Next Issue
Volume 19, December
Previous Issue
Volume 19, October
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
9.6
5.4
Journals
Marine Drugs
Volume 19
Issue 11
share announcement

Mar. Drugs, Volume 19, Issue 11 (November 2021) – 66 articles

Cover Story (view full-size image): The poor therapeutic response to glucocorticoid (GC) treatment is one of the challenges that the management of severe asthma faces. Compounds derived from marine sources have received increasing interest due to their potential for drug development. Based on the pathobiological features associated with GC resistance in severe asthma, many studies have previously described GC resistance mechanisms as potential therapeutic targets. Additionally, other studies have described the potential anti-inflammatory effects of marine-derived active compounds. This article compiles research regarding marine-derived compounds that target the pathogenic molecular mechanisms involved in GC-resistant asthma, and provides a basis for the development of effective marine-derived drugs.View this paper
  • Issues are regarded as officially published after their release is announced to the table of contents alert mailing list.
  • You may sign up for e-mail alerts to receive table of contents of newly released issues.
  • PDF is the official format for papers published in both, html and pdf forms. To view the papers in pdf format, click on the "PDF Full-text" link, and use the free Adobe Reader to open them.
Order results
Result details
Section
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
52 pages, 17327 KiB  
Review
In Silico Prediction of Steroids and Triterpenoids as Potential Regulators of Lipid Metabolism
by Valery M. Dembitsky
Mar. Drugs 2021, 19(11), 650; https://doi.org/10.3390/md19110650 - 22 Nov 2021
Cited by 17 | Viewed by 4919
Abstract
This review focuses on a rare group of steroids and triterpenoids that share common properties as regulators of lipid metabolism. This group of compounds is divided by the type of chemical structure, and they represent: aromatic steroids, steroid phosphate esters, highly oxygenated steroids [...] Read more.
This review focuses on a rare group of steroids and triterpenoids that share common properties as regulators of lipid metabolism. This group of compounds is divided by the type of chemical structure, and they represent: aromatic steroids, steroid phosphate esters, highly oxygenated steroids such as steroid endoperoxides and hydroperoxides, α,β-epoxy steroids, and secosteroids. In addition, subgroups of carbon-bridged steroids, neo steroids, miscellaneous steroids, as well as synthetic steroids containing heteroatoms S (epithio steroids), Se (selena steroids), Te (tellura steroids), and At (astatosteroids) were presented. Natural steroids and triterpenoids have been found and identified from various sources such as marine sponges, soft corals, starfish, and other marine invertebrates. In addition, this group of rare lipids is found in fungi, fungal endophytes, and plants. The pharmacological profile of the presented steroids and triterpenoids was determined using the well-known computer program PASS, which is currently available online for all interested scientists and pharmacologists and is currently used by research teams from more than 130 countries of the world. Our attention has been focused on the biological activities of steroids and triterpenoids associated with the regulation of cholesterol metabolism and related processes such as anti-hyperlipoproteinemic activity, as well as the treatment of atherosclerosis, lipoprotein disorders, or inhibitors of cholesterol synthesis. In addition, individual steroids and triterpenoids were identified that demonstrated rare or unique biological activities such as treating neurodegenerative diseases, Alzheimer’s, and Parkinson’s diseases with a high degree of certainty over 95 percent. For individual steroids or triterpenoids or a group of compounds, 3D drawings of their predicted biological activities are presented. Full article
►▼ Show Figures

Graphical abstract

17 pages, 1109 KiB  
Review
Surface Glucan Structures in Aeromonas spp.
by Elena Mendoza-Barberá, Susana Merino and Juan Tomás
Mar. Drugs 2021, 19(11), 649; https://doi.org/10.3390/md19110649 - 22 Nov 2021
Cited by 11 | Viewed by 2182
Abstract
Aeromonas spp. are generally found in aquatic environments, although they have also been isolated from both fresh and processed food. These Gram-negative, rod-shaped bacteria are mostly infective to poikilothermic animals, although they are also considered opportunistic pathogens of both aquatic and terrestrial homeotherms, [...] Read more.
Aeromonas spp. are generally found in aquatic environments, although they have also been isolated from both fresh and processed food. These Gram-negative, rod-shaped bacteria are mostly infective to poikilothermic animals, although they are also considered opportunistic pathogens of both aquatic and terrestrial homeotherms, and some species have been associated with gastrointestinal and extraintestinal septicemic infections in humans. Among the different pathogenic factors associated with virulence, several cell-surface glucans have been shown to contribute to colonization and survival of Aeromonas pathogenic strains, in different hosts. Lipopolysaccharide (LPS), capsule and α-glucan structures, for instance, have been shown to play important roles in bacterial–host interactions related to pathogenesis, such as adherence, biofilm formation, or immune evasion. In addition, glycosylation of both polar and lateral flagella has been shown to be mandatory for flagella production and motility in different Aeromonas strains, and has also been associated with increased bacterial adhesion, biofilm formation, and induction of the host proinflammatory response. The main aspects of these structures are covered in this review. Full article
(This article belongs to the Special Issue Evaluation of Bioactive Properties of Marine-Derived Polysaccharides and Oligosaccharides)
►▼ Show Figures

Figure 1

15 pages, 2295 KiB  
Article
Selection of Culture Conditions and Cell Morphology for Biocompatible Extraction of β-Carotene from Dunaliella salina
by Guillaume Tanguy, Aline Legat, Olivier Gonçalves, Luc Marchal and Benoît Schoefs
Mar. Drugs 2021, 19(11), 648; https://doi.org/10.3390/md19110648 - 22 Nov 2021
Cited by 1 | Viewed by 2450
Abstract
Biocompatible extraction emerges recently as a means to reduce costs of biotechnology processing of microalgae. In this frame, this study aimed at determining how specific culture conditions and the associated cell morphology impact the biocompatibility and the extraction yield of β-carotene from the [...] Read more.
Biocompatible extraction emerges recently as a means to reduce costs of biotechnology processing of microalgae. In this frame, this study aimed at determining how specific culture conditions and the associated cell morphology impact the biocompatibility and the extraction yield of β-carotene from the green microalga Dunaliella salina using n-decane. The results highlight the relationship between the cell disruption yield and cell volume, the circularity and the relative abundance of naturally permeabilized cells. The disruption rate increased with both the cell volume and circularity. This was particularly obvious for volume and circularity exceeding 1500 µm3 and 0.7, respectively. The extraction of β-carotene was the most biocompatible with small (600 µm3) and circular cells (0.7) stressed in photobioreactor (30% of carotenoids recovery with 15% cell disruption). The naturally permeabilized cells were disrupted first; the remaining cells seems to follow a gradual permeabilization process: reversibility (up to 20 s) then irreversibility and cell disruption. This opens new carotenoid production schemes based on growing robust β-carotene enriched cells to ensure biocompatible extraction. Full article
(This article belongs to the Special Issue Marine Pigments)
►▼ Show Figures

Figure 1

14 pages, 1523 KiB  
Article
First Report of OvoA Gene in Marine Arthropods: A New Candidate Stress Biomarker in Copepods
by Vittoria Roncalli, Chiara Lauritano and Ylenia Carotenuto
Mar. Drugs 2021, 19(11), 647; https://doi.org/10.3390/md19110647 - 20 Nov 2021
Cited by 7 | Viewed by 2058
Abstract
Ovothiol is one of the most powerful antioxidants acting in marine organisms as a defense against oxidative stress during development and in response to environmental cues. The gene involved in the ovothiol biosynthesis, OvoA, is found in almost all metazoans, but open questions [...] Read more.
Ovothiol is one of the most powerful antioxidants acting in marine organisms as a defense against oxidative stress during development and in response to environmental cues. The gene involved in the ovothiol biosynthesis, OvoA, is found in almost all metazoans, but open questions existed on its presence among arthropods. Here, using an in silico workflow, we report a single OvoA gene in marine arthropods including copepods, decapods, and amphipods. Phylogenetic analyses indicated that OvoA from marine arthropods separated from the other marine phyla (e.g., Porifera, Mollusca) and divided into two separate branches, suggesting a possible divergence through evolution. In the copepod Calanus finmarchicus, we suggest that OvoA has a defense role in oxidative stress as shown by its high expression in response to a toxic diet and during the copepodite stage, a developmental stage that includes significant morphological changes. Overall, the results of our study open possibilities for the use of OvoA as a biomarker of stress in copepods and possibly also for other marine holozooplankters. The finding of OvoA in copepods is also promising for the drug discovery field, suggesting the possibility of using copepods as a new source of bioactive compounds to be tested in the marine biotechnological sector. Full article
(This article belongs to the Special Issue Marine Anti-inflammatory and Antioxidant Agents 2021)
►▼ Show Figures

Figure 1

15 pages, 4240 KiB  
Article
Complete Lipooligosaccharide Structure from Pseudoalteromonas nigrifaciens Sq02-Rifr and Study of Its Immunomodulatory Activity
by Rossella Di Guida, Angela Casillo, Antonietta Stellavato, Celeste Di Meo, Soichiro Kawai, Jun Kawamoto, Takuya Ogawa, Tatsuo Kurihara, Chiara Schiraldi and Maria Michela Corsaro
Mar. Drugs 2021, 19(11), 646; https://doi.org/10.3390/md19110646 - 19 Nov 2021
Cited by 3 | Viewed by 1972
Abstract
Lipopolysaccharides (LPS) are surface glycoconjugates embedded in the external leaflet of the outer membrane (OM) of the Gram-negative bacteria. They consist of three regions: lipid A, core oligosaccharide (OS), and O-specific polysaccharide or O-antigen. Lipid A is the glycolipid endotoxin domain that anchors [...] Read more.
Lipopolysaccharides (LPS) are surface glycoconjugates embedded in the external leaflet of the outer membrane (OM) of the Gram-negative bacteria. They consist of three regions: lipid A, core oligosaccharide (OS), and O-specific polysaccharide or O-antigen. Lipid A is the glycolipid endotoxin domain that anchors the LPS molecule to the OM, and therefore, its chemical structure is crucial in the maintenance of membrane integrity in the Gram-negative bacteria. In this paper, we reported the characterization of the lipid A and OS structures from Pseudoalteromonas nigrifaciens Sq02-Rifr, which is a psychrotrophic Gram-negative bacterium isolated from the intestine of Seriola quinqueradiata. The immunomodulatory activity of both LPS and lipid A was also examined. Full article
(This article belongs to the Special Issue Marine Oligosaccharides and Polysaccharides 2.0)
►▼ Show Figures

Figure 1

77 pages, 29279 KiB  
Review
Untapped Potential of Marine-Associated Cladosporium Species: An Overview on Secondary Metabolites, Biotechnological Relevance, and Biological Activities
by Gamal A. Mohamed and Sabrin R. M. Ibrahim
Mar. Drugs 2021, 19(11), 645; https://doi.org/10.3390/md19110645 - 18 Nov 2021
Cited by 29 | Viewed by 2799
Abstract
The marine environment is an underexplored treasure that hosts huge biodiversity of microorganisms. Marine-derived fungi are a rich source of novel metabolites with unique structural features, bioactivities, and biotechnological applications. Marine-associated Cladosporium species have attracted considerable interest because of their ability to produce [...] Read more.
The marine environment is an underexplored treasure that hosts huge biodiversity of microorganisms. Marine-derived fungi are a rich source of novel metabolites with unique structural features, bioactivities, and biotechnological applications. Marine-associated Cladosporium species have attracted considerable interest because of their ability to produce a wide array of metabolites, including alkaloids, macrolides, diketopiperazines, pyrones, tetralones, sterols, phenolics, terpenes, lactones, and tetramic acid derivatives that possess versatile bioactivities. Moreover, they produce diverse enzymes with biotechnological and industrial relevance. This review gives an overview on the Cladosporium species derived from marine habitats, including their metabolites and bioactivities, as well as the industrial and biotechnological potential of these species. In the current review, 286 compounds have been listed based on the reported data from 1998 until July 2021. Moreover, more than 175 references have been cited. Full article
►▼ Show Figures

Figure 1

24 pages, 2775 KiB  
Article
Deep-Water Fish Are Potential Vectors of Ciguatera Poisoning in the Gambier Islands, French Polynesia
by Hélène Taiana Darius, Taina Revel, Philippe Cruchet, Jérôme Viallon, Clémence Mahana iti Gatti, Manoëlla Sibat, Philipp Hess and Mireille Chinain
Mar. Drugs 2021, 19(11), 644; https://doi.org/10.3390/md19110644 - 17 Nov 2021
Cited by 9 | Viewed by 3120
Abstract
Ciguatera poisoning (CP) cases linked to the consumption of deep-water fish occurred in 2003 in the Gambier Islands (French Polynesia). In 2004, on the request of two local fishermen, the presence of ciguatoxins (CTXs) was examined in part of their fish catches, i.e., [...] Read more.
Ciguatera poisoning (CP) cases linked to the consumption of deep-water fish occurred in 2003 in the Gambier Islands (French Polynesia). In 2004, on the request of two local fishermen, the presence of ciguatoxins (CTXs) was examined in part of their fish catches, i.e., 22 specimens representing five deep-water fish species. Using the radioactive receptor binding assay (rRBA) and mouse bioassay (MBA), significant CTX levels were detected in seven deep-water specimens in Lutjanidae, Serranidae, and Bramidae families. Following additional purification steps on the remaining liposoluble fractions for 13 of these samples (kept at −20 °C), these latter were reanalyzed in 2018 with improved protocols of the neuroblastoma cell-based assay (CBA-N2a) and liquid chromatography tandem mass spectrometry (LC–MS/MS). Using the CBA-N2a, the highest CTX-like content found in a specimen of Eumegistus illustris (Bramidae) was 2.94 ± 0.27 µg CTX1B eq. kg−1. Its toxin profile consisted of 52-epi-54-deoxyCTX1B, CTX1B, and 54-deoxyCTX1B, as assessed by LC–MS/MS. This is the first study demonstrating that deep-water fish are potential ciguatera vectors and highlighting the importance of a systematic monitoring of CTXs in all exploited fish species, especially in ciguatera hotspots, including deep-water fish, which constitute a significant portion of the commercial deep-sea fisheries in many Asian–Pacific countries. Full article
(This article belongs to the Special Issue Marine Biotoxins)
►▼ Show Figures

Graphical abstract

14 pages, 1149 KiB  
Article
Formulation, Optimization and In Vivo Evaluation of Fucoidan-Based Cream with Anti-Inflammatory Properties
by Ekaterina D. Obluchinskaya, Olga N. Pozharitskaya, Elena V. Flisyuk and Alexander N. Shikov
Mar. Drugs 2021, 19(11), 643; https://doi.org/10.3390/md19110643 - 17 Nov 2021
Cited by 25 | Viewed by 3253
Abstract
Fucoidan is a polysaccharide found in brown alga with glorious potential for pharmacological activities, among which its anti-inflammatory properties have gained meaningful attention. Due to several advantages of formulations for topical application, this study aimed to develop and optimize a fucoidan-based cream formulation [...] Read more.
Fucoidan is a polysaccharide found in brown alga with glorious potential for pharmacological activities, among which its anti-inflammatory properties have gained meaningful attention. Due to several advantages of formulations for topical application, this study aimed to develop and optimize a fucoidan-based cream formulation and to investigate its anti-inflammatory potential after topical application in vivo. Fucoidan from Fucus vesiculosus L. was used. The cream base consisting of olive oil and Kolliphor RH40 was optimized followed by in vitro agar diffusion and drug release studies. The fucoidan-based cream with 13% Kolliphor P 407, 1% Transcutol P, and 5% PEG400 showed good spreadability, washability, and colloidal stability, and it did not irritate the skin. The kinetics of fucoidan release from the optimized cream exhibited the best fit to the Korsmeyer–Peppas and Higuchi models with R2 > 0.99. Fucoidan release was controlled by drug diffusion and anomalous transport provided by the optimized cream base. The formulation was stable and provided high fucoidan release after storage for 1 year. Topical application of the fucoidan-based cream dose-dependently inhibited carrageenan-induced edema and ameliorated mechanical allodynia in rats. The efficacy of the fucoidan-based cream at a high dose was comparable with the efficacy of diclofenac gel. The fucoidan-based cream could be considered a promising anti-inflammatory formulation. Full article
(This article belongs to the Special Issue Pharmaceutical Formulation of Marine Drugs)
►▼ Show Figures

Figure 1

5 pages, 219 KiB  
Editorial
Bioactive Molecules from Extreme Environments II
by Daniela Giordano
Mar. Drugs 2021, 19(11), 642; https://doi.org/10.3390/md19110642 - 17 Nov 2021
Cited by 3 | Viewed by 1478
Abstract
Marine organisms are known to produce a wide variety of natural products that are unique in terms of diversity, structural, and functional properties [...] Full article
(This article belongs to the Special Issue Bioactive Molecules from Extreme Environments II)
14 pages, 1341 KiB  
Article
Marine Bromophenol Bis(2,3,6-Tribromo-4,5-Dihydroxybenzyl)ether Inhibits Angiogenesis in Human Umbilical Vein Endothelial Cells and Reduces Vasculogenic Mimicry in Human Lung Cancer A549 Cells
by Songtao Dong, Zhongyuan Chen, Li Wang, Yankai Liu, Dimitrios Stagos, Xiukun Lin and Ming Liu
Mar. Drugs 2021, 19(11), 641; https://doi.org/10.3390/md19110641 - 16 Nov 2021
Cited by 6 | Viewed by 2470
Abstract
Angiogenesis, including the growth of new capillary blood vessels from existing ones and the malignant tumors cells formed vasculogenic mimicry, is quite important for the tumor metastasis. Anti-angiogenesis is one of the significant therapies in tumor treatment, while the clinical angiogenesis inhibitors usually [...] Read more.
Angiogenesis, including the growth of new capillary blood vessels from existing ones and the malignant tumors cells formed vasculogenic mimicry, is quite important for the tumor metastasis. Anti-angiogenesis is one of the significant therapies in tumor treatment, while the clinical angiogenesis inhibitors usually exhibit endothelial cells dysfunction and drug resistance. Bis(2,3,6-tribromo-4,5-dihydroxybenzyl)ether (BTDE), a marine algae-derived bromophenol compound, has shown various biological activities, however, its anti-angiogenesis function remains unknown. The present study illustrated that BTDE had anti-angiogenesis effect in vitro through inhibiting human umbilical vein endothelial cells migration, invasion, tube formation, and the activity of matrix metalloproteinases 9 (MMP9), and in vivo BTDE also blocked intersegmental vessel formation in zebrafish embryos. Moreover, BTDE inhibited the migration, invasion, and vasculogenic mimicry formation of lung cancer cell A549. All these results indicated that BTDE could be used as a potential candidate in anti-angiogenesis for the treatment of cancer. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
►▼ Show Figures

Figure 1

16 pages, 3022 KiB  
Article
Probing the Therapeutic Potential of Marine Phyla by SPE Extraction
by Alejandro Moreiras-Figueruelo, Genoveffa Nuzzo, Christian Galasso, Clementina Sansone, Fabio Crocetta, Valerio Mazzella, Carmela Gallo, Giusi Barra, Angela Sardo, Antonella Iuliano, Emiliano Manzo, Giuliana d’Ippolito, Marte Albrigtsen, Jeanette H. Andersen, Adrianna Ianora and Angelo Fontana
Mar. Drugs 2021, 19(11), 640; https://doi.org/10.3390/md19110640 - 16 Nov 2021
Cited by 3 | Viewed by 2167
Abstract
The marine environment is potentially a prolific source of small molecules with significant biological activities. In recent years, the development of new chromatographic phases and the progress in cell and molecular techniques have facilitated the search for marine natural products (MNPs) as novel [...] Read more.
The marine environment is potentially a prolific source of small molecules with significant biological activities. In recent years, the development of new chromatographic phases and the progress in cell and molecular techniques have facilitated the search for marine natural products (MNPs) as novel pharmacophores and enhanced the success rate in the selection of new potential drug candidates. However, most of this exploration has so far been driven by anticancer research and has been limited to a reduced number of taxonomic groups. In this article, we report a test study on the screening potential of an in-house library of natural small molecules composed of 285 samples derived from 57 marine organisms that were chosen from among the major eukaryotic phyla so far represented in studies on bioactive MNPs. Both the extracts and SPE fractions of these organisms were simultaneously submitted to three different bioassays—two phenotypic and one enzymatic—for cytotoxic, antidiabetic, and antibacterial activity. On the whole, the screening of the MNP library selected 11 potential hits, but the distribution of the biological results showed that SPE fractionation increased the positive score regardless of the taxonomic group. In many cases, activity could be detected only in the enriched fractions after the elimination of the bulky effect due to salts. On a statistical basis, sponges and molluscs were confirmed to be the most significant source of cytotoxic and antimicrobial products, but other phyla were found to be effective with the other therapeutic targets. Full article
(This article belongs to the Special Issue Bioassay Platforms for the Disclosure of the Pharmaceutical Potential of Marine Natural Products)
►▼ Show Figures

Figure 1

19 pages, 19548 KiB  
Article
Multi-Omics Analysis of Gene and Protein Candidates Possibly Related to Tetrodotoxin Accumulation in the Skin of Takifugu flavidus
by Huimin Feng, Kun Qiao, Chunchun Wang, Bei Chen, Min Xu, Hua Hao, Zhen Huang, Zhiyu Liu and Qin Wang
Mar. Drugs 2021, 19(11), 639; https://doi.org/10.3390/md19110639 - 15 Nov 2021
Viewed by 2251
Abstract
Pufferfish is increasingly regarded by many as a delicacy. However, the tetrodotoxin (TTX) that accumulates in its body can be lethal upon consumption by humans. TTX is known to mainly accumulate in pufferfish skin, but the accumulation mechanisms are poorly understood. In this [...] Read more.
Pufferfish is increasingly regarded by many as a delicacy. However, the tetrodotoxin (TTX) that accumulates in its body can be lethal upon consumption by humans. TTX is known to mainly accumulate in pufferfish skin, but the accumulation mechanisms are poorly understood. In this study, we aimed to explore the possible mechanism of TTX accumulation in the skin of the pufferfish Takifugu flavidus following treatment with TTX. Through liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis, we detected 37.3% of toxin accumulated in the skin at the end of the rearing period (168 h). Transcriptome and proteome analyses revealed the mechanism and pathways of TTX accumulation in the skin of T. flavidus in detail. Gene ontology and the Kyoto Encyclopedia of Genes and Genomes analyses strongly suggest that cardiac muscle contraction and adrenergic signaling in cardiomyocyte pathways play an important role in TTX accumulation. Moreover, some upregulated and downregulated genes, which were determined via RNA-Seq, were verified with qPCR analysis. This study is the first to use multi-omics profiling data to identify novel regulatory network mechanisms of TTX accumulation in the skin of pufferfish. Full article
►▼ Show Figures

Figure 1

16 pages, 2316 KiB  
Article
From Natural Xanthones to Synthetic C-1 Aminated 3,4-Dioxygenated Xanthones as Optimized Antifouling Agents
by Diana I. S. P. Resende, Joana R. Almeida, Sandra Pereira, Alexandre Campos, Agostinho Lemos, Jeffrey E. Plowman, Ancy Thomas, Stefan Clerens, Vitor Vasconcelos, Madalena Pinto, Marta Correia-da-Silva and Emília Sousa
Mar. Drugs 2021, 19(11), 638; https://doi.org/10.3390/md19110638 - 13 Nov 2021
Cited by 6 | Viewed by 2256
Abstract
Biofouling, which occurs when certain marine species attach and accumulate in artificial submerged structures, represents a serious economic and environmental issue worldwide. The discovery of new non-toxic and eco-friendly antifouling systems to control or prevent biofouling is, therefore, a practical and urgent need. [...] Read more.
Biofouling, which occurs when certain marine species attach and accumulate in artificial submerged structures, represents a serious economic and environmental issue worldwide. The discovery of new non-toxic and eco-friendly antifouling systems to control or prevent biofouling is, therefore, a practical and urgent need. In this work, the antifouling activity of a series of 24 xanthones, with chemical similarities to natural products, was exploited. Nine (1, 2, 4, 6, 8, 16, 19, 21, and 23) of the tested xanthones presented highly significant anti-settlement responses at 50 μM against the settlement of mussel Mytilus galloprovincialis larvae and low toxicity to this macrofouling species. Xanthones 21 and 23 emerged as the most effective larval settlement inhibitors (EC50 = 7.28 and 3.57 µM, respectively). Additionally, xanthone 23 exhibited a therapeutic ratio (LC50/EC50) > 15, as required by the US Navy program attesting its suitability as natural antifouling agents. From the nine tested xanthones, none of the compounds were found to significantly inhibit the growth of the marine biofilm-forming bacterial strains tested. Xanthones 4, 6, 8, 16, 19, 21, and 23 were found to be non-toxic to the marine non-target species Artemia salina (<10% mortality at 50 μM). Insights on the antifouling mode of action of the hit xanthones 21 and 23 suggest that these two compounds affected similar molecular targets and cellular processes in mussel larvae, including that related to mussel adhesion capacity. This work exposes for the first time the relevance of C-1 aminated xanthones with a 3,4-dioxygenated pattern of substitution as new non-toxic products to prevent marine biofouling. Full article
(This article belongs to the Special Issue Marine Benzophenones and Xanthones: Isolation and Synthesis)
►▼ Show Figures

Graphical abstract

25 pages, 2361 KiB  
Review
Antiparasitic Effects of Sulfated Polysaccharides from Marine Hydrobionts
by Natalya N. Besednova, Tatyana S. Zaporozhets, Boris G. Andryukov, Sergey P. Kryzhanovsky, Svetlana P. Ermakova, Tatyana A. Kuznetsova, Anastasia N. Voronova and Mikhail Y. Shchelkanov
Mar. Drugs 2021, 19(11), 637; https://doi.org/10.3390/md19110637 - 12 Nov 2021
Cited by 8 | Viewed by 3135
Abstract
This review presents materials characterizing sulfated polysaccharides (SPS) of marine hydrobionts (algae and invertebrates) as potential means for the prevention and treatment of protozoa and helminthiasis. The authors have summarized the literature on the pathogenetic targets of protozoa on the host cells and [...] Read more.
This review presents materials characterizing sulfated polysaccharides (SPS) of marine hydrobionts (algae and invertebrates) as potential means for the prevention and treatment of protozoa and helminthiasis. The authors have summarized the literature on the pathogenetic targets of protozoa on the host cells and on the antiparasitic potential of polysaccharides from red, brown and green algae as well as certain marine invertebrates. Information about the mechanisms of action of these unique compounds in diseases caused by protozoa has also been summarized. SPS is distinguished by high antiparasitic activity, good solubility and an almost complete absence of toxicity. In the long term, this allows for the consideration of these compounds as effective and attractive candidates on which to base drugs, biologically active food additives and functional food products with antiparasitic activity. Full article
(This article belongs to the Special Issue Marine Glycomics)
►▼ Show Figures

Graphical abstract

9 pages, 1702 KiB  
Article
An Alternative Approach towards C-12 Functionalized Scalaranic Sesterterpenoids Synthesis of 17-Oxo-20-norscalaran-12α,19-O-lactone
by Olga Morarescu, Marina Grinco, Veaceslav Kulciţki, Sergiu Shova and Nicon Ungur
Mar. Drugs 2021, 19(11), 636; https://doi.org/10.3390/md19110636 - 12 Nov 2021
Cited by 3 | Viewed by 1558
Abstract
Scalarane sesterterpenoids emerged as interesting bioactive natural products which were isolated extensively from marine sponges and shell-less mollusks. Some representatives were also reported recently from superior plants. Many scalarane sesterterpenoids displayed a wide spectrum of valuable properties, such as antifeedant, antimicrobial, antifungal, antitubercular, [...] Read more.
Scalarane sesterterpenoids emerged as interesting bioactive natural products which were isolated extensively from marine sponges and shell-less mollusks. Some representatives were also reported recently from superior plants. Many scalarane sesterterpenoids displayed a wide spectrum of valuable properties, such as antifeedant, antimicrobial, antifungal, antitubercular, antitumor, anti-HIV properties, cytotoxicity and stimulation of nerve growth factor synthesis, as well as anti-inflammatory activity. Due to their important biological properties, many efforts have been undertaken towards the chemical synthesis of natural scalaranes. The main synthetic challenges are connected to their complex polycyclic framework, chiral centers and different functional groups, in particular the oxygenated functional groups at the C-12 position, which are prerequisites of the biological activity of many investigated scalaranes. The current work addresses this problem and the synthesis of 17-oxo-20-norscalaran-12α,19-O-lactone is described. It was performed via the 12α-hydroxy-ent-isocopal-13(14)-en-15-al obtained from (-)-sclareol as an accessible starting material. The tetracyclic lactone framework was built following an addition strategy, which includes the intramolecular Michael addition of a diterpenic acetoacetic ester and an intramolecular aldol condensation reaction as key synthetic steps. The structure and stereochemistry of the target compound have been proven by X-Ray diffraction method. Full article
(This article belongs to the Special Issue Tribute to Dr. Guido Cimino’s 80th Birthday and His Outstanding Achievements on Marine Natural Products)
►▼ Show Figures

Figure 1

9 pages, 901 KiB  
Article
Oceanalin B, a Hybrid α,ω-Bifunctionalized Sphingoid Tetrahydroisoquinoline β-Glycoside from the Marine Sponge Oceanapia sp.
by Tatyana N. Makarieva, Natalia V. Ivanchina, Pavel S. Dmitrenok, Alla G. Guzii, Valentin A. Stonik, Doralyn S. Dalisay and Tadeusz F. Molinski
Mar. Drugs 2021, 19(11), 635; https://doi.org/10.3390/md19110635 - 12 Nov 2021
Cited by 7 | Viewed by 2268
Abstract
Oceanalin B (1), an α,ω-bipolar natural product belonging to a rare family of sphingoid tetrahydoisoquinoline β-glycosides, was isolated from the EtOH extract of the lyophilized marine sponge Oceanapia sp. as the second member of the series after oceanalin A (2 [...] Read more.
Oceanalin B (1), an α,ω-bipolar natural product belonging to a rare family of sphingoid tetrahydoisoquinoline β-glycosides, was isolated from the EtOH extract of the lyophilized marine sponge Oceanapia sp. as the second member of the series after oceanalin A (2) from the same animal. The compounds are of particular interest due to their biogenetically unexpected structures as well as their biological activities. The structure and absolute stereochemistry of 1 as a α,ω-bifunctionalized sphingoid tetrahydroisoquinoline β-glycoside was elucidated using NMR, CD and MS spectral analysis and chemical degradation. Oceanalin B exhibited in vitro antifungal activity against Candidaglabrata with a MIC of 25 μg/mL. Full article
(This article belongs to the Special Issue Carbohydrate-Containing Marine Compounds of Mixed Biogenesis)
►▼ Show Figures

Figure 1

13 pages, 1715 KiB  
Article
Anti-Allergic Effect of Low Molecular Weight Digest from Abalone Viscera on Atopic Dermatitis-Induced NC/Nga
by Tae-Hee Kim, Seong-Yeong Heo, Gun-Woo Oh, Won Sun Park, Il-Whan Choi, Zhong-Ji Qian and Won-Kyo Jung
Mar. Drugs 2021, 19(11), 634; https://doi.org/10.3390/md19110634 - 12 Nov 2021
Cited by 4 | Viewed by 2279
Abstract
Abalone viscera (AV) is one of the byproducts of the seafood processing industry. The low molecular weight (<5 kDa) peptides (LMW-AV) obtained from gastrointestinal digestion of AV could suppress allergenic responses on activated HMC-1 human mast cells in our previous study. Regarding the [...] Read more.
Abalone viscera (AV) is one of the byproducts of the seafood processing industry. The low molecular weight (<5 kDa) peptides (LMW-AV) obtained from gastrointestinal digestion of AV could suppress allergenic responses on activated HMC-1 human mast cells in our previous study. Regarding the allergenic response of LMW-AV, in the present study, we further investigated the potential of oral administration of LMW-AV against atopic dermatitis (AD) in a dermatitis-induced model stimulated with Dermatophagoides farinae. The results demonstrated that the LMW-AV reduced a number of clinical symptoms, such as the severity of the dermatitis and serum immunoglobulin E levels. Moreover, LMW-AV could inhibit the expression of chemokines and cytokines. The histological analysis indicated that the LMW-AV has suppressed the eosinophil count and the mast cell infiltration into the upper dermis. The results suggest that LMW-AV can be considered as a promising candidate for AD treatment. Full article
(This article belongs to the Special Issue Marine Products with Anti-allergic and Anti-inflammatory Activities)
►▼ Show Figures

Figure 1

18 pages, 2806 KiB  
Article
Uncovering the Bioactive Potential of a Cyanobacterial Natural Products Library Aided by Untargeted Metabolomics
by Leonor Ferreira, João Morais, Marco Preto, Raquel Silva, Ralph Urbatzka, Vitor Vasconcelos and Mariana Reis
Mar. Drugs 2021, 19(11), 633; https://doi.org/10.3390/md19110633 - 12 Nov 2021
Cited by 12 | Viewed by 4136
Abstract
The Blue Biotechnology and Ecotoxicology Culture Collection (LEGE-CC) holds a vast number of cyanobacteria whose chemical richness is still largely unknown. To expedite its bioactivity screening we developed a natural products library. Sixty strains and four environmental samples were chromatographed, using a semiautomatic [...] Read more.
The Blue Biotechnology and Ecotoxicology Culture Collection (LEGE-CC) holds a vast number of cyanobacteria whose chemical richness is still largely unknown. To expedite its bioactivity screening we developed a natural products library. Sixty strains and four environmental samples were chromatographed, using a semiautomatic HPLC system, yielding 512 fractions that were tested for their cytotoxic activity against 2D and 3D models of human colon carcinoma (HCT 116), and non-cancerous cell line hCMEC/D3. Six fractions showed high cytotoxicity against 2D and 3D cell models (group A), and six other fractions were selected by their effects on 3D cells (group B). The metabolome of each group was organized and characterized using the MolNetEnhancer workflow, and its processing with MetaboAnalyst allowed discrimination of the mass features with the highest fold change, and thus the ones that might be bioactive. Of those, mass features without precedented identification were mostly found in group A, indicating seven possible novel bioactive molecules, alongside in silico putative annotation of five cytotoxic compounds. Manual dereplication of group B tentatively identified nine pheophytin and pheophorbide derivatives. Our approach enabled the selection of 7 out of 60 cyanobacterial strains for anticancer drug discovery, providing new data concerning the chemical composition of these cyanobacteria. Full article
(This article belongs to the Special Issue Marine Drug Discovery through Computer-Aided Approaches)
►▼ Show Figures

Figure 1

17 pages, 1914 KiB  
Article
Unravelling the Anti-Inflammatory and Antioxidant Potential of the Marine Sponge Cliona celata from the Portuguese Coastline
by Joana Alves, Helena Gaspar, Joana Silva, Celso Alves, Alice Martins, Fernando Teodoro, Patrícia Susano, Susete Pinteus and Rui Pedrosa
Mar. Drugs 2021, 19(11), 632; https://doi.org/10.3390/md19110632 - 12 Nov 2021
Cited by 5 | Viewed by 2684
Abstract
Inflammation is a double-edged sword, as it can have both protective effects and harmful consequences, which, combined with oxidative stress (OS), can lead to the development of deathly chronic inflammatory conditions. Over the years, research has evidenced the potential of marine sponges as [...] Read more.
Inflammation is a double-edged sword, as it can have both protective effects and harmful consequences, which, combined with oxidative stress (OS), can lead to the development of deathly chronic inflammatory conditions. Over the years, research has evidenced the potential of marine sponges as a source of effective anti-inflammatory therapeutic agents. Within this framework, the purpose of this study was to evaluate the antioxidant and the anti-inflammatory potential of the marine sponge Cliona celata. For this purpose, their organic extracts (C1–C5) and fractions were evaluated concerning their radical scavenging activity through 2,2-diphenyl-1-picrylhydrazyl radical (DPPH), ferric reducing antioxidant power (FRAP), oxygen radical absorbance capacity (ORAC), and anti-inflammatory activity through a (lipopolysaccharides (LPS)-induced inflammation on RAW 264.7 cells) model. Compounds present in the two most active fractions (F5 and F13) of C4 were tentatively identified by gas chromatography coupled to mass spectrometry (GC-MS). Even though samples displayed low antioxidant activity, they presented a high anti-inflammatory capacity in the studied cellular inflammatory model when compared to the anti-inflammatory standard, dexamethasone. GC-MS analysis led to the identification of n-hexadecanoic acid, cis-9-hexadecenal, and 13-octadecenal in fraction F5, while two major compounds, octadecanoic acid and cholesterol, were identified in fraction F13. The developed studies demonstrated the high anti-inflammatory activity of the marine sponge C. celata extracts and fractions, highlighting its potential for further therapeutic applications. Full article
(This article belongs to the Special Issue Tribute to Dr. Guido Cimino’s 80th Birthday and His Outstanding Achievements on Marine Natural Products)
►▼ Show Figures

Figure 1

10 pages, 1140 KiB  
Communication
Apoptotic Activity of New Oxisterigmatocystin Derivatives from the Marine-Derived Fungus Aspergillus nomius NC06
by Muh. Ade Artasasta, Yanwirasti Yanwirasti, Muhammad Taher, Akmal Djamaan, Ni Putu Ariantari, Ru Angelie Edrada-Ebel and Dian Handayani
Mar. Drugs 2021, 19(11), 631; https://doi.org/10.3390/md19110631 - 11 Nov 2021
Cited by 7 | Viewed by 2599
Abstract
Sponge-derived fungi have recently attracted attention as an important source of interesting bioactive compounds. Aspergillus nomius NC06 was isolated from the marine sponge Neopetrosia chaliniformis. This fungus was cultured on rice medium and yielded four compounds including three new oxisterigmatocystins, namely, J, [...] Read more.
Sponge-derived fungi have recently attracted attention as an important source of interesting bioactive compounds. Aspergillus nomius NC06 was isolated from the marine sponge Neopetrosia chaliniformis. This fungus was cultured on rice medium and yielded four compounds including three new oxisterigmatocystins, namely, J, K, and L (1, 2, and 3), and one known compound, aspergillicin A (4). Structures of the compounds were elucidated by 1D and 2D NMR spectroscopy and by high-resolution mass spectrometry. The isolated compounds were tested for cytotoxic activity against HT 29 colon cancer cells, where compounds 1, 2, and 4 exhibited IC50 values of 6.28, 15.14, and 1.63 µM, respectively. Under the fluorescence microscope by using a double staining method, HT 29 cells were observed to be viable, apoptotic, and necrotic after treatment with the cytotoxic compounds 1, 2, and 4. The result shows that compounds 1 and 2 were able to induce apoptosis and cell death in HT 29 cells. Full article
(This article belongs to the Special Issue Marine Natural Product Chemistry: A Themed Issue Dedicated to Prof. Dr. Peter Proksch on His Research Career)
►▼ Show Figures

Graphical abstract

13 pages, 2281 KiB  
Article
Absolute Structure Determination and Kv1.5 Ion Channel Inhibition Activities of New Debromoaplysiatoxin Analogues
by Sicheng Shen, Weiping Wang, Zijun Chen, Huihui Zhang, Yuchun Yang, Xiaoliang Wang, Peng Fu and Bingnan Han
Mar. Drugs 2021, 19(11), 630; https://doi.org/10.3390/md19110630 - 11 Nov 2021
Cited by 3 | Viewed by 2288
Abstract
Potassium channel Kv1.5 has been considered a key target for new treatments of atrial tachyarrhythmias, with few side effects. Four new debromoaplysiatoxin analogues with a 6/6/12 fused ring system were isolated from marine cyanobacterium Lyngbya sp. Their planar structures were elucidated by HRESIMS, [...] Read more.
Potassium channel Kv1.5 has been considered a key target for new treatments of atrial tachyarrhythmias, with few side effects. Four new debromoaplysiatoxin analogues with a 6/6/12 fused ring system were isolated from marine cyanobacterium Lyngbya sp. Their planar structures were elucidated by HRESIMS, 1D and 2D NMR. The absolute configuration of oscillatoxin J (1) was determined by single-crystal X-ray diffraction, and the absolute configurations of oscillatoxin K (2), oscillatoxin L (3) and oscillatoxin M (4) were confirmed on the basis of GIAO NMR shift calculation followed by DP4 analysis. The current study confirmed the absolute configuration of the pivotal chiral positions (7S, 9S, 10S, 11R, 12S, 15S, 29R and 30R) at traditional ATXs with 6/12/6 tricyclic ring system. Compound 1, 2 and 4 exhibited blocking activities against Kv1.5 with IC50 values of 2.61 ± 0.91 µM, 3.86 ± 1.03 µM and 3.79 ± 1.01 µM, respectively. However, compound 3 exhibited a minimum effect on Kv1.5 at 10 µM. Furthermore, all of these new debromoaplysiatoxin analogs displayed no apparent activity in a brine shrimp toxicity assay. Full article
►▼ Show Figures

Graphical abstract

57 pages, 8482 KiB  
Review
Natural Products from Actinomycetes Associated with Marine Organisms
by Jianing Chen, Lin Xu, Yanrong Zhou and Bingnan Han
Mar. Drugs 2021, 19(11), 629; https://doi.org/10.3390/md19110629 - 10 Nov 2021
Cited by 28 | Viewed by 4971
Abstract
The actinomycetes have proven to be a rich source of bioactive secondary metabolites and play a critical role in the development of pharmaceutical researches. With interactions of host organisms and having special ecological status, the actinomycetes associated with marine animals, marine plants, macroalgae, [...] Read more.
The actinomycetes have proven to be a rich source of bioactive secondary metabolites and play a critical role in the development of pharmaceutical researches. With interactions of host organisms and having special ecological status, the actinomycetes associated with marine animals, marine plants, macroalgae, cyanobacteria, and lichens have more potential to produce active metabolites acting as chemical defenses to protect the host from predators as well as microbial infection. This review focuses on 536 secondary metabolites (SMs) from actinomycetes associated with these marine organisms covering the literature to mid-2021, which will highlight the taxonomic diversity of actinomycetes and the structural classes, biological activities of SMs. Among all the actinomycetes listed, members of Streptomyces (68%), Micromonospora (6%), and Nocardiopsis (3%) are dominant producers of secondary metabolites. Additionally, alkaloids (37%), polyketides (33%), and peptides (15%) comprise the largest proportion of natural products with mostly antimicrobial activity and cytotoxicity. Furthermore, the data analysis and clinical information of SMs have been summarized in this article, suggesting that some of these actinomycetes with multiple host organisms deserve more attention to their special ecological status and genetic factors. Full article
(This article belongs to the Special Issue Bioactive Compounds from Marine Streptomyces)
►▼ Show Figures

Figure 1

24 pages, 3092 KiB  
Review
Structure Characteristics, Biochemical Properties, and Pharmaceutical Applications of Alginate Lyases
by Shu-Kun Gao, Rui Yin, Xiao-Chen Wang, Hui-Ning Jiang, Xiao-Xiao Liu, Wei Lv, Yu Ma and Yan-Xia Zhou
Mar. Drugs 2021, 19(11), 628; https://doi.org/10.3390/md19110628 - 10 Nov 2021
Cited by 21 | Viewed by 3130
Abstract
Alginate, the most abundant polysaccharides of brown algae, consists of various proportions of uronic acid epimers α-L-guluronic acid (G) and β-D-mannuronic acid (M). Alginate oligosaccharides (AOs), the degradation products of alginates, exhibit excellent bioactivities and a great potential for broad applications [...] Read more.
Alginate, the most abundant polysaccharides of brown algae, consists of various proportions of uronic acid epimers α-L-guluronic acid (G) and β-D-mannuronic acid (M). Alginate oligosaccharides (AOs), the degradation products of alginates, exhibit excellent bioactivities and a great potential for broad applications in pharmaceutical fields. Alginate lyases can degrade alginate to functional AOs with unsaturated bonds or monosaccharides, which can facilitate the biorefinery of brown algae. On account of the increasing applications of AOs and biorefinery of brown algae, there is a scientific need to explore the important aspects of alginate lyase, such as catalytic mechanism, structure, and property. This review covers fundamental aspects and recent developments in basic information, structural characteristics, the structure–substrate specificity or catalytic efficiency relationship, property, molecular modification, and applications. To meet the needs of biorefinery systems of a broad array of biochemical products, alginate lyases with special properties, such as salt-activated, wide pH adaptation range, and cold adaptation are outlined. Withal, various challenges in alginate lyase research are traced out, and future directions, specifically on the molecular biology part of alginate lyases, are delineated to further widen the horizon of these exceptional alginate lyases. Full article
(This article belongs to the Special Issue Seaweed-Degrading Enzymes, Functions and Applications of Their Products)
►▼ Show Figures

Figure 1

15 pages, 3074 KiB  
Article
Isolation of Scalarane-Type Sesterterpenoids from the Marine Sponge Dysidea sp. and Stereochemical Reassignment of 12-epi-Phyllactone D/E
by A-Young Shin, Arang Son, Changhoon Choi and Jihoon Lee
Mar. Drugs 2021, 19(11), 627; https://doi.org/10.3390/md19110627 - 09 Nov 2021
Cited by 6 | Viewed by 2264
Abstract
The chemical investigation of the marine sponge Dysidea sp., which was collected from Bohol province in the Philippines, resulted in the identification of 15 new scalarane-type sesterterpenoids (1–14, 16), together with 15 known compounds. The [...] Read more.
The chemical investigation of the marine sponge Dysidea sp., which was collected from Bohol province in the Philippines, resulted in the identification of 15 new scalarane-type sesterterpenoids (1–14, 16), together with 15 known compounds. The chemical structures of the new compounds were elucidated based on NMR spectroscopy and HRMS. The structure of 12-epi-phyllactone D/E (15) isolated during this study was originally identified in 2007. However, careful inspection of our experimental 13C NMR spectrum revealed considerable discrepancies with the reported data at C-9, C-12, C-14, and C-23, leading to the correction of the reported compound to the C-12 epimer of 15, phyllactone D/E. The biological properties of compounds 1–16 were evaluated using the MDA-MB-231 cancer cell line. Compound 7, which bears a pentenone E-ring, exhibits significant cytotoxicity with a GI50 value of 4.21 μM. Full article
►▼ Show Figures

Graphical abstract

16 pages, 4493 KiB  
Article
Heptapeptide Isolated from Isochrysis zhanjiangensis Exhibited Anti-Photoaging Potential via MAPK/AP-1/MMP Pathway and Anti-Apoptosis in UVB-Irradiated HaCaT Cells
by Zhaowan Zheng, Zhenbang Xiao, Yuan-Lin He, Yanfei Tang, Lefan Li, Chunxia Zhou, Pengzhi Hong, Hui Luo and Zhong-Ji Qian
Mar. Drugs 2021, 19(11), 626; https://doi.org/10.3390/md19110626 - 09 Nov 2021
Cited by 18 | Viewed by 2646
Abstract
Marine microalgae can be used as sustainable protein sources in many fields with positive effects on human and animal health. DAPTMGY is a heptapeptide isolated from Isochrysis zhanjiangensis which is a microalga. In this study, we evaluated its anti-photoaging properties and mechanism of [...] Read more.
Marine microalgae can be used as sustainable protein sources in many fields with positive effects on human and animal health. DAPTMGY is a heptapeptide isolated from Isochrysis zhanjiangensis which is a microalga. In this study, we evaluated its anti-photoaging properties and mechanism of action in human immortalized keratinocytes cells (HaCaT). The results showed that DAPTMGY scavenged reactive oxygen species (ROS) and increase the level of endogenous antioxidants. In addition, through the exploration of its mechanism, it was determined that DAPIMGY exerted anti-photoaging effects. Specifically, the heptapeptide inhibits UVB-induced apoptosis through down-regulation of p53, caspase-8, caspase-3 and Bax and up-regulation of Bcl-2. Thus, DAPTMGY, isolated from I. zhanjiangensis, exhibits protective effects against UVB-induced damage. Full article
(This article belongs to the Special Issue Antiphotoaging and Photoprotective Compounds from Marine Organisms)
►▼ Show Figures

Figure 1

19 pages, 15196 KiB  
Review
Extraction and Nano-Sized Delivery Systems for Phlorotannins to Improve Its Bioavailability and Bioactivity
by Tianjian Tong, Xiaoyang Liu and Chenxu Yu
Mar. Drugs 2021, 19(11), 625; https://doi.org/10.3390/md19110625 - 05 Nov 2021
Cited by 7 | Viewed by 2531
Abstract
This review aims to provide an informative summary of studies on extraction and nanoencapsulation of phlorotannins to improve their bioavailability and bioactivity. The origin, structure, and different types of phlorotannins were briefly discussed, and the extraction/purification/characterization methods for phlorotannins were reviewed, with a [...] Read more.
This review aims to provide an informative summary of studies on extraction and nanoencapsulation of phlorotannins to improve their bioavailability and bioactivity. The origin, structure, and different types of phlorotannins were briefly discussed, and the extraction/purification/characterization methods for phlorotannins were reviewed, with a focus on techniques to improve the bioactivities and bioavailability of phlorotannins via nano-sized delivery systems. Phlorotannins are promising natural polyphenol compounds that have displayed high bioactivities in several areas: anticancer, anti-inflammation, anti-HIV, antidiabetic, and antioxidant. This review aims to provide a useful reference for researchers working on developing better utilization strategies for phlorotannins as pharmaceuticals, therapeuticals, and functional food supplements. Full article
(This article belongs to the Special Issue Nanoparticles from Marine Organisms and Their Biological Activity)
►▼ Show Figures

Figure 1

9 pages, 542 KiB  
Article
Zhaoshumycins A and B, Two Unprecedented Antimycin-Type Depsipeptides Produced by the Marine-Derived Streptomyces sp. ITBB-ZKa6
by Zhikai Guo, Shiying Ma, Salman Khan, Hongjie Zhu, Bo Zhang, Shiqing Zhang and Ruihua Jiao
Mar. Drugs 2021, 19(11), 624; https://doi.org/10.3390/md19110624 - 05 Nov 2021
Cited by 7 | Viewed by 2155
Abstract
Marine actinomycetes are prolific chemical sources of complex and novel natural products, providing an excellent chance for new drug discovery. The chemical investigation of the marine-derived Streptomyces sp. ITBB-ZKa6, from Zhaoshu island, Hainan, led to the discovery of two unique antimycin-type depsipeptides, zhaoshumycins [...] Read more.
Marine actinomycetes are prolific chemical sources of complex and novel natural products, providing an excellent chance for new drug discovery. The chemical investigation of the marine-derived Streptomyces sp. ITBB-ZKa6, from Zhaoshu island, Hainan, led to the discovery of two unique antimycin-type depsipeptides, zhaoshumycins A (1) and B (2), along with the isolation of the four known neoantimycins A (3), F (4), D (5), and E (6). The structures of the new compounds 1 and 2 were elucidated on the basis of the analysis of diverse spectroscopic data and biogenetic consideration. Zhaoshumycins A (1) and B (2) represent a new class of depsipeptides, featuring two neoantimycin monomers (only neoantimycin D or neoantimycins D and E) linked to a 1,4-disubstituted benzene ring via an imino group. Initial toxicity tests of 1–6 in MCF7 human breast cancer cells revealed that compounds 5 and 6 possess weak cytotoxic activity. Further structure–activity relationship analysis suggested the importance of the NH2 group at C-34 in 5 and 6 for cytotoxicity in MCF7 cells. Full article
(This article belongs to the Special Issue Bioactive Compounds from Marine Streptomyces)
►▼ Show Figures

Figure 1

18 pages, 4522 KiB  
Article
Gloeothece sp.—Exploiting a New Source of Antioxidant, Anti-Inflammatory, and Antitumor Agents
by Helena M. Amaro, Rita Barros, Tânia Tavares, Raquel Almeida, Isabel Sousa Pinto, Francisco Xavier Malcata and Ana Catarina Guedes
Mar. Drugs 2021, 19(11), 623; https://doi.org/10.3390/md19110623 - 04 Nov 2021
Cited by 1 | Viewed by 1982
Abstract
Bioactive lipidic compounds of microalgae, such as polyunsaturated fatty acids (PUFA) and carotenoids, can avoid or treat oxidation-associated conditions and diseases like inflammation or cancer. This study aimed to assess the bioactive potential of lipidic extracts obtained from Gloeothece sp.–using Generally Recognized as [...] Read more.
Bioactive lipidic compounds of microalgae, such as polyunsaturated fatty acids (PUFA) and carotenoids, can avoid or treat oxidation-associated conditions and diseases like inflammation or cancer. This study aimed to assess the bioactive potential of lipidic extracts obtained from Gloeothece sp.–using Generally Recognized as Safe (GRAS) solvents like ethanol, acetone, hexane:isopropanol (3:2) (HI) and ethyl lactate. The bioactive potential of extracts was assessed in terms of antioxidant (ABTS•+, DPPH•, •NO and O2•assays), anti-inflammatory (HRBC membrane stabilization and Cox-2 screening assay), and antitumor capacity (death by TUNEL, and anti-proliferative by BrdU incorporation assay in AGS cancer cells); while its composition was characterized in terms of carotenoids and fatty acids, by HPLC-DAD and GC-FID methods, respectively. Results revealed a chemopreventive potential of the HI extract owing to its ability to: (I) scavenge -NO• radical (IC50, 1258 ± 0.353 µg·mL−1); (II) inhibit 50% of COX-2 expression at 130.2 ± 7.4 µg·mL−1; (III) protect 61.6 ± 9.2% of lysosomes from heat damage, and (IV) induce AGS cell death by 4.2-fold and avoid its proliferation up to 40% in a concentration of 23.2 ± 1.9 µg·mL−1. Hence, Gloeothece sp. extracts, namely HI, were revealed to have the potential to be used for nutraceutical purposes. Full article
(This article belongs to the Special Issue Marine Carotenoids in Inflammation and Cancer)
►▼ Show Figures

Graphical abstract

11 pages, 2870 KiB  
Article
Echinochrome A Treatment Alleviates Atopic Dermatitis-like Skin Lesions in NC/Nga Mice via IL-4 and IL-13 Suppression
by Hyeong Rok Yun, Sang Woo Ahn, Bomin Seol, Elena A. Vasileva, Natalia P. Mishchenko, Sergey A. Fedoreyev, Valentin A. Stonik, Jin Han, Kyung Soo Ko, Byoung Doo Rhee, Jung Eun Seol and Hyoung Kyu Kim
Mar. Drugs 2021, 19(11), 622; https://doi.org/10.3390/md19110622 - 01 Nov 2021
Cited by 16 | Viewed by 3146
Abstract
Atopic dermatitis (AD) is a chronic inflammatory skin disease in which skin barrier dysfunction leads to dryness, pruritus, and erythematous lesions. AD is triggered by immune imbalance and oxidative stress. Echinochrome A (Ech A), a natural pigment isolated from sea urchins, exerts antioxidant [...] Read more.
Atopic dermatitis (AD) is a chronic inflammatory skin disease in which skin barrier dysfunction leads to dryness, pruritus, and erythematous lesions. AD is triggered by immune imbalance and oxidative stress. Echinochrome A (Ech A), a natural pigment isolated from sea urchins, exerts antioxidant and beneficial effects in various inflammatory disease models. In the present study, we tested whether Ech A treatment alleviated AD-like skin lesions. We examined the anti-inflammatory effect of Ech A on 2,4-dinitrochlorobenzene (DNCB)-induced AD-like lesions in an NC/Nga mouse model. AD-like skin symptoms were induced by treatment with 1% DNCB for 1 week and 0.4% DNCB for 5 weeks in NC/Nga mice. The results showed that Ech A alleviated AD clinical symptoms, such as edema, erythema, and dryness. Treatment with Ech A induced the recovery of epidermis skin lesions as observed histologically. Tewameter® and Corneometer® measurements indicated that Ech A treatment reduced transepidermal water loss and improved stratum corneum hydration, respectively. Ech A treatment also inhibited inflammatory-response-induced mast cell infiltration in AD-like skin lesions and suppressed the expression of proinflammatory cytokines, such as interferon-γ, interleukin-4, and interleukin-13. Collectively, these results suggest that Ech A may be beneficial for treating AD owing to its anti-inflammatory effects. Full article
(This article belongs to the Special Issue Quinonoid Pigments of Echinoderms)
►▼ Show Figures

Figure 1

15 pages, 1942 KiB  
Article
Complete Genome Sequence of Two Deep-Sea Streptomyces Isolates from Madeira Archipelago and Evaluation of Their Biosynthetic Potential
by Pedro Albuquerque, Inês Ribeiro, Sofia Correia, Ana Paula Mucha, Paula Tamagnini, Andreia Braga-Henriques, Maria de Fátima Carvalho and Marta V. Mendes
Mar. Drugs 2021, 19(11), 621; https://doi.org/10.3390/md19110621 - 01 Nov 2021
Cited by 5 | Viewed by 3726
Abstract
The deep-sea constitutes a true unexplored frontier and a potential source of innovative drug scaffolds. Here, we present the genome sequence of two novel marine actinobacterial strains, MA3_2.13 and S07_1.15, isolated from deep-sea samples (sediments and sponge) and collected at Madeira archipelago (NE [...] Read more.
The deep-sea constitutes a true unexplored frontier and a potential source of innovative drug scaffolds. Here, we present the genome sequence of two novel marine actinobacterial strains, MA3_2.13 and S07_1.15, isolated from deep-sea samples (sediments and sponge) and collected at Madeira archipelago (NE Atlantic Ocean; Portugal). The de novo assembly of both genomes was achieved using a hybrid strategy that combines short-reads (Illumina) and long-reads (PacBio) sequencing data. Phylogenetic analyses showed that strain MA3_2.13 is a new species of the Streptomyces genus, whereas strain S07_1.15 is closely related to the type strain of Streptomyces xinghaiensis. In silico analysis revealed that the total length of predicted biosynthetic gene clusters (BGCs) accounted for a high percentage of the MA3_2.13 genome, with several potential new metabolites identified. Strain S07_1.15 had, with a few exceptions, a predicted metabolic profile similar to S. xinghaiensis. In this work, we implemented a straightforward approach for generating high-quality genomes of new bacterial isolates and analyse in silico their potential to produce novel NPs. The inclusion of these in silico dereplication steps allows to minimize the rediscovery rates of traditional natural products screening methodologies and expedite the drug discovery process. Full article
(This article belongs to the Special Issue Bioactive Compounds from Marine Streptomyces)
►▼ Show Figures

Figure 1

Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
 
Displaying articles 1-66
Previous Issue
Next Issue
Back to TopTop