Marine Drugs

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Open AccessReview

A Review on the Valorization of Macroalgal Wastes for Biomethane Production

by Yann Nicolas Barbot, Hashem Al-Ghaili and Roland Benz

Mar. Drugs 2016, 14(6), 120; https://doi.org/10.3390/md14060120 - 21 Jun 2016

Cited by 109 | Viewed by 12860

The increased use of terrestrial crops for biofuel production and the associated environmental, social and ethical issues have led to a search for alternative biomass materials. Terrestrial crops offer excellent biogas recovery, but compete directly with food production, requiring farmland, fresh water and [...] Read more.

The increased use of terrestrial crops for biofuel production and the associated environmental, social and ethical issues have led to a search for alternative biomass materials. Terrestrial crops offer excellent biogas recovery, but compete directly with food production, requiring farmland, fresh water and fertilizers. Using marine macroalgae for the production of biogas circumvents these problems. Their potential lies in their chemical composition, their global abundance and knowledge of their growth requirements and occurrence patterns. Such a biomass industry should focus on the use of residual and waste biomass to avoid competition with the biomass requirements of the seaweed food industry, which has occurred in the case of terrestrial biomass. Overabundant seaweeds represent unutilized biomass in shallow water, beach and coastal areas. These eutrophication processes damage marine ecosystems and impair local tourism; this biomass could serve as biogas feedstock material. Residues from biomass processing in the seaweed industry are also of interest. This is a rapidly growing industry with algae now used in the comestible, pharmaceutical and cosmetic sectors. The simultaneous production of combustible biomethane and disposal of undesirable biomass in a synergistic waste management system is a concept with environmental and resource-conserving advantages. Full article

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Open AccessArticle

Immunomodulatory Effects of the Mycosporine-Like Amino Acids Shinorine and Porphyra-334

by Kathrin Becker, Anja Hartmann, Markus Ganzera, Dietmar Fuchs and Johanna M. Gostner

Mar. Drugs 2016, 14(6), 119; https://doi.org/10.3390/md14060119 - 21 Jun 2016

Cited by 48 | Viewed by 8286

Abstract

Mycosporine-like amino acids (MAAs) are secondary metabolites, produced by a large variety of microorganisms including algae, cyanobacteria, lichen and fungi. MAAs act as UV-absorbers and photo-protectants. MAAs are suggested to exert pharmaceutical relevant bioactivities in the human system. We particularly focused on their [...] Read more.

Mycosporine-like amino acids (MAAs) are secondary metabolites, produced by a large variety of microorganisms including algae, cyanobacteria, lichen and fungi. MAAs act as UV-absorbers and photo-protectants. MAAs are suggested to exert pharmaceutical relevant bioactivities in the human system. We particularly focused on their effect on defence and regulatory pathways that are active in inflamed environments. The MAAs shinorine and porphyra-334 were isolated and purified from the red algae Porphyra sp. using chromatographic methods. The effect of MAAs on central signaling cascades, such as transcription factor nuclear factor kappa b (NF-κB) activation, as well as tryptophan metabolism, was investigated in human myelomonocytic THP-1 and THP-1-Blue cells. Cells were exposed to the MAAs in the presence or absence of lipopolysaccharide (LPS). NF-κB activity and the activity of tryptophan degrading enzyme indoleamine 2,3-dioxygenase (IDO-1) were used as readout. Compounds were tested in the concentration range from 12.5 to 200 µg/mL. Both MAAs were able to induce NF-κB activity in unstimulated THP-1-Blue cells, whereby the increase was dose-dependent and more pronounced with shinorine treatment. While shinorine also slightly superinduced NF-κB in LPS-stimulated cells, porphyra-334 reduced NF-κB activity in this inflammatory background. Modulation of tryptophan metabolism was moderate, suppressive in stimulated cells with the lower treatment concentration of both MAAs and with the unstimulated cells upon porphyra-334 treatment. Inflammatory pathways are affected by MAAs, but despite the structural similarity, diverse effects were observed. Full article

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Open AccessArticle

Synthesis of Pelorol and Its Analogs and Their Inhibitory Effects on Phosphatidylinositol 3-Kinase

by Yongjie Luo, Huixuan Chen, Jiang Weng and Gui Lu

Mar. Drugs 2016, 14(6), 118; https://doi.org/10.3390/md14060118 - 21 Jun 2016

Cited by 8 | Viewed by 5598

Abstract

There are numerous biologically active substances with novel structures and unique physiological functions in marine organisms. These substances are important sources of new lead compounds. Pelorol is a natural product isolated from marine organisms that possesses a novel structure with high bioactivity. In [...] Read more.

There are numerous biologically active substances with novel structures and unique physiological functions in marine organisms. These substances are important sources of new lead compounds. Pelorol is a natural product isolated from marine organisms that possesses a novel structure with high bioactivity. In this paper, the synthesis of pelorol has been completed, and the synthesis of some intermediates has been optimized and scaled up. Five pelorol analogs have also been prepared. Preliminary biological activity testing demonstrated that compounds 5 and 6 might be potential lead compounds for cancer therapy. Full article

(This article belongs to the Special Issue Synthesis of Antitumor Marine Alkaloids and Related Analogues)

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762 KiB

Open AccessArticle

Phallusiasterol C, A New Disulfated Steroid from the Mediterranean Tunicate Phallusia fumigata

by Concetta Imperatore, Maria Senese, Anna Aiello, Paolo Luciano, Stefano Fiorucci, Claudio D’Amore, Adriana Carino and Marialuisa Menna

Mar. Drugs 2016, 14(6), 117; https://doi.org/10.3390/md14060117 - 18 Jun 2016

Cited by 8 | Viewed by 5117

Abstract

A new sulfated sterol, phallusiasterol C (1), has been isolated from the Mediterranean ascidian Phallusia fumigata and its structure has been determined on the basis of extensive spectroscopic (mainly 2D NMR) analysis. The possible role in regulating the pregnane X receptor [...] Read more.

A new sulfated sterol, phallusiasterol C (1), has been isolated from the Mediterranean ascidian Phallusia fumigata and its structure has been determined on the basis of extensive spectroscopic (mainly 2D NMR) analysis. The possible role in regulating the pregnane X receptor (PXR) activity of phallusiasterol C has been investigated; although the new sterol resulted inactive, this study adds more items to the knowledge of the structure-PXR regulating activity relationships in the case of sulfated steroids. Full article

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Open AccessArticle

Synthesis and Anti-Influenza A Virus Activity of 6′-amino-6′-deoxy-glucoglycerolipids Analogs

by Li Ren, Jun Zhang, Haizhen Ma, Linlin Sun, Xiaoshuang Zhang, Guangli Yu, Huashi Guan, Wei Wang and Chunxia Li

Mar. Drugs 2016, 14(6), 116; https://doi.org/10.3390/md14060116 - 18 Jun 2016

Cited by 6 | Viewed by 5952

Abstract

A series of aminoglucoglycerolipids derivatives had been synthesized, including 6′-acylamido-glucoglycerolipids 1a–1f and corresponding 2′-acylamido-glucoglycerolipids 2a–2c bearing different fatty acids, glucosyl diglycerides 3a–3e bearing different functional groups at C-6′ and ether-linked glucoglycerolipids 4a–4c with double-tailed alkyl [...] Read more.

A series of aminoglucoglycerolipids derivatives had been synthesized, including 6′-acylamido-glucoglycerolipids 1a–1f and corresponding 2′-acylamido-glucoglycerolipids 2a–2c bearing different fatty acids, glucosyl diglycerides 3a–3e bearing different functional groups at C-6′ and ether-linked glucoglycerolipids 4a–4c with double-tailed alkyl alcohol. The anti-influenza A virus (IAV) activity was evaluated by the cytopathic effects (CPE) inhibition assay. The results indicated that the integral structure of the aminoglycoglycerolipid was essential for the inhibition of IAV in MDCK cells. Furthermore, oral administration of compound 1d was able to significantly improve survival and decrease pulmonary viral titers in IAV-infected mice, which suggested that compound 1d merited further investigation as a novel anti-IAV candidate in the future. Full article

(This article belongs to the Special Issue Drug Design Based on Marine Natural Product Scaffolds)

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Open AccessArticle

Pharmacokinetics in Mouse and Comparative Effects of Frondosides in Pancreatic Cancer

by Jasem Al Shemaili, Khatija A. Parekh, Robert A. Newman, Björn Hellman, Carl Woodward, Abdu Adem, Peter Collin and Thomas E. Adrian

Mar. Drugs 2016, 14(6), 115; https://doi.org/10.3390/md14060115 - 17 Jun 2016

Cited by 17 | Viewed by 6649

Abstract

The frondosides are triterpenoid glycosides from the Atlantic sea cucumber Cucumaria frondosa. Frondoside A inhibits growth, invasion, metastases and angiogenesis and induces apoptosis in diverse cancer types, including pancreatic cancer. We compared the growth inhibitory effects of three frondosides and their aglycone [...] Read more.

The frondosides are triterpenoid glycosides from the Atlantic sea cucumber Cucumaria frondosa. Frondoside A inhibits growth, invasion, metastases and angiogenesis and induces apoptosis in diverse cancer types, including pancreatic cancer. We compared the growth inhibitory effects of three frondosides and their aglycone and related this to the pharmocokinetics and route of administration. Frondoside A potently inhibited growth of pancreatic cancer cells with an EC₅₀ of ~1 µM. Frondoside B was less potent (EC₅₀ ~2.5 µM). Frondoside C and the aglycone had no effect. At 100 µg/kg, frondoside A administered to CD₂F₁ mice as an i.v. bolus, the Cp_max was 129 nM, Cl_tb was 6.35 mL/min/m², and half-life was 510 min. With i.p. administration the Cp_max was 18.3 nM, Cl_tb was 127 mL/min/m² and half-life was 840 min. Oral dosing was ineffective. Frondoside A (100 µg/kg/day i.p.) markedly inhibited growth cancer xenografts in nude mice. The same dose delivered by oral gavage had no effect. No evidence of acute toxicity was seen with frondoside A. Frondoside A is more potent inhibitor of cancer growth than other frondosides. The glycoside component is essential for bioactivity. Frondoside A is only effective when administered systemically. Based on the current and previous studies, frondoside A appears safe and may be valuable in the treatment of cancer. Full article

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Open AccessArticle

Absorption and Transport of Sea Cucumber Saponins from Apostichopus japonicus

by Shuai Li, Yuanhong Wang, Tingfu Jiang, Han Wang, Shuang Yang and Zhihua Lv

Mar. Drugs 2016, 14(6), 114; https://doi.org/10.3390/md14060114 - 17 Jun 2016

Cited by 15 | Viewed by 6724

Abstract

The present study is focused on the intestinal absorption of sea cucumber saponins. We determined the pharmacokinetic characteristics and bioavailability of Echinoside A and Holotoxin A₁; the findings indicated that the bioavailability of Holotoxin A₁ was lower than Echinoside A. [...] Read more.

The present study is focused on the intestinal absorption of sea cucumber saponins. We determined the pharmacokinetic characteristics and bioavailability of Echinoside A and Holotoxin A₁; the findings indicated that the bioavailability of Holotoxin A₁ was lower than Echinoside A. We inferred that the differences in chemical structure between compounds was a factor that explained their different characteristics of transport across the intestine. In order to confirm the absorption characteristics of Echinoside A and Holotoxin A₁, we examined their transport across Caco-2 cell monolayer and effective permeability by single-pass intestinal perfusion. The results of Caco-2 cell model indicate that Echinoside A is transported by passive diffusion, and not influenced by the exocytosis of P-glycoprotein (P-gp, expressed in the apical side of Caco-2 monolayers as the classic inhibitor). The intestinal perfusion also demonstrated well the absorption of Echinoside A and poor absorption of Holotoxin A₁, which matched up with the result of the Caco-2 cell model. The results demonstrated our conjecture and provides fundamental information on the relationship between the chemical structure of these sea cucumber saponins and their absorption characteristics, and we believe that our findings build a foundation for the further metabolism study of sea cucumber saponins and contribute to the further clinical research of saponins. Full article

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

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Open AccessReview

Nutraceuticals and Bioactive Components from Fish for Dyslipidemia and Cardiovascular Risk Reduction

by Giulia Chiesa, Marco Busnelli, Stefano Manzini and Cinzia Parolini

Mar. Drugs 2016, 14(6), 113; https://doi.org/10.3390/md14060113 - 08 Jun 2016

Cited by 34 | Viewed by 10735

Abstract

Cardiovascular disease remains the most common health problem in developed countries, and residual risk after implementing all current therapies is still high. Permanent changes in lifestyle may be hard to achieve and people may not always be motivated enough to make the recommended [...] Read more.

Cardiovascular disease remains the most common health problem in developed countries, and residual risk after implementing all current therapies is still high. Permanent changes in lifestyle may be hard to achieve and people may not always be motivated enough to make the recommended modifications. Emerging research has explored the application of natural food-based strategies in disease management. In recent years, much focus has been placed on the beneficial effects of fish consumption. Many of the positive effects of fish consumption on dyslipidemia and heart diseases have been attributed to n-3 polyunsaturated fatty acids (n-3 PUFAs, i.e., EPA and DHA); however, fish is also an excellent source of protein and, recently, fish protein hydrolysates containing bioactive peptides have shown promising activities for the prevention/management of cardiovascular disease and associated health complications. The present review will focus on n-3 PUFAs and bioactive peptides effects on cardiovascular disease risk factors. Moreover, since considerable controversy exists regarding the association between n-3 PUFAs and major cardiovascular endpoints, we have also reviewed the main clinical trials supporting or not this association. Full article

(This article belongs to the Special Issue Marine Natural Products that Target Metabolic Disorders)

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2896 KiB

Open AccessCommunication

Synthesis of Phthalimide Derivatives as Potential PPAR-γ Ligands

by So Hyeon Eom, Sen Liu, Mingzhi Su, Tae Hwan Noh, Jongki Hong, Nam Deuk Kim, Hae Young Chung, Min Hye Yang and Jee H. Jung

Mar. Drugs 2016, 14(6), 112; https://doi.org/10.3390/md14060112 - 08 Jun 2016

Cited by 13 | Viewed by 6679

Abstract

Paecilocin A, a phthalide derivative isolated from the jellyfish-derived fungus Paecilomyces variotii, activates PPAR-γ (Peroxisome proliferator-activated receptor gamma) in rat liver Ac2F cells. Based on a SAR (Structure-activity relationships) study and in silico analysis of paecilocin A-mimetic derivatives, additional N-substituted phthalimide [...] Read more.

Paecilocin A, a phthalide derivative isolated from the jellyfish-derived fungus Paecilomyces variotii, activates PPAR-γ (Peroxisome proliferator-activated receptor gamma) in rat liver Ac2F cells. Based on a SAR (Structure-activity relationships) study and in silico analysis of paecilocin A-mimetic derivatives, additional N-substituted phthalimide derivatives were synthesized and evaluated for PPAR-γ agonistic activity in both murine liver Ac2F cells and in human liver HepG2 cells by luciferase assay, and for adipogenic activity in 3T3-L1 cells. Docking simulation indicated PD6 was likely to bind most strongly to the ligand binding domain of PPAR-γ by establishing crucial H-bonds with key amino acid residues. However, in in vitro assays, PD1 and PD2 consistently displayed significant PPAR-γ activation in Ac2F and HepG2 cells, and adipogenic activity in 3T3-L1 preadipocytes. Full article

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Open AccessArticle

Enzymatic Hydrolysis of Alginate to Produce Oligosaccharides by a New Purified Endo-Type Alginate Lyase

by Benwei Zhu, Meijuan Chen, Heng Yin, Yuguang Du and Limin Ning

Mar. Drugs 2016, 14(6), 108; https://doi.org/10.3390/md14060108 - 06 Jun 2016

Cited by 55 | Viewed by 7703

Abstract

Enzymatic hydrolysis of sodium alginate to produce alginate oligosaccharides has drawn increasing attention due to its advantages of containing a wild reaction condition, excellent gel properties and specific products easy for purification. However, the efficient commercial enzyme tools are rarely available. A new [...] Read more.

Enzymatic hydrolysis of sodium alginate to produce alginate oligosaccharides has drawn increasing attention due to its advantages of containing a wild reaction condition, excellent gel properties and specific products easy for purification. However, the efficient commercial enzyme tools are rarely available. A new alginate lyase with high activity (24,038 U/mg) has been purified from a newly isolated marine strain, Cellulophaga sp. NJ-1. The enzyme was most active at 50 °C and pH 8.0 and maintained stability at a broad pH range (6.0–10.0) and temperature below 40 °C. It had broad substrate specificity toward sodium alginate, heteropolymeric MG blocks (polyMG), homopolymeric M blocks (polyM) and homopolymeric G blocks (polyG), and possessed higher affinity toward polyG (15.63 mM) as well as polyMG (23.90 mM) than polyM (53.61 mM) and sodium alginate (27.21 mM). The TLC and MS spectroscopy analysis of degradation products suggested that it completely hydrolyzed sodium alginate into oligosaccharides of low degrees of polymerization (DPs). The excellent properties would make it a promising tool for full use of sodium alginate to produce oligosaccharides. Full article

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Open AccessArticle

Cembranoids from a Chinese Collection of the Soft Coral Lobophytum crassum

by Min Zhao, Shimiao Cheng, Weiping Yuan, Yiyuan Xi, Xiubao Li, Jianyong Dong, Kexin Huang, Kirk R. Gustafson and Pengcheng Yan

Mar. Drugs 2016, 14(6), 111; https://doi.org/10.3390/md14060111 - 03 Jun 2016

Cited by 21 | Viewed by 6059

Abstract

Ten new cembrane-based diterpenes, locrassumins A–G (1–7), (–)-laevigatol B (8), (–)-isosarcophine (9), and (–)-7R,8S-dihydroxydeepoxysarcophytoxide (10), were isolated from a South China Sea collection of the soft coral Lobophytum crassum [...] Read more.

Ten new cembrane-based diterpenes, locrassumins A–G (1–7), (–)-laevigatol B (8), (–)-isosarcophine (9), and (–)-7R,8S-dihydroxydeepoxysarcophytoxide (10), were isolated from a South China Sea collection of the soft coral Lobophytum crassum, together with eight known analogues (11–18). The structures of the new compounds were determined by extensive spectroscopic analysis and by comparison with previously reported data. Locrassumin C (3) possesses an unprecedented tetradecahydrobenzo[3,4]cyclobuta[1,2][8]annulene ring system. Compounds 1, 7, 12, 13, and 17 exhibited moderate inhibition against lipopolysaccharide (LPS)-induced nitric oxide (NO) production with IC₅₀ values of 8–24 μM. Full article

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

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Open AccessArticle

Identification of Angiotensin I-Converting Enzyme Inhibitory Peptides Derived from Enzymatic Hydrolysates of Razor Clam Sinonovacula constricta

by Yun Li, Faizan A. Sadiq, Li Fu, Hui Zhu, Minghua Zhong and Muhammad Sohail

Mar. Drugs 2016, 14(6), 110; https://doi.org/10.3390/md14060110 - 03 Jun 2016

Cited by 27 | Viewed by 6779

Abstract

Angiotensin I-converting enzyme (ACE) inhibitory activity of razor clam hydrolysates produced using five proteases, namely, pepsin, trypsin, alcalase, flavourzyme and proteases from Actinomucor elegans T3 was investigated. Flavourzyme hydrolysate showed the highest level of degree of hydrolysis (DH) (45.87%) followed by A. elegans [...] Read more.

Angiotensin I-converting enzyme (ACE) inhibitory activity of razor clam hydrolysates produced using five proteases, namely, pepsin, trypsin, alcalase, flavourzyme and proteases from Actinomucor elegans T3 was investigated. Flavourzyme hydrolysate showed the highest level of degree of hydrolysis (DH) (45.87%) followed by A. elegans T3 proteases hydrolysate (37.84%) and alcalase (30.55%). The A. elegans T3 proteases was observed to be more effective in generating small peptides with ACE-inhibitory activity. The 3 kDa membrane permeate of A. elegans T3 proteases hydrolysate showed the highest ACE-inhibitory activity with an IC₅₀ of 0.79 mg/mL. After chromatographic separation by Sephadex G-15 gel filtration and reverse phase-high performance liquid chromatography, the potent fraction was subjected to MALDI/TOF-TOF MS/MS for identification. A novel ACE-inhibitory peptide (VQY) was identified exhibiting an IC₅₀ of 9.8 μM. The inhibitory kinetics investigation by Lineweaver-Burk plots demonstrated that the peptide acts as a competitive ACE inhibitor. The razor clam hydrolysate obtained by A. elegans T3 proteases could serve as a source of functional peptides with ACE-inhibitory activity for physiological benefits. Full article

(This article belongs to the Special Issue Marine Proteins and Peptides)

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Open AccessArticle

Coral Carbonic Anhydrases: Regulation by Ocean Acidification

by Didier Zoccola, Alessio Innocenti, Anthony Bertucci, Eric Tambutté, Claudiu T. Supuran and Sylvie Tambutté

Mar. Drugs 2016, 14(6), 109; https://doi.org/10.3390/md14060109 - 03 Jun 2016

Cited by 36 | Viewed by 9377

Abstract

Global change is a major threat to the oceans, as it implies temperature increase and acidification. Ocean acidification (OA) involving decreasing pH and changes in seawater carbonate chemistry challenges the capacity of corals to form their skeletons. Despite the large number of studies [...] Read more.

Global change is a major threat to the oceans, as it implies temperature increase and acidification. Ocean acidification (OA) involving decreasing pH and changes in seawater carbonate chemistry challenges the capacity of corals to form their skeletons. Despite the large number of studies that have investigated how rates of calcification respond to ocean acidification scenarios, comparatively few studies tackle how ocean acidification impacts the physiological mechanisms that drive calcification itself. The aim of our paper was to determine how the carbonic anhydrases, which play a major role in calcification, are potentially regulated by ocean acidification. For this we measured the effect of pH on enzyme activity of two carbonic anhydrase isoforms that have been previously characterized in the scleractinian coral Stylophora pistillata. In addition we looked at gene expression of these enzymes in vivo. For both isoforms, our results show (1) a change in gene expression under OA (2) an effect of OA and temperature on carbonic anhydrase activity. We suggest that temperature increase could counterbalance the effect of OA on enzyme activity. Finally we point out that caution must, thus, be taken when interpreting transcriptomic data on carbonic anhydrases in ocean acidification and temperature stress experiments, as the effect of these stressors on the physiological function of CA will depend both on gene expression and enzyme activity. Full article

(This article belongs to the Special Issue Marine Proteins and Peptides)

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Open AccessArticle

Biosynthetic Functional Gene Analysis of Bis-Indole Metabolites from 25D7, a Clone Derived from a Deep-Sea Sediment Metagenomic Library

by Xia Yan, Xi-Xiang Tang, Dan Qin, Zhi-Wei Yi, Mei-Juan Fang, Zhen Wu and Ying-Kun Qiu

Mar. Drugs 2016, 14(6), 107; https://doi.org/10.3390/md14060107 - 01 Jun 2016

Cited by 3 | Viewed by 5286

Abstract

This work investigated the metabolites and their biosynthetic functional hydroxylase genes of the deep-sea sediment metagenomic clone 25D7. 5-Bromoindole was added to the 25D7 clone derived Escherichia coli fermentation broth. The new-generated metabolites and their biosynthetic byproducts were located through LC-MS, in which [...] Read more.

This work investigated the metabolites and their biosynthetic functional hydroxylase genes of the deep-sea sediment metagenomic clone 25D7. 5-Bromoindole was added to the 25D7 clone derived Escherichia coli fermentation broth. The new-generated metabolites and their biosynthetic byproducts were located through LC-MS, in which the isotope peaks of brominated products emerged. Two new brominated bis-indole metabolites, 5-bromometagenediindole B (1), and 5-bromometagenediindole C (2) were separated under the guidance of LC-MS. Their structures were elucidated on the basis of 1D and 2D NMR spectra (COSY, HSQC, and HMBC). The biosynthetic functional genes of the two new compounds were revealed through LC-MS and transposon mutagenesis analysis. 5-Bromometagenediindole B (1) also demonstrated moderately cytotoxic activity against MCF7, B16, CNE2, Bel7402, and HT1080 tumor cell lines in vitro. Full article

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

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Open AccessArticle

Topical Formulation Comprising Fatty Acid Extract from Cod Liver Oil: Development, Evaluation and Stability Studies

by Biljana Ilievska, Thorsteinn Loftsson, Martha Asdis Hjalmarsdottir and Gudrun Marta Asgrimsdottir

Mar. Drugs 2016, 14(6), 105; https://doi.org/10.3390/md14060105 - 01 Jun 2016

Cited by 12 | Viewed by 8481

Abstract

The purpose of this study was to develop a pharmaceutical formulation containing fatty acid extract rich in free omega-3 fatty acids such as eicosapentaenoic acid and docosahexaenoic acid for topical use. Although the health benefits of cod liver oil and other fish oils [...] Read more.

The purpose of this study was to develop a pharmaceutical formulation containing fatty acid extract rich in free omega-3 fatty acids such as eicosapentaenoic acid and docosahexaenoic acid for topical use. Although the health benefits of cod liver oil and other fish oils taken orally as a dietary supplement have been acknowledged and exploited, it is clear that their use can be extended further to cover their antibacterial properties. In vitro evaluation showed that 20% (v/v) fatty acid extract exhibits good activity against strains of the Gram-positive bacteria Staphylococcus aureus, Enterococcus faecalis, Streptoccoccus pyogenes and Streptoccoccus pneumonia. Therefore, free polyunsaturated fatty acids from cod liver oil or other fish oils can be used as safe and natural antibacterial agents. In this study, ointment compositions containing free fatty acids as active antibacterial agents were prepared by using various natural waxes and characterized. The effects of different waxes, such as carnauba wax, ozokerite wax, laurel wax, beeswax, rice bran wax, candelilla wax and microcrystalline wax, in the concentration range of 1% to 5% (w/w) on the ointment texture, consistency and stability were evaluated. The results showed significant variations in texture, sensory and rheological profiles. This was attributed to the wax’s nature and chain composition. Microcrystalline wax gave the best results but laurel wax, beeswax and rice bran wax exhibited excellent texturing, similar sensory profiles and well-balanced rheological properties. Full article

(This article belongs to the Special Issue Marine Fatty Acids-2016)

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Open AccessArticle

Metals of Deep Ocean Water Increase the Anti-Adipogenesis Effect of Monascus-Fermented Product via Modulating the Monascin and Ankaflavin Production

by Tzu-Ying Lung, Li-Ya Liao, Jyh-Jye Wang, Bai-Luh Wei, Ping-Yi Huang and Chun-Lin Lee

Mar. Drugs 2016, 14(6), 106; https://doi.org/10.3390/md14060106 - 27 May 2016

Cited by 8 | Viewed by 5402

Abstract

Deep ocean water (DOW) obtained from a depth of more than 200 m includes abundant nutrients and minerals. DOW was proven to positively increase monascin (MS) and ankaflavin (AK) production and the anti-adipogenesis effect of Monascus-fermented red mold dioscorea (RMD). However, the [...] Read more.

Deep ocean water (DOW) obtained from a depth of more than 200 m includes abundant nutrients and minerals. DOW was proven to positively increase monascin (MS) and ankaflavin (AK) production and the anti-adipogenesis effect of Monascus-fermented red mold dioscorea (RMD). However, the influences that the major metals in DOW have on Monascus secondary metabolite biosynthesis and anti-adipogenesis remain unknown. Therefore, the major metals in DOW were used as the culture water to produce RMD. The secondary metabolites production and anti-adipogenesis effect of RMD cultured with various individual metal waters were investigated. In the results, the addition of water with Mg, Ca, Zn, and Fe increased MS and AK production and inhibited mycotoxin citrinin (CT). However, the positive influence may be contributed to the regulation of pigment biosynthesis. Furthermore, in the results of cell testing, higher lipogenesis inhibition was seen in the treatments of various ethanol extracts of RMD cultured with water containing Mg, K, Zn, and Fe than in those of RMD cultured with ultra-pure water. In conclusion, various individual metals resulted in different effects on MS and AK productions as well as the anti-adipogenesis effect of RMD, but the specific metals contained in DOW may cause synergistic or comprehensive effects that increase the significantly positive influence. Full article

(This article belongs to the Special Issue Marine Natural Products that Target Metabolic Disorders)

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Open AccessArticle

Exploitable Lipids and Fatty Acids in the Invasive Oyster Crassostrea gigas on the French Atlantic Coast

by Flore Dagorn, Aurélie Couzinet-Mossion, Melha Kendel, Peter G. Beninger, Vony Rabesaotra, Gilles Barnathan and Gaëtane Wielgosz-Collin

Mar. Drugs 2016, 14(6), 104; https://doi.org/10.3390/md14060104 - 24 May 2016

Cited by 15 | Viewed by 6288

Abstract

Economic exploitation is one means to offset the cost of controlling invasive species, such as the introduced Pacific oyster (Crassostrea gigas Thunberg) on the French Atlantic coast. Total lipid and phospholipid (PL) fatty acids (FAs) and sterols were examined in an invasive [...] Read more.

Economic exploitation is one means to offset the cost of controlling invasive species, such as the introduced Pacific oyster (Crassostrea gigas Thunberg) on the French Atlantic coast. Total lipid and phospholipid (PL) fatty acids (FAs) and sterols were examined in an invasive population of C. gigas in Bourgneuf Bay, France, over four successive seasons, with a view to identify possible sources of exploitable substances. The total lipid level (% dry weight) varied from 7.1% (winter) to 8.6% (spring). Of this, PLs accounted for 28.1% (spring) to 50.4% (winter). Phosphatidylcholine was the dominant PL throughout the year (up to 74% of total PLs in winter). Plasmalogens were identified throughout the year as a series of eleven dimethylacetals (DMAs) with chain lengths between C₁₆ and C₂₀ (up to 14.5% of PL FAs + DMAs in winter). Thirty-seven FAs were identified in the PL FAs. Eicosapentaenoic acid (20:5n-3 EPA/7.53% to 14.5%) and docosahexaenoic acid (22:6n-3 DHA/5.51% to 9.5%) were the dominant polyunsaturated FAs in all seasons. Two non-methylene-interrupted dienoic (NMID) FAs were identified in all seasons: 7,13-docosadienoic and 7,15-docosadienoic acids, the latter being present at relatively high levels (up to 9.6% in winter). Twenty free sterols were identified, including cholesterol at 29.9% of the sterol mixture and about 33% of phytosterols. C. gigas tissues thus contained exploitable lipids for health benefits or as a potential source of high-quality commercial lecithin. Full article

(This article belongs to the Special Issue Marine Fatty Acids-2016)

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Mar. Drugs, Volume 14, Issue 6 (June 2016) – 17 articles

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