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Mar. Drugs, Volume 15, Issue 5 (May 2017)

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Cover Story In the present work, collagen was obtained by pepsin extraction of skin from two species of teleost [...] Read more.
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Open AccessFeature PaperArticle Transcriptome Analysis of Core Dinoflagellates Reveals a Universal Bias towards “GC” Rich Codons
Mar. Drugs 2017, 15(5), 125; doi:10.3390/md15050125
Received: 7 March 2017 / Revised: 11 April 2017 / Accepted: 20 April 2017 / Published: 27 April 2017
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Abstract
Although dinoflagellates are a potential source of pharmaceuticals and natural products, the mechanisms for regulating and producing these compounds are largely unknown because of extensive post-transcriptional control of gene expression. One well-documented mechanism for controlling gene expression during translation is codon bias, whereby
[...] Read more.
Although dinoflagellates are a potential source of pharmaceuticals and natural products, the mechanisms for regulating and producing these compounds are largely unknown because of extensive post-transcriptional control of gene expression. One well-documented mechanism for controlling gene expression during translation is codon bias, whereby specific codons slow or even terminate protein synthesis. Approximately 10,000 annotatable genes from fifteen “core” dinoflagellate transcriptomes along a range of overall guanine and cytosine (GC) content were used for codonW analysis to determine the relative synonymous codon usage (RSCU) and the GC content at each codon position. GC bias in the analyzed dataset and at the third codon position varied from 51% and 54% to 66% and 88%, respectively. Codons poor in GC were observed to be universally absent, but bias was most pronounced for codons ending in uracil followed by adenine (UA). GC bias at the third codon position was able to explain low abundance codons as well as the low effective number of codons. Thus, we propose that a bias towards codons rich in GC bases is a universal feature of core dinoflagellates, possibly relating to their unique chromosome structure, and not likely a major mechanism for controlling gene expression. Full article
(This article belongs to the Special Issue Advances and New Perspectives in Marine Biotechnology II 2016)
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Open AccessArticle Bioresponsive Materials for Drug Delivery Based on Carboxymethyl Chitosan/Poly(γ-Glutamic Acid) Composite Microparticles
Mar. Drugs 2017, 15(5), 127; doi:10.3390/md15050127
Received: 27 March 2017 / Revised: 14 April 2017 / Accepted: 17 April 2017 / Published: 28 April 2017
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Abstract
Carboxymethyl chitosan (CMCS) microparticles are a potential candidate for hemostatic wound dressing. However, its low swelling property limits its hemostatic performance. Poly(γ-glutamic acid) (PGA) is a natural polymer with excellent hydrophilicity. In the current study, a novel CMCS/PGA composite microparticles with a dual-network
[...] Read more.
Carboxymethyl chitosan (CMCS) microparticles are a potential candidate for hemostatic wound dressing. However, its low swelling property limits its hemostatic performance. Poly(γ-glutamic acid) (PGA) is a natural polymer with excellent hydrophilicity. In the current study, a novel CMCS/PGA composite microparticles with a dual-network structure was prepared by the emulsification/internal gelation method. The structure and thermal stability of the composite were determined by Fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRD), scanning electron microscope (SEM), X-ray photoelectron spectroscopy (XPS), and thermogravimetric analysis (TGA). The effects of preparation conditions on the swelling behavior of the composite were investigated. The results indicate that the swelling property of CMCS/PGA composite microparticles is pH sensitive. Levofloxacin (LFX) was immobilized in the composite microparticles as a model drug to evaluate the drug delivery performance of the composite. The release kinetics of LFX from the composite microparticles with different structures was determined. The results suggest that the CMCS/PGA composite microparticles are an excellent candidate carrier for drug delivery. Full article
(This article belongs to the Special Issue Marine Chitin)
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Open AccessArticle Thielavins W–Z7, New Antifouling Thielavins from the Marine-Derived Fungus Thielavia sp. UST030930-004
Mar. Drugs 2017, 15(5), 128; doi:10.3390/md15050128
Received: 7 April 2017 / Revised: 25 April 2017 / Accepted: 26 April 2017 / Published: 29 April 2017
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Abstract
Eleven new depsides—thielavins W–Z (14) and thielavins Z1–Z7 (511)—and also four known thielavins—A, H, J, and K (1215)—were isolated from the ethyl acetate extract of a marine-derived fungal
[...] Read more.
Eleven new depsides—thielavins W–Z (14) and thielavins Z1–Z7 (511)—and also four known thielavins—A, H, J, and K (1215)—were isolated from the ethyl acetate extract of a marine-derived fungal strain Thielavia sp UST030930-004. All of these compounds were evaluated for antifouling activity against cyprids of the barnacle Balanus (=Amphibalanus) amphitrite. The results showed that compounds 1–3 and 6–13 were active, with EC50 values ranging from 2.95 ± 0.59 to 69.19 ± 9.51 μM, respectively. The inhibitive effect of compounds 13 and 7 was reversible. This is the first description of the antifouling activity of thielavins against barnacle cyprids. Full article
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Open AccessArticle Chemistry and Selective Tumor Cell Growth Inhibitory Activity of Polyketides from the South China Sea Sponge Plakortis sp.
Mar. Drugs 2017, 15(5), 129; doi:10.3390/md15050129
Received: 1 March 2017 / Revised: 17 April 2017 / Accepted: 28 April 2017 / Published: 3 May 2017
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Abstract
Simplextone E (1), a new metabolite of polyketide origin, was isolated with eight known analogues (29) from the South China Sea sponge Plakortis sp. The relative configuration of the new compound was elucidated by a detailed analysis
[...] Read more.
Simplextone E (1), a new metabolite of polyketide origin, was isolated with eight known analogues (29) from the South China Sea sponge Plakortis sp. The relative configuration of the new compound was elucidated by a detailed analysis of the spectroscopic data and quantum mechanical calculation of NMR chemical shifts, aided by the newly reported DP4+ approach. Its absolute configuration was determined by the TDDFT/ECD calculation. Simplextone E (1) is proven to be one of the isomers of simplextone D. The absolute configuration at C-8 in alkyl chain of plakortone Q (2) was also assigned based on the NMR calculation. In the preliminary in vitro bioassay, compounds 6 and 7 showed a selective growth inhibitory activity against HCT-116 human colon cancer cells with IC50 values of 8.3 ± 2.4 and 8.4 ± 2.3 μM, corresponding to that of the positive control, adriamycin (IC50 4.1 μM). The two compounds also showed selective activities towards MCF-7 human breast cancer and K562 human erythroleukemia cells while compound 3 only displayed weak activity against K562 cells. Full article
(This article belongs to the Special Issue Marine Drugs as Antitumour Agents 2017)
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Open AccessArticle Undariopsis peterseniana Promotes Hair Growth by the Activation of Wnt/β-Catenin and ERK Pathways
Mar. Drugs 2017, 15(5), 130; doi:10.3390/md15050130
Received: 16 March 2017 / Revised: 27 April 2017 / Accepted: 2 May 2017 / Published: 30 May 2017
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Abstract
In this study, we investigated the effect and mechanism of Undariopsis peterseniana, an edible brown alga, on hair growth. The treatment of vibrissa follicles with U. peterseniana extract ex vivo for 21 days significantly increased the hair-fiber lengths. The U. peterseniana extract
[...] Read more.
In this study, we investigated the effect and mechanism of Undariopsis peterseniana, an edible brown alga, on hair growth. The treatment of vibrissa follicles with U. peterseniana extract ex vivo for 21 days significantly increased the hair-fiber lengths. The U. peterseniana extract also significantly accelerated anagen initiation in vivo. Moreover, we found that U. peterseniana extract was able to open the KATP channel, which may contribute to increased hair growth. The U. peterseniana extract decreased 5α-reductase activity and markedly increased the proliferation of dermal papilla cells, a central regulator of the hair cycle. The U. peterseniana extract increased the levels of cell cycle proteins, such as Cyclin D1, phospho(ser780)-pRB, Cyclin E, phospho-CDK2, and CDK2. The U. peterseniana extract also increased the phosphorylation of ERK and the levels of Wnt/β-catenin signaling proteins such as glycogen synthase kinase-3β (GSK-3β) and β-catenin. These results suggested that the U. peterseniana extract had the potential to influence hair growth by dermal papilla cells proliferation through the activation of the Wnt/β-catenin and ERK pathways. We isolated a principal of the U. peterseniana extract, which was subsequently identified as apo-9′-fucoxanthinone, a trichogenic compound. The results suggested that U. peterseniana extract may have a pivotal role in the treatment of alopecia. Full article
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Open AccessArticle Hydrolysates of Fish Skin Collagen: An Opportunity for Valorizing Fish Industry Byproducts
Mar. Drugs 2017, 15(5), 131; doi:10.3390/md15050131
Received: 21 March 2017 / Revised: 20 April 2017 / Accepted: 2 May 2017 / Published: 5 May 2017
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Abstract
During fish processing operations, such as skinning and filleting, the removal of collagen-containing materials can account for up to 30% of the total fish byproducts. Collagen is the main structural protein in skin, representing up to 70% of dry weight depending on the
[...] Read more.
During fish processing operations, such as skinning and filleting, the removal of collagen-containing materials can account for up to 30% of the total fish byproducts. Collagen is the main structural protein in skin, representing up to 70% of dry weight depending on the species, age and season. It has a wide range of applications including cosmetic, pharmaceutical, food industry, and medical. In the present work, collagen was obtained by pepsin extraction from the skin of two species of teleost and two species of chondrychtyes with yields varying between 14.16% and 61.17%. The storage conditions of the skins appear to influence these collagen extractions yields. Pepsin soluble collagen (PSC) was enzymatically hydrolyzed and the resultant hydrolysates were ultrafiltrated and characterized. Electrophoretic patterns showed the typical composition of type I collagen, with denaturation temperatures ranged between 23 °C and 33 °C. In terms of antioxidant capacity, results revealed significant intraspecific differences between hydrolysates, retentate, and permeate fractions when using β-Carotene and DPPH methods and also showed interspecies differences between those fractions when using DPPH and ABTS methods. Under controlled conditions, PSC hydrolysates from Prionace glauca, Scyliorhinus canicula, Xiphias gladius, and Thunnus albacares provide a valuable source of peptides with antioxidant capacities constituting a feasible way to efficiently upgrade fish skin biomass. Full article
(This article belongs to the Special Issue Marine Proteins and Peptides)
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Open AccessFeature PaperArticle Anti-Inflammatory Activity and Structure-Activity Relationships of Brominated Indoles from a Marine Mollusc
Mar. Drugs 2017, 15(5), 133; doi:10.3390/md15050133
Received: 14 March 2017 / Revised: 18 April 2017 / Accepted: 2 May 2017 / Published: 6 May 2017
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Abstract
Marine molluscs are rich in biologically active natural products that provide new potential sources of anti-inflammatory agents. Here we used bioassay guided fractionation of extracts from the muricid Dicathais orbita to identify brominated indoles with anti-inflammatory activity, based on the inhibition of nitric
[...] Read more.
Marine molluscs are rich in biologically active natural products that provide new potential sources of anti-inflammatory agents. Here we used bioassay guided fractionation of extracts from the muricid Dicathais orbita to identify brominated indoles with anti-inflammatory activity, based on the inhibition of nitric oxide (NO) and tumour necrosis factor α (TNFα) in lipopolysaccharide (LPS) stimulated RAW264.7 macrophages and prostaglandin E2 (PGE2) in calcium ionophore-stimulated 3T3 ccl-92 fibroblasts. Muricid brominated indoles were then compared to a range of synthetic indoles to determine structure-activity relationships. Both hypobranchial gland and egg extracts inhibited the production of NO significantly with IC50 of 30.8 and 40 μg/mL, respectively. The hypobranchial gland extract also inhibited the production of TNFα and PGE2 with IC50 of 43.03 µg/mL and 34.24 µg/mL, respectively. The purified mono-brominated indole and isatin compounds showed significant inhibitory activity against NO, TNFα, and PGE2, and were more active than dimer indoles and non-brominated isatin. The position of the bromine atom on the isatin benzene ring significantly affected the activity, with 5Br > 6Br > 7Br. The mode of action for the active hypobranchial gland extract, 6-bromoindole, and 6-bromoisatin was further tested by the assessment of the translocation of nuclear factor kappa B (NFκB) in LPS-stimulated RAW264.7 mouse macrophage. The extract (40 µg/mL) significantly inhibited the translocation of NFκB in the LPS-stimulated RAW264.7 macrophages by 48.2%, whereas 40 µg/mL of 6-bromoindole and 6-bromoistain caused a 60.7% and 63.7% reduction in NFκB, respectively. These results identify simple brominated indoles as useful anti-inflammatory drug leads and support the development of extracts from the Australian muricid D. orbita, as a new potential natural remedy for the treatment of inflammation. Full article
(This article belongs to the Special Issue Marine Compounds and Inflammation II, 2017)
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Open AccessArticle Assessment of Heparanase-Mediated Angiogenesis Using Microvascular Endothelial Cells: Identification of λ-Carrageenan Derivative as a Potent Anti Angiogenic Agent
Mar. Drugs 2017, 15(5), 134; doi:10.3390/md15050134
Received: 17 March 2017 / Revised: 21 April 2017 / Accepted: 27 April 2017 / Published: 9 May 2017
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Abstract
Heparanase is overexpressed by tumor cells and degrades the extracellular matrix proteoglycans through cleavage of heparan sulfates (HS), allowing pro-angiogenic factor release and thus playing a key role in tumor angiogenesis and metastasis. Here we propose new HS analogs as potent heparanase inhibitors:
[...] Read more.
Heparanase is overexpressed by tumor cells and degrades the extracellular matrix proteoglycans through cleavage of heparan sulfates (HS), allowing pro-angiogenic factor release and thus playing a key role in tumor angiogenesis and metastasis. Here we propose new HS analogs as potent heparanase inhibitors: Heparin as a positive control, Dextran Sulfate, λ-Carrageenan, and modified forms of them obtained by depolymerization associated to glycol splitting (RD-GS). After heparanase activity assessment, 11 kDa RD-GS-λ-Carrageenan emerged as the most effective heparanase inhibitor with an IC50 of 7.32 ng/mL compared to 10.7 ng/mL for the 16 kDa unfractionated heparin. The fractionated polysaccharides were then tested in a heparanase-rich medium-based in vitro model, mimicking tumor microenvironment, to determine their effect on microvascular endothelial cells (HSkMEC) angiogenesis. As a preliminary study, we identified that under hypoxic and nutrient poor conditions, MCF-7 cancer cells released much more mature heparanase in their supernatant than in normal conditions. Then a MatrigelTM assay using HSkMEC cultured under hypoxic conditions in the presence (or not) of this heparanase-rich supernatant was realized. Adding heparanase-rich media strongly enhanced angiogenic network formation with a production of twice more pseudo-vessels than with the control. When sulfated polysaccharides were tested in this angiogenesis assay, RD-GS-λ-Carrageenan was identified as a promising anti-angiogenic agent. Full article
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Open AccessArticle The Structure and Nephroprotective Activity of Oligo-Porphyran on Glycerol-Induced Acute Renal Failure in Rats
Mar. Drugs 2017, 15(5), 135; doi:10.3390/md15050135
Received: 1 February 2017 / Revised: 23 April 2017 / Accepted: 4 May 2017 / Published: 9 May 2017
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Abstract
Porphyran is a sulfate galactan in the cell wall of Porphyra. Its acid hydrolysis product, oligo-porphyran (OP), was prepared and the structure studied by electrospray ionization time-of-flight mass spectrometry (ESI-TOF-MS). This oligosaccharide was mainly composed of monosulfate-oligo-galactan, disufate-oligo-galactan, trisulfate-oligo-galactan, trisulfate oligo-methyl-galactan, and
[...] Read more.
Porphyran is a sulfate galactan in the cell wall of Porphyra. Its acid hydrolysis product, oligo-porphyran (OP), was prepared and the structure studied by electrospray ionization time-of-flight mass spectrometry (ESI-TOF-MS). This oligosaccharide was mainly composed of monosulfate-oligo-galactan, disufate-oligo-galactan, trisulfate-oligo-galactan, trisulfate oligo-methyl-galactan, and 3,6-anhydrogalactose with the degree of polymerization ranging from 1 to 8. The effects of OP were investigated in the glycerol-induced acute renal failure (ARF) model. Compared with the normal group, rats from the glycerol-induced group exhibited collecting duct and medullary ascending limb dilation and casts. The OP-treated group exerted a protective effect against glycerol-induced changes. The results showed that the administration of OP markedly decreased mortality in female ARF rats. For male ARF rats, all of which survived, OP significantly decreased the blood urea nitrogen and serum creatinine levels. Ion levels in plasma and urine were significantly changed in ARF rats, whereas OP treatment almost recovered ion levels back to normal. This study showed a noticeable renal morphologic and functional protection by OP in glycerol-induced ARF rats. Full article
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Open AccessFeature PaperArticle Transcriptomic Profiling of the Allorecognition Response to Grafting in the Demosponge Amphimedon queenslandica
Mar. Drugs 2017, 15(5), 136; doi:10.3390/md15050136
Received: 30 March 2017 / Revised: 3 May 2017 / Accepted: 5 May 2017 / Published: 11 May 2017
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Abstract
Sponges, despite their simple body plan, discriminate between self and nonself with remarkable specificity. Sponge grafting experiments simulate the effects of natural self or nonself contact under laboratory conditions. Here we take a transcriptomic approach to investigate the temporal response to self and
[...] Read more.
Sponges, despite their simple body plan, discriminate between self and nonself with remarkable specificity. Sponge grafting experiments simulate the effects of natural self or nonself contact under laboratory conditions. Here we take a transcriptomic approach to investigate the temporal response to self and nonself grafts in the marine demosponge Amphimedon queenslandica. Auto- and allografts were established, observed and sampled over a period of three days, over which time the grafts either rejected or accepted, depending on the identity of the paired individuals, in a replicable and predictable manner. Fourteen transcriptomes were generated that spanned the auto- and allograft responses. Self grafts fuse completely in under three days, and the process appears to be controlled by relatively few genes. In contrast, nonself grafting results in a complete lack of fusion after three days, and appears to involve a broad downregulation of normal biological processes, rather than the mounting of an intense defensive response. Full article
(This article belongs to the Special Issue Advances and New Perspectives in Marine Biotechnology II 2016)
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Open AccessArticle Three New Indole Diterpenoids from the Sea-Anemone-Derived Fungus Penicillium sp. AS-79
Mar. Drugs 2017, 15(5), 137; doi:10.3390/md15050137
Received: 8 February 2017 / Revised: 24 March 2017 / Accepted: 10 May 2017 / Published: 12 May 2017
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Abstract
Three new indolediterpenoids, namely, 22-hydroxylshearinine F (1), 6-hydroxylpaspalinine (2), and 7-O-acetylemindole SB (3), along with eight related known analogs (411), were isolated from the sea-anemone-derived fungus Penicillium sp. AS-79. The structures
[...] Read more.
Three new indolediterpenoids, namely, 22-hydroxylshearinine F (1), 6-hydroxylpaspalinine (2), and 7-O-acetylemindole SB (3), along with eight related known analogs (411), were isolated from the sea-anemone-derived fungus Penicillium sp. AS-79. The structures and relative configurations of these compounds were determined by a detailed interpretation of the spectroscopic data, and their absolute configurations were determined by ECD calculations (1 and 2) and single-crystal X-ray diffraction (3). Some of these compounds exhibited prominent activity against aquatic and human pathogenic microbes. Full article
(This article belongs to the Special Issue Bioactive Compounds from Marine Microbes II, 2017)
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Open AccessArticle Anti-Pigmentary Effect of (-)-4-Hydroxysattabacin from the Marine-Derived Bacterium Bacillus sp.
Mar. Drugs 2017, 15(5), 138; doi:10.3390/md15050138
Received: 10 January 2017 / Revised: 19 April 2017 / Accepted: 8 May 2017 / Published: 13 May 2017
Cited by 1 | PDF Full-text (3315 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Bioactivity-guided isolation of a crude extract from a culture broth of Bacillus sp. has led to the isolation of (-)-4-hydroxysattabacin (1). The inhibitory effect of (-)-4-hydroxysattabacin (1) was investigated on melanogenesis in the murine melanoma cell line, B16F10, and human melanoma cell line,
[...] Read more.
Bioactivity-guided isolation of a crude extract from a culture broth of Bacillus sp. has led to the isolation of (-)-4-hydroxysattabacin (1). The inhibitory effect of (-)-4-hydroxysattabacin (1) was investigated on melanogenesis in the murine melanoma cell line, B16F10, and human melanoma cell line, MNT-1, as well as a pigmented 3D-human skin model. (-)-4-Hydroxysattabacin treatment decreased melanin contents in a dose-dependent manner in α-melanocyte stimulating hormone (α-MSH)-stimulated B16F10 cells. Quantitative real time PCR (qRT–PCR) demonstrated that treatment with (-)-4-hydroxysattabacin down-regulated several melanogenic genes, including tyrosinase, tyrosinase-related protein 1 (TRP-1), and tyrosinase-related protein 2 (TRP-2) while their enzymatic activities were unaffected. The anti-melanogenic effects of (-)-4-hydroxysattabacin were further demonstrated in a pigmented 3D human epidermal skin model, MelanodermTM, and manifested as whitening and regression of melanocyte activation in the tissue. Full article
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Open AccessArticle A New Ergosterol Analog, a New Bis-Anthraquinone and Anti-Obesity Activity of Anthraquinones from the Marine Sponge-Associated Fungus Talaromyces stipitatus KUFA 0207
Mar. Drugs 2017, 15(5), 139; doi:10.3390/md15050139
Received: 6 April 2017 / Revised: 3 May 2017 / Accepted: 10 May 2017 / Published: 16 May 2017
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Abstract
A new ergosterol analog, talarosterone (1) and a new bis-anthraquinone derivative (3) were isolated, together with ten known compounds including palmitic acid, ergosta-4,6,8(14),22-tetraen-3-one, ergosterol-5,8-endoperoxide, cyathisterone (2), emodin (4a), questinol (4b), citreorosein (
[...] Read more.
A new ergosterol analog, talarosterone (1) and a new bis-anthraquinone derivative (3) were isolated, together with ten known compounds including palmitic acid, ergosta-4,6,8(14),22-tetraen-3-one, ergosterol-5,8-endoperoxide, cyathisterone (2), emodin (4a), questinol (4b), citreorosein (4c), fallacinol (4d), rheoemodin (4e) and secalonic acid A (5), from the ethyl acetate extract of the culture of the marine sponge-associated fungus Talaromyces stipitatus KUFA 0207. The structures of the new compounds were established based on extensive 1D and 2D spectral analysis, and in the case of talarosterone (1), the absolute configurations of its stereogenic carbons were determined by X-ray crystallographic analysis. The structure and stereochemistry of cyathisterone (2) was also confirmed by X-ray analysis. The anthraquinones 4ae and secalonic acid A (5) were tested for their anti-obesity activity using the zebrafish Nile red assay. Only citreorosein (4c) and questinol (4b) exhibited significant anti-obesity activity, while emodin (4a) and secalonic acid A (5) caused toxicity (death) for all exposed zebrafish larvae after 24 h. Full article
(This article belongs to the Special Issue Marine Products for Health and Beauty)
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Open AccessArticle Cereus sinensis Polysaccharide and Its Immunomodulatory Properties in Human Monocytic Cells
Mar. Drugs 2017, 15(5), 140; doi:10.3390/md15050140
Received: 16 March 2017 / Revised: 24 April 2017 / Accepted: 4 May 2017 / Published: 18 May 2017
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Abstract
In this study, the extraction conditions of the crude polysaccharide from Cereus sinensis were optimized by response surface methodology. The optimum extraction conditions were: a ratio of raw material to water volume of 1:80 (g/mL); an extraction temperature of 72 °C; and an
[...] Read more.
In this study, the extraction conditions of the crude polysaccharide from Cereus sinensis were optimized by response surface methodology. The optimum extraction conditions were: a ratio of raw material to water volume of 1:80 (g/mL); an extraction temperature of 72 °C; and an extraction time of 3 h. Then, a purified polysaccharide named Cereus sinensis polysaccharide-1 (CSP-1) was obtained from the crude polysaccharide by the Diethylaminoethyl cellulose-52 (DEAE-52) cellulose chromatography column and Sephadex G-100 column. The molecular weight and monosaccharide composition of CSP-1 was determined through Gel Permeation Chromatography (GPC) and Gas Chromatography–Mass Spectrometer (GS–MS), respectively. The results showed that CSP-1 with an average molecular weight of 56,335 Da was composed of l-(−)-Fucose, d-(+)-Mannose, d-Glucose and mainly possessed 1→2, 1→2, 6, 1→4, and 1→4, 6 of glycosyl linkages. The immunomodulatory activities of CSP-1 were also evaluated using lipopolysaccharide (LPS)-induced human monocytic (THP-1) cells. The results demonstrated that CSP-1 dose-dependently protected against LPS-induced toxicity, and CSP-1 significantly inhibited the Toll-like receptor 4 (TLR-4) mRNA, myeloid differentiation factor 88 (MyD88) mRNA and tumour necrosis factor receptor-associated factor-6 (TRAF-6) mRNA expression of the LPS-induced THP-1 cells, as well as suppressing reactive oxygen species (ROS) generation. Full article
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Open AccessArticle Preparation and Characterization of Chitosan Obtained from Shells of Shrimp (Litopenaeus vannamei Boone)
Mar. Drugs 2017, 15(5), 141; doi:10.3390/md15050141
Received: 5 April 2017 / Revised: 3 May 2017 / Accepted: 8 May 2017 / Published: 15 May 2017
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Abstract
The main source of commercial chitosan is the extensive deacetylation of its parent polymer chitin. It is present in green algae, the cell walls or fungi and in the exoskeleton of crustaceans. A novel procedure for preparing chitosan from shrimp shells was developed.
[...] Read more.
The main source of commercial chitosan is the extensive deacetylation of its parent polymer chitin. It is present in green algae, the cell walls or fungi and in the exoskeleton of crustaceans. A novel procedure for preparing chitosan from shrimp shells was developed. The procedure involves two 10-minutes bleaching steps with ethanol after the usual demineralization and deproteinization processes. Before deacetylation, chitin was immersed in 12.5 M NaOH, cooled down and kept frozen for 24 h. The obtained chitosan was characterized using scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), UV, X-ray diffraction (XRD) and viscosimetry. Samples of white chitosan with acetylation degrees below 9 % were obtained, as determined by FTIR and UV-first derivative spectroscopy. The change in the morphology of samples was followed by SEM. The ash content of chitosan samples were all below 0.063 % . Chitosan was soluble in 1 % acetic acid with insoluble contents of 0.62 % or less. XRD patterns exhibited the characteristic peaks of chitosan centered at 10 and 20 degrees in 2 θ . The molecular weight of chitosan was between 2.3 and 2.8 × 10 5 g/mol. It is concluded that the procedure developed in the present work allowed obtaining chitosans with physical and chemical properties suitable for pharmaceutical applications. Full article
(This article belongs to the Special Issue Marine Chitin)
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Open AccessArticle Morphogenetically-Active Barrier Membrane for Guided Bone Regeneration, Based on Amorphous Polyphosphate
Mar. Drugs 2017, 15(5), 142; doi:10.3390/md15050142
Received: 10 April 2017 / Revised: 4 May 2017 / Accepted: 8 May 2017 / Published: 17 May 2017
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Abstract
We describe a novel regeneratively-active barrier membrane which consists of a durable electrospun poly(ε-caprolactone) (PCL) net covered with a morphogenetically-active biohybrid material composed of collagen and inorganic polyphosphate (polyP). The patch-like fibrous collagen structures are decorated with small amorphous polyP nanoparticles (50 nm)
[...] Read more.
We describe a novel regeneratively-active barrier membrane which consists of a durable electrospun poly(ε-caprolactone) (PCL) net covered with a morphogenetically-active biohybrid material composed of collagen and inorganic polyphosphate (polyP). The patch-like fibrous collagen structures are decorated with small amorphous polyP nanoparticles (50 nm) formed by precipitation of this energy-rich and enzyme-degradable (alkaline phosphatase) polymer in the presence of calcium ions. The fabricated PCL-polyP/collagen hybrid mats are characterized by advantageous biomechanical properties, such as enhanced flexibility and stretchability with almost unaltered tensile strength of the PCL net. The polyP/collagen material promotes the attachment and increases the viability/metabolic activity of human mesenchymal stem cells compared to cells grown on non-coated mats. The gene expression studies revealed that cells, growing onto polyP/collagen coated mats show a significantly (two-fold) higher upregulation of the steady-state-expression of the angiopoietin-2 gene used as an early marker for wound healing than cells cultivated onto non-coated mats. Based on our results we propose that amorphous polyP, stabilized onto a collagen matrix, might be a promising component of functionally-active barrier membranes for guided tissue regeneration in medicine and dentistry. Full article
(This article belongs to the Special Issue Advances and New Perspectives in Marine Biotechnology II 2016)
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Open AccessArticle Lobophorin K, a New Natural Product with Cytotoxic Activity Produced by Streptomyces sp. M-207 Associated with the Deep-Sea Coral Lophelia pertusa
Mar. Drugs 2017, 15(5), 144; doi:10.3390/md15050144
Received: 24 February 2017 / Revised: 11 May 2017 / Accepted: 15 May 2017 / Published: 19 May 2017
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Abstract
The present article describes the isolation of a new natural product of the lobophorin family, designated as lobophorin K (1), from cultures of the marine actinobacteria Streptomyces sp. M-207, previously isolated from the cold-water coral Lophelia pertusa collected at 1800 m
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The present article describes the isolation of a new natural product of the lobophorin family, designated as lobophorin K (1), from cultures of the marine actinobacteria Streptomyces sp. M-207, previously isolated from the cold-water coral Lophelia pertusa collected at 1800 m depth during an expedition to the submarine Avilés Canyon. Its structure was determined using a combination of spectroscopic techniques, mainly ESI-TOF MS and 1D and 2D NMR. This new natural product displayed cytotoxic activity against two human tumor cell lines, such as pancreatic carcinoma (MiaPaca-2) and breast adenocarcinoma (MCF-7). Lobophorin K also displayed moderate and selective antibiotic activity against pathogenic Gram-positive bacteria such as Staphylococcus aureus. Full article
(This article belongs to the Special Issue Natural Products from Marine Actinomycetes)
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Open AccessArticle The Venom Repertoire of Conus gloriamaris (Chemnitz, 1777), the Glory of the Sea
Mar. Drugs 2017, 15(5), 145; doi:10.3390/md15050145
Received: 21 April 2017 / Revised: 15 May 2017 / Accepted: 17 May 2017 / Published: 20 May 2017
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Abstract
The marine cone snail Conus gloriamaris is an iconic species. For over two centuries, its shell was one of the most prized and valuable natural history objects in the world. Today, cone snails have attracted attention for their remarkable venom components. Many conotoxins
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The marine cone snail Conus gloriamaris is an iconic species. For over two centuries, its shell was one of the most prized and valuable natural history objects in the world. Today, cone snails have attracted attention for their remarkable venom components. Many conotoxins are proving valuable as research tools, drug leads, and drugs. In this article, we present the venom gland transcriptome of C. gloriamaris, revealing this species’ conotoxin repertoire. More than 100 conotoxin sequences were identified, representing a valuable resource for future drug discovery efforts. Full article
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Review

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Open AccessReview A Review Study on Macrolides Isolated from Cyanobacteria
Mar. Drugs 2017, 15(5), 126; doi:10.3390/md15050126
Received: 27 January 2017 / Revised: 21 April 2017 / Accepted: 24 April 2017 / Published: 26 April 2017
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Abstract
Cyanobacteria are rich sources of structurally-diverse molecules with promising pharmacological activities. Marine cyanobacteria have been proven to be true producers of some significant bioactive metabolites from marine invertebrates. Macrolides are a class of bioactive compounds isolated from marine organisms, including marine microorganisms in
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Cyanobacteria are rich sources of structurally-diverse molecules with promising pharmacological activities. Marine cyanobacteria have been proven to be true producers of some significant bioactive metabolites from marine invertebrates. Macrolides are a class of bioactive compounds isolated from marine organisms, including marine microorganisms in particular. The structural characteristics of macrolides from cyanobacteria mainly manifest in the diversity of carbon skeletons, complexes of chlorinated thiazole-containing molecules and complex spatial configuration. In the present work, we systematically reviewed the structures and pharmacological activities of macrolides from cyanobacteria. Our data would help establish an effective support system for the discovery and development of cyanobacterium-derived macrolides. Full article
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Open AccessReview New Peptides Isolated from Marine Cyanobacteria, an Overview over the Past Decade
Mar. Drugs 2017, 15(5), 132; doi:10.3390/md15050132
Received: 15 March 2017 / Revised: 28 April 2017 / Accepted: 2 May 2017 / Published: 5 May 2017
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Abstract
Marine cyanobacteria are significant sources of structurally diverse marine natural products with broad biological activities. In the past 10 years, excellent progress has been made in the discovery of marine cyanobacteria-derived peptides with diverse chemical structures. Most of these peptides exhibit strong pharmacological
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Marine cyanobacteria are significant sources of structurally diverse marine natural products with broad biological activities. In the past 10 years, excellent progress has been made in the discovery of marine cyanobacteria-derived peptides with diverse chemical structures. Most of these peptides exhibit strong pharmacological activities, such as neurotoxicity and cytotoxicity. In the present review, we summarized peptides isolated from marine cyanobacteria since 2007. Full article
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Open AccessFeature PaperReview Marine Fish Proteins and Peptides for Cosmeceuticals: A Review
Mar. Drugs 2017, 15(5), 143; doi:10.3390/md15050143
Received: 28 February 2017 / Revised: 5 May 2017 / Accepted: 11 May 2017 / Published: 18 May 2017
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Abstract
Marine fish provide a rich source of bioactive compounds such as proteins and peptides. The bioactive proteins and peptides derived from marine fish have gained enormous interest in nutraceutical, pharmaceutical, and cosmeceutical industries due to their broad spectrum of bioactivities, including antioxidant, antimicrobial,
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Marine fish provide a rich source of bioactive compounds such as proteins and peptides. The bioactive proteins and peptides derived from marine fish have gained enormous interest in nutraceutical, pharmaceutical, and cosmeceutical industries due to their broad spectrum of bioactivities, including antioxidant, antimicrobial, and anti-aging activities. Recently, the development of cosmeceuticals using marine fish-derived proteins and peptides obtained from chemical or enzymatical hydrolysis of fish processing by-products has increased rapidly owing to their activities in antioxidation and tissue regeneration. Marine fish-derived collagen has been utilized for the development of cosmeceutical products due to its abilities in skin repair and tissue regeneration. Marine fish-derived peptides have also been utilized for various cosmeceutical applications due to their antioxidant, antimicrobial, and matrix metalloproteinase inhibitory activities. In addition, marine fish-derived proteins and hydrolysates demonstrated efficient anti-photoaging activity. The present review highlights and presents an overview of the current status of the isolation and applications of marine fish-derived proteins and peptides. This review also demonstrates that marine fish-derived proteins and peptides have high potential for biocompatible and effective cosmeceuticals. Full article
(This article belongs to the Special Issue Marine Proteins and Peptides)
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