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Mar. Drugs, Volume 1, Issue 1 (December 2003), Pages 1-65

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Editorial

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Open AccessEditorial Marine Drugs -A New International Journal
Mar. Drugs 2003, 1(1), 1-2; doi:10.3390/md101001
Received: 16 September 2003 / Accepted: 15 November 2003 / Published: 15 November 2003
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Open AccessEditorial The Journal Marine Drugs and the First International Symposium on Marine Drugs (2004)
Mar. Drugs 2003, 1(1), 3-4; doi:10.3390/md101003
Received: 19 September 2003 / Accepted: 15 November 2003 / Published: 15 November 2003
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Research

Jump to: Editorial

Open AccessArticle Drugs from the Sea - Opportunities and Obstacles
Mar. Drugs 2003, 1(1), 5-17; doi:10.3390/md101005
Received: 15 October 2003 / Accepted: 13 November 2003 / Published: 26 November 2003
Cited by 33 | PDF Full-text (110 KB) | HTML Full-text | XML Full-text
Abstract
The supply problem with regard to drug development and sustainable production lies in the limited amounts of biomass of most marine invertebrates available from wild stocks. Thus, most pharmacologically active marine natural products can only be isolated in minute yields. Total synthesis of
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The supply problem with regard to drug development and sustainable production lies in the limited amounts of biomass of most marine invertebrates available from wild stocks. Thus, most pharmacologically active marine natural products can only be isolated in minute yields. Total synthesis of pharmacologically active natural products has been successfully established but is in many cases economically not feasible due to the complexity of the molecular structures and the low yields. To solve the pressing supply issue in marine drug discovery, other strategies appear to be more promising. One of these is mariculture which has successfully been established with the bryozoan Bugula neritina (the source of the bryostatins) and the tunicate Ecteinascidia turbinata (the source of ET-743). Another strategy involves partial synthesis from precursors which are biotechnologically available. An example is ET-743 that can be partially synthesized from safracin B which is a metabolite of Pseudomonas fluorescens. There have been many examples of striking structural similarities between natural products obtained from marine invertebrates and those of microbial origin which suggests that microorganisms living in their invertebrate hosts could be the actual producers of these secondary metabolites. With regard to sustainable biotechnological production of pharmacologically important metabolites from marine invertebrates and their “endosymbionts”, a more advanced strategy is to focus on cloning and expression of the respective key biosynthetic gene clusters. This molecular biological approach will open up new avenues for biotechnological production of drugs or drug candidates from the sea. Full article
Open AccessArticle 13-Epi-9-deacetoxyxenicin, a Cytotoxic Diterpene from the Soft Coral Asterospicularia laurae (Alcyonacea)
Mar. Drugs 2003, 1(1), 18-26; doi:10.3390/md101018
Received: 14 February 2003 / Accepted: 16 October 2003 / Published: 15 November 2003
Cited by 8 | PDF Full-text (139 KB) | HTML Full-text | XML Full-text
Abstract
An investigation of the soft coral Asterospicularia laurae collected on the Great Barrier Reef, Australia, afforded the cytotoxic diterpene 13-epi-9-deacetoxyxenicin (1) in addition to the known metabolites 13-epi-9-deacetylxenicin (2) and gorgosterol. 13-Epi-9-deacetoxyxenicin readily underwent an autoxidation reaction in solution to afford a single
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An investigation of the soft coral Asterospicularia laurae collected on the Great Barrier Reef, Australia, afforded the cytotoxic diterpene 13-epi-9-deacetoxyxenicin (1) in addition to the known metabolites 13-epi-9-deacetylxenicin (2) and gorgosterol. 13-Epi-9-deacetoxyxenicin readily underwent an autoxidation reaction in solution to afford a single product, the hydroperoxide 3. Structures, stereochemistry, and NMR assignments were established by high resolution NMR spectroscopy and by comparison with published data for known compounds. Full article
Open AccessArticle Rigidin E, a New Pyrrolopyrimidine Alkaloid from a Papua New Guinea Tunicate Eudistoma Species
Mar. Drugs 2003, 1(1), 27-33; doi:10.3390/md101027
Received: 18 September 2003 / Accepted: 13 November 2003 / Published: 26 November 2003
Cited by 11 | PDF Full-text (65 KB) | HTML Full-text | XML Full-text
Abstract A new pyrrolopyrimidine alkaloid, rigidin E (1) and the known metabolites rigidin (2) and 1-methylherbipoline (3) have been isolated from a Papua New Guinea tunicate Eudistoma sp. A combination of spectroscopic data were used to determine the structures of these metabolites. Full article
Open AccessArticle Reassembled Biosynthetic Pathway for a Large-scale Synthesis of CMP-Neu5Ac
Mar. Drugs 2003, 1(1), 34-45; doi:10.3390/md101034
Received: 10 October 2003 / Accepted: 13 November 2003 / Published: 26 November 2003
Cited by 4 | PDF Full-text (189 KB) | HTML Full-text | XML Full-text
Abstract
CMP-Neu5Ac is an important sugar nucleotide for biosynthesis of sialic acid and its conjugates. In this paper, a large-scale production system of CMP-Neu5Ac by a single strain is reported. The co-expression of Neu5Ac aldolase (EC4.1.3.3) and CMP-Neu5Ac synthetase (EC 2.7.7.43) was achieved by
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CMP-Neu5Ac is an important sugar nucleotide for biosynthesis of sialic acid and its conjugates. In this paper, a large-scale production system of CMP-Neu5Ac by a single strain is reported. The co-expression of Neu5Ac aldolase (EC4.1.3.3) and CMP-Neu5Ac synthetase (EC 2.7.7.43) was achieved by constructing individual genes into one plasmid and having a single culture that has both NeuAc aldolase and CMP-Neu5Ac synthetase activities. Overall this system only employed N-acetylmannosamine, excess of pyruvate and CTP to produce CMP-Neu5Ac. This work has demonstrated that a large-scale synthesis of sialic acid-derived oligosaccharides could be achieved economically and efficiently through a single, biosynthetic pathway engineered microorganism. Full article
Open AccessArticle Long-Chain Acetylenic Ketones from the Micronesian Sponge Haliclona sp. Importance of the 1-yn-3-ol Group for Antitumor Activity
Mar. Drugs 2003, 1(1), 46-53; doi:10.3390/md101046
Received: 13 October 2003 / Accepted: 13 November 2003 / Published: 26 November 2003
Cited by 6 | PDF Full-text (149 KB) | HTML Full-text | XML Full-text
Abstract
Two new long-chain C33 polyacetylenic compounds, halicynones A and B were isolated from the marine sponge Haliclona sp. along with known analogs. The known compound pellynol A possessing a 1-yn-3-ol terminus, exhibited strong antitumor activity against the human colon tumor cell line
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Two new long-chain C33 polyacetylenic compounds, halicynones A and B were isolated from the marine sponge Haliclona sp. along with known analogs. The known compound pellynol A possessing a 1-yn-3-ol terminus, exhibited strong antitumor activity against the human colon tumor cell line HCT-116 (IC50 0.026 μg/mL), however, the corresponding 1-yn-3-one, halicynone A, was inactive, which suggests an important role for the terminal 1-yn-3-ol functional group in mediating cytotoxic activity. Full article
Open AccessArticle Pseudopterosin Biosynthesis: Aromatization of the Diterpene Cyclase Product, Elisabethatriene
Mar. Drugs 2003, 1(1), 54-65; doi:10.3390/md101054
Received: 15 October 2003 / Accepted: 13 November 2003 / Published: 26 November 2003
Cited by 15 | PDF Full-text (144 KB) | HTML Full-text | XML Full-text
Abstract
Putative precursors in pseudopterosin biosynthesis, the hydrocarbons isoelisabethatriene (10) and erogorgiaene (11), have been identified from an extract of Pseudopterogorgia elisabethae collected in the Florida Keys. Biosynthetic experiments designed to test the utilization of these compounds in pseudopterosin production revealed that erogorgiaene is
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Putative precursors in pseudopterosin biosynthesis, the hydrocarbons isoelisabethatriene (10) and erogorgiaene (11), have been identified from an extract of Pseudopterogorgia elisabethae collected in the Florida Keys. Biosynthetic experiments designed to test the utilization of these compounds in pseudopterosin production revealed that erogorgiaene is transformed to pseudopterosins A-D. Together with our previous data, it is now apparent that early steps in pseudopterosin biosynthesis involve the cyclization of geranylgeranyl diphosphate to elisabethatriene followed by the dehydrogenation and aromatization to erogorgiaene. Full article

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