Marine Drugs

15 pages, 2447 KiB

Open AccessArticle

Enhanced Lipid Production and Molecular Dynamics under Salinity Stress in Green Microalga Chlamydomonas reinhardtii (137C)

by Thanapa Atikij, Yolani Syaputri, Hitoshi Iwahashi, Thanit Praneenararat, Sophon Sirisattha, Hakuto Kageyama and Rungaroon Waditee-Sirisattha

Mar. Drugs 2019, 17(8), 484; https://doi.org/10.3390/md17080484 - 20 Aug 2019

Cited by 30 | Viewed by 4167

Abstract

Microalgal lipids are a source of valuable nutritional ingredients in biotechnological industries, and are precursors to biodiesel production. Here, the effects of salt-induced stresses, including NaCl, KCl, and LiCl stresses, on the production of lipid in green microalga Chlamydomonas reinhardtii (137c) were investigated. [...] Read more.

Microalgal lipids are a source of valuable nutritional ingredients in biotechnological industries, and are precursors to biodiesel production. Here, the effects of salt-induced stresses, including NaCl, KCl, and LiCl stresses, on the production of lipid in green microalga Chlamydomonas reinhardtii (137c) were investigated. NaCl stress dramatically increased saturated fatty acids (SFAs), which accounted for 70.2% of the fatty acid methyl ester (FAMEs) under stress. In contrary, KCl stress led to a slight increase in SFAs (47.05%) with the remaining being polyunsaturated fatty acids (PUFAs) (45.77%). RT-PCR analysis revealed that the genes involved in FA biosynthesis, such as PDH2, ACCase, MAT and KAS2, were up-regulated by NaCl-induced stress. Conversely, the genes responsible for the Kennedy pathway were suppressed. The alteration of FA homeostasis was further assessed by overexpressing MAT, the enzyme responsible for the production of malonyl-ACP, a key building block for FA biosynthesis, in the cyanobacterium Synechococcus elongatus PCC 7942. Intracellular FA composition was affected, with a predominant synthesis of SFAs in transformed cells. Owing to the diversity and relative abundance of SFAs, monounsaturated fatty acid (MUFAs) and PUFAs enable the feasibility of using microorganisms as a source of microalgal lipids or valuable nutritional ingredients; salt-induced stress and expression of MAT are useful in providing precursors for enhanced lipid production. Full article

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11 pages, 1097 KiB

Open AccessArticle

Secondary Metabolites with α-Glucosidase Inhibitory Activity from the Mangrove Fungus Mycosphaerella sp. SYSU-DZG01

by Pei Qiu, Zhaoming Liu, Yan Chen, Runlin Cai, Guangying Chen and Zhigang She

Mar. Drugs 2019, 17(8), 483; https://doi.org/10.3390/md17080483 - 20 Aug 2019

Cited by 17 | Viewed by 3405

Abstract

Four new metabolites, asperchalasine I (1), dibefurin B (2) and two epicoccine derivatives (3 and 4), together with seven known compounds (5–11) were isolated from a mangrove fungus Mycosphaerella sp. SYSU-DZG01. The structures [...] Read more.

Four new metabolites, asperchalasine I (1), dibefurin B (2) and two epicoccine derivatives (3 and 4), together with seven known compounds (5–11) were isolated from a mangrove fungus Mycosphaerella sp. SYSU-DZG01. The structures of compounds 1–4 were established from extensive spectroscopic data and HRESIMS analysis. The absolute configuration of 1 was deduced by comparison of ECD data with that of a known structure. The stereostructures of 2–4 were further confirmed by single-crystal X-ray diffraction. Compounds 1, 8 and 9 exhibited significant α-glucosidase inhibitory activity with IC₅₀ values of 17.1, 26.7 and 15.7 μM, respectively. Compounds 1, 4, 6 and 8 showed antioxidant activity by scavenging DPPH· with EC₅₀ values ranging from 16.3 to 85.8 μM. Full article

(This article belongs to the Special Issue Enzyme Inhibitor from Marine Organisms)

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10 pages, 964 KiB

Open AccessArticle

Phenazine Derivatives with Anti-Inflammatory Activity from the Deep-Sea Sediment-Derived Yeast-Like Fungus Cystobasidium laryngis IV17-028

by Hwa-Sun Lee, Jong Soon Kang, Byeoung-Kyu Choi, Hyi-Seung Lee, Yeon-Ju Lee, Jihoon Lee and Hee Jae Shin

Mar. Drugs 2019, 17(8), 482; https://doi.org/10.3390/md17080482 - 19 Aug 2019

Cited by 11 | Viewed by 3509

Abstract

Three new phenazine derivatives (1–3), along with known compounds (4–7) of saphenic acid derivatives, were isolated from a deep-sea sediment-derived yeast-like fungus Cystobasidium larynigs collected from the Indian Ocean. The structures of the new compounds [...] Read more.

Three new phenazine derivatives (1–3), along with known compounds (4–7) of saphenic acid derivatives, were isolated from a deep-sea sediment-derived yeast-like fungus Cystobasidium larynigs collected from the Indian Ocean. The structures of the new compounds (1–3) were determined by analysis of spectroscopic data, semi-synthesis and comparison of optical rotation values. All the isolated compounds (1–7), except for 2, showed nitric oxide (NO) production inhibitory effect against lipopolysaccharide (LPS)-induced murine macrophage RAW 264.7 cells without cytotoxicity at concentrations up to 30 μg/mL. This is the first report on the yeast-like fungus Cystobasidium laryngis producing phenazines and anti-inflammatory activity of 1–7 including saphenic acid (4). Full article

(This article belongs to the Special Issue Deep-Sea Natural Products II)

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11 pages, 3633 KiB

Open AccessArticle

Anti-Inflammatory Cembrane-Type Diterpenoids and Prostaglandins from Soft Coral Lobophytum sarcophytoides

by Hongjie Shen, Xiaowan Liu, Minghua Jiang, Guangyuan Luo, Zhenger Wu, Bin Chen, Jing Li, Lan Liu and Senhua Chen

Mar. Drugs 2019, 17(8), 481; https://doi.org/10.3390/md17080481 - 19 Aug 2019

Cited by 14 | Viewed by 3155

Abstract

Two new cembrane-type diterpenoids, lobophytins A (1) and B (3), and four new prostaglandins, (5E)-PGB₂ (10), (5E)-13,14-dihydro-PGB₂ (11), 13,14-dihydro-PGB₂ (12) and 13,14-dihydro-PGB₂-Me (13 [...] Read more.

Two new cembrane-type diterpenoids, lobophytins A (1) and B (3), and four new prostaglandins, (5E)-PGB₂ (10), (5E)-13,14-dihydro-PGB₂ (11), 13,14-dihydro-PGB₂ (12) and 13,14-dihydro-PGB₂-Me (13), together with ten known compounds were isolated from the soft coral Lobophytum sarcophytoides. The structures of these new secondary metabolites were identified by high resolution mass spectrometry (HR-ESIMS), nuclear magnetic resonance (NMR) and electron circular dichroism (ECD) analyses, as well as the modified Mosher’s method. Compounds 6, 7, 9, 10, 12, 13, 15 and 16 showed potential anti-inflammatory activity by inhibiting the production of nitric oxide (NO) in RAW264.7 cells that were activated by lipopolysaccharide, with IC₅₀ values ranging from 7.1 to 32.1 μM and were better than the positive control indomethacin, IC₅₀ = 39.8 μM. Full article

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10 pages, 1875 KiB

Open AccessArticle

New Diterpenes with a Fused 6-5-6-6 Ring System Isolated from the Marine Sponge-Derived Fungus Trichoderma harzianum

by Takeshi Yamada, Ayano Fujii and Takashi Kikuchi

Mar. Drugs 2019, 17(8), 480; https://doi.org/10.3390/md17080480 - 19 Aug 2019

Cited by 14 | Viewed by 2828

Abstract

New diterpenes, namely, trichodermanins F–H, with a fused 6-5-6-6 ring system were isolated from the fungus Trichoderma harzianum OUPS-111D-4 separated from a marine sponge Halichondria okadai. These chemical structures were elucidated by 1D and 2D NMR as well as high-resolution fast atom [...] Read more.

New diterpenes, namely, trichodermanins F–H, with a fused 6-5-6-6 ring system were isolated from the fungus Trichoderma harzianum OUPS-111D-4 separated from a marine sponge Halichondria okadai. These chemical structures were elucidated by 1D and 2D NMR as well as high-resolution fast atom bombardment mass spectrometry (HRFABMS) spectral analyses. We established their absolute stereostructures by application of the modified Mosher’s method or circular dichroism (CD) spectroscopy. In addition, their cytotoxicities were assessed using several cancer cell lines, with 1 and 2 exhibiting modest activities. Full article

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17 pages, 4275 KiB

Open AccessArticle

Characterization of an Alkaline GH49 Dextranase from Marine Bacterium Arthrobacter oxydans KQ11 and Its Application in the Preparation of Isomalto-Oligosaccharide

by Hongfei Liu, Wei Ren, Mingsheng Ly, Haifeng Li and Shujun Wang

Mar. Drugs 2019, 17(8), 479; https://doi.org/10.3390/md17080479 - 19 Aug 2019

Cited by 15 | Viewed by 3433

Abstract

A GH49 dextranase gene DexKQ was cloned from marine bacteria Arthrobacter oxydans KQ11. It was recombinantly expressed using an Escherichia coli system. Recombinant DexKQ dextranase of 66 kDa exhibited the highest catalytic activity at pH 9.0 and 55 °C. kcat/Km of recombinant DexKQ [...] Read more.

A GH49 dextranase gene DexKQ was cloned from marine bacteria Arthrobacter oxydans KQ11. It was recombinantly expressed using an Escherichia coli system. Recombinant DexKQ dextranase of 66 kDa exhibited the highest catalytic activity at pH 9.0 and 55 °C. kcat/Km of recombinant DexKQ at the optimum condition reached 3.03 s⁻¹ μM⁻¹, which was six times that of commercial dextranase (0.5 s⁻¹ μM⁻¹). DexKQ possessed a Km value of 67.99 µM against dextran T70 substrate with 70 kDa molecular weight. Thin-layer chromatography (TLC) analysis showed that main hydrolysis end products were isomalto-oligosaccharide (IMO) including isomaltotetraose, isomaltopantose, and isomaltohexaose. When compared with glucose, IMO could significantly improve growth of Bifidobacterium longum and Lactobacillus rhamnosus and inhibit growth of Escherichia coli and Staphylococcus aureus. This is the first report of dextranase from marine bacteria concerning recombinant expression and application in isomalto-oligosaccharide preparation. Full article

(This article belongs to the Special Issue Marine Bacteria as Sources of Bioactive Compounds)

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10 pages, 1801 KiB

Open AccessArticle

New Benzofuranoids and Phenylpropanoids from the Mangrove Endophytic Fungus, Aspergillus sp. ZJ-68

by Runlin Cai, Hongming Jiang, Zhenming Zang, Chunyuan Li and Zhigang She

Mar. Drugs 2019, 17(8), 478; https://doi.org/10.3390/md17080478 - 18 Aug 2019

Cited by 14 | Viewed by 3293

Abstract

Three new benzofuranoids, asperfuranoids A–C (1–3), two new phenylpropanoid derivatives (6 and 7), and nine known analogues (4, 5, and 8–14) were isolated from the liquid substrate fermentation cultures of the [...] Read more.

Three new benzofuranoids, asperfuranoids A–C (1–3), two new phenylpropanoid derivatives (6 and 7), and nine known analogues (4, 5, and 8–14) were isolated from the liquid substrate fermentation cultures of the mangrove endopytic fungus Aspergillus sp. ZJ-68. The structures of the new compounds were determined by extensive spectroscopic data interpretation. The absolute configurations of 1–3 were assigned via the combination of Mosher’s method, and experimental and calculated electronic circular dichroism (ECD) data. Compounds 4 and 5 were a pair of enantiomers and their absolute configurations were established for the first time on the basis of their ECD spectra aided with ECD calculations. All isolated compounds (1–14) were evaluated for their enzyme inhibitory activity against α-glucosidase and antibacterial activities against four pathogenic bacteria (Staphylococcus aureus, Escherichia coli, Bacillus subtilis, and Pseudomonas aeruginosa). Among them, compound 6 exhibited potent inhibitory activity against α-glucosidase in a standard in vitro assay, with an IC₅₀ value of 12.4 μM, while compounds 8 and 11 showed activities against S. aureus, E. coli, and B. subtilis, with MIC values in the range of 4.15 to 12.5 μg/mL. Full article

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23 pages, 835 KiB

Open AccessReview

The Phylum Bryozoa as a Promising Source of Anticancer Drugs

by Blanca Figuerola and Conxita Avila

Mar. Drugs 2019, 17(8), 477; https://doi.org/10.3390/md17080477 - 17 Aug 2019

Cited by 34 | Viewed by 6989

Abstract

Recent advances in sampling and novel techniques in drug synthesis and isolation have promoted the discovery of anticancer agents from marine organisms to combat this major threat to public health worldwide. Bryozoans, which are filter-feeding, aquatic invertebrates often characterized by a calcified skeleton, [...] Read more.

Recent advances in sampling and novel techniques in drug synthesis and isolation have promoted the discovery of anticancer agents from marine organisms to combat this major threat to public health worldwide. Bryozoans, which are filter-feeding, aquatic invertebrates often characterized by a calcified skeleton, are an excellent source of pharmacologically interesting compounds including well-known chemical classes such as alkaloids and polyketides. This review covers the literature for secondary metabolites isolated from marine cheilostome and ctenostome bryozoans that have shown potential as cancer drugs. Moreover, we highlight examples such as bryostatins, the most known class of marine-derived compounds from this animal phylum, which are advancing through anticancer clinical trials due to their low toxicity and antineoplastic activity. The bryozoan antitumor compounds discovered until now show a wide range of chemical diversity and biological activities. Therefore, more research focusing on the isolation of secondary metabolites with potential anticancer properties from bryozoans and other overlooked taxa covering wider geographic areas is needed for an efficient bioprospecting of natural products. Full article

(This article belongs to the Special Issue Antitumor Compounds from Marine Invertebrates)

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15 pages, 951 KiB

Open AccessArticle

New Linear Precursors of cIDPR Derivatives as Stable Analogs of cADPR: A Potent Second Messenger with Ca²⁺-Modulating Activity Isolated from Sea Urchin Eggs

by Stefano D’Errico, Emy Basso, Andrea Patrizia Falanga, Maria Marzano, Tullio Pozzan, Vincenzo Piccialli, Gennaro Piccialli, Giorgia Oliviero and Nicola Borbone

Mar. Drugs 2019, 17(8), 476; https://doi.org/10.3390/md17080476 - 17 Aug 2019

Cited by 7 | Viewed by 2993

Abstract

Herein, we report on the synthesis of a small set of linear precursors of an inosine analogue of cyclic ADP-ribose (cADPR), a second messenger involved in Ca²⁺ mobilization from ryanodine receptor stores firstly isolated from sea urchin eggs extracts. The synthesized compounds [...] Read more.

Herein, we report on the synthesis of a small set of linear precursors of an inosine analogue of cyclic ADP-ribose (cADPR), a second messenger involved in Ca²⁺ mobilization from ryanodine receptor stores firstly isolated from sea urchin eggs extracts. The synthesized compounds were obtained starting from inosine and are characterized by an N1-alkyl chain replacing the “northern” ribose and a phosphate group attached at the end of the N1-alkyl chain and/or 5′-sugar positions. Preliminary Ca²⁺ mobilization assays, performed on differentiated C2C12 cells, are reported as well. Full article

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17 pages, 5087 KiB

Open AccessFeature PaperArticle

Scopularides Revisited: Molecular Networking Guided Exploration of Lipodepsipeptides in Australian Marine Fish Gastrointestinal Tract-Derived Fungi

by Ahmed H. Elbanna, Zeinab G. Khalil, Paul V. Bernhardt and Robert J. Capon

Mar. Drugs 2019, 17(8), 475; https://doi.org/10.3390/md17080475 - 16 Aug 2019

Cited by 22 | Viewed by 4900

Abstract

Chemical analysis of a cultivation of an Australian Mugil mullet gastrointestinal tract (GIT) derived fungus, Scopulariopsis sp. CMB-F458, yielded the known lipodepsipeptides scopularides A (1) and B (2). A comparative global natural product social (GNPS) molecular networking analysis of [...] Read more.

Chemical analysis of a cultivation of an Australian Mugil mullet gastrointestinal tract (GIT) derived fungus, Scopulariopsis sp. CMB-F458, yielded the known lipodepsipeptides scopularides A (1) and B (2). A comparative global natural product social (GNPS) molecular networking analysis of ×63 co-isolated fungi, detected two additional fungi producing new scopularides, with Beauveria sp. CMB-F585 yielding scopularides C–G (3–7) and Scopulariopsis sp. CMB-F115 yielding scopularide H (8). Structures inclusive of absolute configurations were assigned by detailed spectroscopic and C₃ Marfey’s analysis, together with X-ray analyses of 3 and 8, and biosynthetic considerations. Scopularides A–H (1–8) did not exhibit significant growth inhibitory activity against a selection of Gram positive (+ve) and negative (−ve) bacteria, a fungus, or a panel of three human carcinoma cell lines. Full article

(This article belongs to the Special Issue Molecular Networking as a Strategy in Discovery of Marine Bioactive Compounds)

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26 pages, 4957 KiB

Open AccessReview

The Anticancer Drug Discovery Potential of Marine Invertebrates from Russian Pacific

by Vladimir L. Katanaev, Salvatore Di Falco and Yuri Khotimchenko

Mar. Drugs 2019, 17(8), 474; https://doi.org/10.3390/md17080474 - 16 Aug 2019

Cited by 15 | Viewed by 5127

Abstract

Despite huge efforts by academia and pharmaceutical industry, cancer remains the second cause of disease-related death in developed countries. Novel sources and principles of anticancer drug discovery are in urgent demand. Marine-derived natural products represent a largely untapped source of future drug candidates. [...] Read more.

Despite huge efforts by academia and pharmaceutical industry, cancer remains the second cause of disease-related death in developed countries. Novel sources and principles of anticancer drug discovery are in urgent demand. Marine-derived natural products represent a largely untapped source of future drug candidates. This review focuses on the anticancer drug discovery potential of marine invertebrates from the North-West Pacific. The issues of biodiversity, chemodiversity, and the anticancer pharmacophore diversity this region hides are consecutively discussed. These three levels of diversity are analyzed from the point of view of the already discovered compounds, as well as from the assessment of the overall, still undiscovered and enormous potential. We further go into the predictions of the economic and societal benefits the full-scale exploration of this potential offers, and suggest strategic measures to be taken on the national level in order to unleash such full-scale exploration. The transversal and multi-discipline approach we attempt to build for the case of marine invertebrate-based anticancer drug discovery from a given region can be applied to other regions and disease conditions, as well as up-scaled to global dimensions. Full article

(This article belongs to the Special Issue Antitumor Compounds from Marine Invertebrates)

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14 pages, 3214 KiB

Open AccessArticle

Padina pavonica Extract Promotes In Vitro Differentiation and Functionality of Human Primary Osteoblasts

by Mariagiulia Minetti, Giulia Bernardini, Manuele Biazzo, Gilles Gutierrez, Michela Geminiani, Teresa Petrucci and Annalisa Santucci

Mar. Drugs 2019, 17(8), 473; https://doi.org/10.3390/md17080473 - 15 Aug 2019

Cited by 8 | Viewed by 4565

Abstract

Marine algae have gained much importance in the development of nutraceutical products due to their high content of bioactive compounds. In this work, we investigated the activity of Padina pavonica with the aim to demonstrate the pro-osteogenic ability of its extract on human [...] Read more.

Marine algae have gained much importance in the development of nutraceutical products due to their high content of bioactive compounds. In this work, we investigated the activity of Padina pavonica with the aim to demonstrate the pro-osteogenic ability of its extract on human primary osteoblast (HOb). Our data indicated that the acetonic extract of P. pavonica (EPP) is a safe product as it did not show any effect on osteoblast viability. At the same time, EPP showed to possess a beneficial effect on HOb functionality, triggering their differentiation and mineralization abilities. In particular EPP enhanced the expression of the earlier differentiation stage markers: a 5.4-fold increase in collagen type I alpha 1 chain (COL1A1), and a 2.3-fold increase in alkaline phosphatase (ALPL), as well as those involved in the late differentiation stage: a 3.7-fold increase in osteocalcin (BGLAP) expression and a 2.8-fold in osteoprotegerin (TNFRSF11B). These findings were corroborated by the enhancement in ALPL enzymatic activity (1.7-fold increase) and by the reduction of receptor activator of nuclear factor-κB ligand (RANKL) and osteoprotegerin (OPG) ratio (0.6-fold decrease). Moreover, EPP demonstrated the capacity to enhance the bone nodules formation by 3.2-fold in 4 weeks treated HOb. Therefore, EPP showed a significant capability of promoting osteoblast phenotype. Given its positive effect on bone homeostasis, EPP could be used as a useful nutraceutical product that, in addition to a healthy lifestyle and diet, can be able to contrast and prevent bone diseases, especially those connected with ageing, such as osteoporosis (OP). Full article

(This article belongs to the Special Issue Seaweeds Secondary Metabolites: Successes in and/or Probable Therapeutic Applications)

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13 pages, 1942 KiB

Open AccessArticle

A Collection of Bioactive Nitrogen-Containing Molecules from the Marine Sponge Acanthostrongylophora ingens

by Germana Esposito, Linh H. Mai, Arlette Longeon, Alfonso Mangoni, Emilie Durieu, Laurent Meijer, Rob Van Soest, Valeria Costantino and Marie-Lise Bourguet-Kondracki

Mar. Drugs 2019, 17(8), 472; https://doi.org/10.3390/md17080472 - 15 Aug 2019

Cited by 7 | Viewed by 3921

Abstract

Thirteen nitrogen-containing molecules (1a/1b and 2–12) were isolated from the Indonesian sponge Acanthostrongylophora ingens, highlighting the richness of this organism as a source of alkaloids. Their structures were elucidated using one- and two-dimensional NMR spectroscopy and [...] Read more.

Thirteen nitrogen-containing molecules (1a/1b and 2–12) were isolated from the Indonesian sponge Acanthostrongylophora ingens, highlighting the richness of this organism as a source of alkaloids. Their structures were elucidated using one- and two-dimensional NMR spectroscopy and HR-ESI-MS, while the stereochemistry of the diketopiperazines was established using Marfey’s method. All compounds were screened in our standard bioactivity assays, including antibacterial, antikinases, and amyloid β-42 assays. The most interesting bioactivity result was obtained with the known acanthocyclamine A (3), which revealed for the first time a specific Escherichia coli antimicrobial activity and an inhibitory effect on amyloid β-42 production induced by aftin-5 and no cytotoxicity at the dose of 26 µM. These results highlight the potentiality of a bipiperidine scaffold as a promising skeleton for preventing or reducing the production of amyloid β-42, a key player in the initiation of Alzheimer’s disease. Full article

(This article belongs to the Special Issue New Challenges in Structure Elucidation of Marine Natural Products: NMR Analyses and Other Advanced Methods)

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16 pages, 725 KiB

Open AccessReview

Current Stage of Marine Ceramic Grafts for 3D Bone Tissue Regeneration

by Patricia Diaz-Rodriguez, Miriam López-Álvarez, Julia Serra, Pío González and Mariana Landín

Mar. Drugs 2019, 17(8), 471; https://doi.org/10.3390/md17080471 - 15 Aug 2019

Cited by 19 | Viewed by 5086

Abstract

Bioceramic scaffolds are crucial in tissue engineering for bone regeneration. They usually provide hierarchical porosity, bioactivity, and mechanical support supplying osteoconductive properties and allowing for 3D cell culture. In the case of age-related diseases such as osteoarthritis and osteoporosis, or other bone alterations [...] Read more.

Bioceramic scaffolds are crucial in tissue engineering for bone regeneration. They usually provide hierarchical porosity, bioactivity, and mechanical support supplying osteoconductive properties and allowing for 3D cell culture. In the case of age-related diseases such as osteoarthritis and osteoporosis, or other bone alterations as alveolar bone resorption or spinal fractures, functional tissue recovery usually requires the use of grafts. These bone grafts or bone void fillers are usually based on porous calcium phosphate grains which, once disposed into the bone defect, act as scaffolds by incorporating, to their own porosity, the intergranular one. Despite their routine use in traumatology and dental applications, specific graft requirements such as osteoinductivity or balanced dissolution rate are still not completely fulfilled. Marine origin bioceramics research opens the possibility to find new sources of bone grafts given the wide diversity of marine materials still largely unexplored. The interest in this field has also been urged by the limitations of synthetic or mammalian-derived grafts already in use and broadly investigated. The present review covers the current stage of major marine origin bioceramic grafts for bone tissue regeneration and their promising properties. Both products already available on the market and those in preclinical phases are included. To understand their clear contribution to the field, the main clinical requirements and the current available biological-derived ceramic grafts with their advantages and limitations have been collected. Full article

(This article belongs to the Special Issue 3D Cell Culture Based on Marine Resources)

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14 pages, 3973 KiB

Open AccessArticle

The Protective Effect of Mycosporine-Like Amino Acids (MAAs) from Porphyra yezoensis in a Mouse Model of UV Irradiation-Induced Photoaging

by Rui Ying, Zhaohui Zhang, Huiying Zhu, Bafang Li and Hu Hou

Mar. Drugs 2019, 17(8), 470; https://doi.org/10.3390/md17080470 - 14 Aug 2019

Cited by 16 | Viewed by 3872

Abstract

The objective of this research was to extract and prepare mycosporine-like amino acids (MAAs) and investigate the mechanism by which they act against UV-induced skin photoaging in Institute of Cancer Research (ICR ) mice. MAAs such as porphyra-334 and shinorine were extracted from [...] Read more.

The objective of this research was to extract and prepare mycosporine-like amino acids (MAAs) and investigate the mechanism by which they act against UV-induced skin photoaging in Institute of Cancer Research (ICR ) mice. MAAs such as porphyra-334 and shinorine were extracted from Porphyra yezoensis, separated, and purified using column chromatography with SA-2 cation exchange resin. The effects of MAAs on the activity of endogenous antioxidant enzymes, namely total superoxide dismutase (T-SOD), glutathione peroxidase (GSH-Px), catalase (CAT), and malondialdehyde (MDA) were analyzed in mouse skin tissue. Pathological changes of skin tissue caused by ultraviolet radiation and the arrangement of collagen were observed by Hematoxylin-Eosin (HE) staining and scanning electron microscopy (SEM). Interleukin 1β (IL-1β), IL-6, and IL-10 were detected using the quantitative real-time reverse transcription-polymerase chain reaction (qPCR) and Enzyme Linked Immunosorbent Assay (ELISA). The concentration and expression of these proinflammatory cytokines was associated with the presence of nuclear factor (NF)-κB. The results show that MAA compounds from Porphyra yezoensis could suppress UV-induced photoaging of skin by inhibiting the reduction of endogenous antioxidant enzymes. Compared to the control group, the concentrations of SOD, GSH-Px, and CAT increased significantly in skin tissue homogenate following the external administration of MAAs (p < 0.05, p < 0.01), while the content of MDA decreased significantly (p < 0.05). Meanwhile, the administration of MAAs was associated with down-regulations in the concentration and mRNA expression of NF-κB, IL-1β, IL-6, and IL-10. The results suggest that MAAs could protect skin from photodamage by increasing antioxidant enzyme activities and inhibiting inflammation. Full article

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24 pages, 3385 KiB

Open AccessArticle

The Sialic Acid-Dependent Nematocyst Discharge Process in Relation to Its Physical-Chemical Properties Is a Role Model for Nanomedical Diagnostic and Therapeutic Tools

by Ruiyan Zhang, Li Jin, Ning Zhang, Athanasios K. Petridis, Thomas Eckert, Georgios Scheiner-Bobis, Martin Bergmann, Axel Scheidig, Roland Schauer, Mingdi Yan, Samurdhi A. Wijesundera, Bengt Nordén, Barun K. Chatterjee and Hans-Christian Siebert

Mar. Drugs 2019, 17(8), 469; https://doi.org/10.3390/md17080469 - 12 Aug 2019

Cited by 10 | Viewed by 4333

Abstract

Formulas derived from theoretical physics provide important insights about the nematocyst discharge process of Cnidaria (Hydra, jellyfishes, box-jellyfishes and sea-anemones). Our model description of the fastest process in living nature raises and answers questions related to the material properties of the cell- and [...] Read more.

Formulas derived from theoretical physics provide important insights about the nematocyst discharge process of Cnidaria (Hydra, jellyfishes, box-jellyfishes and sea-anemones). Our model description of the fastest process in living nature raises and answers questions related to the material properties of the cell- and tubule-walls of nematocysts including their polysialic acid (polySia) dependent target function. Since a number of tumor-cells, especially brain-tumor cells such as neuroblastoma tissues carry the polysaccharide chain polySia in similar concentration as fish eggs or fish skin, it makes sense to use these findings for new diagnostic and therapeutic approaches in the field of nanomedicine. Therefore, the nematocyst discharge process can be considered as a bionic blue-print for future nanomedical devices in cancer diagnostics and therapies. This approach is promising because the physical background of this process can be described in a sufficient way with formulas presented here. Additionally, we discuss biophysical and biochemical experiments which will allow us to define proper boundary conditions in order to support our theoretical model approach. PolySia glycans occur in a similar density on malignant tumor cells than on the cell surfaces of Cnidarian predators and preys. The knowledge of the polySia-dependent initiation of the nematocyst discharge process in an intact nematocyte is an essential prerequisite regarding the further development of target-directed nanomedical devices for diagnostic and therapeutic purposes. The theoretical description as well as the computationally and experimentally derived results about the biophysical and biochemical parameters can contribute to a proper design of anti-tumor drug ejecting vessels which use a stylet-tubule system. Especially, the role of nematogalectins is of interest because these bridging proteins contribute as well as special collagen fibers to the elastic band properties. The basic concepts of the nematocyst discharge process inside the tubule cell walls of nematocysts were studied in jellyfishes and in Hydra which are ideal model organisms. Hydra has already been chosen by Alan Turing in order to figure out how the chemical basis of morphogenesis can be described in a fundamental way. This encouraged us to discuss the action of nematocysts in relation to morphological aspects and material requirements. Using these insights, it is now possible to discuss natural and artificial nematocyst-like vessels with optimized properties for a diagnostic and therapeutic use, e.g., in neurooncology. We show here that crucial physical parameters such as pressure thresholds and elasticity properties during the nematocyst discharge process can be described in a consistent and satisfactory way with an impact on the construction of new nanomedical devices. Full article

(This article belongs to the Special Issue Marine Glycobiology, Glycomics and Lectins)

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46 pages, 14252 KiB

Open AccessReview

Coral and Coral-Associated Microorganisms: A Prolific Source of Potential Bioactive Natural Products

by Vo Thanh Sang, Ton That Huu Dat, Le Ba Vinh, Le Canh Viet Cuong, Phung Thi Thuy Oanh, Hoang Ha, Young Ho Kim, Hoang Le Tuan Anh and Seo Young Yang

Mar. Drugs 2019, 17(8), 468; https://doi.org/10.3390/md17080468 - 11 Aug 2019

Cited by 55 | Viewed by 8760

Abstract

Marine invertebrates and their associated microorganisms are rich sources of bioactive compounds. Among them, coral and its associated microorganisms are promising providers of marine bioactive compounds. The present review provides an overview of bioactive compounds that are produced by corals and coral-associated microorganisms, [...] Read more.

Marine invertebrates and their associated microorganisms are rich sources of bioactive compounds. Among them, coral and its associated microorganisms are promising providers of marine bioactive compounds. The present review provides an overview of bioactive compounds that are produced by corals and coral-associated microorganisms, covering the literature from 2010 to March 2019. Accordingly, 245 natural products that possess a wide range of potent bioactivities, such as anti-inflammatory, cytotoxic, antimicrobial, antivirus, and antifouling activities, among others, are described in this review. Full article

(This article belongs to the Special Issue Bioactive Compounds from Coral Reef Organisms)

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32 pages, 1968 KiB

Open AccessReview

Marine Collagen as A Promising Biomaterial for Biomedical Applications

by Ye-Seon Lim, Ye-Jin Ok, Seon-Yeong Hwang, Jong-Young Kwak and Sik Yoon

Mar. Drugs 2019, 17(8), 467; https://doi.org/10.3390/md17080467 - 10 Aug 2019

Cited by 175 | Viewed by 13946

Abstract

This review focuses on the expanding role of marine collagen (MC)-based scaffolds for biomedical applications. A scaffold—a three-dimensional (3D) structure fabricated from biomaterials—is a key supporting element for cell attachment, growth, and maintenance in 3D cell culture and tissue engineering. The mechanical and [...] Read more.

This review focuses on the expanding role of marine collagen (MC)-based scaffolds for biomedical applications. A scaffold—a three-dimensional (3D) structure fabricated from biomaterials—is a key supporting element for cell attachment, growth, and maintenance in 3D cell culture and tissue engineering. The mechanical and biological properties of the scaffolds influence cell morphology, behavior, and function. MC, collagen derived from marine organisms, offers advantages over mammalian collagen due to its biocompatibility, biodegradability, easy extractability, water solubility, safety, low immunogenicity, and low production costs. In recent years, the use of MC as an increasingly valuable scaffold biomaterial has drawn considerable attention from biomedical researchers. The characteristics, isolation, physical, and biochemical properties of MC are discussed as an understanding of MC in optimizing the subsequent modification and the chemistries behind important tissue engineering applications. The latest technologies behind scaffold processing are assessed and the biomedical applications of MC and MC-based scaffolds, including tissue engineering and regeneration, wound dressing, drug delivery, and therapeutic approach for diseases, especially those associated with metabolic disturbances such as obesity and diabetes, are discussed. Despite all the challenges, MC holds great promise as a biomaterial for developing medical products and therapeutics. Full article

(This article belongs to the Special Issue 3D Cell Culture Based on Marine Resources)

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15 pages, 1061 KiB

Open AccessArticle

Transcriptomic Analysis of Marine Gastropod Hemifusus tuba Provides Novel Insights into Conotoxin Genes

by Ronghua Li, Michaël Bekaert, Luning Wu, Changkao Mu, Weiwei Song, Herve Migaud and Chunlin Wang

Mar. Drugs 2019, 17(8), 466; https://doi.org/10.3390/md17080466 - 10 Aug 2019

Cited by 6 | Viewed by 3579

Abstract

The marine gastropod Hemifusus tuba is served as a luxury food in Asian countries and used in traditional Chinese medicine to treat lumbago and deafness. The lack of genomic data on H. tuba is a barrier to aquaculture development and functional characteristics of [...] Read more.

The marine gastropod Hemifusus tuba is served as a luxury food in Asian countries and used in traditional Chinese medicine to treat lumbago and deafness. The lack of genomic data on H. tuba is a barrier to aquaculture development and functional characteristics of potential bioactive molecules are poorly understood. In the present study, we used high-throughput sequencing technologies to generate the first transcriptomic database of H. tuba. A total of 41 unique conopeptides were retrieved from 44 unigenes, containing 6-cysteine frameworks belonging to four superfamilies. Duplication of mature regions and alternative splicing were also found in some of the conopeptides, and the de novo assembly identified a total of 76,306 transcripts with an average length of 824.6 nt, of which including 75,620 (99.1%) were annotated. In addition, simple sequence repeats (SSRs) detection identified 14,000 unigenes containing 20,735 SSRs, among which, 23 polymorphic SSRs were screened. Thirteen of these markers could be amplified in Hemifusus ternatanus and seven in Rapana venosa. This study provides reports of conopeptide genes in Buccinidae for the first time as well as genomic resources for further drug development, gene discovery and population resource studies of this species. Full article

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13 pages, 2443 KiB

Open AccessCommunication

Bioactive Brominated Oxindole Alkaloids from the Red Sea Sponge Callyspongia siphonella

by Seham S. El-Hawary, Ahmed M. Sayed, Rabab Mohammed, Hossam M. Hassan, Mostafa E. Rateb, Elham Amin, Tarek A. Mohammed, Mohamed El-Mesery, Abdullatif Bin Muhsinah, Abdulrhman Alsayari, Harald Wajant, Mohamed A. Anany and Usama Ramadan Abdelmohsen

Mar. Drugs 2019, 17(8), 465; https://doi.org/10.3390/md17080465 - 09 Aug 2019

Cited by 42 | Viewed by 4514

Abstract

In the present study, LC-HRESIMS-assisted dereplication along with bioactivity-guided isolation led to targeting two brominated oxindole alkaloids (compounds 1 and 2) which probably play a key role in the previously reported antibacterial, antibiofilm, and cytotoxicity of Callyspongia siphonella crude extracts. Both metabolites [...] Read more.

In the present study, LC-HRESIMS-assisted dereplication along with bioactivity-guided isolation led to targeting two brominated oxindole alkaloids (compounds 1 and 2) which probably play a key role in the previously reported antibacterial, antibiofilm, and cytotoxicity of Callyspongia siphonella crude extracts. Both metabolites showed potent antibacterial activity against Gram-positive bacteria, Staphylococcus aureus (minimum inhibitory concentration (MIC) = 8 and 4 µg/mL) and Bacillus subtilis (MIC = 16 and 4 µg/mL), respectively. Furthermore, they displayed moderate biofilm inhibitory activity in Pseudomonas aeruginosa (49.32% and 41.76% inhibition, respectively), and moderate in vitro antitrypanosomal activity (13.47 and 10.27 µM, respectively). In addition, they revealed a strong cytotoxic effect toward different human cancer cell lines, supposedly through induction of necrosis. This study sheds light on the possible role of these metabolites (compounds 1 and 2) in keeping fouling organisms away from the sponge outer surface, and the possible applications of these defensive molecules in the development of new anti-infective agents. Full article

(This article belongs to the Collection Bioactive Compounds from Marine Invertebrates)

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29 pages, 4956 KiB

Open AccessReview

Metabolites from Marine Microorganisms, Micro, and Macroalgae: Immense Scope for Pharmacology

by Noora Barzkar, Saeid Tamadoni Jahromi, Hadi Bolooki Poorsaheli and Fabio Vianello

Mar. Drugs 2019, 17(8), 464; https://doi.org/10.3390/md17080464 - 08 Aug 2019

Cited by 99 | Viewed by 8003

Abstract

Marine organisms produce a large array of natural products with relevance in drug discovery. These compounds have biological activities such as antioxidant, antibacterial, antitumor, antivirus, anticoagulant, anti-inflammatory, antihypertensive, antidiabetic, and so forth. Consequently, several of the metabolites have made it to the advanced [...] Read more.

Marine organisms produce a large array of natural products with relevance in drug discovery. These compounds have biological activities such as antioxidant, antibacterial, antitumor, antivirus, anticoagulant, anti-inflammatory, antihypertensive, antidiabetic, and so forth. Consequently, several of the metabolites have made it to the advanced stages of clinical trials, and a few of them are commercially available. In this review, novel information on natural products isolated from marine microorganisms, microalgae, and macroalgae are presented. Given due research impetus, these marine metabolites might emerge as a new wave of promising drugs. Full article

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13 pages, 1694 KiB

Open AccessArticle

Purification, Characterization and Evaluation of Inhibitory Mechanism of ACE Inhibitory Peptides from Pearl Oyster (Pinctada fucata martensii) Meat Protein Hydrolysate

by Pengru Liu, Xiongdiao Lan, Muhammad Yaseen, Shanguang Wu, Xuezhen Feng, Liqin Zhou, Jianhua Sun, Anping Liao, Dankui Liao and Lixia Sun

Mar. Drugs 2019, 17(8), 463; https://doi.org/10.3390/md17080463 - 08 Aug 2019

Cited by 45 | Viewed by 4620

Abstract

Angiotensin-I-converting enzyme (ACE) inhibitory peptides derived from natural products have shown a blood pressure lowering effect with no side effects. In this study, two novel ACE inhibitory peptides (His-Leu-His-Thr, HLHT and Gly-Trp-Ala, GWA) were purified from pearl oyster (Pinctada fucata martensii) [...] Read more.

Angiotensin-I-converting enzyme (ACE) inhibitory peptides derived from natural products have shown a blood pressure lowering effect with no side effects. In this study, two novel ACE inhibitory peptides (His-Leu-His-Thr, HLHT and Gly-Trp-Ala, GWA) were purified from pearl oyster (Pinctada fucata martensii) meat protein hydrolysate with alkaline protease by ultrafiltration, polyethylene glycol methyl ether modified immobilized metal ion affinity medium, and reverse-phase high performance liquid chromatography. Both peptides exhibited high ACE inhibitory activity with IC₅₀ values of 458.06 ± 3.24 μM and 109.25 ± 1.45 μM, respectively. Based on the results of a Lineweaver-Burk plot, HLHT and GWA were found to be non-competitive inhibitor and competitive inhibitor respectively, which were confirmed by molecular docking. Furthermore, the pearl oyster meat protein hydrolysate exhibited an effective antihypertensive effect on SD rats. These results conclude that pearl oyster meat protein is a potential resource of ACE inhibitory peptides and the purified peptides, HLHT and GWA, can be exploited as functional food ingredients against hypertension. Full article

(This article belongs to the Special Issue Advancements in Purification, Isolation and Chemical Profiling to Expedite the Discovery of Marine Natural Products)

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15 pages, 6365 KiB

Open AccessArticle

Comparison of Physicochemical Characteristics and Fibril Formation Ability of Collagens Extracted from the Skin of Farmed River Puffer (Takifugu obscurus) and Tiger Puffer (Takifugu rubripes)

by Shan-Shan Wang, Ying Yu, Yong Sun, Nan Liu and De-Qing Zhou

Mar. Drugs 2019, 17(8), 462; https://doi.org/10.3390/md17080462 - 07 Aug 2019

Cited by 8 | Viewed by 3728

Abstract

Acid-soluble collagen (ASC) and pepsin-soluble collagen (PSC) from the skin of river puffer (ASC-RP and PSC-RP) and tiger puffer (ASC-TP and PSC-TP) were extracted and physicochemically examined. Denaturation temperature (T_d) for all the collagens was found to be 25.5–29.5 °C, which [...] Read more.

Acid-soluble collagen (ASC) and pepsin-soluble collagen (PSC) from the skin of river puffer (ASC-RP and PSC-RP) and tiger puffer (ASC-TP and PSC-TP) were extracted and physicochemically examined. Denaturation temperature (T_d) for all the collagens was found to be 25.5–29.5 °C, which was lower than that of calf skin collagen (35.9 °C). Electrophoretic patterns indicated all four samples were type I collagen with molecular form of (α₁)₂α₂. FTIR spectra confirmed the extracted collagens had a triple-helical structure, and that the degree of hydrogen bonding in ASC was higher than PSC. All the extracted collagens could aggregate into fibrils with D-periodicity. The fibril formation rate of ASC-RP and PSC-RP was slightly higher than ASC-TP and PSC-TP. Turbidity analysis revealed an increase in fibril formation rate when adding a low concentration of NaCl (less than 300 mM). The fibril formation ability was suppressed with further increasing of NaCl concentration, as illustrated by a reduction in the turbidity and formation degree. SEM analysis confirmed the well-formed interwoven structure of collagen fibrils after 24 h of incubation. Summarizing the experimental results suggested that the extracted collagens from the skin of river puffer and tiger puffer could be considered a viable substitute to mammalian-derived collagens for further use in biomaterial applications. Full article

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11 pages, 1680 KiB

Open AccessArticle

Bioactive Capnosanes and Cembranes from the Soft Coral Klyxum flaccidum

by Wan-Ru Tseng, Atallah F. Ahmed, Chiung-Yao Huang, Yi-Ying Tsai, Chi-Jen Tai, Raha S. Orfali, Tsong-Long Hwang, Yi-Hsuan Wang, Chang-Feng Dai and Jyh-Horng Sheu

Mar. Drugs 2019, 17(8), 461; https://doi.org/10.3390/md17080461 - 07 Aug 2019

Cited by 15 | Viewed by 3202

Abstract

Two new capnosane-based diterpenoids, flaccidenol A (1) and 7-epi-pavidolide D (2), two new cembranoids, flaccidodioxide (3) and flaccidodiol (4), and three known compounds 5 to 7 were characterized from the marine soft coral [...] Read more.

Two new capnosane-based diterpenoids, flaccidenol A (1) and 7-epi-pavidolide D (2), two new cembranoids, flaccidodioxide (3) and flaccidodiol (4), and three known compounds 5 to 7 were characterized from the marine soft coral Klyxum flaccidum, collected off the coast of the island of Pratas. The structures of the new compounds were determined by extensive spectroscopic analyses, including 1D and 2D nuclear magnetic resonance (NMR) spectroscopy, and spectroscopic data comparison with related structures. The rare capnosane diterpenoids were isolated herein from the genus Klyxum for the first time. The cytotoxicity of compounds 1 to 7 against the proliferation of a limited panel of cancer cell lines was assayed. The isolated diterpenoids also exhibited anti-inflammatory activity through suppression of superoxide anion generation and elastase release in the N-formyl-methionyl-leucyl-phenylalanine/cytochalasin B (fMLF/CB)-stimulated human neutrophils. Furthermore, 1 and 7 also exhibited cytotoxicity toward the tested cancer cells, and 7 could effectively inhibit elastase release. It is worth noting that the biological activities of 7 are reported for the first time in this paper. Full article

(This article belongs to the Special Issue Marine Natural Products Discovery: In Memory of Late Prof. Tatsuo Higa)

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12 pages, 914 KiB

Open AccessArticle

Light Intensity and Nitrogen Concentration Impact on the Biomass and Phycoerythrin Production by Porphyridium purpureum

by Juan Eduardo Sosa-Hernández, Laura Isabel Rodas-Zuluaga, Carlos Castillo-Zacarías, Magdalena Rostro-Alanís, Reynaldo de la Cruz, Danay Carrillo-Nieves, Carmen Salinas-Salazar, Claudio Fuentes Grunewald, Carole A. Llewellyn, Eugenia J. Olguín, Robert W. Lovitt, Hafiz M. N. Iqbal and Roberto Parra-Saldívar

Mar. Drugs 2019, 17(8), 460; https://doi.org/10.3390/md17080460 - 07 Aug 2019

Cited by 27 | Viewed by 5390

Abstract

Several factors have the potential to influence microalgae growth. In the present study, nitrogen concentration and light intensity were evaluated in order to obtain high biomass production and high phycoerythrin accumulation from Porphyridium purpureum. The range of nitrogen concentrations evaluated in the [...] Read more.

Several factors have the potential to influence microalgae growth. In the present study, nitrogen concentration and light intensity were evaluated in order to obtain high biomass production and high phycoerythrin accumulation from Porphyridium purpureum. The range of nitrogen concentrations evaluated in the culture medium was 0.075–0.450 g L⁻¹ and light intensities ranged between 30 and 100 μmol m⁻² s⁻¹. Surprisingly, low nitrogen concentration and high light intensity resulted in high biomass yield and phycoerythrin accumulation. Thus, the best biomass productivity (0.386 g L⁻¹ d⁻¹) and biomass yield (5.403 g L⁻¹) were achieved with NaNO₃ at 0.075 g L⁻¹ and 100 μmol m⁻² s⁻¹. In addition, phycoerythrin production was improved to obtain a concentration of 14.66 mg L⁻¹ (2.71 mg g⁻¹ of phycoerythrin over dry weight). The results of the present study indicate that it is possible to significantly improve biomass and pigment production in Porphyridium purpureum by limiting nitrogen concentration and light intensity. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Marine Microalgae)

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20 pages, 1989 KiB

Open AccessReview

Microalgal Enzymes with Biotechnological Applications

by Giorgio Maria Vingiani, Pasquale De Luca, Adrianna Ianora, Alan D.W. Dobson and Chiara Lauritano

Mar. Drugs 2019, 17(8), 459; https://doi.org/10.3390/md17080459 - 05 Aug 2019

Cited by 45 | Viewed by 6448

Abstract

Enzymes are essential components of biological reactions and play important roles in the scaling and optimization of many industrial processes. Due to the growing commercial demand for new and more efficient enzymes to help further optimize these processes, many studies are now focusing [...] Read more.

Enzymes are essential components of biological reactions and play important roles in the scaling and optimization of many industrial processes. Due to the growing commercial demand for new and more efficient enzymes to help further optimize these processes, many studies are now focusing their attention on more renewable and environmentally sustainable sources for the production of these enzymes. Microalgae are very promising from this perspective since they can be cultivated in photobioreactors, allowing the production of high biomass levels in a cost-efficient manner. This is reflected in the increased number of publications in this area, especially in the use of microalgae as a source of novel enzymes. In particular, various microalgal enzymes with different industrial applications (e.g., lipids and biofuel production, healthcare, and bioremediation) have been studied to date, and the modification of enzymatic sequences involved in lipid and carotenoid production has resulted in promising results. However, the entire biosynthetic pathways/systems leading to synthesis of potentially important bioactive compounds have in many cases yet to be fully characterized (e.g., for the synthesis of polyketides). Nonetheless, with recent advances in microalgal genomics and transcriptomic approaches, it is becoming easier to identify sequences encoding targeted enzymes, increasing the likelihood of the identification, heterologous expression, and characterization of these enzymes of interest. This review provides an overview of the state of the art in marine and freshwater microalgal enzymes with potential biotechnological applications and provides future perspectives for this field. Full article

(This article belongs to the Special Issue Marine Enzymes: Sources, Biochemistry and Bioprocesses for Marine Biotechnology)

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20 pages, 1101 KiB

Open AccessReview

Possibilities of Fucoidan Utilization in the Development of Pharmaceutical Dosage Forms

by Aleksandra Citkowska, Marta Szekalska and Katarzyna Winnicka

Mar. Drugs 2019, 17(8), 458; https://doi.org/10.3390/md17080458 - 05 Aug 2019

Cited by 104 | Viewed by 8181

Abstract

Fucoidan is a polysaccharide built from L-fucose molecules. The main source of this polysaccharide is the extracellular matrix of brown seaweed (Phaeophyta), but it can be also isolated from invertebrates such as sea urchins (Echinoidea) and sea cucumbers ( [...] Read more.

Fucoidan is a polysaccharide built from L-fucose molecules. The main source of this polysaccharide is the extracellular matrix of brown seaweed (Phaeophyta), but it can be also isolated from invertebrates such as sea urchins (Echinoidea) and sea cucumbers (Holothuroidea). Interest in fucoidan is related to its broad biological activity, including possible antioxidant, anti-inflammatory, antifungal, antiviral or antithrombotic effects. The potential application of fucoidan in the pharmaceutical technology is also due to its ionic nature. The negative charge of the molecule results from the presence of sulfate residues in the C-2 and C-4 positions, occasionally in C-3, allowing the formation of complexes with other oppositely charged molecules. Fucoidan is non-toxic, biodegradable and biocompatible compound approved by Food and Drug Administration (FDA) as Generally Recognized As Safe (GRAS) category as food ingredient. Fucoidan plays an important role in the pharmaceutical technology, so in this work aspects concerning its pharmaceutical characteristics and designing of various dosage forms (nanoparticles, liposomes, microparticles, and semisolid formulations) with fucoidan itself and with its combinations with other polymers or components that give a positive charge were reviewed. Advantages and limitations of fucoidan utilization in the pharmaceutical technology were also discussed. Full article

(This article belongs to the Special Issue Marine Polysaccharides in Pharmaceutical Applications)

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17 pages, 1941 KiB

Open AccessArticle

Enhancing the Extraction of Polysaccharides and Antioxidants from Macroalgae Using Sequential Hydrothermal-Assisted Extraction Followed by Ultrasound and Thermal Technologies

by Marco Garcia-Vaquero, John V. O’Doherty, Brijesh K. Tiwari, Torres Sweeney and Gaurav Rajauria

Mar. Drugs 2019, 17(8), 457; https://doi.org/10.3390/md17080457 - 05 Aug 2019

Cited by 59 | Viewed by 5980

Abstract

Fucose sulphated polysaccharides (FSPs) and glucans have recently attracted the attention of the scientific community due to their wide range of biological activities. Both polysaccharides should ideally be selectively extracted using innovative technologies with high extraction efficiency. This study aims to: (1) Optimise [...] Read more.

Fucose sulphated polysaccharides (FSPs) and glucans have recently attracted the attention of the scientific community due to their wide range of biological activities. Both polysaccharides should ideally be selectively extracted using innovative technologies with high extraction efficiency. This study aims to: (1) Optimise the extraction variables used in hydrothermal-assisted extraction (HAE) to obtain high yields of FSPs, total glucans, and antioxidants from Laminaria hyperborea; (2) to apply these optimised protocols to other brown macroalgae; and (3) to explore the application of ultrasound and thermal technologies to increase the recovery of polysaccharides from the residual biomass. Box-Behnken design (three-factor, four-levels) was employed to optimise the HAE variables, and principal component analysis was used to evaluate the recovery of polysaccharides from the residual biomass. The optimal HAE conditions were 120 °C, 80.9 min, and 12.02 mL/g macroalgae from L. hyperborea. The best sequential application of ultrasound and thermal treatment achieved an additional 2971.7 ± 61.9 mg fucose/100 g dried macroalgal residue (dmr) from Ascophyllum nodosum and 908.0 ± 51.4 mg total glucans/100 g dmr from L. hyperborea macroalgal residues. Full article

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14 pages, 3449 KiB

Open AccessArticle

Herring Milt Protein Hydrolysate Improves Insulin Resistance in High-Fat-Diet-Induced Obese Male C57BL/6J Mice

by Yanwen Wang, Jacques Gagnon, Sandhya Nair and Shelly Sha

Mar. Drugs 2019, 17(8), 456; https://doi.org/10.3390/md17080456 - 03 Aug 2019

Cited by 15 | Viewed by 4125

Abstract

Protein consumption influences glucose homeostasis, but the effect depends on the type and origin of proteins ingested. The present study was designed to determine the effect of herring milt protein hydrolysate (HPH) on insulin function and glucose metabolism in a mouse model of [...] Read more.

Protein consumption influences glucose homeostasis, but the effect depends on the type and origin of proteins ingested. The present study was designed to determine the effect of herring milt protein hydrolysate (HPH) on insulin function and glucose metabolism in a mouse model of diet-induced obesity. Male C57BL/6J mice were pretreated with a low-fat diet or a high-fat diet for 6 weeks. Mice on the high-fat diet were divided into four groups where one group continued on the high-fat diet and the other three groups were fed a modified high-fat diet where 15%, 35%, and 70%, respectively, of casein was replaced with an equal percentage of protein derived from HPH. After 10 weeks, mice that continued on the high-fat diet showed significant increases in body weight, blood glucose, insulin, and leptin levels and exhibited impaired oral glucose tolerance, insulin resistance, and pancreatic β-cell dysfunction. Compared to mice fed the high-fat diet, the 70% replacement of dietary casein with HPH protein reduced body weight, semi-fasting blood glucose, fasting blood glucose, insulin, leptin, and cholesterol levels and improved glucose tolerance, homeostasis model assessment of insulin resistance (HOMA-IR), and homeostasis model assessment of β-cell function (HOMA-β) indices. The 35% replacement of dietary casein with HPH protein showed moderate effects, while the 15% replacement of dietary casein with HPH protein had no effects. This is the first study demonstrating that replacing dietary casein with the same amount of protein derived from HPH can prevent high-fat-diet-induced obesity and insulin resistance. Full article

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15 pages, 4115 KiB

Open AccessArticle

Long-Chain Bases from Sea Cucumber Alleviate Obesity by Modulating Gut Microbiota

by Shiwei Hu, Yangli Xu, Xiang Gao, Shijie Li, Wei Jiang, Yu Liu, Laijin Su and Huicheng Yang

Mar. Drugs 2019, 17(8), 455; https://doi.org/10.3390/md17080455 - 01 Aug 2019

Cited by 43 | Viewed by 4348

Abstract

This study evaluated the effects of long-chain bases from sea cucumber (SC-LCBs) on modulation of the gut microbiota and inhibition of obesity in high fat diet-fed mice. Results showed that SC-LCBs exerted significant antiobese effects, which were associated with the inhibition of hyperglycemia [...] Read more.

This study evaluated the effects of long-chain bases from sea cucumber (SC-LCBs) on modulation of the gut microbiota and inhibition of obesity in high fat diet-fed mice. Results showed that SC-LCBs exerted significant antiobese effects, which were associated with the inhibition of hyperglycemia and lipid accumulation. SC-LCBs also regulated serum adipocytokines toward to normal levels. SC-LCBs caused significant decreases in Firmicutes, Actinobacteria phylum, and obesity-related bacteria (Desulfovibro, Bifidobacterium, Romboutsia etc. genus). SC-LCBs also elevated Bacteroidetes, Proteobacteria, Verrucomicrobia phylum, and short chain fatty acids (SCFAs)-producing bacteria (Bacteroides, Lactobacillus, Lachnospiraceae_NK4A136_group etc. genus). Moreover, serum and fecal lipoplysaccharide (LPS) concentrations and its dependent toll-line receptor 4 pathway were inhibited by SC-LCBs treatment. SC-LCBs caused increases in fecal SCFAs and their mediated G-protein-coupled receptors proteins. These suggest that SC-LCBs alleviate obesity by altering gut microbiota. Thus, it sought to indicate that SC-LCBs can be developed as food supplement for the obesity control and the human gut health. Full article

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Mar. Drugs, Volume 17, Issue 8 (August 2019) – 53 articles

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