimilarities in the pattern of TSD within crocodilians despitediffering climates. The phylogenetic advantages of TSD in crocodiliansare concerned with the overall reproductive strategy of theanimals. Those crocodilians which are incubated and grow tomaturity under optimal environmental conditions will be bothlarge and male. Larger males are more likely to produce moreoffspring. A review of the effects of the environment on sexdetermination in amphibians and fish suggests that there isa general relationship between size and sex in vertebrates     

Mites in the mist: How unique is a rainforest canopy-knockdown fauna?

Abstract We intensively sampled the parasitiform mite faunas of three subtropical rainforest canopy habitats (leaves, bark, hanging humus) and three forest floor habitats (leaf litter, fungal sporocarps, arthropod associates) in the Green Mountains section of Lamington National Park, Queensland, and compared them to 423 specimens collected from the canopy by pyrethrin knockdown (PKD). In total, 165 species (80% new to science) were identified, including 58 from PKD. Few species occurred in more than one habitat, and complementarity averaged 96 ± 1%. About half of the species from PKD were found in canopy habitats, but less than 10% occurred in forest floor habitats. Thus, the canopy fauna is composed primarily of canopy specialists, not of forest floor mites, and habitat specificity is a major component of acarine diversity. An Incidence-based Coverage estimator (generated by the EstimateS program) proved useful in predicting asymptotes for collector's curves. Conservative extrapolations from this study suggest that more than 2000 species of mites live in subtropical rainforest in the Green Mountains.     

The butterfly Danaus chrysippus (L.) in East Africa: polymorphism and morph-ratio clines within a complex, extensive and dynamic hybrid zone

Samples of the polymorphic butterfly Danaus chrysippus are analysed from six well separated sites in East Africa. Morph-ratio clines are described for four diallelic genes A, B, C and L, each of which influences the visual phenotype. Each of the four clines has a different orientation, consistent with an hypothesis that the polymorphism originated from hybridization between a number of polytypic denies which have at various times undergone range expansion. Allopatric subspeciation in isolated Pleistocene refugia is postulated. The phenotype of each geographical race is shared with one of the morphs within the hybrid zone; other sympatrically maintained polymorphic forms are normally confined to the hybrid zone. Wright's isolation-by-distance model best explains the present distribution of gene frequencies. Morph-ratios differ significantly between the sexes and are sometimes associated with heterozygote excess; gametic and genotypic disequilibria are general throughout the region and suggest the clines are maintained by strong natural selection. Seasonal cycling of phenotype frequency is believed to result from extensive migratory movements rather than natural selection. Female-biased sex-ratio, which is also seasonal, and Haldanc rule effects, result from hybrid breakdown when genetically distinct demes meet and interbreed. Oscillating sex-ratios and frequency of colour genes are functionally linked by negative feedback. The polymorphism owes its origin to allopatrie evolution but is now maintained sympatrically.     

Cat Interferon inhibits Feline Leukaemia Virus Infection in Cell Culture

TRANSMISSION of feline leukaemia can be accomplished with tissue extracts from cases which occur naturally¹. Virus particles which are morphologically indistinguishable from the murine and avian C-type viruses are present in cats with the transmitted disease². Feline leukaemia virus (FeLV) replicates in cat cell cultures³ and infected cells are demonstrable by the indirect immunofiuorescent antibody test which detects FeLV group-specific antigen as granular punctate fluorescence in the cytoplasm of acetone fixed cells⁴; this method allows easy quantitation of the antiviral effect of interferon. We report the production and assay of feline interferon using the fluorescent antibody test with FeLV infected cat cell cultures.     

MtPM25 is an atypical hydrophobic late embryogenesis‐abundant protein that dissociates cold and desiccation‐aggregated proteins

Late embryogenesis‐abundant (LEA) proteins are one of the components involved in desiccation tolerance (DT) by maintaining cellular structures in the dry state. Among them, MtPM25, a member of the group 5 is specifically associated with DT in Medicago truncatula seeds. Its function is unknown and its classification as a LEA protein remains elusive. Here, evidence is provided that MtPM25 is a hydrophobic, intrinsically disordered protein that shares the characteristics of canonical LEA proteins. Screening protective activities by testing various substrates against freezing, heating and drying indicates that MtPM25 is unable to protect membranes but able to prevent aggregation of proteins during stress. Prevention of aggregation was also found for the water soluble proteome of desiccation‐sensitive radicles. This inhibition was significantly higher than that of MtEM6, one of the most hydrophilic LEA protein associated with DT. Moreover, when added after the stress treatment, MtPM25 is able to rapidly dissolve aggregates in a non‐specific manner. Sorption isotherms show that when it is unstructured, MtPM25 absorbs up to threefold more water than MtEM6. MtPM25 is likely to act as a protective molecule during drying and plays an additional role as a repair mechanism compared with other LEA proteins.     

Modifications of the metapostnotum and origin of the 'propodeal triangle' in Hymenoptera Aculeata

The metapostnotum of aculeate Hymenoptera shows three trends of modification: simple reduction in Bethyloidea, invagination and reduction in Vespoidea and enlargement (forming the ‘propodeal triangle’) in Sphecoidea (including bees). The second phragma is also variously modified in thete three groups to allow maximal development of the dorsal longitudinal indirect flight muscles of the mesothorax.