Targeting Enzymatic Pathways with Marine‐Derived Clinical Agents

Pereira, Renato B.; Dasari, Ramesh; Lefranc, Florence; Kornienko, Alexander; Kiss, Róbert; Gomes, Nelson G.M.

doi:10.1002/9783527805921.ch10

Cited by 2 publications

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References 105 publications

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“…Bioprospection of marine organisms as producers of structurally complex and biologically active metabolites has been particularly rewarding as there are now over 29,000 marine natural products, approximately 41% being discovered in the last ten years [1]. So far, the clinical utility of marine-derived agents has been translated into the development of seven drugs approved by the Food and Drug Administration (FDA) and the European Medicines Agency (EMA) [2,3]. The discovery of increasing numbers of marine natural products has also spurred the investigation of the medicinal chemistry of diketopiperazines which appear to abound in the marine environment [4,5].…”

Section: General Considerationsmentioning

confidence: 99%

Double the Chemistry, Double the Fun: Structural Diversity and Biological Activity of Marine-Derived Diketopiperazine Dimers

et al. 2019

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While several marine natural products bearing the 2,5-diketopiperazine ring have been reported to date, the unique chemistry of dimeric frameworks appears to remain neglected. Frequently reported from marine-derived strains of fungi, many naturally occurring diketopiperazine dimers have been shown to display a wide spectrum of pharmacological properties, particularly within the field of cancer and antimicrobial therapy. While their structures illustrate the unmatched power of marine biosynthetic machinery, often exhibiting unsymmetrical connections with rare linkage frameworks, enhanced binding ability to a variety of pharmacologically relevant receptors has been also witnessed. The existence of a bifunctional linker to anchor two substrates, resulting in a higher concentration of pharmacophores in proximity to recognition sites of several receptors involved in human diseases, portrays this group of metabolites as privileged lead structures for advanced pre-clinical and clinical studies. Despite the structural novelty of various marine diketopiperazine dimers and their relevant bioactive properties in several models of disease, to our knowledge, this attractive subclass of compounds is reviewed here for the first time.

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Section: General Considerationsmentioning

confidence: 99%

Double the Chemistry, Double the Fun: Structural Diversity and Biological Activity of Marine-Derived Diketopiperazine Dimers

et al. 2019

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“…The increasing number of reports on the structural variety and pharmacological properties of naturally occurring compounds obtained from marine invertebrates [ 1 , 2 ] has been driving the focus on several taxonomic groups, namely Heterobranchia mollusks [ 3 , 4 ].…”

Section: Introductionmentioning

confidence: 99%

Profiling of Heterobranchia Sea Slugs from Portuguese Coastal Waters as Producers of Anti-Cancer and Anti-Inflammatory Agents

et al. 2018

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Bioprospection of marine invertebrates has been predominantly biased by the biological richness of tropical regions, thus neglecting macro-organisms from temperate ecosystems. Species that were not the object of studies on their biochemical composition include the Heterobranchia gastropods Armina maculata, Armina tigrina and Aglaja tricolorata, inhabitants of the Portuguese Atlantic coastal waters. Here, we present for the first time the fatty acid profile of neutral lipids and homarine content of these three species. Qualitative and quantitative differences in the fatty acid content among species points to the existence of a fatty acid profile of neutral lipids, particularly of each genus. The results from cytotoxicity assays, using the acetonic extracts of the gastropods on human gastric adenocarcinoma (AGS) and human lung adenocarcinoma (A549) cell lines, revealed a pronounced cytotoxic effect of the A. tigrina extract on both cell lines (IC50 values of 68.75 and 69.77 μg mL−1 for AGS and A549, respectively). It is worth noting the significant reduction of NO levels in LPS-challenged RAW 264.7 macrophages exposed to A. tricolorata extract, at concentrations as low as 125 μg mL−1.

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Targeting Enzymatic Pathways with Marine‐Derived Clinical Agents

Cited by 2 publications

References 105 publications

Double the Chemistry, Double the Fun: Structural Diversity and Biological Activity of Marine-Derived Diketopiperazine Dimers

Double the Chemistry, Double the Fun: Structural Diversity and Biological Activity of Marine-Derived Diketopiperazine Dimers

Profiling of Heterobranchia Sea Slugs from Portuguese Coastal Waters as Producers of Anti-Cancer and Anti-Inflammatory Agents

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