ABSTRACT
By activity-guided fractionation based on inhibition of nitric oxide (NO) and prostaglandin E2 (PGE2), six fistularin compounds (1-6) were isolated from the marine sponge Ecionemia acervus (order Astrophorida). Based on stereochemical structure determination using Mosher's method, fistularin-3 was assigned as a new stereoisomer. On the basis of the stereochemistry of fistularin-3, the stereochemical homogeneity of all six compounds was established by comparing carbon and proton chemical shifts. For fistularin-1 (1) and -2 (2), quantum calculations were performed to confirm their stereochemistry. In a co-culture system of human epithelial Caco-2 cells and THP-1 macrophages, all six isolated compounds showed potent anti-inflammatory activities. These bioactive fistularins inhibited the production of NO, PGE2, TNF-α, IL-1ß, and IL-6 induced by lipopolysaccharide and interferon gamma. Inducible NO synthase and cyclooxygenase-2 expression and MAPK phosphorylation were downregulated in response to the inhibition of NF-κB nuclear translocation. Among the compounds tested, fistularin-1 (1) and 19-deoxyfistularin-3 (4) showed the highest activity. These findings suggest the potential use of the marine sponge E. acervus and its metabolites as pharmaceuticals for the treatment of inflammation-related diseases including inflammatory bowel disease.
Subject(s)
Anti-Inflammatory Agents/pharmacology , Inflammatory Bowel Diseases/drug therapy , Isoxazoles/pharmacology , Porifera/metabolism , Tyrosine/analogs & derivatives , Animals , Anti-Inflammatory Agents/isolation & purification , Caco-2 Cells , Coculture Techniques , Cytokines/metabolism , Dinoprostone/metabolism , Humans , Inflammation Mediators/metabolism , Inflammatory Bowel Diseases/immunology , Inflammatory Bowel Diseases/metabolism , Isoxazoles/isolation & purification , Molecular Structure , NF-kappa B/metabolism , Nitric Oxide/metabolism , Signal Transduction , Stereoisomerism , Structure-Activity Relationship , THP-1 Cells , Tyrosine/isolation & purification , Tyrosine/pharmacologyABSTRACT
In this work, we demonstrate the preparation of hybrid thin films based on double-walled carbon nanotubes and graphene for electrochemical sensing applications. The hybrid films were synthesized on polycrystalline copper foil by thermal chemical vapor deposition under low pressure. This carbonaceous hybrid film has exhibited high transparency with a transmittance of 94.3 %. The occurrence of this hybrid material on the electrode surface of screen-printed electrodes was found to increase electroactive surface area by 1.4 times, whereas electrochemical current was enhanced by 2.4 times. Such a highly transparent and conductive hybrid film was utilized as a transducing platform of enzymatic electrochemical arsenic(V) sensor. The as-prepared sensor shows the linear detection of arsenic(V) in the range from 1 to 10 ppb, with a limit of detection as low as 0.287 ppb. These findings provide a promising approach to develop new multifunctional electrochemical sensing systems for environmental monitoring and biomedical diagnostics.
