Three new species,a new combination,and a neotypification in <Emphasis Type="Italic">Dahlstedtia</Emphasis> (Leguminosae,Millettieae, Papilionoideae) from South America

Three new species of Dahlstedtia, D. burkartii, D. dehiscens, and D. lewisiana, are described from South America, and their relationships with related species are discussed. Dahlstedtia burkartii, from Argentina, has pink flowers with standard straight, whereas D. dehiscens and D. lewisiana, both from Brazil, have purplish to lilac flowers with a reflexed standard petal. A new combination, Dahlstedtia peckoltii, is proposed based on Lonchocarpus peckoltii and a neotype is selected for the latter. Information about geographic distribution and phenology of the species is provided.     

Bobgunnia, a new African genus of tribe Swartzieae (Fabaceae, Faboideae)

A new genus, Bobgunnia, is established in tribe Swartzieae for the African species of Swartzia. Two new combinations are made: B. fistuloides and B. madagascariensis. The new genus has seeds, unlike the remainder of tribe Swartzieae but like the other tribes of Faboideae. The systematic position of Swartzieae is reevaluated.     

Design,synthesis of novel pyranotriazolopyrimidines and evaluation of their anti-soybean lipoxygenase,anti-xanthine oxidase,and cytotoxic activities

The synthesis of 14-(aryl)-14H-naphto[2,1-b]pyrano[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine-2-yl) acetamidoximes 2a–e has been accomplished by reaction of 2-acetonitrile derivatives 1a–e with hydroxylamine. Cyclocondensation reaction of precursors 2a–e with some elctrophilic species such as ethylorthoformate, acetic anhydride, and methyl-acetoacetate provided the new oxadiazole derivatives 3a–e, 4a–e, and 5a–e, respectively. On the other hand, the reaction of precursors 2a–e with 2-chloropropanoyl chloride afforded the new acetimidamides 6a–e which evolve under reflux of toluene to the new oxadiazoles 7a–e. The synthetic compounds were screened for their anti-xanthine oxidase, anti-soybean lipoxygenase, and cytotoxic activities. Moderate to weak xanthine oxidase and soybean lipoxygenase inhibitions were obtained but significant cytotoxic activities were noted. The most cytotoxic activities were recorded mainly (i) 5a was the most active (IC_50?=_?4.0?μM) and selective against MCF-7 and (ii) 2a was cytotoxic against the four cell lines with selectivity for MCF-7 and OVCAR-3 (IC_50?=_?17 and 12?μM, respectively) while 2e is highly selective against OVCAR-3 (IC_50?=_?10?μM).     

A revision of Casimirella,including Humirianthera (Icacinaceae)

Casimirella Hassler (1913) is accepted and Humirianthera Huber (1914) considered a synonym. Casimirella diversifolia and C. lanata from Brazil are described as new species. Casimirella ampla (Miers) based on Leretia ampla Miers, C. crispula (Howard) based on Humirianthera crispula Howard, and C. rupestris (Ducke) based on Humirianthera rupestris Ducke are new combinations.     

Conferin,potent antioxidant and anti-inflammatory isoflavone from Caragana conferta Benth

Conferin (1), a new isoflavone, has been isolated from the ethyl acetate soluble fraction of Caragana conferta Benth. along with seven known compounds, namely biochanin A (2), p-hydroxybenzoic acid (3), 3,5- dimethoxybenzoic acid (4), ursolic acid (5), erythrodiol (6), pinoresinol (7), and syringresinol (8), reported for the first time from this species. The structure of the new isoflavone was deduced on the basis of spectroscopic studies. Compounds 1 and 2 were investigated for biological activities and showed significant anti-inflammatory activity in carrageenan induced paw edema of rats. Evaluation of antioxidant activity by the radical scavenging method indicated that compound 1 is a potent antioxidant while 2 is moderately active. It was also shown that the reducing capability of compound 2 was remarkably increased in a concentration dependent manner as compared to 1. Compound 1 showed moderate inhibitory activity against the enzyme lipoxygenase, while 2 showed weak activity.     

New monogeneans from the bathydemersal southern African endemic catshark,Holohalaelurus regani (Gilchrist, 1922)

The catshark genus Holohalaelurus Fowler is currently represented by five species distributed off the southern and eastern parts of the African coast. Very few parasitological records exist for any of these five species, representing a significant knowledge gap. We report the first monogenean species from the bathydemersal species Holohalaelurus regani (Gilchrist): a new species of Microbothriidae Price, 1936, Leptomicrobothrium holohalaelure n. sp. from the dorsal skin surface, and a new species of Hexabothriidae Price, 1942 representing a new genus, Scyliorhinocotyle narvaezae n. gen., n. sp., from the gill lamellae. Both monogenean records represent the first for any member of the catshark genus Holohalaelurus. Previously we focused on the identification of monogenean taxa of emerging veterinary importance for public aquaria. We now begin a focused effort to document a generally unexplored monogenean biodiversity from diverse marine habitats off South Africa.

     

Design and synthesis of antimicrobial,anticoagulant, and anticholinesterase hybrid molecules from 4-methylumbelliferone

We designed and synthesized new series of diverse triazoles, isoxazoles, isoxazolines, and aziridines linked 4-methylumbelliferone 1 using intermolecular 1,3-dipolar cycloaddition reactions. Structures of these compounds were established on the basis of ¹H NMR, ¹³C NMR, and ESI-HRMS. All prepared compounds were evaluated for their antimicrobial, anticoagulant, and anticholinesterase activities. Interestingly, among the tested molecules, some of the analogs displayed better activities than the parent 4-methylumbelliferone 1 such as 6a and 6d for their antifungal properties. Moreover, compounds 4, 5, 6, and 7 showed the importance of the added fragments to 4-methylumbelliferone 1 via the linker methylene to have good activity.     

Thermal solvent-free synthesis of chromonyl chalcones,pyrazolines and their in vitro antibacterial,antifungal activities

A facile and ecofriendly synthesis of new chromonyl chalcones 3a-b from 3-formylchromone 1 and active methyl compounds 2a-b is reported under thermal solvent-free heating condition in good yields. The chromonyl chalcones 3a-b were used as intermediates under green condition for the synthesis of new bioactive pyrazoline derivatives 4a-f. The compounds were tested for antimicrobial activity by disk diffusion assay with slight modifications against Gram-positive, Gram-negative strains of bacteria as well as fungal strains. The investigation of antimicrobial screening revealed that compounds 3a-b and 4a-f showed antibacterial and antifungal activities.     

Description of nine new species of Heliura Butler from South America (Lepidoptera,Erebidae, Arctiinae,Arctiini, Ctenuchina)

Nine new species of the genus Heliura are described from Brazil (H. brasiliana sp. nov., H. olivocolora sp. nov., H. pulcherrima sp. nov., and H. laerteae sp. nov.), Ecuador (H. ecuadoris sp. nov.), Peru (H. flavipennis sp. nov. and H. peruana sp. nov.), and Venezuela (Heliura albiventris sp. nov. and H. juliani sp. nov.). They are illustrated in habitus and genitalia, and their phylogenetic affinities are discussed based on morphological evidence.     

New species,new genera,and new records in Cerambycidae from Peru (Coleoptera)

Three new species and two new genera of longhorn beetles are described from Peru: Cosmoplatus polis n. sp. (Pteroplatini), Hemilocallia grishami n. gen., n. sp. (Calliini) and Arabela ramirezi n. gen., n. sp. (Hemilophini). Esmeralda laetifica Bates, 1869 (Prioninae), Stratone transversalis (Chevrolat, 1862) (Cerambycinae), Gymnocerina cratosomoides (Bates, 1862) (Lamiinae), and Trachysomus verrucosus (Olivier, 1795) (Lamiinae) are new records for Peru.     

New lanostane-type triterpenoids, inonotsutriols D, and E, from Inonotus obliquus

Two new lanostane-type triterpenoids, inonotsutriols D (1) and E (2), were isolated from the sclerotia of Inonotus obliquus (Pers.: Fr.) Pil. (Japanese name: kabanoanatake; Russian name: chaga). Their structures were determined to be lanost-8-ene-3β,22R,24R-triol (1) and lanost-8-ene-3β,22R,24S-triol (2) on the basis of spectral data, including 2D NMR analysis. In addition, major compounds, inotodiol (3), trametenolic acid (4), 3β-hydroxylanosta-8,24-dien-21-al (5), 21-hydroxylanosterol (6), inonotsuoxide A (7) and inonotsuoxide B (8) were identified, and all compounds, except 2, were evaluated for their cancer cell growth inhibitory activity against P388, HL-60, L1210 and KB cell lines.     

Discovery of a broad spectrum antiproliferative agent with selectivity for DDR1 kinase: cell line-based assay,kinase panel,molecular docking,and toxicity studies

Herein, we report compound KST9046, a new agent possessing quinazoline-urea scaffold. Preliminary biological evaluation done by the National Cancer Institute (NCI), USA, showed a great inhibitory effect of KST9046 over the 60 cell-line tumor panel. Accordingly, it was selected for a dose-response assay; a broad spectrum antiproliferative activity with GI₅₀ ranging from 1.3 to 3.9?µM was exerted. To explore a potential kinase inhibitory effect, KST9046 was applied at a single dose of 10?µM against a kinase panel of 347 different enzymes representing >50% of the predicted human protein kinome. Interestingly, selective inhibition of 76% was observed on DDR1 kinase. Further, KST9046 showed an IC₅₀ value of 4.38?µM for DDR1. A molecular docking model presented KST9046 as a potential type III inhibitor for DDR1 kinase with an allosteric mode of interaction, which may offer an explanation for its selectivity. As further investigation, CYP450 assay was carried out for KST9046, it showed a promising toxicity profile against four different isoforms. Based on these findings, KST9046 can be further evaluated as a promising safe new hit for the development of broad spectrum anticancer agents with a selectivity for DDR1 kinase.     

Fluorescence,circular dichroism,NMR, and docking studies of the interaction of the alkaloid malbrancheamide with calmodulin

A new malbrancheamide analogue, isomalbrancheamide B (3), along with three known compounds, malbrancheamide (1), isomalbrancheamide (2), and premalbrancheamide (4), were isolated in higher yields from the alkaloid fraction of the fungus Malbranchea aurantiaca. The interaction of the alkaloids 1–4 with calmodulin (CaM) was analyzed using different enzymatic, fluorescence, spectroscopic, nuclear magnetic resonance (NMR), and molecular modelling techniques. On the basis of the enzymatic and fluorescence experiments, malbrancheamides 1–3 are classical CaM inhibitors. Compound 4, however, did not quench the extrinsic fluorescence of the CaM biosensor indicating that it could be a functional inhibitor. Circular dichroism, NMR, and molecular modelling studies revealed that 1 binds to CaM in the same hydrophobic pocket than the chlorpromazine and trifluoperazine, two classical CaM inhibitors. Thus, malbrancheamide and related monochlorinated analogues are compounds with a high potential for the development of new therapeutic agents, involving CaM as their molecular target.     

Macromitrium maolanense Zeyou Zhang,D.D.Li,Jing Yu & S.L.Guo,a new species from China based on molecular and morphological evidence

Introduction. During a field excursion in Guizhou Province, China, we collected some interesting moss specimens with branch leaves subulate in the upper part, partially and variably bistratose laminae, and a Macromitrium-like epiphytic growth habit on tree trunks. We present morphological and phylogenetic arguments for recognising these plants as a new moss species in the genus Macromitrium Brid. (Orthotrichaceae).

Methods. We compared the morphology of the potential new species with closely related species of Macromitrium, and constructed a phylogenetic tree based on ITS2, trnL and trnG including sampling from 14 other morphologically similar species of Macromitrium.

Key results. The proposed new species belongs to the genus Macromitrium (Orthotrichaceae, Musci). It is closely related to M. gymnostomum Sull. & Lesq. in the phylogenetic tree and according to gametophytic morphological features, represents a hitherto undescribed species.

Conclusions. A new moss species, Macromitrium maolanense Zeyou Zhang, D.D.Li, Jing Yu & S.L.Guo, is described and illustrated. The new species can be distinguished from all congeners by the combination of the following features of the branch leaves: (1) oblong-lanceolate, lanceolate to linear-lanceolate, gradually narrowed to an easily broken subula; (2) rather obscure upper and medial cells, often with blackish stains among cells, densely pluripapillose; (3) variably and partially bistratose laminae in the upper 1/3 portion; (4) basal cells clear, hyaline and smooth, those near costae forming a ‘cancellina region’; and (5) with numerous brownish, clavate gemmae on upper portion. We also discuss the principal distinctive characters separating the new species from its nearest congeners.     

Novel tetrazole and cyanamide derivatives as inhibitors of cyclooxygenase-2 enzyme: design,synthesis, anti-inflammatory evaluation,ulcerogenic liability and docking study

Nineteen new compounds containing tetrazole and/or cyanamide moiety have been designed and synthesised. Their structures were confirmed using spectroscopic methods and elemental analyses. Anti-inflammatory activity for all the synthesised compounds was evaluated in vivo. The most active compounds 4c, 5a, 5d–f, 8a and b and 9a and b were further investigated for their ulcerogenic liability and analgesic activity. Pyrazoline derivatives 9b and 8b bearing trimethoxyphenyl part and SO₂NH₂ or SO₂Me pharmacophore showed equal or nearly the same ulcerogenic liability (UI: 0.5, 0.75, respectively), to celecoxib (UI: 0.50). Most of tested compounds showed potent central and/or peripheral analgesic activities. Histopathological investigations were done to evaluate test compounds effect on rat's gastric tissue. The obtained results were in consistent with the in vitro data on COX evaluation. Docking study was also done for all the target compounds inside COX-2-active site.     

New is not always better: low breeding success and different occupancy patterns in newly built nests of a long-lived species,the white stork Ciconia ciconia

Capsule An increase in new nest building in a white stork population revealed that they were built further from human settlement and on non-typical structures; such nests had lower breeding success resulting from later breeding.

Aim To determine why some birds build new nests rather than occupy older ones, and how new nests affect breeding performance compared to old nests, in a long-lived bird, the white stork.

Methods We compared new nest construction in 2010 with a long-term data set on white stork in Western Poland from 1974 to 2009. For data from 2010, we analysed nest location and breeding biology in detail.

Results Since 1974, the proportion of new build nests was ca. 1.6%; in 2010 this was 13.2%. Pairs in new nests bred later than pairs in old, and had smaller clutches and lower breeding success. New nests were located further from settlements and tended to be built on different structures. A significantly lower proportion of new nests were re-occupied in subsequent years.

Conclusions Pairs may build new nests to gain experience in nest building, cooperation and foraging for subsequent seasons or because of competitive pressure when the environment is close to carrying capacity. Breeding success can be initially very low.     

Clinical examples of 3D dose distribution reconstruction,based on the actual MLC leaves movement,for dynamic treatment techniques

AimTo present practical examples of our new algorithm for reconstruction of 3D dose distribution, based on the actual MLC leaf movement.BackgroundDynaLog and RTplan files were used by DDcon software to prepare a new RTplan file for dose distribution reconstruction.Materials and methodsFour different clinically relevant scenarios were used to assess the feasibility of the proposed new approach: (1) Reconstruction of whole treatment sessions for prostate cancer; (2) Reconstruction of IMRT verification treatment plan; (3) Dose reconstruction in breast cancer; (4) Reconstruction of interrupted arc and complementary plan for an interrupted VMAT treatment session of prostate cancer. The applied reconstruction method was validated by comparing reconstructed and measured fluence maps. For all statistical analysis, the U Mann–Whitney test was used.ResultsIn the first two and the fourth cases, there were no statistically significant differences between the planned and reconstructed dose distribution (p = 0.910, p = 0.975, p = 0.893, respectively). In the third case the differences were statistically significant (p = 0.015). Treatment plan had to be reconstructed.ConclusionDeveloped dose distribution reconstruction algorithm presents a very useful QA tool. It provides means for 3D dose distribution verification in patient volume and allows to evaluate the influence of actual MLC leaf motion on the dose distribution.     

Phylogeny and systematics of the Acrapex apicestriata (Bethune-Baker, 1911) species complex (Lepidoptera,Noctuidae, Noctuinae,Apameini, Sesamiina) with the description of eight new species from the Afrotropics

Twelve morphologically similar species of Acrapex Hampson 1894, (Lepidoptera, Noctuidae, Noctuinae, Apameini, Sesamiina), from Western, Central and Eastern Africa are reviewed. Eight of these species are new to science and are described: Acrapex akunamatata n. sp. and A. incrassata n. sp. from Kenya; A. gracilis n. sp., A. iringa n. sp., A. lukumbura n. sp. and A. rungwe n. sp. from Tanzania; A. soyema n. sp. from Ethiopia; and A. zoutoi n. sp. from Benin. All 12 species belong to a species complex that we hereby define as the Acrapex apicestriata group. Host-plants for three of the new species are recorded: Setaria incrassata (Hochst.) Hack. for Acrapex incrassata; Cymbopogon pospishilii (K. Schum.) C.E. Hubb. for A. rungwe; and Andropogon perligulatus Stapf. for A. zoutoi. We also conducted molecular phylogenetic analyses (using maximum likelihood and Bayesian inference) on a six gene multimarker molecular dataset (four mitochondrial and two nuclear gene fragments; 4581 nucleotides in length) consisting of 15 Acrapex species (including seven species from the apicestriata group) and four outgroups species from the subtribe Sesamiina (from genera Busseola Thurau 1904, Sciomesa Tams & Bowden 1953, Pirateolea Moyal, Le Ru, Conlong, Cugala, Defabachew, Matama-Kauma, Pallangyo & Van den Berg 2010 and Sesamia Boisduval & Guenée 1852). Both maximum likelihood and Bayesian inference analyses yield a similar and well-supported topology, which supports the monophyly of the apicestriata group.