7β-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues

With the purpose of identifying novel selective κ opioid receptor (KOR) antagonists as potential antidepressants from nepenthone analogues, starting from N-nor-N-cyclopropylmethyl-nepenthone (SLL-020ACP), a highly selective and potent KOR agonist, a series of 7β-methyl-nepenthone analogues was conceived, synthesized and assayed on opioid receptors based on the concept of hybridization. According to the pharmacological results, the functional reversal observed in orvinol analogues by introduction of 7β-methyl substituent could not be reproduced in nepenthone analogues. Alternatively, introduction of 7β-methyl substituent was associated with substantial loss of both subtype selectivity and potency but not efficacy for nepenthone analogues, which was not found in 7β-methyl orvinol analogues. Surprisingly, SLL-603, a 7β-methyl analogue of SLL-020ACP, was identified to be a KOR full agonist. The possible molecular mechanism for the heterogeneity in activity cliff was also investigated. In conclusion, 7β-methyl substituent was a structural locus associated with activity cliff and demonstrated as a pharmacological heterogeneity between nepenthone and orvinol analogues that warrants further investigations.     

Factors affecting the co-existence of the serpentine endemic Mimulus nudatus Curran and its presumed progenitor, Mimulus guttatus Fischer ex DC

Population genetics theory suggests that two species which are reproductively isolated only by postzygotic barriers cannot co-exist in sympatry since the rarer population will become extinct. Mimulus nudatus and Mimulus guttatus are two closely related species that are isolated by a postzygotic barrier operating at the seed provisioning stage. On several sites on die serpentine soils of Lake and Napa counties, California, M. nudatus and M. guttatus live in sympatry and flowering times of the species overlap, so the species are sometimes flowering next to each other. We investigated whether there was any reduction in fertility of M. nudatus and M. guttatus caused by interspecific crosses when growing in sympatry. The pollinators of M. nudatus and M. guttatus were identified. Small sweat bees, Dialictus sp., preferentially visited the smaller flowered M. nudatus species and honey bees, Apis mellifera , preferred the larger flowered M. guttatus . In spite of most pollinator visits being intra-specinc, individuals of bodi bee species made transitions between the Mimulus species. This will result in greater pollen transfer from M. guttatus to M. nudatus than vice versa because firstly, M. guttatus produces more pollen and secondly, the sweat bees were too small to touch the stigma of a M. guttatus flower. This asymmetry in gene flow was detected by a greater reduction in viable seed produced by M. nudatus plants when surrounded by M. guttatus plants dian vice versa. Only when M. nudatus was the maternal parent could any hybrids be detected in field produced seed. To enable M. nudatus and M. guttatus to co-exist in sympatry, the two species may thus need to be sufficiendy ecologically different. Such ecological differentiation was attributed to the greater drought tolerance of M. nudatus . In addition, greenhouse experiments suggested that M. nudatus may have evolved greater tolerance to calcium deficient soils.     

Classification of insects by echolocating greater horseshoe bats

Summary Echolocating greater horseshoe bats (Rhinolophus ferrumequinum) detect insects by concentrating on the characteristic amplitude- and frequency modulation pattern fluttering insects impose on the returning echoes. This study shows that horseshoe bats can also further analyse insect echoes and thus recognize and categorize the kind of insect they are echolocating.Four greater horseshoe bats were trained in a twoalternative forced-choice procedure to choose the echo of one particular insect species turning its side towards the bat (Fig. 1). The bats were able to discriminate with over 90% correct choices between the reward-positive echo and the echoes of other insect species all fluttering with exactly the same wingbeat rate (Fig. 4).When the angular orientation of the reward-positive insect was changed (Fig. 2), the bats still preferred these unknown echoes over echoes from other insect species (Fig. 5) without any further training. Because the untrained bats did not show any prey preference, this indicates that the bats were able to perform an aspect-anglein-dependent classification of insects.Finally we tested what parameters in the echo were responsible for species recognition. It turned out that the bats especially used the small echo-modulations in between glints as a source of information (Fig. 7). Neither the amplitudenor the frequencymodulation of the echoes alone was sufficient for recognition of the insect species (Fig. 8). Bats performed a pattern recognition task based on complex computations of several acoustic parameters, an ability which might be termed cognitive.Abbreviations AM amplitude modulation - CF constant frequency - FM frequency modulation - S+ positive stimulus - S- negative stimulus     

Picture perception in monkeys and pigeons: Transfer of rightside-up versus upside-down discrimination of photographic objects across conceptual categories

Monkeys and pigeons were trained to discriminate between normally oriented full frontal pictures of humans and upside-down reversals of the same pictures as stimuli. Monkeys displayed a high level of transfer to the new pictures of full frontal and rear views of humans and silhouettes, but failed to transfer to the close-up and far human faces. Pigeons showed poorer transfer to the silhouettes and higher transfer to the far human faces than did monkeys. Further transfer tests were performed with non-human pictures, including monkeys, birds, mammals, and man-made objects. Pigeons failed to transfer to the non-human pictures. This indicates that the pigeons had learned to classify the pictures based on some concrete features specific to the humans and that the transfer to the new versions of human pictures could be explained by simple stimulus generalization based on perceptual similarity. Two out of four monkeys did transfer fairly well to the non-human pictures, except for the man-made objects. High levels of transfer to the non-human natural pictures suggested that the monkeys classified the pictures on the basis of the orientation of objects represented by the pictorial displays. A preliminary report was presented by the first author (M. J.) at the 13th Congress of the International Primatological Society, Nagoya, Japan, 1990. The present research was supported in part by a Grant-in-Aid for General Scientific Research, the Ministry of Education, Science, and Culture, No. 02301017 (principal researcher:Tadasu Oyama, Nihon University) to M. J. The monkey experiments were conducted at the Primate Research Institute, Kyoto University, and the pigeon experiments at the Department of Psychology, Chiba University.     

“关于建立植物区系特征参数的设想”的理论问题

本文就“关于建立植物区系特征参数的设想”一文中几个主要理论问题即植物区系的有关概念、植物分类系统的主要缺陷和植物区系的特征等进行了分析和讨论,并提出了自己的主张和看法。     

Understanding diversity in coral-algal symbiosis: a cluster-based approach to interpreting fine-scale genetic variation in the genus <Emphasis Type="Italic">Symbiodinium</Emphasis>

Reef corals associate with an extraordinary diversity of dinoflagellate endosymbionts (genus Symbiodinium), and this diversity has become critical to understanding how corals respond to environmental changes. A popular molecular marker for Symbiodinium diversity, the Internal Transcribed Spacer-2 (ITS-2) region of ribosomal DNA, has revealed hundreds of distinct variants that are generally interpreted as representing different species, even though many have not been systematically tested for functional or ecological differentiation. Many of these variants are only minimally divergent from one another (1 bp or less), and others occupy basal nodes of traditional species phylogenies (“living ancestors”), indicating that some Symbiodinium ITS-2 diversity may represent intraspecific sequence variation. This hypothesis was tested for Symbiodinium clades A–D (the dominant symbionts of reef corals) through the construction of statistical parsimony networks of ITS-2 sequence diversity, and identification of clusters of closely related sequences within these networks. Initial assessments indicated that ecological differentiation exists between, but not within, these clusters. This approach, although imperfect in its ability to identify species boundaries in all cases, nevertheless dramatically reduces “species” diversity in Symbiodinium (from ~175 to 35). This testable alternative hypothesis indicates that, in Symbiodinium, “species” consist of clusters of closely related ITS-2 sequences diverging from ancestral variants that are typically ecologically dominant. A cluster-based view of Symbiodinium ITS-2 diversity improves our ability to: (1) construct well-supported symbiont phylogenies; (2) establish functional niches for symbiont species; and (3) understand flexibility and specificity within coral-algal symbioses. This cluster-based approach can ultimately be integrated with emerging population-level datasets (microsatellites and microsatellite flanking regions) to improve understanding of species diversity in Symbiodinium. Electronic supplementary material  The online version of this article (doi:) contains supplementary material, which is available to authorized users. Communicated by Biology Editor Dr Ruth Gates     

Increasing the emphasis of vocational qualifications

Understanding how people think and how people organise knowledge are always major concerns for educational researchers. Hence, educators have developed various ways of representing learners' ‘cognitive structures‘. This article provides a review of the use of five methods of representing cognitive structures - free word association, controlled word association, tree construction, concept map and flow map. Through comparing the types of analyses that are generated from these cognitive structure representation methods, this paper discusses the applications, as well as the limitations, among these methods.     

Attempting to break the code in student comprehension of genetic concepts

Conducted in Israel, this research probes students' understanding of the relationships between genetic concepts. Four populations were examined: 9th graders (14–15 year olds), who were exposed to genetics for the first time (n = 184); 12th graders (17–18 year olds), who were studying biology as their main subject (n = 121); college pre-service teachers, who had not yet earned a degree (n = 29); and university pre-service teachers, who had earned biology degrees and were seeking teacher certification (n = 22). Three research instruments were used: a written questionnaire, interviews, and concept maps. The questions were open-ended to enable the identification of students' patterns of comprehensive thinking and understanding, not identifiable in multiple choice testing. Alternative conceptions and compartmentalisation between related concepts were identified. Based on these findings, genetic instruction in 9th and 12th grade and in college needs improvement.