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https://www.readbyqxmd.com/read/28214232/new-nitrofurans-amenable-by-isocyanide-multicomponent-chemistry-are-active-against-multidrug-resistant-and-poly-resistant-mycobacterium-tuberculosis
#1
Mikhail Krasavin, Vladislav Parchinsky, Grigory Kantin, Olga Manicheva, Marine Dogonadze, Tatiana Vinogradova, Bianka Karge, Mark Brönstrup
A set of structurally diverse N-amino δ-lactams decorated with a 5-nitro-2-furyl moiety was synthesized using isocyanide-based multicomponent chemistry and evaluated for antibacterial activity. Three compounds displayed a selective and potent (MIC 22-33μM) inhibition of M. tuberculosis H37Rv strain growth, while other Gram-positive (MRSA and E. faecium) or Gram-negative (E. coli, P. aeruginosa, A. baumannii, K. pneumoniae) pathogens were not affected. The compounds also displayed moderate-low cytotoxicity, as demonstrated in cell line viability assays...
February 4, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28213548/effects-of-gelling-agent-and-extracellular-signaling-molecules-on-the-culturability-of-marine-bacteria
#2
Anita Mac Rygaard, Mariane Schmidt Thøgersen, Kristian Fog Nielsen, Lone Gram, Mikkel Bentzon-Tilia
Only 1 % of marine bacteria are currently culturable using standard laboratory procedures and this is a major obstacle for our understanding of the biology of marine microorganisms and for the discovery of novel microbial natural products. Therefore, the purpose of the present study was to investigate if improved cultivation conditions, including the use of an alternative gelling agent, and supplementation with signaling molecules, could improve the culturability of bacteria from seawater. Substituting agar with gellan gum improved viable counts 3 - 40-fold, depending on medium composition and incubation conditions, with a maximum of 6...
February 17, 2017: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/28208715/biotransformation-and-detoxification-of-xylidine-orange-dye-using-immobilized-cells-of-marine-derived-lysinibacillus-sphaericus-d3
#3
Prabha Devi, Solimabi Wahidullah, Farhan Sheikh, Rochelle Pereira, Niteen Narkhede, Divya Amonkar, Supriya Tilvi, Ram Murthy Meena
Lysinibacillus sphaericus D3 cell-immobilized beads in natural gel sodium alginate decolorized the xylidine orange dye 1-(dimethylphenylazo)-2-naphthol-6-sulfonic acid sodium salt in the laboratory. Optimal conditions were selected for decolorization and the products formed were evaluated for toxicity by disc diffusion assay against common marine bacteria which revealed the non-toxic nature of the dye-degraded products. Decolorization of the brightly colored dye to colorless products was measured on an Ultra Violet-Vis spectrophotometer and its biodegradation products monitored on Thin Layer Chromatographic plate and High Performance Liquid Chromatography (HPLC)...
February 8, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28163017/small-molecule-inhibitors-of-the-sox18-transcription-factor
#4
Frank Fontaine, Jeroen Overman, Mehdi Moustaqil, Sreeman Mamidyala, Angela Salim, Kamesh Narasimhan, Nina Prokoph, Avril A B Robertson, Linda Lua, Kirill Alexandrov, Peter Koopman, Robert J Capon, Emma Sierecki, Yann Gambin, Ralf Jauch, Matthew A Cooper, Johannes Zuegg, Mathias Francois
Pharmacological modulation of transcription factors (TFs) has only met little success over the past four decades. This is mostly due to standard drug discovery approaches centered on blocking protein/DNA binding or interfering with post-translational modifications. Recent advances in the field of TF biology have revealed a central role of protein-protein interaction in their mode of action. In an attempt to modulate the activity of SOX18 TF, a known regulator of vascular growth in development and disease, we screened a marine extract library for potential small-molecule inhibitors...
January 27, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28159305/microscopic-characterisation-of-black-crusts-on-different-substrates
#5
J S Pozo-Antonio, M F C Pereira, C S A Rocha
Black crusts on different substrates (carbonate and silicate stones, cement-based mortar and carbonate detrital deposits) in urban environments were characterized microscopically by analysing their morphologies and compositions. The objective of this article is to study the interaction between the substrate and the crust and the influence of the environmental conditions on the crust development. On the one hand, the internal structure and morphology of each sample were evaluated with stereo and scanning electron microscopies...
February 1, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28154844/de-orphaning-the-marine-natural-product-%C3%A2-marinopyrrole-a-by-computational-target-prediction-and-biochemical-validation
#6
P Schneider, G Schneider
Exploring the full potential of bioactive natural products and phenotypic screening hits for drug discovery and design requires profound understanding of the macromolecular targets involved. We present a computational method for target prediction, and showcase its practical applicability, taking the marine anticancer compound (±)-marinopyrrole A as an example. With an overall accuracy of 67%, the ligand-based method employed identified the natural product as a potent glucocorticoid, cholecystokinin, and orexin receptor antagonist...
February 3, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28143426/the-marine-triterpene-glycoside-frondoside-a-induces-p53-independent-apoptosis-and-inhibits-autophagy-in-urothelial-carcinoma-cells
#7
Sergey A Dyshlovoy, Ramin Madanchi, Jessica Hauschild, Katharina Otte, Winfried H Alsdorf, Udo Schumacher, Vladimir I Kalinin, Alexandra S Silchenko, Sergey A Avilov, Friedemann Honecker, Valentin A Stonik, Carsten Bokemeyer, Gunhild von Amsberg
BACKGROUND: Advanced urothelial carcinomas represent a considerable clinical challenge as they are difficult to treat. Platinum-based combination regimens obtain response rates ranging from 40 to 70% in first-line therapy of advanced urothelial carcinoma. In the majority of cases, however, the duration of these responses is limited, and when progression occurs, the outcome is generally poor. Therefore, novel therapeutic strategies are urgently needed. The purpose of the current research is to investigate the anticancer effects and the mode of action of the marine triterpene glycoside frondoside A in p53-wild type and p53-deficient human urothelial carcinoma cells...
February 1, 2017: BMC Cancer
https://www.readbyqxmd.com/read/28134828/exploring-the-impacts-of-anthropogenic-disturbance-on-seawater-and-sediment-microbial-communities-in-korean-coastal-waters-using-metagenomics-analysis
#8
Nam-Il Won, Ki-Hwan Kim, Ji Hyoun Kang, Sang Rul Park, Hyuk Je Lee
The coastal ecosystems are considered as one of the most dynamic and vulnerable environments under various anthropogenic developments and the effects of climate change. Variations in the composition and diversity of microbial communities may be a good indicator for determining whether the marine ecosystems are affected by complex forcing stressors. DNA sequence-based metagenomics has recently emerged as a promising tool for analyzing the structure and diversity of microbial communities based on environmental DNA (eDNA)...
January 27, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28131452/leaching-of-two-fungicides-in-spent-mushroom-substrate-amended-soil-influence-of-amendment-rate-fungicide-ageing-and-flow-condition
#9
Alba Álvarez-Martín, María J Sánchez-Martín, José M Ordax, Jesús M Marín-Benito, M Sonia Rodríguez-Cruz
A study has been conducted on the leaching of two fungicides, tebuconazole and cymoxanil, in a soil amended with spent mushroom substrate (SMS), with an evaluation of how different factors influence this process. The objective was based on the potential use of SMS as a biosorbent for immobilizing pesticides in vulnerable soils, and the need to know how it could affect the subsequent transport of these retained compounds. Breakthrough curves (BTCs) for (14)C-fungicides, non-incubated and incubated over 30days, were obtained in columns packed with an unamended soil (S), and this soil amended with SMS at rates of 5% (S+SMS5) and 50% (S+SMS50) under saturated and saturated-unsaturated flows...
January 25, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28128950/naphthablins-b-and-c-meroterpenoids-identified-from-the-marine-sediment-derived-streptomyces-sp-cp26-58-using-hela-cell-based-cytological-profiling
#10
Hana Martucci, Scott E Campit, Stephanie R Gee, Walter M Bray, Trevor Gokey, A King Cada, Ten-Yang Yen, Katsuhiko Minoura, Anton B Guliaev, R Scott Lokey, Taro Amagata
HeLa cell-based cytological profiling (CP) was applied to an extract library of marine sediment-derived actinomycetes to discover new cytotoxic secondary metabolites. Among the hit strains, Streptomyces sp. CP26-58 was selected for further investigation to identify its cytotoxic metabolites. CP revealed that the known ionophore tetronasin (1) was responsible for the cytotoxic effect found in the extract. Furthermore, three naphthoquinone meroterpenoids, naphthablin A (2) and two new derivatives designated as naphthablins B (3) and C (4), were isolated from other cytotoxic fractions...
January 27, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28108094/metabolic-profiling-identification-of-metabolites-formed-in-mediterranean-mussels-mytilus-galloprovincialis-after-diclofenac-exposure
#11
Bénilde Bonnefille, Lauren Arpin-Pont, Elena Gomez, Hélène Fenet, Frédérique Courant
Despite the growing concern on the presence of pharmaceutically active compounds in the environment, few studies have been conducted on their metabolism in marine organisms. In this study, a non-targeted strategy based on the generation of chemical profiles generated by liquid chromatography combined with high resolution mass spectrometry was used to highlight metabolite production by the Mediterranean mussel (Mytilus galloprovincialis) after diclofenac exposure. This method allowed revealing the production of 13 metabolites in mussel tissues...
January 17, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28095778/the-pangenome-of-antarctic-pseudoalteromonas-bacteria-evolutionary-and-functional-insights
#12
Emanuele Bosi, Marco Fondi, Valerio Orlandini, Elena Perrin, Isabel Maida, Donatella de Pascale, Maria Luisa Tutino, Ermenegilda Parrilli, Angelina Lo Giudice, Alain Filloux, Renato Fani
BACKGROUND: Pseudoalteromonas is a genus of ubiquitous marine bacteria used as model organisms to study the biological mechanisms involved in the adaptation to cold conditions. A remarkable feature shared by these bacteria is their ability to produce secondary metabolites with a strong antimicrobial and antitumor activity. Despite their biotechnological relevance, representatives of this genus are still lacking (with few exceptions) an extensive genomic characterization, including features involved in the evolution of secondary metabolites production...
January 17, 2017: BMC Genomics
https://www.readbyqxmd.com/read/28089692/in%C3%A2-vitro-bioaccessibility-of-the-marine-biotoxins-okadaic-acid-dinophysistoxin-2-and-their-7-o-acyl-fatty-acid-ester-derivatives-in-raw-and-steamed-shellfish
#13
Diana Manita, Ricardo N Alves, Ana Catarina Braga, Fabiola H S Fogaça, António Marques, Pedro Reis Costa
Okadaic acid (OA), Dinophysistoxins (DTX1 and DTX2) and their acyl-derivatives (DTX3) are marine toxins responsible for the human diarrhetic shellfish poisoning. To date the amount of toxins ingested from consumption of shellfish has been considered equal to the amount of toxins available for uptake by the human body. The aim of this study is to assess the OA, DTX2 and DTX3 fractions released from raw and steamed mussels and cockles into the digestive fluids (bioaccessibility) using a static in vitro digestion model...
January 12, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28081159/osmoregulation-in-the-halophilic-bacterium-halomonas-elongata-a-case-study-for-integrative-systems-biology
#14
Viktoria Kindzierski, Silvia Raschke, Nicole Knabe, Frank Siedler, Beatrix Scheffer, Katharina Pflüger-Grau, Friedhelm Pfeiffer, Dieter Oesterhelt, Alberto Marin-Sanguino, Hans-Jörg Kunte
Halophilic bacteria use a variety of osmoregulatory methods, such as the accumulation of one or more compatible solutes. The wide diversity of compounds that can act as compatible solute complicates the task of understanding the different strategies that halophilic bacteria use to cope with salt. This is specially challenging when attempting to go beyond the pathway that produces a certain compatible solute towards an understanding of how the metabolic network as a whole addresses the problem. Metabolic reconstruction based on genomic data together with Flux Balance Analysis (FBA) is a promising tool to gain insight into this problem...
2017: PloS One
https://www.readbyqxmd.com/read/28074955/total-synthesis-and-biological-activity-of-dolastatin-16
#15
Loida O Casalme, Arisa Yamauchi, Akinori Sato, Julie G Petitbois, Yasuyuki Nogata, Erina Yoshimura, Tatsufumi Okino, Taiki Umezawa, Fuyuhiko Matsuda
The total synthesis of dolastatin 16, a macrocyclic depsipeptide first isolated from the sea hare Dolabella auricularia as a potential antineoplastic metabolite by Pettit et al., was achieved in a convergent manner. Dolastatin 16 was reported by Tan to exhibit strong antifouling activity, and thus shows promise for inhibiting the attachment of marine benthic organisms such as Amphibalanus amphitrite to ships and submerged artificial structures. Therefore, dolastatin 16 is a potential compound for a new, environmentally friendly antifouling material to replace banned tributyltin-based antifouling paints...
February 1, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28073536/microelectrode-array-mea-platform-as-a-sensitive-tool-to-detect-and-evaluate-ostreopsis-cf-ovata-toxicity
#16
Susanna Alloisio, Valentina Giussani, Mario Nobile, Mariachiara Chiantore, Antonio Novellino
In the last decade, the occurrence of harmful dinoflagellate blooms of the genus Ostreopsis has increased both in frequency and in geographic distribution with adverse impacts on public health and the economy. Ostreopsis species are producers of palytoxin-like toxins (putative palytoxin and ovatoxins) which are among the most potent natural non-protein compounds known to date, exhibiting extreme toxicity in mammals, including humans. Most existing toxicological data are derived from in vivo mouse assay and are related to acute effects of pure palytoxin, without considering that the toxicity mechanism of dinoflagellates can be dependent on the varying composition of complex biotoxins mixture and on the presence of cellular components...
May 2016: Harmful Algae
https://www.readbyqxmd.com/read/28056571/compounds-compositions-and-methods-of-agelastatin-alkaloids-patent-evaluation-of-wo2015042239-a1
#17
Takehiko Yoshimitsu, Han W Tun
Agelastatins are a family of tetracyclic alkaloids isolated from marine sponges. The patent examined in this publication covers the chemical synthesis of agelastatins A to F and eight analogues and their therapeutic use against hematologic malignancies. The claim on the chemical synthesis features a novel biomimetic cyclization of a tricyclic precursor, which streamlines scalable access to agelastatins and their analogues. This new synthetic approach can potentially expedite the research on these compounds for therapeutic use against cancers by making them more easily available...
January 5, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28055195/nontargeted-screening-of-halogenated-organic-compounds-in-bottlenose-dolphins-tursiops-truncatus-from-rio-de-janeiro-brazil
#18
Mariana B Alonso, Keith A Maruya, Nathan G Dodder, José Lailson-Brito, Alexandre Azevedo, Elitieri Santos-Neto, Joao P M Torres, Olaf Malm, Eunha Hoh
To catalog the diversity and abundance of halogenated organic compounds (HOCs) accumulating in high trophic marine species from the southwestern Atlantic Ocean, tissue from bottlenose dolphins (Tursiops truncatus) stranded or incidentally captured along the coast of Rio de Janeiro, Brazil, were analyzed by a nontargeted approach based on GC×GC/TOF-MS. A total of 158 individual HOCs from 32 different structural classes were detected in the blubber of 4 adult male T. truncatus. Nearly 90% of the detected compounds are not routinely monitored in the environment...
January 27, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28034290/marine-algae-as-a-prospective-source-for-antidiabetic-compounds-a-brief-review
#19
S P Unnikrishnan, A M Jayasri
Diabetes mellitus (DM) is a metabolic disorder characterized by chronic hyperglycaemia, which is attributed by several life threatening complications including atherosclerosis, nephropathy, and retinopathy. The current therapies available for the management of DM mainly include oral antidiabetic drugs and insulin injections. However, continuous use of synthetic drugs provides lower healing with many side effects. Therefore, there is an urge for safe and efficient antidiabetic drugs for the management of DM...
December 29, 2016: Current Diabetes Reviews
https://www.readbyqxmd.com/read/28028206/two-distinct-pools-of-b12-analogs-reveal-community-interdependencies-in-the-ocean
#20
Katherine R Heal, Wei Qin, Francois Ribalet, Anthony D Bertagnolli, Willow Coyote-Maestas, Laura R Hmelo, James W Moffett, Allan H Devol, E Virginia Armbrust, David A Stahl, Anitra E Ingalls
Organisms within all domains of life require the cofactor cobalamin (vitamin B12), which is produced only by a subset of bacteria and archaea. On the basis of genomic analyses, cobalamin biosynthesis in marine systems has been inferred in three main groups: select heterotrophic Proteobacteria, chemoautotrophic Thaumarchaeota, and photoautotrophic Cyanobacteria. Culture work demonstrates that many Cyanobacteria do not synthesize cobalamin but rather produce pseudocobalamin, challenging the connection between the occurrence of cobalamin biosynthesis genes and production of the compound in marine ecosystems...
January 10, 2017: Proceedings of the National Academy of Sciences of the United States of America
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