Old and new hypotheses about the homology of the compound bones from the cheek and otico-occipital regions of the anuran skull

We studied the larval development of compound bones from the otico-occipital and cheek regions in species of the neobatrachian genera Batrachyla, Hylorina, Leptodactylus, Odontophrynus and Pleurodema. Comparisons were made using a set of Ambystoma spp. (Caudata) and Ceratophrys ornata (Anura; Ceratophryidae) larvae. As suggested by previous studies, we verified the compound nature of the exoccipital (two centers, anurans only), frontoparietal (one center, most anurans and Ambystoma; three centers, some anurans), and squamosal (two centers, all anurans and Ambystoma) bones. We discuss old and new homology hypotheses for each of the compound bone centers in the context of the most widely accepted scenario of lissamphibian origins and relationships, i.e., monophyletic Lissamphibia that includes the clade Batrachia (Caudata + Anura) and the most divergent Gymnophiona. Our findings have a direct impact on our understanding of the composition of the skull in Lissamphibia. We recognized the presence of the following bones: (i) opisthotic (fused to the exoccipital) and tabular (fused to the squamosal) in Batrachia (Anura + Caudata) and (ii) supratemporal (fused to the parietal portion of the frontoparietal) in Anura. Separate centers of the parietal were found only in Pleurodema.     

Distribution and interspecific correlation of root biomass density in an arid Elaeagnus angustifolia–Achnatherum splendens community

Main objective of this study was to determine the interspecific relationships between two dominant species in terms of root distribution in a typical arid tree-herbage (Elaeagnus angustifolia–Achnatherum splendens) community at Xidatan, Pingluo County, Ningxia Autonomous Region, Northwest China. Eight concentric zones (namely, Z1–Z8) were set from the bases of E. angustifolia individuals to the open lands and five soil profiles were excavated in each zone. Each soil profile was divided into five layers at the depths of 0–10 cm, 10–30 cm, 30–60 cm, 60–100 cm and 100–150 cm. Roots were collected for each species, and soil water content (SWC) and soil bulk density (SBD) were measured for each layer. We found noteworthy roots layer separation in the sub-canopy zones (Z1–Z4). The soil layers with highest fine root biomass density (FRBD) of A. splendens was primarily in the 0–10 cm, which were significantly shallower than those of E. angustifolia; whereas in the inter-canopy zones (Z5–Z8), inconsistent separation, or even overlapping of highest-FRBD-layers emerged between the two dominant species. Correlation analyses showed that negative correlations of FRBD between the two species mainly occurred in those soil layers with relatively higher FRBD and lower SWC. In contrast, positive correlations corresponded with relatively lower FRBD and higher SWC.     

Community congruence of plants,invertebrates and birds in natural and constructed shallow open-water wetlands: Do we need to monitor multiple assemblages?

Biomonitoring is a common means of evaluating wetlands. It is based on the premise that the community composition of one taxonomic group is indicative of overall biology and the underlying environmental conditions at a wetland. To be a good bioindicator, there must be adequate concordance between the indicator group and other biotic assemblages. Otherwise, multi-assemblage monitoring is necessary to glean a complete picture of wetland condition. In 32 sites ranging from reference wetlands to stormwater retention ponds, we evaluated concordance in community composition among the six most commonly monitored wetland assemblages: waterfowl, wetland dependent songbirds, aquatic macroinvertebrates, and plants in the wet meadow, emergent, and open-water vegetation zones. We also assessed agreement in environmental correlates among these six assemblages and investigated the impact of human disturbance on cross-assemblage concordance. We found that cross-assemblage concordance was positive (p < 0.03 in 14 of 15 pair-wise comparisons, p = 0.06 in 15th case), but relatively low (Mantel R values 0.11–0.37), suggesting that the assemblages are mediocre surrogates for one another. Yet, we found very strong agreement among environmental correlates of the six assemblages, especially along the first axis of assemblage-specific ordinations (mean Spearman rho = 0.923), indicating that despite low concordance, the six assemblages are likely responding to the same environmental gradients. Thus, while a single assemblage may not serve as a surrogate for the other assemblages, it should yield an adequate estimate of underlying environmental conditions and the degree of disturbance. Most important among the environmental correlates were sediment and water nutrient levels, shoreline slope, and the size of wet meadow and emergent vegetation zones. Perhaps most interestingly, we found that the strength of cross-assemblage concordance was greatest in reference wetlands and was lower (p ≤ 0.05) in constructed wetlands. This implies that cross-assemblage concordance present in undisturbed sites may not persist in disturbed wetlands where several of these cross-assemblage relationships deteriorate. Furthermore, a general change in cross-assemblage concordance may itself be indicative of human disturbance in wetlands.     

2-OMe-lysophosphatidylcholine analogues are GPR119 ligands and activate insulin secretion from βTC-3 pancreatic cells: Evaluation of structure-dependent biological activity

GPR119 receptor has been proposed as a metabolic regulator playing a pivotal role in the modulation of glucose homeostasis in type 2 diabetes. GPR119 was identified on pancreatic β cells and its ligands have the ability to enhance glucose-stimulated insulin secretion (GSIS). Lysophosphatidylcholine (LPC) was shown to potentiate GSIS and our present studies indicate that 2-methoxy-lysophosphatidylcholine (2-OMe-LPC) analogues, unable to undergo 1 → 2 acyl migration, stimulate GSIS from murine βTC-3 pancreatic cells even more efficiently. Moreover, biological assays in engineered Tango? GPR119-bla U2OS cells were carried out to ascertain the agonist activity of 2-OMe-LPC at GPR119. 2-OMe-LPC possessing in sn-1 position the residues of myristic, palmitic, stearic and oleic acid were also evaluated as factors regulating [Ca^2 +]_i mobilization and cAMP levels. Extension of these studies to R- and S-enantiomers of 14:0 2-OMe-LPC revealed that the overall impact on GSIS does not depend on chirality, however, the intracellular calcium mobilization data show that the R enantiomer is significantly more active than S one. Taking into account differences in chemical structure between various native LPCs and their 2-methoxy counterparts the possible binding mode of 2-OMe-LPC to the GPR119 receptor was determined using molecular modeling approach.     

Ambulatory dispersal of the susceptible and propargite-resistant strains of Tetranychus urticae and its influence on pesticide resistance dynamics

The distribution of resistant individuals is determined by the amount of movement between populations. The differential rate of dispersal of a susceptible and a pesticide-resistant strain could influence the resistance dynamics under field conditions. The dispersal rate and dispersal efficiency of the susceptible and propargite-resistant strains of Tetranychus urticae were measured in separate-release and mixed-release experiments. The diffusion coefficient (D) of both strains did not differ significantly (P > 0.344) and an estimate of the asymptotic rate of advance (2 √ rD) (for one generation) was estimated at 0.1047 and 0.0930 cm per degree day for the susceptible and propargite-resistant strains, respectively. The dispersal efficiency of the two strains differed significantly (P < 0.005) as more susceptible mites than propargite-resistant mites crossed into specified zones more quickly after 290 and 366 degree days. Significantly (P < 0.05) higher number of susceptible adults, immatures and eggs were found in the outer most zone of an arena as compared to that of the propargite-resistant mites. The bioassay of the two strains showed a similar pattern of the spread of the adult females across the specified zones in the mixed-release experiment. The relatively lower dispersive tendency of the propargite-resistant T. urticae and the smaller proportion of adult females exhibiting that behaviour increase the chances of developing resistant ‘hotspots’ in field specially after an acaricide application.     

Discovery and structure–activity relationship studies of quinolinone derivatives as potent IL-2 suppressive agents

The quinolinone skeleton has been utilized to develop various mechanism-based immune modulators. However, the effects of quinolinone derivatives on the release of T cell-associated interleukin-2 (IL-2) have not been established. In this study, a series of novel quinolinone derivatives was synthesized, and their immunosuppressive activity was evaluated by measuring suppression of IL-2 release from activated Jurkat T cells. Optimizing the three side chains around the quinolinone skeleton revealed the most active compound: 11l. This compound exhibits potent inhibitory activity toward IL-2 release in both 12-o-tetradecanoylphorbol-13-acetate (PMA)/A23187 (ionomycin) (IC₅₀ = 80 ± 10 nM) and anti-CD3/CD28-stimulated Jurkat T cells (83% inhibition at 10 μM) without cytotoxic effects. Further investigation into the underlying mechanism of 11l indicated the suppression of NF-κB and nuclear factor of activated T cells (NFAT) promoter activities in Jurkat T cells.     

Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: Selectivity switching by C/Si exchange

We previously reported that bis-phenol derivatives, including LG190178 (3a), possess not only vitamin D receptor (VDR) agonistic activity, but also androgen receptor (AR) antagonistic activity. Here, we describe the design, synthesis and evaluation of silicon-containing bis-phenol derivatives, with the objective of obtaining increased selectivity toward VDR or AR. We found that replacement of the quaternary carbon in the bis-phenol skeleton with silicon increased AR-antagonistic activity and reduced VDR-agonistic activity, that is, the AR selectivity of the silicon-containing compounds was higher than that of corresponding carbon compounds. To our knowledge, this is the first report of nuclear receptor (NR) selectivity switching by sila-substitution (C/Si exchange). Among the compounds synthesized, AR-selective ligand (S,R)-3b exhibited more potent anti-androgenic activity (IC₅₀ = 0.072 μM) than hydroxyflutamide, a well-known androgen antagonist (IC₅₀ = 1.4 μM), in SC-3 cell proliferation assay. These results suggest that sila-substitution is a useful approach for structural development of selective AR ligands.     

Chemical composition,angiotensin I-converting enzyme (ACE) inhibitory,antioxidant and antimicrobial activities of the essential oil from south Tunisian Ajuga pseudoiva Rob. Lamiaceae

The essential oil of Ajuga pseudoiva, collected from Tunisia, was analyzed using gas chromatography–mass spectroscopy. Thirty-two compounds accounting for 95.76% of the total oil were identified. Sesquiterpenes were found to be the most abundant components of A. pseudoiva oil. And they were mainly represented by viridiflorol (30.17%), germacrene B (9.26%) (α, β and γ)-eudesmol (8.11%) and aromadendrene (7.45%). The essential oil of A. pseudoiva showed radical scavengers activity (IC₅₀ = 0.72 mg/mL) and displayed lipid peroxidation inhibitory activity (IC₅₀ = 0.6 mg/mL). A. pseudoiva essential oil was also found to exhibit a dose-dependent ACE inhibitory activity with an IC₅₀ value of 65.5 μg/mL. Moreover, the antimicrobial activity of the essential oil was tested against 17 species of microorganisms, and the results obtained showed significant antibacterial activity against the Gram-positive and Gram-negative bacteria, with inhibition zones and minimal inhibitory concentration values of 14–32 mm and 84–137 μg/mL and 6–21 mm and 105–336 μg/mL, respectively. Higher activity was also found against several fungal strains.     

Gene-based copy number variation study reveals a microdeletion at 12q24 that influences height in the Korean population

Height is a classic polygenic trait with high heritability (h² = 0.8). Recent genome-wide association studies have revealed many independent loci associated with human height. In addition, although many studies have reported an association between copy number variation (CNV) and complex diseases, few have explored the relationship between CNV and height. Recent studies reported that single nucleotide polymorphisms (SNPs) are highly correlated with common CNVs, suggesting that it is warranted to survey CNVs to identify additional genetic factors affecting heritable traits such as height.This study tested the hypothesis that there would be CNV regions (CNVRs) associated with height nearby genes from the GWASs known to affect height. We identified regions containing > 1% copy number deletion frequency from 3667 population-based cohort samples using the Illumina HumanOmni1-Quad BeadChip. Among the identified CNVRs, we selected 15 candidate regions that were located within 1 Mb of 283 previously reported genes. To assess the effect of these CNVRs on height, statistical analyses were conducted with samples from a case group of 370 taller (upper 10%) individuals and a control group of 1828 individuals (lower 50%).We found that a newly identified 17.7 kb deletion at chromosomal position 12q24.33, approximately 171.6 kb downstream of GPR133, significantly correlated with height; this finding was validated using quantitative PCR. These results suggest that CNVs are potentially important in determining height and may contribute to height variation in human populations.     

Discovery and optimization of N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamides as novel GPR119 agonists

The discovery and optimization of novel N-(3-(1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-4-yloxy)phenyl)benzenesulfonamide GPR119 agonists is described. Modification of the pyridylphthalimide motif of the molecule with R¹ = –Me and R² = –ⁱPr substituents, incorporated with a 6-fluoro substitution on the central phenyl ring offered a potent and metabolically stable tool compound 22.     

Synthesis and antimicrobial studies of novel derivatives of 4-(4-formyl-3-phenyl-1H-pyrazol-1-yl)benzoic acid as potent anti-Acinetobacter baumannii agents

Microbial resistance to antibiotics is a global concern. The World Health Organization (WHO) has identified antimicrobial resistance as one the three greatest threats for human beings in the 21st century. Without urgent and coordinated action, the world is moving toward a post-antibiotic era, in which normal infections or minor injuries may become fatal. In an effort to find new agents, we report the synthesis and antimicrobial activities of 40 novel 1,3-diphenyl pyrazole derivatives. These compounds have shown zones of growth inhibition up to 85 mm against Acinetobacter baumannii. We tested the active compounds against this Gram-negative bacterium in minimum inhibitory concentration (MIC) tests and found activity with concentration as low as 4 μg/mL.     

The exon/intron organization of the globin gene of Scapharca inaequivalvis homodimeric hemoglobin: unusual intron homology with other bivalve mollusc globin genes

In this study, we have investigated the positions of introns in the globin gene of Scapharca inaequivalvis homodimeric hemoglobin. We found the three exon/two intron organization typical of vertebrate globin genes, with the two introns in highly conserved positions, as it occurs in the A and B globin genes of the tetrameric hemoglobin from the same organism, confirming the absence of the so-called `central intron' found in the globin genes of plants and of some invertebrates. We identified two homodimeric globin genes (3207 and 2723 bp) that differ only with respect to the size of the first intron. Sequence analysis of the two first introns (1668 and 1364 bp) has revealed that they are highly homologous, except for a 569- and 296-bp insertion in each intron I. Interestingly, the two first introns contain regions with an unusually high identity (∼80%) with regions of the first intron of the congeneric clam Anadara trapezia and the related clam Barbatia reveana globin genes, suggesting that these uncoding regions may have played a regulatory role that has subsequently been lost during the course of the evolution.     

Vertebrate extracellular calcium-sensing receptor evolution: Selection in relation to life history and habitat

Ionic calcium (Ca^2 +) supports essential functions within physiological systems, and consequently its concentration is homeostatically regulated within narrow bounds in the body fluids of animals through endocrine effects at ion-transporting osmoregulatory tissues. In vertebrates, extracellular Ca^2 + is detected at the cell surface by the extracellular calcium-sensing receptor (CaSR), a member of the G protein-coupled receptor (GPCR) superfamily. Interestingly, the taxonomic distribution of CaSRs is restricted to vertebrates, with some CaSR-like receptors apparently present in non-vertebrate chordates. Since bone is a known Ca^2 + storage site and is characteristically restricted to the vertebrate lineage, we hypothesized a functional association of CaSR with vertebrate skeleton that may have an ancient origin. Protein sequence alignment and phylogenetic analysis of vertebrate CaSRs and related GPCRs of the glutamate receptor-like family expose similarities and indel differences among these receptors, and reveal the evolutionary history of CaSRs. Evolutionary selection was tested statistically by evaluating the relationship between non-synonymous (replacement, dN) versus synonymous (silent, dS) amino acid substitution rates (as dN/dS) of protein-coding DNA sequences among branches of the estimated protein phylogeny. On a background of strong purifying selection (dN/dS < 1) in the CaSR phylogeny, statistical evidence for adaptive evolution (dN/dS > 1) was detected on some branches to major clades in the CaSR phylogeny, especially to the tetrapod vertebrate CaSRs and chordate CaSR-like branches. Testing also revealed overall purifying selection at the codon level. At some sites relaxation from strong purifying selection was seen, but evidence for adaptive evolution was not detected for individual sites. The results suggest purifying selection of CaSRs, and of adaptive evolution among some major vertebrate clades, reflecting clade specific differences in natural history and organismal biology, including skeletal involvement in calcium homeostasis.     

Maxillary tooth growth in the adult male babirusa (genus Babyrousa)

The growth of the maxillary canine teeth of the babirusa (genus Babyrousa) was studied on a sample of 149 adult male babirusa skulls from twenty-two international museum and private collections. Skulls from Buru, Sulawesi and the Togian Islands were represented. The continuous growth process was summarised into five stages (‘A’–‘E’) according to the position of the tip of the tooth over the bones of the skull. The supracutaneous portion of the tooth grew in a curve-linear fashion dorso-caudally, and was orientated such that the tips grew towards the midline of the cranium. The teeth of Sulawesi and Togian babirusa grew more dorsally over the nasal and frontal bones. Measurements were made on a subset of 45 teeth from Sulawesi babirusa skulls. The subcutaneous portion of the maxillary canine tooth (n = 22) increased in size from 37.3 mm (95% CI: 29.9–44.4 mm) in growth stage ‘B’ to 54.3 mm (49.4–59.2 mm) in growth stage ‘E’ as the erupted portion of the tooth (n = 19) lengthened from 81.3 mm (43.8–118.9 mm) in growth stage ‘A’ to 215.3 mm (177.8–252.9 mm) in growth stage ‘E’. The apical end of the tooth was open and thin-walled. The lumen of the tooth was filled with a cone of well vascularised dental pulp that extended almost to the tip of the tooth. The angle of curvature of the tooth within the alveolus (n = 22) decreased from 19.8 (17.3–22.3) degrees in growth stage ‘B’ to 7.4 (5.7–9.0) degrees in growth stage ‘E’. The corresponding supracutaneous angle of curvature (n = 25) reduced from 36.8 (33.6–40.1) degrees in growth stage ‘A’ to 10.7 (8.6–12.8) degrees in growth stage ‘E’.     

Construction history of the Deason House,Jones County,Mississippi

The Deason House is located in the heart of the Piney Woods region in the town of Ellisville, Mississippi. During the American Civil War, the Deason House became the epicenter for an event that started a rebellion against the Confederate government. On 5 October 1863, a Confederate deserter named Newton Knight allegedly shot and killed Confederate Major Amos McLemore in the Deason House, which eventually lead to the formation of the Free State of Jones. Despite the historical importance of the house, oral accounts and written documents have failed to provide accurate construction history of the structure. We coupled techniques of dendrochronology and geophysical survey to better understand the construction history of the Deason House and cultural activities of its inhabitants. We extracted 35 Pinus palustris (Mill.) timbers along the west-facing exterior weatherboards and from various logs within the second-floor attic, 25 of which were successfully crossdated against a P. palustris reference chronology located 15 km south in De Soto National Forest (1742–2013). The Deason House chronology anchored against the De Soto time series during the period 1742–1875 (r = 0.55, t = 4.01, p < 0.0001) and extended the reference chronology back to the year 1680 CE. Clustering of cutting- and near-cutting dates from timbers revealed 3 possible stages of construction. First, the house likely existed as a single-pen structure built in the winter of 1835/1836, based on two timbers with wane/bark that were affixed to the original chimney made of clay bricks fired on the homestead. Second, based on the clustering of 1855 cutting dates, we suggest this was the most likely time the original structure was expanded with a vestibule, porch, and larger 4-room house. Finally, six timbers revealed a back addition was constructed in the year 1866. Ground penetrating radar (GPR) helped provide evidence mentioned in written records that the back addition (1866) existed as the detached kitchen then was affixed to the structure ca. 1890. The GPR data revealed geophysical anomalies that indicated the original sites of the detached kitchen, water well, livestock pen, privies, and trash pit. Through the use of dendrochronological analyses and geophysical survey, we were able to provide an updated history of the Deason House construction dynamics and cultural activities of its inhabitants beyond the historical record.     

Design,synthesis and antibacterial activity studies of thiazole derivatives as potent ecKAS III inhibitors

Two series of thiazole derivatives containing amide skeleton were synthesized and developed as potent Escherichia coli β-ketoacyl-(acyl-carrier-protein) synthase III (ecKAS III) inhibitors. All the 24 new synthesized compounds were assayed for antibacterial activity against the respective Gram-negative and Gram-positive bacterial strains, including E. coli, Pseudomonas aeruginosa, Bacillus subtilis and Staphylococcus aureus. In which, 10 compounds with broad-spectrum antibacterial activities were further tested for their ecKAS III inhibitory activity. Last, we have successfully found that compound 4e showed both the promising broad antibacterial activity with MIC of 1.56–6.25 μg/mL against the representative bacterial stains, and also processed the most potent ecKAS III inhibitory activity with IC₅₀ of 5.3 μM. In addition, docking simulation also carried out in this study to give a potent prediction binding mode between the small molecule and ecKAS III (PDB code: 1hnj) protein.     

Effect of FSH on E2/GPR30-mediated mouse oocyte maturation in vitro

Mammalian oocyte restores meiosis can be stimulated by follicle-stimulating hormone (FSH) under normal physiological conditions. G-protein coupled receptor 30 (GPR30), an non-classical estrogen membrane receptor, has been widely reported in teleost oocyte maturation. However, it remains unknown whether GPR30 involves the role of FSH in mammalian cumulus expansion and oocyte maturation. Here, we used mouse cumulus-oocyte complexes (COCs) as a model to investigate how FSH affects the in vitro maturation of mouse oocytes mediated by 17β-estradiol (E₂)/GPR30 signaling. Our study reveals that FSH starts regulating mouse cumulus expansion precisely at 8 h in in vitro culture. ELISA measurement of E₂ levels in culture medium revealed that FSH activated aromatase to promote E₂ production in vitro in cultured mouse COCs. Moreover, the results of real-time quantitative PCR indicated that FSH-induced in vitro maturation of mouse oocytes was regulated by the estrogen-signaling pathway mediated by GPR30; FSH treatment markedly increased the mRNA expression of HAS2, PTGS2, and GREM1 in COCs. Exploration of the underlying mechanism suggested that E₂ produced by mouse COCs regulated the phosphorylation level of extracellular signal-regulated kinase 1/2 (ERK1/2) through GPR30 and thereby promoted mouse cumulus-cell expansion and oocyte maturation. In conclusion, our study reveals that FSH induced estrogen production in mouse COCs through aromatase, and that aromatase/GPR30/ERK1/2 signaling is involved in FSH-induced cumulus expansion.     

New halogenated 3-phenylcoumarins as potent and selective MAO-B inhibitors

With the aim to find out the structural features for the MAO inhibitory activity and selectivity, in the present communication we report the synthesis and pharmacological evaluation of a new series of bromo-6-methyl-3-phenylcoumarin derivatives (with bromo atom in both different benzene rings of the skeleton) with and without different number of methoxy substituent at the 3-phenyl ring. The methoxy substituents were introduced, in this new scaffold, in the meta and/or para positions of the 3-phenyl ring. The synthesized compounds 3–7 were evaluated as MAO-A and B inhibitors using R-(?)-deprenyl (selegiline) and iproniazide as reference inhibitors, showing, most of them, MAO-B inhibitory activities in the low nanomolar range. Compounds 4 (IC₅₀ = 11.05 nM), 5 (IC₅₀ = 3.23 nM) and 6 (IC₅₀ = 7.12 nM) show higher activity than selegiline (IC₅₀ = 19.60 nM) and higher MAO-B selectivity, with more than 9050-fold, 30,960-fold and 14,045-fold inhibition levels, with respect to the MAO-A isoform.     

A multivariate analysis integrating ecological,socioeconomic and physical characteristics to investigate urban forest cover and plant diversity in Beijing,China

Understanding the factors driving the variation in urban green space and plant communities in heterogeneous urban landscapes is crucial for maintaining biodiversity and important ecosystem services. In this study, we used a combination of field surveys, remote sensing, census data and spatial analysis to investigate the interrelationships among geographical and social-economic variables across 328 different urban structural units (USUs) and how they may influence the distributions of urban forest cover, plant diversity and abundance, within the central urban area of Beijing, China. We found that the urban green space coverage varied substantially across different types of USUs, with higher in agricultural lands (N = 15), parks (N = 46) and lowest in utility zones (N = 36). The amount of urban green space within USUs declines exponentially with the distance to urban center. Our study suggested that geographical, social and economic factors were closely related with each other in urban ecological systems, and have important impacts on urban forest coverage and abundance. The percentage of forest as well as high and low density urban areas were mainly responsible for variations in the data across all USUs and all land use/land cover types, and thus are important constituents and ecological indicators for understanding and modeling urban environment. Herb richness is more strongly correlated with tree and shrub density than with tree and shrub richness (r = −0.472, p < 0.05). However, other geographic and socioeconomic factors showed no significant relationships with urban plant diversity or abundance.     

(E)-2-Styrylchromones as potential anti-norovirus agents

Human noroviruses (NoV) are now recognized as the most frequent cause of outbreaks and sporadic cases of acute gastroenteritis. Despite the significant economic impact and considerable morbidity of norovirus disease, no drug or vaccine is currently available to treat or prevent this disease, therefore the discovery of anti-norovirus drugs is urgent.In the present work, a total of 12 structure related chromone and (E)-2-styrylchromones were evaluated for their potential anti-norovirus activity using the murine norovirus (MNV) as a surrogate model for human NoV.From the 12 compounds studied, six (E)-2-styrylchromones were found to have with interesting anti-norovirus activity. The best compounds of the series were (E)-5-hydroxy-2-styrylchromone and (E)-4′-methoxy-2-styrylchromone with an IC₅₀ ≈ 7 μM. A first insight into the mechanism of action of these compounds was possible. An interesting relationship between the anti-norovirus activity and the chemical structure was observed. The present study points out that the (E)-2-styrylchromones skeleton is an important one which deserves to be developed and further explored as new antiviral drugs against NoV.