9 research outputs found

    Bioactive Sesterterpenes and Triterpenes from Marine Sponges: Occurrence and Pharmacological Significance

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    Marine ecosystems (>70% of the planet's surface) comprise a continuous resource of immeasurable biological activities and immense chemical entities. This diversity has provided a unique source of chemical compounds with potential bioactivities that could lead to potential new drug candidates. Many marine-living organisms are soft bodied and/or sessile. Consequently, they have developed toxic secondary metabolites or obtained them from microorganisms to defend themselves against predators [1]. For the last 30–40 years, marine invertebrates have been an attractive research topic for scientists all over the world. A relatively small number of marine plants, animals and microbes have yielded more than 15,000 natural products including numerous compounds with potential pharmaceutical potential. Some of these have already been launched on the pharmaceutical market such as Prialt® (ziconotide; potent analgesic) and Yondelis® (trabectedin or ET-743; antitumor) while others have entered clinical trials, e.g., alpidin and kahalalide F. Amongst the vast array of marine natural products, the terpenoids are one of the more commonly reported and discovered to date. Sesterterpenoids (C25) and triterpenoids (C30) are of frequent occurrence, particularly in marine sponges, and they show prominent bioactivities. In this review, we survey sesterterpenoids and triterpenoids obtained from marine sponges and highlight their bioactivities

    Monarch Diet Flight Data

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    Data to accompany  Larval diet impacts flight performance in monarch butterflies from two populations by    (Article DOI: 10.1111/een.13255) by Ali Ebada1, Jacobus C. de Roode1, Ania A. Majewska2 Institutional affiliations: 1 Department of Biology, Emory University, Atlanta, GA 30322, USA 2 Department of Physiology and Pharmacology, College of Veterinary Medicine, University of Georgia, Athens, GA 30602, USA Corresponding author: Ania A. Majewska ([email protected]). Each row represents an individual monarch. Flight metrics are aggregate values for a successful flight. </p

    indigo-dc/udocker: udocker 1.3.0

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    udocker v1.3.0 see the changelog and the documentation for further information. Changelog: https://github.com/indigo-dc/udocker/blob/devel3/CHANGELOG.md Documentation: https://indigo-dc.github.io/udocker/ udocker release supports for Python 2.6, 2.7 and >= 3.6 Follow this steps to install and run udocker: wget https://github.com/indigo-dc/udocker/releases/download/v1.3.0/udocker-1.3.0.tar.gz tar zxvf udocker-1.3.0.tar.gz export PATH=`pwd`/udocker:$PATH Test with: udocker --help udocker instal

    Methods for isolation, purification and structural elucidation of bioactive secondary metabolites from marine invertebrates

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    In the past few decades, marine natural products bioprospecting has yielded a considerable number of drug candidates. Two marine natural products have recently been admitted as new drugs: Prialt (also known as ziconotide) as a potent analgesic for severe chronic pain and Yondelis (known also as trabectedin or E-743) as antitumor agent for the treatment of advanced soft tissue sarcoma. In this protocol, methods for bioactivity-guided isolation, purification and identification of secondary metabolites from marine invertebrates such as sponges, tunicates, soft corals and crinoids are discussed. To achieve this goal, solvent extraction of usually freeze-dried sample of marine organisms is performed. Next, the extract obtained is fractionated by liquid-liquid partitioning followed by various chromatographic separation techniques including thin layer chromatography, vacuum liquid chromatography, column chromatography (CC) and preparative high-performance reversed-phase liquid chromatography. Isolation of bioactive secondary metabolites is usually monitored by bioactivity assays, e.g., antioxidant (2,2-diphenyl-1-picryl hydrazyl) and cytotoxicity (microculture tetrazolium) activities that ultimately yield the active principles. Special care should be taken when performing isolation procedures adapted to the physical and chemical characteristics of the compounds isolated, particularly their lipo- or hydrophilic characters. Examples of isolation of compounds of different polarities from extracts of various marine invertebrates will be presented in this protocol. Structure elucidation is achieved using recent spectroscopic techniques, especially 2D NMR and mass spectrometry analysis

    Two new triterpenoids and a new naphthoquinone derivative isolated from a hard coral-derived fungus Scopulariopsis sp.

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    Scopulariopsis sp. isolated from the Red Sea hard coral Stylophora sp. yielded two new triterpenoids (1-2) and a new naphthoquinone derivative (8) when cultured on white beans. In addition, fourteen known compounds including three triterpene analogues (3-5), two sesquiterpenoids (6-7), two polyketides (9-10) and seven nitrogenous compounds (11-17) were isolated. All structures were determined through extensive analysis of the NMR and MS data as well as by comparison with literature data. All isolated compounds were evaluated for their cytotoxic, antibacterial and antitubercular activities. However, none of them showed significant activity. (C) 2016 Elsevier B.V. All rights reserved.Egyptian government (Ministry of Higher Education); Manchot-FoundationSCI(E)ARTICLE126-13011

    Two New Jaspamide Derivatives from the Marine Sponge Jaspis splendens

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    Two new jaspamide derivatives 2 and 3, together with the parent compound jaspamide (1) have been isolated from the marine sponge Jaspis splendens collected in Kalimantan (Indonesia). The structures of the new compounds were unambiguously elucidated based on 1D and 2D NMR spectral data, mass spectrometry and comparison with jaspamide (1). The new derivatives inhibited the growth of mouse lymphoma (L5178Y) cell line in vitro with IC50 values of &lt;0.1 μg/mL

    indigo-dc/udocker: udocker 1.3.4

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    udocker v1.3.4 see the changelog and the documentation for further information. Changelog: https://github.com/indigo-dc/udocker/blob/master/CHANGELOG.md Documentation: https://indigo-dc.github.io/udocker/ udocker release for Python 2.7 and >= 3.6 Follow these steps to install and run udocker: wget https://github.com/indigo-dc/udocker/releases/download/v1.3.4/udocker-1.3.4.tar.gz tar zxvf udocker-1.3.4.tar.gz export PATH=`pwd`/udocker:$PATH Test with: udocker --help udocker instal

    Xanthones and sesquiterpene derivatives from a marine-derived fungus Scopulariopsis sp.

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    Two new xanthone derivatives, 12-dimethoxypinselin (1) and 12-O-acetyl-AGI-B4 (2), as well as two new phenolic bisabolane-type sesquiterpenes, 11,12-dihydroxysydonic acid (15) and 1-hydroxyboivinianic acid (16), together with one new alkaloid, scopulamide (21) and one new cc-pyrone derivative, scopupyrone (26), in addition to twenty-three known compounds (3-14,17-20, 22-25, 27-29) were isolated from solid rice cultures of the marine-derived fungus Scopulariopsis sp. obtained from the Red Sea hard coral Stylophora sp. All compounds were unambiguously identified through extensive NMR spectroscopic analyses, and by comparison with the literature. Marfey&apos;s reaction was performed to determine the absolute configuration of scopulamide (21) and TDDFT-ECD calculations were used to assign the configuration of AGI-B4 (3) and scopupyrone (26). All isolated compounds were evaluated for their cytotoxicity against L5178Y mouse lymphoma cells and the structure-activity relationships were discussed. (C) 2016 Elsevier Ltd. All rights reserved.Egyptian Government (Ministry of High Education); Hungarian National Research Foundation [OTKA K105871]; National Information Infrastructure Development Institute [NIIFI 10038]; Manchot FoundationSCI(E)[email protected]; [email protected]

    Arthrinins A-D: Novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp.

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    Bioassay-guided fractionation of a methanolic extract of the fungus Arthrinium sp., isolated from the Mediterranean sponge Geodia cydonium, afforded 10 natural products including five new diterpenoids, arthrinins A-D (1-4) and myrocin D (5). In addition, five known compounds were obtained, which included myrocin A (6), norlichexanthone (7), anomalin A (8), decarboxycitrinone (9) and 2,5-dimethyl-7-hydroxychromone (10). The structures of all isolated compounds were unambiguously elucidated based on extensive 1D and 2D NMR and HR-MS analyzes. The absolute configuration of arthrinins A-D (1-4) was established by the convenient Mosher method performed in NMR tubes and by interpretation of the ROESY spectra. Antiproliferative activity of the isolated compounds was assessed in vitro against four different tumor cell lines, including mouse lymphoma (L5178Y), human chronic myelogenous leukemia (K562), human ovarian cancer (A2780) and cisplatin-resistant ovarian cancer cells (A2780CisR), using the MTT assay. Norlichexanthone (7) and anomalin A (8) exhibited the strongest activities with IC50 values ranging from 0.40 to 74.0 mu M depending on the cell line investigated. This was paralleled by the inhibitory activity of both compounds against 16 cancer related protein kinases including aurora-B, PIM1, and VEGF-R2. In vitro IC50 values of 7 and 8 against these three protein kinases ranged from 0.3 to 11.7 mu M. Further investigation of the potential antitumoral activity of compounds 5-8 was performed in an in vitro angiogenesis assay against human umbilical vascular endothelial cells (HUVEC) sprouting induced by vascular endothelial growth factor A (VEGF-A). Anomalin A (8), myrocin D (5) and myrocin A (6) inhibited VEGF-A dependent endothelial cell sprouting with IC50 values of 1.8, 2.6 and 3.7 mu lM, respectively, whereas norlichexanthone (7) was inactive. (C) 2011 Elsevier Ltd. All rights reserved.Biochemistry &amp; Molecular BiologyChemistry, MedicinalChemistry, OrganicSCI(E)0ARTICLE154644-46511
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