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Marine Bioactive Natural Product Studies in Europe

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A special issue of Marine Drugs (ISSN 1660-3397).

Deadline for manuscript submissions: closed (30 November 2018) | Viewed by 38175

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Special Issue Editor

Dr. Päivi Tammela

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Guest Editor

Drug Research Program, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5E, FI-00014 Helsinki, Finland
Interests: drug discovery; screening; antimicrobials; natural products

Special Issue Information

Dear Colleagues

Marine natural products as a source of bioactive compounds have attracted increased attention during the past decades, and several large-scale explorations of marine natural products have been launched especially in Europe. The biodiversity in marine resources offers great possibilities for discovering novel bioactive compounds with potential use, for example, in drug discovery for various therapeutic applications. Marine natural products have been particularly important in development of novel anticancer, antimicrobial and analgesic agents. However, the biodiversity and structural complexity of compounds stemming from marine natural products bring along several challenges that needs to be overcome in the process.

This special issue of Marine Drugs aims to assemble a collection of recent studies on marine bioactive natural products carried out in Europe, and to highlight some of the solutions developed by scientists to enhance the discovery of bioactive marine compounds.

Dr. Päivi Tammela
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Marine Drugs is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

marine natural products
drug discovery
bioactive
anticancer
antimicrobial
analgesic
natural product chemistry

Published Papers (5 papers)

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Research

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18 pages, 1606 KiB

Open AccessArticle

Potential Usefulness of a Wakame/Carob Functional Snack for the Treatment of Several Aspects of Metabolic Syndrome: From In Vitro to In Vivo Studies

by Cristina Martínez-Villaluenga, Elena Peñas, Daniel Rico, Ana Belén Martin-Diana, Maria P. Portillo, Maria Teresa Macarulla, Daniel Antonio De Luis and Jonatan Miranda

Mar. Drugs 2018, 16(12), 512; https://doi.org/10.3390/md16120512 - 17 Dec 2018

Cited by 10 | Viewed by 3693

Abstract

Metabolic syndrome (MetS) greatly increases the risk of cardiovascular diseases and type 2 diabetes mellitus. The aim of this study was to evaluate the efficacy of functional snacks containing a combination of wakame (W) and carob pod (CP) flours in reducing markers associated with MetS. The mechanisms of action underlying these effects were also evaluated. In vitro approaches were carried out in mature 3T3-L1 adipocytes and RAW 264.7 macrophages treated with different doses of extracts from W, CP, or a combination of both. Furthermore, an in vivo experiment was conducted in rats with MetS treated with normal-caloric diets containing different snack formulations with combinations of 1/50 (snack A) or 1/5 of wakame/carob (snack B). In vitro experiments results indicated that both W and CP had delipidating effects, but only the latter induced anti-inflammatory and anti-hypertensive effects. As far as the in vivo study is concerned, snack B was ineffective and snack A showed an anti-hypertensive effect in rats with MetS. The present study shows for the first time the in vitro efficacy of a W and CP combination as an anti-inflammatory, delipidating, and anti-hypertensive tool, and its potential usefulness in treating MetS. Full article

(This article belongs to the Special Issue Marine Bioactive Natural Product Studies in Europe)

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26 pages, 19704 KiB

Open AccessArticle

Synthesis and Antiproliferative Activity of Marine Bromotyrosine Purpurealidin I and Its Derivatives

by Chinmay Bhat, Polina Ilina, Irene Tilli, Manuela Voráčová, Tanja Bruun, Victoria Barba, Nives Hribernik, Katja-Emilia Lillsunde, Eero Mäki-Lohiluoma, Tobias Rüffer, Heinrich Lang, Jari Yli-Kauhaluoma, Paula Kiuru and Päivi Tammela

Mar. Drugs 2018, 16(12), 481; https://doi.org/10.3390/md16120481 - 03 Dec 2018

Cited by 7 | Viewed by 4846

Abstract

The first total synthesis of the marine bromotyrosine purpurealidin I (1) using trifluoroacetoxy protection group and its dimethylated analog (29) is reported along with 16 simplified bromotyrosine derivatives lacking the tyramine moiety. Their cytotoxicity was evaluated against the human malignant melanoma cell line (A-375) and normal skin fibroblast cells (Hs27) together with 33 purpurealidin-inspired simplified amides, and the structure–activity relationships were investigated. The synthesized simplified analogs without the tyramine part retained the cytotoxic activity. Purpurealidin I (1) showed no selectivity but its simplified pyridin-2-yl derivative (36) had the best improvement in selectivity (Selectivity index 4.1). This shows that the marine bromotyrosines are promising scaffolds for developing cytotoxic agents and the full understanding of the elements of their SAR and improving the selectivity requires further optimization of simplified bromotyrosine derivatives. Full article

(This article belongs to the Special Issue Marine Bioactive Natural Product Studies in Europe)

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12 pages, 5830 KiB

Open AccessArticle

Marine Microalgae: Promising Source for New Bioactive Compounds

by Caterina R. De Vera, Guillermo Díaz Crespín, Antonio Hernández Daranas, Sofia Montalvão Looga, Katja-Emilia Lillsunde, Päivi Tammela, Merja Perälä, Vesa Hongisto, Johannes Virtanen, Heiko Rischer, Christian D. Muller, Manuel Norte, José J. Fernández and María L. Souto

Mar. Drugs 2018, 16(9), 317; https://doi.org/10.3390/md16090317 - 06 Sep 2018

Cited by 43 | Viewed by 6976

Abstract

The study of marine natural products for their bioactive potential has gained strength in recent years. Oceans harbor a vast variety of organisms that offer a biological and chemical diversity with metabolic abilities unrivalled in terrestrial systems, which makes them an attractive target for bioprospecting as an almost untapped resource of biotechnological applications. Among them, there is no doubt that microalgae could become genuine “cell factories” for the biological synthesis of bioactive substances. Thus, in the course of inter-laboratory collaboration sponsored by the European Union (7th FP) into the MAREX Project focused on the discovery of novel bioactive compounds of marine origin for the European industry, a bioprospecting study on 33 microalgae strains was carried out. The strains were cultured at laboratory scale. Two extracts were prepared for each one (biomass and cell free culture medium) and, thus, screened to provide information on the antimicrobial, the anti-proliferative, and the apoptotic potential of the studied extracts. The outcome of this study provides additional scientific data for the selection of Alexandrium tamarensis WE, Gambierdiscus australes, Prorocentrum arenarium, Prorocentrum hoffmannianum, and Prorocentrum reticulatum (Pr-3) for further investigation and offers support for the continued research of new potential drugs for human therapeutics from cultured microalgae. Full article

(This article belongs to the Special Issue Marine Bioactive Natural Product Studies in Europe)

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10 pages, 1186 KiB

Open AccessArticle

Pharmacokinetic and Tissue Distribution of Fucoidan from Fucus vesiculosus after Oral Administration to Rats

by Olga N. Pozharitskaya, Alexander N. Shikov, Natalya M. Faustova, Ekaterina D. Obluchinskaya, Vera M. Kosman, Heikki Vuorela and Valery G. Makarov

Mar. Drugs 2018, 16(4), 132; https://doi.org/10.3390/md16040132 - 18 Apr 2018

Cited by 93 | Viewed by 7024

Abstract

Fucus vesiculosus L., known as bladderwrack, belongs to the brown seaweeds, which are widely distributed throughout northern Russia, Atlantic shores of Europe, the Baltic Sea, Greenland, the Azores, the Canary Islands, and shores of the Pacific Ocean. Fucoidan is a major fucose-rich sulfated polysaccharide found in Fucus (F.) vesiculosus. The pharmacokinetic profiling of active compounds is essential for drug development and approval. The aim of the study was to evaluate the pharmacokinetics and tissue distribution of fucoidan in rats after a single-dose oral administration. Fucoidan was isolated from F. vesiculosus. The method of measuring anti-activated factor X (anti-Xa) activity by amidolytic assay was used to analyze the plasma and tissue concentrations of fucoidan. The tissue distribution of fucoidan after intragastric administration to the rats was characterized, and it exhibited considerable heterogeneity. Fucoidan preferentially accumulates in the kidneys (AUC_0–t = 10.74 µg·h/g; C_max = 1.23 µg/g after 5 h), spleen (AUC_0–t = 6.89 µg·h/g; C_max = 0.78 µg/g after 3 h), and liver (AUC_0–t = 3.26 µg·h/g; C_max = 0.53 µg/g after 2 h) and shows a relatively long absorption time and extended circulation in the blood, with a mean residence time (MRT) = 6.79 h. The outcome of this study provides additional scientific data for traditional use of fucoidan-containing plants and offers tangible support for the continued development of new effective pharmaceuticals using fucoidan. Full article

(This article belongs to the Special Issue Marine Bioactive Natural Product Studies in Europe)

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Review

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30 pages, 866 KiB

Open AccessReview

Fucoidan Structure and Activity in Relation to Anti-Cancer Mechanisms

by Geert Van Weelden, Marcin Bobiński, Karolina Okła, Willem Jan Van Weelden, Andrea Romano and Johanna M. A. Pijnenborg

Mar. Drugs 2019, 17(1), 32; https://doi.org/10.3390/md17010032 - 07 Jan 2019

Cited by 204 | Viewed by 15146

Abstract

Fucoidan is a natural derived compound found in different species of brown algae and in some animals, that has gained attention for its anticancer properties. However, the exact mechanism of action is currently unknown. Therefore, this review will address fucoidans structure, the bioavailability, and all known different pathways affected by fucoidan, in order to formulate fucoidans structure and activity in relation to its anti-cancer mechanisms. The general bioactivity of fucoidan is difficult to establish due to factors like species-related structural diversity, growth conditions, and the extraction method. The main pathways influenced by fucoidan are the PI3K/AKT, the MAPK pathway, and the caspase pathway. PTEN seems to be important in the fucoidan-mediated effect on the AKT pathway. Furthermore, the interaction with VEGF, BMP, TGF-β, and estrogen receptors are discussed. Also, fucoidan as an adjunct seems to have beneficial effects, for both the enhanced effectiveness of chemotherapy and reduced toxicity in healthy cells. In conclusion, the multipotent character of fucoidan is promising in future anti-cancer treatment. However, there is a need for more specified studies of the structure–activity relationship of fucoidan from the most promising seaweed species. Full article

(This article belongs to the Special Issue Marine Bioactive Natural Product Studies in Europe)

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