A high throughput screen performed to identify catalytic inhibitors of the oncogenic fusion form of cAMP-dependent protein kinase A catalytic subunit alpha (J-PKAcα) found an individual fraction from an organic extract of the marine soft coral as active. Bioassay-guided isolation led to the identification of a 2-amino adenine alkaloid acroamine A (), the first secondary metabolite discovered from this genus and previously reported as a synthetic product. As a naturally occurring protein kinase inhibitor, to unambiguously assign its chemical structure using modern spectroscopic and spectrometric techniques, five -methylated derivatives acroamines A-A (-) were semisynthesized.
View Article and Find Full Text PDFNeopetrotaurines A-C (-), unusual alkaloids possessing two isoquinoline-derived moieties that are linked via a unique taurine bridge, were isolated from a sp. marine sponge. These new compounds have proton-deficient structural scaffolds that are difficult to unambiguously assign using only conventional 2- and 3-bond H-C and H-N heteronuclear correlation data.
View Article and Find Full Text PDFSix new sesquiterpene coumarin ethers, namely turcicanol A (), turcicanol A acetate (), turcicanol B (), turcica ketone (), 11'-dehydrokaratavicinol (), and galbanaldehyde (), and one new sulfur-containing compound, namely turcicasulphide (), along with thirty-two known secondary metabolites were isolated from the root of the endemic species Akalın, Miski, & Tuncay through a bioassay-guided isolation approach. The structures of the new compounds were elucidated by spectroscopic analysis and comparison with the literature. Cell growth inhibition of colon cancer cell lines (COLO205 and HCT116) and kidney cancer cell lines (UO31 and A498) was used to guide isolation.
View Article and Find Full Text PDFSeven new peptaibols named tolypocladamides A-G have been isolated from an extract of the fungus , which inhibits the interaction between Raf and oncogenic Ras in a cell-based high-throughput screening assay. Each peptaibol contains 11 amino acid residues, an octanoyl or decanoyl fatty acid chain at the N-terminus, and a leucinol moiety at the C-terminus. The peptaibol sequences were elucidated on the basis of 2D NMR and mass spectral fragmentation analyses.
View Article and Find Full Text PDFBackground: Once considered to be a congenital condition, the epidemiology of right-sided colonic diverticulosis (RCD) is evolving. Acute diverticulitis (AD) is a complication of RCD which is frequently misdiagnosed as appendicitis, resulting in unnecessary surgery, as there is strong evidence supporting medical management for right-sided AD. In general, the incidence of AD correlates with the prevalence of RCD, which shows marked geographic variation.
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