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Mar. Drugs, Volume 3, Issue 2 (June 2005), Pages 22-77

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Open AccessArticle New Cytotoxic and Antibacterial Compounds Isolated from the Sea Hare, Aplysia kurodai
Mar. Drugs 2005, 3(2), 22-28; doi:10.3390/md302022
Received: 31 January 2005 / Accepted: 15 April 2005 / Published: 16 April 2005
Cited by 4 | PDF Full-text (68 KB) | HTML Full-text | XML Full-text
Abstract
The extract of the sea hare, Aplysia kurodai, showed cytotoxicity against HeLa cells and antibacterial activity against Staphylococcus aureus. Bioassay-guided purification afforded four active compounds, which were identified to be laurinterol, laurinterol acetate, debromolaurinterol, and debromolaurinterol acetate by spectroscopic analysis. [...] Read more.
The extract of the sea hare, Aplysia kurodai, showed cytotoxicity against HeLa cells and antibacterial activity against Staphylococcus aureus. Bioassay-guided purification afforded four active compounds, which were identified to be laurinterol, laurinterol acetate, debromolaurinterol, and debromolaurinterol acetate by spectroscopic analysis. Although the acetates were derived from laurinterol and debromolaurinterol before, this is the first isolation of the acetates from natural sources. Full article
Open AccessArticle Secomycalolide A: A New Proteasome Inhibitor Isolated from a Marine Sponge of the Genus Mycale
Mar. Drugs 2005, 3(2), 29-35; doi:10.3390/md302029
Received: 28 April 2005 / Accepted: 25 May 2005 / Published: 1 June 2005
Cited by 18 | PDF Full-text (73 KB) | HTML Full-text | XML Full-text
Abstract A new oxazole-containing proteasome inhibitor, secomycalolide A, together with known mycalolide A and 30-hydroxymycalolide A, was isolated from a marine sponge of the genus Mycale. They showed proteasome inhibitory activities with IC50 values of 11-45 μg/mL. Full article
Open AccessArticle Quality not Quantity: The Role of Marine Natural Products in Drug Discovery and Reverse Chemical Proteomics
Mar. Drugs 2005, 3(2), 36-63; doi:10.3390/md302036
Received: 15 April 2005 / Accepted: 30 May 2005 / Published: 1 June 2005
Cited by 12 | PDF Full-text (514 KB) | HTML Full-text | XML Full-text
Abstract
Reverse chemical proteomics combines affinity chromatography with phage display and promises to be a powerful new platform technology for the isolation of natural product receptors, facilitating the drug discovery process by rapidly linking biologically active small molecules to their cellular receptors and [...] Read more.
Reverse chemical proteomics combines affinity chromatography with phage display and promises to be a powerful new platform technology for the isolation of natural product receptors, facilitating the drug discovery process by rapidly linking biologically active small molecules to their cellular receptors and the receptors’ genes. In this paper we review chemical proteomics and reverse chemical proteomics and show how these techniques can add value to natural products research. We also report on techniques for the derivatisation of polystyrene microtitre plates with cleavable linkers and marine natural products that can be used in chemical proteomics or reverse chemical proteomics. Specifically, we have derivatised polystyrene with palau’amine and used reverse chemical proteomics to try and isolate the human receptors for this potent anticancer marine drug. Full article
Open AccessArticle Verrucarin A Inhibition of MAP Kinase Activation in a PMA-stimulated Promyelocytic Leukemia Cell Line
Mar. Drugs 2005, 3(2), 64-73; doi:10.3390/md302064
Received: 4 March 2005 / Accepted: 2 June 2005 / Published: 2 June 2005
Cited by 12 | PDF Full-text (116 KB) | HTML Full-text | XML Full-text
Abstract
Verrucarin A is an inhibitor of protein synthesis. In this study, we examined the inhibitory action of verrucarin A on signal molecules. Verrucarin A partially inhibited the IL-8 production of a PMA-stimulated promyelocytic leukemia cell line (HL-60 cells), and the effect was [...] Read more.
Verrucarin A is an inhibitor of protein synthesis. In this study, we examined the inhibitory action of verrucarin A on signal molecules. Verrucarin A partially inhibited the IL-8 production of a PMA-stimulated promyelocytic leukemia cell line (HL-60 cells), and the effect was related to the inhibition of NF-κB activation at noncytotoxic concentrations. Moreover, the inhibition of mitogen activated protein (MAP) kinase by verrucarin A was especially strong with p38- and JNK-phosphorylation. The findings show a new action of verrucarin A, and it is expected that this action relaxes the signal activation in response to stress. Full article

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Open AccessCorrection Publisher's Note added on 9 October 2006
Mar. Drugs 2005, 3(2), 74-77; doi:10.3390/md3020074
Published: 9 October 2006
PDF Full-text (103 KB) | HTML Full-text | XML Full-text
Abstract Publisher's Note added on 9 October 2006 : Pages 74-77 are taken as blank pages. Full article

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