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Marine Drugs
Special Issues
Marine Natural Products and Obesity 2020
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Marine Natural Products and Obesity 2020

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

Deadline for manuscript submissions: closed (31 January 2021) | Viewed by 17656

Special Issue Editors

Dr. Ralph Urbatzka

E-Mail Website
Guest Editor
CIIMAR – Interdisciplinary Centre of Marine and Environmental Research, Matosinhos, Portugal
Interests: bioactivity screening; natural products; elucidation of molecular mechanism; obesity and related diseases; cyanobacteria bioactive compounds
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Vitor Vasconcelos

E-Mail Website
Co-Guest Editor
1. Faculdade de Ciências da Universidade do Porto, 4169-007 Porto, Portugal
2. CIIMAR, Interdisciplinary Centre of Marine and Environmental Research of the University of Porto, 4450-208 Porto, Portugal
Interests: cyanobacteria; toxins; cyanotoxins; marine biotechnology; secondary metabolites; cyanobacterial blooms; ecotoxicology; environmental contamination
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The prevalence of obesity and related co-morbidities is increasing worldwide, posing serious health problems. Changes in lifestyle and diet are the best remedies to fight obesity; however, many people still rely on medical aids. Marine organisms have been prolific in the production of bioactive compounds for many diseases and promise to be an excellent source of naturally derived molecules and novel nutraceuticals. Bioactive compounds from diverse marine organisms, including marine algae, bacteria, sponges, fungi, crustaceans and fish, have been described as having beneficial activities towards obesity .

This Special Issue will highlight progress in the following topics: the use of bioactive compounds from marine organisms for the treatment of obesity and obesity-related co-morbidities (e.g., diabetes, fatty liver, hyperlipidemia); the isolation of novel compounds; the bioactivity screening of marine organisms; and the elucidation of molecular modes of action of marine bioactive compounds.

Dr. Ralph Urbatzka
Prof. Vítor Vasconcelos
Guest Editors

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 bioactive compounds
  • obesity and related co-morbidities (diabetes, fatty liver, hyperlipidemia)
  • bioactivity screening
  • structural elucidation
  • molecular mode of action

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Published Papers (4 papers)

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Research

13 pages, 1914 KiB  
Article
Inhibition of Intestinal Lipid Absorption by Cyanobacterial Strains in Zebrafish Larvae
by Marta Bellver, Susana Lemos da Costa, Begoña Astrain Sanchez, Vitor Vasconcelos and Ralph Urbatzka
Mar. Drugs 2021, 19(3), 161; https://doi.org/10.3390/md19030161 - 18 Mar 2021
Cited by 9 | Viewed by 3708
Abstract
Obesity is a complex metabolic disease, which is increasing worldwide. The reduction of dietary lipid intake is considered an interesting pathway to reduce fat absorption and to affect the chronic energy imbalance. In this study, zebrafish larvae were used to analyze effects of [...] Read more.
Obesity is a complex metabolic disease, which is increasing worldwide. The reduction of dietary lipid intake is considered an interesting pathway to reduce fat absorption and to affect the chronic energy imbalance. In this study, zebrafish larvae were used to analyze effects of cyanobacteria on intestinal lipid absorption in vivo. In total, 263 fractions of a cyanobacterial library were screened for PED6 activity, a fluorescent reporter of intestinal lipases, and 11 fractions reduced PED6 activity > 30%. Toxicity was not observed for those fractions, considering mortality, malformations or digestive physiology (protease inhibition). Intestinal long-chain fatty acid uptake (C16) was reduced, but not short-chain fatty acid uptake (C5). Alteration of lipid classes by high-performance thin-layer chromatography (HPTLC) or lipid processing by fluorescent HPTLC was analyzed, and 2 fractions significantly reduced the whole-body triglyceride level. Bioactivity-guided feature-based molecular networking of LC-MS/MS data identified 14 significant bioactive mass peaks (p < 0.01, correlation > 0.95), which consisted of 3 known putative and 11 unknown compounds. All putatively identified compounds were known to be involved in lipid metabolism and obesity. Summarizing, some cyanobacterial strains repressed intestinal lipid absorption without any signs of toxicity and could be developed in the future as nutraceuticals to combat obesity. Full article
(This article belongs to the Special Issue Marine Natural Products and Obesity 2020)
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18 pages, 3352 KiB  
Article
Syntheses and Glycosidase Inhibitory Activities, and in Silico Docking Studies of Pericosine E Analogs Methoxy-Substituted at C6
by Yoshihide Usami, Megumi Higuchi, Koji Mizuki, Mizuki Yamamoto, Mao Kanki, Chika Nakasone, Yuya Sugimoto, Makio Shibano, Yoshihiro Uesawa, Junko Nagai, Hiroki Yoneyama and Shinya Harusawa
Mar. Drugs 2020, 18(4), 221; https://doi.org/10.3390/md18040221 - 20 Apr 2020
Cited by 5 | Viewed by 2683
Abstract
Inspired by the significant α-glucosidase inhibitory activities of (+)- and (−)-pericosine E, we herein designed and synthesized 16 analogs of these marine natural products bearing a methoxy group instead of a chlorine atom at C6. Four of these compounds exhibited moderate α-glucosidase inhibitory [...] Read more.
Inspired by the significant α-glucosidase inhibitory activities of (+)- and (−)-pericosine E, we herein designed and synthesized 16 analogs of these marine natural products bearing a methoxy group instead of a chlorine atom at C6. Four of these compounds exhibited moderate α-glucosidase inhibitory activities, which were weaker than those of the corresponding chlorine-containing species. The four compounds could be prepared by coupling reactions utilizing the (−)-pericosine B moiety. An additional in silico docking simulation suggested that the reason of reduced activity of the C6-methoxylated analogs might be an absence of hydrogen bonding between a methoxy group with the surrounding amino acid residues in the active site in α-glucosidase. Full article
(This article belongs to the Special Issue Marine Natural Products and Obesity 2020)
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16 pages, 2004 KiB  
Article
The Marine Seagrass Halophila stipulacea as a Source of Bioactive Metabolites against Obesity and Biofouling
by Sawssen Bel Mabrouk, Mariana Reis, Maria Lígia Sousa, Tiago Ribeiro, Joana R. Almeida, Sandra Pereira, Jorge Antunes, Filipa Rosa, Vitor Vasconcelos, Lotfi Achour, Adnen Kacem and Ralph Urbatzka
Mar. Drugs 2020, 18(2), 88; https://doi.org/10.3390/md18020088 - 29 Jan 2020
Cited by 25 | Viewed by 5997
Abstract
Marine organisms, including seagrasses, are important sources of biologically active molecules for the treatment of human diseases. In this study, organic extracts of the marine seagrass Halophila stipulacea obtained by different polarities from leaves (L) and stems (S) (hexane [HL, HS], ethyl acetate [...] Read more.
Marine organisms, including seagrasses, are important sources of biologically active molecules for the treatment of human diseases. In this study, organic extracts of the marine seagrass Halophila stipulacea obtained by different polarities from leaves (L) and stems (S) (hexane [HL, HS], ethyl acetate [EL, ES], and methanol [ML, MS]) were tested for different bioactivities. The screening comprehended the cytotoxicity activity against cancer cell lines grown as a monolayer culture or as multicellular spheroids (cancer), glucose uptake in cells (diabetes), reduction of lipid content in fatty acid-overloaded liver cells (steatosis), and lipid-reducing activity in zebrafish larvae (obesity), as well as the antifouling activity against marine bacteria (microfouling) and mussel larval settlement (macrofouling). HL, EL, HS, and ES extracts showed statistically significant cytotoxicity against cancer cell lines. The extracts did not have any significant effect on glucose uptake and on the reduction of lipids in liver cells. The EL and ML extracts reduced neutral lipid contents on the larvae of zebrafish with EC50 values of 2.2 µg/mL for EL and 1.2 µg/mL for ML. For the antifouling activity, the HS and ML extracts showed a significant inhibitory effect (p < 0.05) against the settlement of Mytilus galloprovincialis plantigrade larvae. The metabolite profiling using HR-LC-MS/MS and GNPS (The Global Natural Product Social Molecular Networking) analyses identified a variety of known primary and secondary metabolites in the extracts, along with some unreported molecules. Various compounds were detected with known activities on cancer (polyphenols: Luteolin, apeginin, matairesinol), on metabolic diseases (polyphenols: cirsimarin, spiraeoside, 2,4-dihydroxyheptadec-16-ynyl acetate; amino acids: N-acetyl-L-tyrosine), or on antifouling (fatty acids: 13-decosenamide; cinnamic acids: 3-hydroxy-4-methoxycinnamic acid, alpha-cyano-4-hydroxycinnamic), which could be, in part, responsible for the observed bioactivities. In summary, this study revealed that Halophila stipulacea is a rich source of metabolites with promising activities against obesity and biofouling and suggests that this seagrass could be useful for drug discovery in the future. Full article
(This article belongs to the Special Issue Marine Natural Products and Obesity 2020)
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30 pages, 3951 KiB  
Article
Modulation of the Liver Protein Carbonylome by the Combined Effect of Marine Omega-3 PUFAs and Grape Polyphenols Supplementation in Rats Fed an Obesogenic High Fat and High Sucrose Diet
by Lucía Méndez, Silvia Muñoz, Bernat Miralles-Pérez, Maria Rosa Nogués, Sara Ramos-Romero, Josep Lluis Torres and Isabel Medina
Mar. Drugs 2020, 18(1), 34; https://doi.org/10.3390/md18010034 - 30 Dec 2019
Cited by 9 | Viewed by 4202
Abstract
Diet-induced obesity has been linked to metabolic disorders such as cardiovascular diseases and type 2 diabetes. A factor linking diet to metabolic disorders is oxidative stress, which can damage biomolecules, especially proteins. The present study was designed to investigate the effect of marine [...] Read more.
Diet-induced obesity has been linked to metabolic disorders such as cardiovascular diseases and type 2 diabetes. A factor linking diet to metabolic disorders is oxidative stress, which can damage biomolecules, especially proteins. The present study was designed to investigate the effect of marine omega-3 polyunsaturated fatty acids (PUFAs) (eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA)) and their combination with grape seed polyphenols (GSE) on carbonyl-modified proteins from plasma and liver in Wistar Kyoto rats fed an obesogenic diet, namely high-fat and high-sucrose (HFHS) diet. A proteomics approach consisting of fluorescein 5-thiosemicarbazide (FTSC) labelling of protein carbonyls, visualization of FTSC-labelled protein on 1-DE or 2-DE gels, and protein identification by MS/MS was used for the protein oxidation assessment. Results showed the efficiency of the combination of both bioactive compounds in decreasing the total protein carbonylation induced by HFHS diet in both plasma and liver. The analysis of carbonylated protein targets, also referred to as the ‘carbonylome’, revealed an individual response of liver proteins to supplements and a modulatory effect on specific metabolic pathways and processes due to, at least in part, the control exerted by the supplements on the liver protein carbonylome. This investigation highlights the additive effect of dietary fish oils and grape seed polyphenols in modulating in vivo oxidative damage of proteins induced by the consumption of HFHS diets. Full article
(This article belongs to the Special Issue Marine Natural Products and Obesity 2020)
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