Marine Drugs

19 pages, 1782 KiB

Open AccessArticle

Exploitation of Filamentous and Picoplanktonic Cyanobacteria for Cosmetic Applications: Potential to Improve Skin Structure and Preserve Dermal Matrix Components

by Janaína Morone, Graciliana Lopes, Marco Preto, Vítor Vasconcelos and Rosário Martins

Mar. Drugs 2020, 18(9), 486; https://doi.org/10.3390/md18090486 - 22 Sep 2020

Cited by 35 | Viewed by 5562

Abstract

The use of natural products in skin care formulations gained interest as a concern for modern societies. The undesirable side effects of synthetic compounds, as well as the associated environmental hazards, have driven investigation on photosynthetic organisms as sustainable sources of effective and [...] Read more.

The use of natural products in skin care formulations gained interest as a concern for modern societies. The undesirable side effects of synthetic compounds, as well as the associated environmental hazards, have driven investigation on photosynthetic organisms as sustainable sources of effective and environmentally friendly ingredients. The use of natural extracts in cosmetics has been highlighted and, along with plants and algae, cyanobacteria have come into focus. Due to their low culture demands, high grow rates and ability to produce a wide variability of bioactive metabolites, cyanobacteria emerged as an economic and sustainable base for the cosmetic industry. In this study, we evaluated the potential of ethanol extracts of picocyanobacteria strains of the genera Cyanobium and Synechocystis and filamentous strains of the genera Nodosilinea, Phormidium and Tychonema for skin applications, with focus in the field of anti-aging. The extracts were analyzed for their pigment profile, phenolic content, antioxidant potential, cytotoxicity against keratinocytes (HaCat), fibroblasts (3T3L1), endothelial cells (hCMEC/D3) and capacity to inhibit hyaluronidase (HAase). The total carotenoid content ranged from 118.69 to 383.89 μg g⁻¹ of dry biomass, and the total phenolic content from 1.07 to 2.45 mg GAE g⁻¹. Identified carotenoids consisted of zeaxanthin, lutein, canthaxanthin, echinenone and β-carotene, with zeaxanthin and lutein being the most representative (49.82 and 79.08 μg g⁻¹, respectively). The highest antioxidant potential was found for Phormidium sp. LEGE 05292 and Tychonema sp. LEGE 07196 for superoxide anion radical (O₂^•−) scavenging (IC₅₀ of 822.70 and 924 μg mL⁻¹, respectively). Low or no cytotoxicity were registered. Regarding HAase inhibition, Tychonema sp. LEGE 07196 and Cyanobium sp. LEGE 07175 showed the best IC₅₀ (182.74 and 208.36 μg mL⁻¹, respectively). In addition, an increase in fibroblast proliferation was registered with these same strains. From this work, the ethanol extracts of the species Tychonema sp. and Cyanobium sp. are particularly interesting for their potential application in anti-aging formulations, once they stimulated fibroblast proliferation and inhibit hyaluronic acid digestion. Full article

(This article belongs to the Special Issue Micro- and Macroalgal Compounds in Cosmetics)

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17 pages, 3069 KiB

Open AccessArticle

Fucoidan from Ascophyllum nodosum Suppresses Postprandial Hyperglycemia by Inhibiting Na⁺/Glucose Cotransporter 1 Activity

by Xindi Shan, Xueliang Wang, Hao Jiang, Chao Cai, Jiejie Hao and Guangli Yu

Mar. Drugs 2020, 18(9), 485; https://doi.org/10.3390/md18090485 - 22 Sep 2020

Cited by 19 | Viewed by 3520

Abstract

We previously demonstrated that fucoidan with a type II structure inhibited postprandial hyperglycemia by suppressing glucose uptake, but the mechanism remains elusive. Here, we aimed to assess whether the effect of glucose absorption inhibition was related to the basic structure of fucoidans and [...] Read more.

We previously demonstrated that fucoidan with a type II structure inhibited postprandial hyperglycemia by suppressing glucose uptake, but the mechanism remains elusive. Here, we aimed to assess whether the effect of glucose absorption inhibition was related to the basic structure of fucoidans and preliminarily clarified the underlying mechanism. Fucoidans with type II structure and type I structure were prepared from Ascophyllumnodosum (AnF) or Laminariajaponica (LjF) and Kjellmaniellacrassifolia (KcF), respectively. The effects of various fucoidans on suppressing postprandial hyperglycemia were investigated using in vitro (Caco-2 monolayer model), semi-in vivo (everted gut sac model), and in vivo (oral glucose tolerance test, OGTT) assays. The results showed that only AnF with a type II structure, but not LjF or KcF with type I structure, could inhibit the glucose transport in the Caco-2 monolayer and everted gut sac models. A similar result was seen in the OGTT of Kunming mice and leptin receptor-deficient (db/db) mice, where only AnF could effectively inhibit glucose transport into the bloodstream. Furthermore, AnF (400 mg/kg/d) treatment decreased the fasting blood glucose, HbA1c, and fasting insulin levels, while increasing the serum glucagon-like peptide-1 (GLP-1) level in obese leptin receptor-deficient (db/db) mice. Furthermore, surface plasmon resonance (SPR) analysis revealed the specific binding of AnF to Na⁺/glucose cotransporter 1 (SGLT1), which indicated the effect of AnF on postprandial hyperglycemia could be due to its suppression on SGLT1 activity. Taken together, this study suggests that AnF with a type II structure can be a promising candidate for hyperglycemia treatment. Full article

(This article belongs to the Special Issue Fucoidans)

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19 pages, 3733 KiB

Open AccessArticle

The Rhodamine Isothiocyanate Analogue as a Quorum Sensing Inhibitor Has the Potential to Control Microbially-Induced Biofouling

by Yu Song, Shengjie Zhang, Yanhua Zeng, Jianming Zhu, Xiaopeng Du, Zhonghua Cai and Jin Zhou

Mar. Drugs 2020, 18(9), 484; https://doi.org/10.3390/md18090484 - 22 Sep 2020

Cited by 3 | Viewed by 2562

Abstract

Quorum sensing inhibitors (QSIs) have been proven to be an innovative approach to interfering with biofilm formation, since this process is regulated by QS signals. However, most studies have focused on single-species biofilm formation, whereas studies of the effects of signal interference on [...] Read more.

Quorum sensing inhibitors (QSIs) have been proven to be an innovative approach to interfering with biofilm formation, since this process is regulated by QS signals. However, most studies have focused on single-species biofilm formation, whereas studies of the effects of signal interference on the development of multispecies biofilm, especially in the natural environment, are still lacking. Here we develop and evaluate the anti-biofilm capability of a new QSI (rhodamine isothiocyanate analogue, RIA) in natural seawater. During the experiment, biofilm characteristics, microbial communities/functions and network interactions were monitored at 36, 80, and 180 h, respectively. The results showed that the biomass and 3D structure of the biofilm were significantly different in the presence of the QSI. The expression of genes involved in extracellular polysaccharide synthesis was also downregulated in the QSI-treated group. Dramatic differences in microbial composition, β-diversity and functions between the RIA-treated group and the control group were also observed, especially in the early stage of biofilm development. Furthermore, co-occurrence model analysis showed that RIA reduced the complexity of the microbial network. This study demonstrates that rhodamine isothiocyanate analogue is an efficient QS inhibitor and has potential applications in controlling biofouling caused by multispecies biofilm, especially in the early stage of biofouling formation. Full article

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17 pages, 2161 KiB

Open AccessArticle

Phosphatidylserine from Portunus trituberculatus Eggs Alleviates Insulin Resistance and Alters the Gut Microbiota in High-Fat-Diet-Fed Mice

by Shiwei Hu, Mengyu Du, Laijin Su and Huicheng Yang

Mar. Drugs 2020, 18(9), 483; https://doi.org/10.3390/md18090483 - 22 Sep 2020

Cited by 22 | Viewed by 3238

Abstract

Portunus trituberculatus eggs contain phospholipids, whose components and bioactivity are unclear. Here, we investigated the fatty acid composition of phosphatidylserine from P. trituberculatus eggs (Pt-PS). Moreover, its effects on insulin resistance and gut microbiota were also evaluated in high-fat-diet-fed mice. Our [...] Read more.

Portunus trituberculatus eggs contain phospholipids, whose components and bioactivity are unclear. Here, we investigated the fatty acid composition of phosphatidylserine from P. trituberculatus eggs (Pt-PS). Moreover, its effects on insulin resistance and gut microbiota were also evaluated in high-fat-diet-fed mice. Our results showed that Pt-PS accounted for 26.51% of phospholipids and contained abundant polyunsaturated fatty acids (more than 50% of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA)). Animal experiments indicated that Pt-PS significantly decreased body weight and adipose weight gain, improved hyperglycemia and hyperinsulinemia, mitigated insulin resistance, and regulated circulatory cytokines. Pt-PS activated insulin receptor substrate 1 (IRS1) and increased the levels of IRS1-associated phosphatidylinositol 3-hydroxy kinase (PI3K), phosphorylated protein kinase B (Akt) protein, and plasma membrane glucose transporter 4 protein. Furthermore, Pt-PS modified the gut microbiota, inducing, especially, a dramatic decrease in the ratio of Firmicutes to Bacteroidetes at the phylum level, as well as a remarkable improvement in their subordinate categories. Pt-PS also reduced fecal lipopolysaccharide concentration and enhanced fecal acetate, propionate, and butyrate concentrations. Additionally, the effects of Pt-PS on alleviation of insulin resistance and regulation of intestinal bacteria were better than those of phosphatidylserine from soybean. These results suggest that Pt-PS mitigates insulin resistance by altering the gut microbiota. Therefore, Pt-PS may be developed as an effective food supplement for the inhibition of insulin resistance and the regulation of human gut health. Full article

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31 pages, 2980 KiB

Open AccessReview

Blue-Print Autophagy in 2020: A Critical Review

by Sergey A. Dyshlovoy

Mar. Drugs 2020, 18(9), 482; https://doi.org/10.3390/md18090482 - 21 Sep 2020

Cited by 8 | Viewed by 5531

Abstract

Autophagy is an elegant and complex biological process that has recently attracted much attention from the scientific community. The compounds which are capable of control and modulation of this process have a promising potential as therapeutics for a number of pathological conditions, including [...] Read more.

Autophagy is an elegant and complex biological process that has recently attracted much attention from the scientific community. The compounds which are capable of control and modulation of this process have a promising potential as therapeutics for a number of pathological conditions, including cancer and neurodegenerative disorders. At the same time, due to the relatively young age of the field, there are still some pitfalls in the autophagy monitoring assays and interpretation of the experimental data. This critical review provides an overview of the marine natural compounds, which have been reported to affect autophagy. The time period from the beginning of 2016 to the middle of 2020 is covered. Additionally, the published data and conclusions based on the experimental results are re-analyzed with regard to the guidelines developed by Klionsky and colleagues (Autophagy. 2016; 12(1): 1–222), which are widely accepted by the autophagy research community. Remarkably and surprisingly, more than half of the compounds reported to be autophagy activators or inhibitors could not ultimately be assigned to either category. The experimental data reported for those substances could indicate both autophagy activation and inhibition, requiring further investigation. Thus, the reviewed molecules were divided into two groups: having validated and non-validated autophagy modulatory effects. This review gives an analysis of the recent updates in the field and raises an important problem of standardization in the experimental design and data interpretation. Full article

(This article belongs to the Special Issue Marine Drugs Acting as Autophagy Modulators)

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18 pages, 4141 KiB

Open AccessArticle

Effect of Enzymatically Extracted Fucoidans on Angiogenesis and Osteogenesis in Primary Cell Culture Systems Mimicking Bone Tissue Environment

by Julia Ohmes, Yuejun Xiao, Fanlu Wang, Maria Dalgaard Mikkelsen, Thuan Thi Nguyen, Harald Schmidt, Andreas Seekamp, Anne S. Meyer and Sabine Fuchs

Mar. Drugs 2020, 18(9), 481; https://doi.org/10.3390/md18090481 - 21 Sep 2020

Cited by 19 | Viewed by 3543

Abstract

Angiogenesis, the formation of new blood vessels from existing ones, is an essential process for successful bone regeneration. Further, angiogenesis is a key factor for the development of bone-related disorders like osteosarcoma or arthritis. Fucoidans, sulfated polysaccharides from brown algae, have been shown [...] Read more.

Angiogenesis, the formation of new blood vessels from existing ones, is an essential process for successful bone regeneration. Further, angiogenesis is a key factor for the development of bone-related disorders like osteosarcoma or arthritis. Fucoidans, sulfated polysaccharides from brown algae, have been shown to affect angiogenesis as well as a series of other physiological processes including inflammation or infection. However, the chemical properties of fucoidan which define the biological activity vary tremendously, making a prediction of the bioactivity or the corresponding therapeutic effect difficult. In this study, we compare the effect of four chemically characterized high molecular weight fucoidan extracts from Fucus distichus subsp. evanescens (FE_crude and fractions F1, F2, F3) on angiogenic and osteogenic processes in bone-related primary mono- and co-culture cell systems. By determining the gene expression and protein levels of the regulatory molecules vascular endothelial growth factor (VEGF), angiopoietin-1 (ANG-1), ANG-2 and stromal-derived factor 1 (SDF-1), we show that the extracted fucoidans negatively influence angiogenic and osteogenic processes in both the mono- and co-culture systems. We demonstrate that purer fucoidan extracts with a high fucose and sulfate content show stronger effects on these processes. Immunocytochemistry of the co-culture system revealed that treatment with FE_F3, containing the highest fucose and sulfate content, impaired the formation of angiogenic tube-like structures, indicating the anti-angiogenic properties of the tested fucoidans. This study highlights how chemical properties of fucoidan influence its bioactivity in a bone-related context and discusses how the observed phenotypes can be explained on a molecular level—knowledge that is indispensable for future therapies based on fucoidans. Full article

(This article belongs to the Special Issue Marine Organisms for Bone Regeneration - 2020)

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14 pages, 2883 KiB

Open AccessArticle

Neutral Lipids, Glycolipids, and Phospholipids, Isolated from Sandfish (Arctoscopus japonicus) Eggs, Exhibit Anti-Inflammatory Activity in LPS-Stimulated RAW264.7 Cells through NF-κB and MAPKs Pathways

by Weerawan Rod-in, Chaiwat Monmai, Il-sik Shin, SangGuan You and Woo Jung Park

Mar. Drugs 2020, 18(9), 480; https://doi.org/10.3390/md18090480 - 21 Sep 2020

Cited by 18 | Viewed by 4475

Abstract

Total lipids were extracted from sandfish (Arctoscopus japonicus), and then they were separated into the following three lipid fractions: neutral lipids, glycolipids, and phospholipids. In this study, we analyzed the lipid fractions of A. japonicus eggs and we determined their anti-inflammatory [...] Read more.

Total lipids were extracted from sandfish (Arctoscopus japonicus), and then they were separated into the following three lipid fractions: neutral lipids, glycolipids, and phospholipids. In this study, we analyzed the lipid fractions of A. japonicus eggs and we determined their anti-inflammatory activity in RAW264.7 macrophage cells. In these three lipid-fractions, the main fatty acids were as follows: palmitic acid (16:0), oleic acid (18:1n-9), docosahexaenoic acid (DHA, 22:6n-3), and eicosapentaenoic acid (EPA, 20:5n-3). Among the lipid fractions, phospholipids showed the highest concentration of DHA and EPA (21.70 ± 1.92 and 18.96 ± 1.27, respectively). The three lipid fractions of A. japonicus significantly suppressed the production of NO in macrophages. Moreover, they also significantly inhibited the expression of iNOS, COX-2, IL-6, IL-1β, and TNF-α, in a dose-dependent manner. Furthermore, the lipid fractions of A. japonicus suppressed the nuclear translocation of NF-κB p65 subunits in a dose-dependent manner. In addition, they attenuated the activation of MAPKs (p38, ERK1/2, and JNK) phosphorylation in LPS-stimulated RAW264.7 cells. These results indicate that all the lipid fractions of A. japonicus exert anti-inflammatory activity by suppressing the activation of NF-κB and MAPK pathways. Therefore, the lipid fractions of A. japonicus might be potentially used as anti-inflammatory agents. Full article

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10 pages, 1309 KiB

Open AccessArticle

Absolute Configurations and Chitinase Inhibitions of Quinazoline-Containing Diketopiperazines from the Marine-Derived Fungus Penicillium polonicum

by Xing-Chen Guo, Ya-Hui Zhang, Wen-Bin Gao, Li Pan, Hua-Jie Zhu and Fei Cao

Mar. Drugs 2020, 18(9), 479; https://doi.org/10.3390/md18090479 - 21 Sep 2020

Cited by 26 | Viewed by 2925

Abstract

Three new quinazoline-containing diketopiperazines, polonimides A–C (1–3), along with four analogues (4–7), were obtained from the marine-derived fungus Penicillium polonicum. Among them, 2 and 4, 3 and 5 were epimers, respectively, resulting the [...] Read more.

Three new quinazoline-containing diketopiperazines, polonimides A–C (1–3), along with four analogues (4–7), were obtained from the marine-derived fungus Penicillium polonicum. Among them, 2 and 4, 3 and 5 were epimers, respectively, resulting the difficulty in the determination of their configurations. The configurations of 1–3 were determined by 1D nuclear overhauser effect (NOE), Marfey and electron circular dichroism (ECD) methods. Nuclear magnetic resonance (NMR) calculation with the combination of DP4plus probability method was used to distinguish the absolute configurations of C-3 in 3 and 5. All of 1–7 were tested for their chitinase inhibitory activity against OfHex1 and OfChi-h and cytotoxicity against A549, HGC-27 and UMUC-3 cell lines. Compounds 1–7 exhibited weak activity towards OfHex1 and strong activity towards OfChi-h at a concentration of 10.0 μM, with the inhibition rates of 0.7%–10.3% and 79.1%–95.4%, respectively. Interestingly, 1–7 showed low cytotoxicity against A549, HGC-27 and UMUC-3 cell lines, suggesting that good prospect of this cluster of metabolites for drug discovery. Full article

(This article belongs to the Special Issue Fungal Natural Products: An Ongoing Source for New Drug Leads)

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17 pages, 9023 KiB

Open AccessArticle

Virtual Screening of Marine Natural Compounds by Means of Chemoinformatics and CDFT-Based Computational Peptidology

by Norma Flores-Holguín, Juan Frau and Daniel Glossman-Mitnik

Mar. Drugs 2020, 18(9), 478; https://doi.org/10.3390/md18090478 - 20 Sep 2020

Cited by 30 | Viewed by 3307

Abstract

This work presents the results of a computational study of the chemical reactivity and bioactivity properties of the members of the theopapuamides A-D family of marine peptides by making use of our proposed methodology named Computational Peptidology (CP) that has been successfully considered [...] Read more.

This work presents the results of a computational study of the chemical reactivity and bioactivity properties of the members of the theopapuamides A-D family of marine peptides by making use of our proposed methodology named Computational Peptidology (CP) that has been successfully considered in previous studies of this kind of molecular system. CP allows for the determination of the global and local descriptors that come from Conceptual Density Functional Theory (CDFT) that can give an idea about the chemical reactivity properties of the marine natural products under study, which are expected to be related to their bioactivity. At the same time, the validity of the procedure based on the adoption of the KID (Koopmans In DFT) technique, as well as the MN12SX/Def2TZVP/H₂O model chemistry is successfully verified. Together with several chemoinformatic tools that can be used to improve the process of virtual screening, some additional properties of these marine peptides are identified related to their ability to behave as useful drugs. With the further objective of analyzing their bioactivity, some useful parameters for future QSAR studies, their predicted biological targets, and the ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) parameters related to the theopapuamides A-D pharmacokinetics are also reported. Full article

(This article belongs to the Special Issue Virtual Screening of Marine Natural Products)

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18 pages, 2037 KiB

Open AccessFeature PaperArticle

Insights into the Light Response of Skeletonema marinoi: Involvement of Ovothiol

by Alfonsina Milito, Ida Orefice, Arianna Smerilli, Immacolata Castellano, Alessandra Napolitano, Christophe Brunet and Anna Palumbo

Mar. Drugs 2020, 18(9), 477; https://doi.org/10.3390/md18090477 - 20 Sep 2020

Cited by 15 | Viewed by 3956

Abstract

Diatoms are one of the most widespread groups of microalgae on Earth. They possess extraordinary metabolic capabilities, including a great ability to adapt to different light conditions. Recently, we have discovered that the diatom Skeletonema marinoi produces the natural antioxidant ovothiol B, until [...] Read more.

Diatoms are one of the most widespread groups of microalgae on Earth. They possess extraordinary metabolic capabilities, including a great ability to adapt to different light conditions. Recently, we have discovered that the diatom Skeletonema marinoi produces the natural antioxidant ovothiol B, until then identified only in clams. In this study, we investigated the light-dependent modulation of ovothiol biosynthesis in S. marinoi. Diatoms were exposed to different light conditions, ranging from prolonged darkness to low or high light, also differing in the velocity of intensity increase (sinusoidal versus square-wave distribution). The expression of the gene encoding the key ovothiol biosynthetic enzyme, ovoA, was upregulated by high sinusoidal light mimicking natural conditions. Under this situation higher levels of reactive oxygen species and nitric oxide as well as ovothiol and glutathione increase were detected. No ovoA modulation was observed under prolonged darkness nor low sinusoidal light. Unnatural conditions such as continuous square-wave light induced a very high oxidative stress leading to a drop in cell growth, without enhancing ovoA gene expression. Only one of the inducible forms of nitric oxide synthase, nos2, was upregulated by light with consequent production of NO under sinusoidal light and darkness conditions. Our data suggest that ovothiol biosynthesis is triggered by a combined light stress caused by natural distribution and increased photon flux density, with no influence from the daily light dose. These results open new perspectives for the biotechnological production of ovothiols, which are receiving a great interest for their biological activities in human model systems. Full article

(This article belongs to the Special Issue Sulfur-Containing Marine Bioactives)

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59 pages, 8614 KiB

Open AccessReview

Marine Cyanobacteria and Microalgae Metabolites—A Rich Source of Potential Anticancer Drugs

by Arijit Mondal, Sankhadip Bose, Sabyasachi Banerjee, Jayanta Kumar Patra, Jai Malik, Sudip Kumar Mandal, Kaitlyn L. Kilpatrick, Gitishree Das, Rout George Kerry, Carmela Fimognari and Anupam Bishayee

Mar. Drugs 2020, 18(9), 476; https://doi.org/10.3390/md18090476 - 19 Sep 2020

Cited by 66 | Viewed by 7398

Abstract

Cancer is at present one of the utmost deadly diseases worldwide. Past efforts in cancer research have focused on natural medicinal products. Over the past decades, a great deal of initiatives was invested towards isolating and identifying new marine metabolites via pharmaceutical companies, [...] Read more.

Cancer is at present one of the utmost deadly diseases worldwide. Past efforts in cancer research have focused on natural medicinal products. Over the past decades, a great deal of initiatives was invested towards isolating and identifying new marine metabolites via pharmaceutical companies, and research institutions in general. Secondary marine metabolites are looked at as a favorable source of potentially new pharmaceutically active compounds, having a vast structural diversity and diverse biological activities; therefore, this is an astonishing source of potentially new anticancer therapy. This review contains an extensive critical discussion on the potential of marine microbial compounds and marine microalgae metabolites as anticancer drugs, highlighting their chemical structure and exploring the underlying mechanisms of action. Current limitation, challenges, and future research pathways were also presented. Full article

(This article belongs to the Special Issue Marine-Derived Products for Biomedicine)

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16 pages, 4461 KiB

Open AccessArticle

Diphlorethohydroxycarmalol Attenuates Palmitate-Induced Hepatic Lipogenesis and Inflammation

by Seon-Heui Cha, Yongha Hwang, Soo-Jin Heo and Hee-Sook Jun

Mar. Drugs 2020, 18(9), 475; https://doi.org/10.3390/md18090475 - 18 Sep 2020

Cited by 13 | Viewed by 3538

Abstract

Non-alcoholic fatty liver disease (NAFLD) is a common cause of chronic liver disease, encompassing a range of conditions caused by lipid deposition within liver cells, and is also associated with obesity and metabolic diseases. Here, we investigated the protective effects of diphlorethohydroxycarmalol (DPHC), [...] Read more.

Non-alcoholic fatty liver disease (NAFLD) is a common cause of chronic liver disease, encompassing a range of conditions caused by lipid deposition within liver cells, and is also associated with obesity and metabolic diseases. Here, we investigated the protective effects of diphlorethohydroxycarmalol (DPHC), which is a polyphenol isolated from an edible seaweed, Ishige okamurae, on palmitate-induced lipotoxicity in the liver. DPHC treatment repressed palmitate-induced cytotoxicity, triglyceride content, and lipid accumulation. DPHC prevented palmitate-induced mRNA and protein expression of SREBP (sterol regulatory element-binding protein) 1, C/EBP (CCAAT-enhancer-binding protein) α, ChREBP (carbohydrate-responsive element-binding protein), and FAS (fatty acid synthase). In addition, palmitate treatment reduced the expression levels of phosphorylated AMP-activated protein kinase (AMPK) and sirtuin (SIRT)1 proteins, and DPHC treatment rescued this reduction. Moreover, DPHC protected palmitate-induced liver toxicity and lipogenesis, as well as inflammation, and enhanced AMPK and SIRT1 signaling in zebrafish. These results suggest that DPHC possesses protective effects against palmitate-induced toxicity in the liver by preventing lipogenesis and inflammation. DPHC could be used as a potential therapeutic or preventive agent for fatty liver diseases. Full article

(This article belongs to the Special Issue Bioactive Compounds from Brown Algae)

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16 pages, 3164 KiB

Open AccessArticle

Antitumour Effects of Astaxanthin and Adonixanthin on Glioblastoma

by Shohei Tsuji, Shinsuke Nakamura, Takashi Maoka, Tetsuya Yamada, Takahiko Imai, Takuya Ohba, Tomohiro Yako, Masahiro Hayashi, Ken Endo, Masanao Saio, Hideaki Hara and Masamitsu Shimazawa

Mar. Drugs 2020, 18(9), 474; https://doi.org/10.3390/md18090474 - 18 Sep 2020

Cited by 20 | Viewed by 5418

Abstract

Several antitumour drugs have been isolated from natural products and many clinical trials are underway to evaluate their potential. There have been numerous reports about the antitumour effects of astaxanthin against several tumours but no studies into its effects against glioblastoma. Astaxanthin is [...] Read more.

Several antitumour drugs have been isolated from natural products and many clinical trials are underway to evaluate their potential. There have been numerous reports about the antitumour effects of astaxanthin against several tumours but no studies into its effects against glioblastoma. Astaxanthin is a red pigment found in crustaceans and fish and is also synthesized in Haematococcus pluvialis; adonixanthin is an intermediate product of astaxanthin. It is known that both astaxanthin and adonixanthin possess radical scavenging activity and can confer a protective effect on several damages. In this study, we clarified the antitumour effects of astaxanthin and adonixanthin using glioblastoma models. Specifically, astaxanthin and adonixanthin showed an ability to suppress cell proliferation and migration in three types of glioblastoma cells. Furthermore, these compounds were confirmed to transfer to the brain in a murine model. In the murine orthotopic glioblastoma model, glioblastoma progression was suppressed by the oral administration of astaxanthin and adonixanthin at 10 and 30 mg/kg, respectively, for 10 days. These results suggest that both astaxanthin and adonixanthin have potential as treatments for glioblastoma. Full article

(This article belongs to the Special Issue Marine Carotenoids in Inflammation and Cancer)

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16 pages, 2311 KiB

Open AccessArticle

Jeju Magma-Seawater Inhibits α-MSH-Induced Melanogenesis via CaMKKβ-AMPK Signaling Pathways in B16F10 Melanoma Cells

by Minhyeok Song, Jihyun Lee, Young-Joo Kim, Dang Hieu Hoang, Wonchae Choe, Insug Kang, Sung Soo Kim and Joohun Ha

Mar. Drugs 2020, 18(9), 473; https://doi.org/10.3390/md18090473 - 18 Sep 2020

Cited by 7 | Viewed by 3302

Abstract

Melanin protects skin from ultraviolet radiation, toxic drugs, and chemicals. Its synthesis is sophisticatedly regulated by multiple mechanisms, including transcriptional and enzymatic controls. However, uncontrolled excessive production of melanin can cause serious dermatological disorders, such as freckles, melasma, solar lentigo, and cancer. Moreover, [...] Read more.

Melanin protects skin from ultraviolet radiation, toxic drugs, and chemicals. Its synthesis is sophisticatedly regulated by multiple mechanisms, including transcriptional and enzymatic controls. However, uncontrolled excessive production of melanin can cause serious dermatological disorders, such as freckles, melasma, solar lentigo, and cancer. Moreover, melanogenesis disorders are also linked to neurodegenerative diseases. Therefore, there is a huge demand for safer and more potent inhibitors of melanogenesis. In the present study, we report novel inhibitory effects of Jeju magma-seawater (JMS) on melanogenesis induced by α-melanocyte stimulating hormone (α-MSH) in B16F10 melanoma cells. JMS is the abundant underground seawater found in Jeju Island, a volcanic island of Korea. Research into the physiological effects of JMS is rapidly increasing due to its high contents of various minerals that are essential to human health. However, little is known about the effects of JMS on melanogenesis. Here, we demonstrate that JMS safely and effectively inhibits α-MSH-induced melanogenesis via the CaMKKβ (calcium/calmodulin-dependent protein kinase β)-AMPK (5′ adenosine monophosphate-activated protein kinase) signaling pathway. We further demonstrate that AMPK inhibits the signaling pathways of protein kinase A and MAPKs (mitogen-activated protein kinase), which are critical for melanogenesis-related gene expression. Our results highlight the potential of JMS as a novel therapeutic agent for ameliorating skin pigmentation-related disorders. Full article

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18 pages, 4536 KiB

Open AccessArticle

Fermented Oyster Extract Promotes Insulin-Like Growth Factor-1-Mediated Osteogenesis and Growth Rate

by Ilandarage Menu Neelaka Molagoda, Jayasingha Arachchige Chathuranga Chanaka Jayasingha, Yung Hyun Choi, Eui Kyun Park, You-Jin Jeon, Bae-Jin Lee and Gi-Young Kim

Mar. Drugs 2020, 18(9), 472; https://doi.org/10.3390/md18090472 - 18 Sep 2020

Cited by 9 | Viewed by 4392

Abstract

Fermented oyster (Crassostrea gigas) extract (FO) prevents ovariectomy-induced osteoporosis by inhibiting osteoclastogenesis and activating osteogenesis. However, the molecular mechanisms underlying FO-mediated bone formation and growth rate are unclear. In the current study, we found that FO significantly upregulated the expression of [...] Read more.

Fermented oyster (Crassostrea gigas) extract (FO) prevents ovariectomy-induced osteoporosis by inhibiting osteoclastogenesis and activating osteogenesis. However, the molecular mechanisms underlying FO-mediated bone formation and growth rate are unclear. In the current study, we found that FO significantly upregulated the expression of growth-promoting genes in zebrafish larvae including insulin-like growth factor 1 (zigf-1), insulin-like growth factor binding protein 3 (zigfbp-3), growth hormone-1 (zgh-1), growth hormone receptor-1 (zghr-1), growth hormone receptor alpha (zghra), glucokinase (zgck), and cholecystokinin (zccka). In addition, zebrafish larvae treated with 100 μg/mL FO increased in total body length (3.89 ± 0.13 mm) at 12 days post fertilization (dpf) compared to untreated larvae (3.69 ± 0.02 mm); this effect was comparable to that of the β-glycerophosphate-treated zebrafish larvae (4.00 ± 0.02 mm). Furthermore, FO time- and dose-dependently increased the extracellular release of IGF-1 from preosteoblast MC3T3-E1 cells, which was accompanied by high expression of IGF-1. Pharmacological inhibition of IGF-1 receptor (IGF-1R) using picropodophyllin (PPP) significantly reduced FO-mediated vertebrae formation (from 9.19 ± 0.31 to 5.53 ± 0.35) and growth performance (from 3.91 ± 0.02 to 3.69 ± 0.01 mm) in zebrafish larvae at 9 dpf. Similarly, PPP significantly decreased FO-induced calcium deposition in MC3T3-E1 cells by inhibiting GSK-3β phosphorylation at Ser9. Additionally, DOI hydrochloride, a potent stabilizer of GSK-3β, reduced FO-induced nuclear translocation of RUNX2. Transient knockdown of IGF-1Rα/β using specific silencing RNA also resulted in a significant decrease in calcium deposition and reduction in GSK-3β phosphorylation at Ser9 in MC3T3-E1 cells. Altogether, these results indicate that FO increased phosphorylated GSK-3β at Ser9 by activating the autocrine IGF-1-mediated IGF-1R signaling pathway, thereby promoting osteogenesis and growth performance. Therefore, FO is a potential nutritional supplement for bone formation and growth. Full article

(This article belongs to the Special Issue Marine Organisms for Bone Regeneration - 2020)

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44 pages, 4355 KiB

Open AccessReview

Sea Cucumber Derived Type I Collagen: A Comprehensive Review

by Tharindu R.L. Senadheera, Deepika Dave and Fereidoon Shahidi

Mar. Drugs 2020, 18(9), 471; https://doi.org/10.3390/md18090471 - 18 Sep 2020

Cited by 67 | Viewed by 10367

Abstract

Collagen is the major fibrillar protein in most living organisms. Among the different types of collagen, type I collagen is the most abundant one in tissues of marine invertebrates. Due to the health-related risk factors and religious constraints, use of mammalian derived collagen [...] Read more.

Collagen is the major fibrillar protein in most living organisms. Among the different types of collagen, type I collagen is the most abundant one in tissues of marine invertebrates. Due to the health-related risk factors and religious constraints, use of mammalian derived collagen has been limited. This triggers the search for alternative sources of collagen for both food and non-food applications. In this regard, numerous studies have been conducted on maximizing the utilization of seafood processing by-products and address the need for collagen. However, less attention has been given to marine invertebrates and their by-products. The present review has focused on identifying sea cucumber as a potential source of collagen and discusses the general scope of collagen extraction, isolation, characterization, and physicochemical properties along with opportunities and challenges for utilizing marine-derived collagen. Full article

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13 pages, 2706 KiB

Open AccessArticle

Ishophloroglucin A Isolated from Ishige okamurae Suppresses Melanogenesis Induced by α-MSH: In Vitro and In Vivo

by Xining Li, Hye-Won Yang, Yunfei Jiang, Jae-Young Oh, You-Jin Jeon and Bomi Ryu

Mar. Drugs 2020, 18(9), 470; https://doi.org/10.3390/md18090470 - 17 Sep 2020

Cited by 20 | Viewed by 3102

Abstract

Diphlorethohydroxycarmalol (DPHC) isolated from Ishige okamurae (IO) showed potential whitening effects against UV-B radiation. However, the components of IO as well as their molecular mechanism against α-melanocyte-stimulating hormone (α-MSH) have not yet been investigated. Thus, this study aimed to investigate the inhibitory effects [...] Read more.

Diphlorethohydroxycarmalol (DPHC) isolated from Ishige okamurae (IO) showed potential whitening effects against UV-B radiation. However, the components of IO as well as their molecular mechanism against α-melanocyte-stimulating hormone (α-MSH) have not yet been investigated. Thus, this study aimed to investigate the inhibitory effects of Ishophloroglucin A (IPA), a phlorotannin isolated from brown algae IO, and its crude extract (IOE), in melanogenesis in vivo in an α-MSH-induced zebrafish model and in B16F10 melanoma cells in vitro. Molecular docking studies of the phlorotannins were carried out to determine their inhibitory effects and to elucidate their mode of interaction with tyrosinase, a glycoprotein related to melanogenesis. In addition, morphological changes and melanin content decreased in the α-MSH-induced zebrafish model after IPA and IOE treatment. Furthermore, Western blotting results revealed that IPA upregulated the extracellular related protein expression in α-MSH-stimulated B16F10 cells. Hence, these results suggest that IPA isolated from IOE has a potential for use in the pharmaceutical and cosmetic industries. Full article

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17 pages, 3638 KiB

Open AccessArticle

16S rRNA Sequencing and Metagenomics Study of Gut Microbiota: Implications of BDB on Type 2 Diabetes Mellitus

by Liang Zhang, Jiao Luo, Xiangqian Li, Shuju Guo and Dayong Shi

Mar. Drugs 2020, 18(9), 469; https://doi.org/10.3390/md18090469 - 17 Sep 2020

Cited by 9 | Viewed by 3683

Abstract

Gut microbiota has a critical role in metabolic diseases, including type 2 diabetes mellitus (T2DM). 3-bromo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl)-1,2-benzenediol (BDB) is a natural bromophenol isolated from marine red alga Rhodomela confervoides. Our latest research showed that BDB could alleviate T2DM in diabetic BKS db mice. [...] Read more.

Gut microbiota has a critical role in metabolic diseases, including type 2 diabetes mellitus (T2DM). 3-bromo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl)-1,2-benzenediol (BDB) is a natural bromophenol isolated from marine red alga Rhodomela confervoides. Our latest research showed that BDB could alleviate T2DM in diabetic BKS db mice. To find out whether BDB modulates the composition of the gut microbiota during T2DM treatment, 24 BKS db diabetic mice were randomly grouped to receive BDB (n = 6), metformin (n = 6), or the vehicle (n = 6) for 7 weeks in a blinded manner. Non-diabetic BKS mice (n = 6) were used as normal control. Diabetic mice treated with BDB or metformin demonstrated significant reductions in fasting blood glucose (FBG) levels compared with the vehicle-treated mice in the 7th week. Pyrosequencing of the V3–V4 regions of the 16S rRNA gene revealed the changes of gut microbiota in response to BDB treatment. The result demonstrated short-chain acid (SCFA) producing bacteria Lachnospiraceae and Bacteroides were found to be significantly more abundant in the BDB and metformin treated group than the vehicle-treatment diabetic group. Remarkably, at the genus levels, Akkermansia elevated significantly in the BDB-treatment group. Metagenomic results indicated that BDB may alleviate the metabolic disorder of diabetic mice by promoting propanoate metabolism and inhibiting starch and sucrose metabolism, amino sugar and nucleotide sugar metabolism. In conclusion, our study suggests that the anti-diabetic effect of BDB is closely related to the modulating structure of gut microbiota and the improvement of functional metabolism genes of intestinal microorganisms. Full article

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16 pages, 4297 KiB

Open AccessArticle

Optimization of Extraction of Bioactive Peptides from Monkfish (Lophius litulon) and Characterization of Their Role in H₂O₂-Induced Lesion

by Xiaoxiao Tian, Jiawen Zheng, Baogui Xu, Jiena Ye, Zuisu Yang and Falei Yuan

Mar. Drugs 2020, 18(9), 468; https://doi.org/10.3390/md18090468 - 17 Sep 2020

Cited by 16 | Viewed by 2850

Abstract

Background: Marine fish meat has been widely used for the extraction of bioactive peptides. This study was aimed to optimize the preparation of monkfish muscle peptides (LPs) using response surface methodology (RSM) and explore the antioxidant activities of <1 kDa LPs. Methods: Peptides [...] Read more.

Background: Marine fish meat has been widely used for the extraction of bioactive peptides. This study was aimed to optimize the preparation of monkfish muscle peptides (LPs) using response surface methodology (RSM) and explore the antioxidant activities of <1 kDa LPs. Methods: Peptides were prepared from the muscles of monkfish (Lophius litulon), and five proteases were tested to hydrolyze muscle proteins. The hydrolysate that was treated using neutrase showed the highest degree of hydrolysis (DH) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging activities. Results: The optimized conditions were as follows: water/material ratio of 5.4:1, a time span of 5 h, pH of 7.0, enzyme concentration of 2000 U/g, and temperature of 45 °C; the maximum DPPH scavenging activity and DH were 92.861% and 19.302%, respectively. LPs exhibited appreciable antioxidant activities, including DPPH radical, hydroxyl radical, 2,2′-azinobis-3-ethylbenzthiazoline-6-sulphonate (ABTS) radical, and superoxide anion scavenging activities. LPs attenuated H₂O₂-related oxidative injury in RAW264.7 cells, reduced the reactive oxygen species (ROS) and malondialdehyde (MDA) levels, and increased the superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), and catalase (CAT) levels. Conclusion: We concluded that LPs could be an ideal source of bioactive peptides from monkfish and also have pharmaceutical potential. Full article

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26 pages, 1403 KiB

Open AccessReview

Comprehensive Utilization of Marine Microalgae for Enhanced Co-Production of Multiple Compounds

by Ruijuan Ma, Baobei Wang, Elvis T. Chua, Xurui Zhao, Kongyong Lu, Shih-Hsin Ho, Xinguo Shi, Lemian Liu, Youping Xie, Yinghua Lu and Jianfeng Chen

Mar. Drugs 2020, 18(9), 467; https://doi.org/10.3390/md18090467 - 16 Sep 2020

Cited by 37 | Viewed by 5588

Abstract

Marine microalgae are regarded as potential feedstock because of their multiple valuable compounds, including lipids, pigments, carbohydrates, and proteins. Some of these compounds exhibit attractive bioactivities, such as carotenoids, ω-3 polyunsaturated fatty acids, polysaccharides, and peptides. However, the production cost of bioactive compounds [...] Read more.

Marine microalgae are regarded as potential feedstock because of their multiple valuable compounds, including lipids, pigments, carbohydrates, and proteins. Some of these compounds exhibit attractive bioactivities, such as carotenoids, ω-3 polyunsaturated fatty acids, polysaccharides, and peptides. However, the production cost of bioactive compounds is quite high, due to the low contents in marine microalgae. Comprehensive utilization of marine microalgae for multiple compounds production instead of the sole product can be an efficient way to increase the economic feasibility of bioactive compounds production and improve the production efficiency. This paper discusses the metabolic network of marine microalgal compounds, and indicates their interaction in biosynthesis pathways. Furthermore, potential applications of co-production of multiple compounds under various cultivation conditions by shifting metabolic flux are discussed, and cultivation strategies based on environmental and/or nutrient conditions are proposed to improve the co-production. Moreover, biorefinery techniques for the integral use of microalgal biomass are summarized. These techniques include the co-extraction of multiple bioactive compounds from marine microalgae by conventional methods, super/subcritical fluids, and ionic liquids, as well as direct utilization and biochemical or thermochemical conversion of microalgal residues. Overall, this review sheds light on the potential of the comprehensive utilization of marine microalgae for improving bioeconomy in practical industrial application. Full article

(This article belongs to the Special Issue Bioactive Compounds Derived from Marine Microalgae 2.0)

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11 pages, 2517 KiB

Open AccessArticle

Biochemical Characterization of a Novel Endo-1,3-β-Glucanase from the Scallop Chlamys farreri

by Zhijian Li, Weizhi Liu and Qianqian Lyu

Mar. Drugs 2020, 18(9), 466; https://doi.org/10.3390/md18090466 - 16 Sep 2020

Cited by 6 | Viewed by 2635

Abstract

Endo-1,3-β-glucanases derived from marine mollusks have attracted much attention in recent years because of their unique transglycosylation activity. In this study, a novel endo-1,3-β-glucanase from the scallop Chlamys farreri, named L_cf, was biochemically characterized. Unlike in earlier studies on marine [...] Read more.

Endo-1,3-β-glucanases derived from marine mollusks have attracted much attention in recent years because of their unique transglycosylation activity. In this study, a novel endo-1,3-β-glucanase from the scallop Chlamys farreri, named L_cf, was biochemically characterized. Unlike in earlier studies on marine mollusk endo-1,3-β-glucanases, L_cf was expressed in vitro first. Enzymatic analysis demonstrated that L_cf preferred to hydrolyze laminarihexaose than to hydrolyze laminarin. Furthermore, L_cf was capable of catalyzing transglycosylation reactions with different kinds of glycosyl acceptors. More interestingly, the transglycosylation specificity of L_cf was different from that of other marine mollusk endo-1,3-β-glucanases, although they share a high sequence identity. This study enhanced our understanding of the diverse enzymatic specificities of marine mollusk endo-1,3-β-glucanases, which facilitated development of a unique endo-1,3-β-glucanase tool in the synthesis of novel glycosides. Full article

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13 pages, 2118 KiB

Open AccessArticle

Anti-Neuroinflammatory Agent, Restricticin B, from the Marine-Derived Fungus Penicillium janthinellum and Its Inhibitory Activity on the NO Production in BV-2 Microglia Cells

by Byeoung-Kyu Choi, Song-Hee Jo, Dong-Kug Choi, Phan Thi Hoai Trinh, Hwa-Sun Lee, Van Anh Cao, Tran Thi Thanh Van and Hee Jae Shin

Mar. Drugs 2020, 18(9), 465; https://doi.org/10.3390/md18090465 - 14 Sep 2020

Cited by 11 | Viewed by 3331

Abstract

A new compound containing a triene, a tetrahydropyran ring and glycine ester functionalities, restricticin B (1), together with four known compounds (2–5) were obtained from the EtOAc extract of the marine-derived fungus Penicillium janthinellum. The planar [...] Read more.

A new compound containing a triene, a tetrahydropyran ring and glycine ester functionalities, restricticin B (1), together with four known compounds (2–5) were obtained from the EtOAc extract of the marine-derived fungus Penicillium janthinellum. The planar structure of 1 was determined by detailed analyses of MS, 1D and 2D NMR data. The relative and absolute configurations of 1 were established via the analyses of NOESY spectroscopy data, the comparison of optical rotation values with those of reported restricticin derivatives and electronic circular dichroism (ECD). All the compounds were screened for their anti-neuroinflammatory effects in lipopolysaccharide (LPS)-induced BV-2 microglia cells. Restricticin B (1) and N-acetyl restricticin (2) exhibited anti-neuroinflammatory effects by suppressing the production of pro-inflammatory mediators in activated microglial cells. Full article

(This article belongs to the Special Issue Marine Compounds and Inflammation II)

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17 pages, 6010 KiB

Open AccessArticle

Diversity of Conopeptides and Their Precursor Genes of Conus Litteratus

by Xinjia Li, Wanyi Chen, Dongting Zhangsun and Sulan Luo

Mar. Drugs 2020, 18(9), 464; https://doi.org/10.3390/md18090464 - 14 Sep 2020

Cited by 14 | Viewed by 3251

Abstract

The venom of various Conus species is composed of a rich variety of unique bioactive peptides, commonly referred to as conotoxins (conopeptides). Most conopeptides have specific receptors or ion channels as physiologically relevant targets. In this paper, high-throughput transcriptome sequencing was performed to [...] Read more.

The venom of various Conus species is composed of a rich variety of unique bioactive peptides, commonly referred to as conotoxins (conopeptides). Most conopeptides have specific receptors or ion channels as physiologically relevant targets. In this paper, high-throughput transcriptome sequencing was performed to analyze putative conotoxin transcripts from the venom duct of a vermivorous cone snail species, Conus litteratus native to the South China Sea. A total of 128 putative conotoxins were identified, most of them belonging to 22 known superfamilies, with 43 conotoxins being regarded as belonging to new superfamilies. Notably, the M superfamily was the most abundant in conotoxins among the known superfamilies. A total of 15 known cysteine frameworks were also described. The largest proportion of cysteine frameworks were VI/VII (C-C-CC-C-C), IX (C-C-C-C-C-C) and XIV (C-C-C-C). In addition, five novel cysteine patterns were also discovered. Simple sequence repeat detection results showed that di-nucleotide was the major type of repetition, and the codon usage bias results indicated that the codon usage bias of the conotoxin genes was weak, but the M, O1, O2 superfamilies differed in codon preference. Gene cloning indicated that there was no intron in conotoxins of the B1- or J superfamily, one intron with 1273–1339 bp existed in a mature region of the F superfamily, which is different from the previously reported gene structure of conotoxins from other superfamilies. This study will enhance our understanding of conotoxin diversity, and the new conotoxins discovered in this paper will provide more potential candidates for the development of pharmacological probes and marine peptide drugs. Full article

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8 pages, 1988 KiB

Open AccessArticle

Sarmentosamide, an Anti-Aging Compound from a Marine-Derived Streptomyces sp. APmarine042

by Eun-Soo Lee, Eun-Young Lee, Jisoo Yoon, Ahreum Hong, Sang-Jip Nam and Jaeyoung Ko

Mar. Drugs 2020, 18(9), 463; https://doi.org/10.3390/md18090463 - 10 Sep 2020

Cited by 3 | Viewed by 3773

Abstract

Many bioactive materials have been isolated from marine microorganisms, including alkaloids, peptides, lipids, mycosporine-like amino acids, glycosides, and isoprenoids. Some of these compounds have great potential in the cosmetic industry due to their photo-protective, anti-aging, and anti-oxidant activities. In this study, sarmentosamide ( [...] Read more.

Many bioactive materials have been isolated from marine microorganisms, including alkaloids, peptides, lipids, mycosporine-like amino acids, glycosides, and isoprenoids. Some of these compounds have great potential in the cosmetic industry due to their photo-protective, anti-aging, and anti-oxidant activities. In this study, sarmentosamide (1) was isolated from marine-derived Streptomyces sp. APmarine042, after which its capacity to decrease skin aging was examined in-vitro. Sarmentosamide (1) was found to significantly reduce UVB-induced matrix metalloproteinase-1 (MMP-1) expression in normal human dermal fibroblasts (NHDFs) by inhibiting the extracellular signal-regulated kinase (ERK) and the c-Jun N-terminal kinase (JNK) phosphorylation, which are regulatory pathways upstream of MMP-1 transcription. Additionally, we confirmed that sarmentosamide (1) decreased tumor necrosis factor-alpha (TNF-α), induced MMP-1 secretion in NHDFs, and exhibited free-radical scavenging activity, as demonstrated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. Therefore, our study suggests that sarmentosamide (1) could be a promising anti-aging agent that acts via the downregulation of MMP-1 expression. Full article

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11 pages, 3587 KiB

Open AccessArticle

Ameliorating Effect of Pentadecapeptide Derived from Cyclina sinensis on Cyclophosphamide-Induced Nephrotoxicity

by Xiaoxia Jiang, Zhexin Ren, Biying Zhao, Shuyao Zhou, Xiaoguo Ying and Yunping Tang

Mar. Drugs 2020, 18(9), 462; https://doi.org/10.3390/md18090462 - 9 Sep 2020

Cited by 28 | Viewed by 3622

Abstract

Cyclophosphamide (CTX) is a widely used anticancer drug with severe nephrotoxicity. The pentadecapeptide (RVAPEEHPVEGRYLV) from Cyclina sinensis (SCSP) has been shown to affect immunity and to protect the liver. Hence, the purpose of this study was to investigate the ameliorating effect of SCSP [...] Read more.

Cyclophosphamide (CTX) is a widely used anticancer drug with severe nephrotoxicity. The pentadecapeptide (RVAPEEHPVEGRYLV) from Cyclina sinensis (SCSP) has been shown to affect immunity and to protect the liver. Hence, the purpose of this study was to investigate the ameliorating effect of SCSP on CTX-induced nephrotoxicity in mice. We injected male ICR mice with CTX (80 mg/kg·day) and measured the nephrotoxicity indices, levels of antioxidant enzymes, malondialdehyde (MDA), inflammatory factors, as well as the major proteins of the NF-κB and apoptotic pathways. Cyclophosphamide induced kidney injury; the levels of kidney-injury indicators and cytokines recovered remarkably in mice after receiving SCSP. The activities of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), and catalase (CAT) increased, while there was a significant decrease in MDA levels. The kidney tissue damage induced by CTX was also repaired to a certain extent. In addition, SCSP significantly inhibited inflammatory factors and apoptosis by regulating the NF-κB and apoptotic pathways. Our study shows that SCSP has the potential to ameliorate CTX-induced nephrotoxicity and may be used as a therapeutic adjuvant to ameliorate CTX-induced nephrotoxicity. Full article

(This article belongs to the Special Issue Nutraceuticals and Pharmaceuticals from Marine Fish and Invertebrates)

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20 pages, 1308 KiB

Open AccessArticle

Characterization of the CAZy Repertoire from the Marine-Derived Fungus Stemphylium lucomagnoense in Relation to Saline Conditions

by Wissal Ben Ali, David Navarro, Abhishek Kumar, Elodie Drula, Annick Turbé-Doan, Lydie Oliveira Correia, Stéphanie Baumberger, Emmanuel Bertrand, Craig B. Faulds, Bernard Henrissat, Giuliano Sciara, Tahar Mechichi and Eric Record

Mar. Drugs 2020, 18(9), 461; https://doi.org/10.3390/md18090461 - 9 Sep 2020

Cited by 11 | Viewed by 4017

Abstract

Even if the ocean represents a large part of Earth’s surface, only a few studies describe marine-derived fungi compared to their terrestrial homologues. In this ecosystem, marine-derived fungi have had to adapt to the salinity and to the plant biomass composition. This articles [...] Read more.

Even if the ocean represents a large part of Earth’s surface, only a few studies describe marine-derived fungi compared to their terrestrial homologues. In this ecosystem, marine-derived fungi have had to adapt to the salinity and to the plant biomass composition. This articles studies the growth of five marine isolates and the tuning of lignocellulolytic activities under different conditions, including the salinity. A de novo transcriptome sequencing and assembly were used in combination with a proteomic approach to characterize the Carbohydrate Active Enzymes (CAZy) repertoire of one of these strains. Following these approaches, Stemphylium lucomagnoense was selected for its adapted growth on xylan in saline conditions, its high xylanase activity, and its improved laccase activities in seagrass-containing cultures with salt. De novo transcriptome sequencing and assembly indicated the presence of 51 putative lignocellulolytic enzymes. Its secretome composition was studied in detail when the fungus was grown on either a terrestrial or a marine substrate, under saline and non-saline conditions. Proteomic analysis of the four S. lucomagnoense secretomes revealed a minimal suite of extracellular enzymes for plant biomass degradation and highlighted potential enzyme targets to be further studied for their adaptation to salts and for potential biotechnological applications. Full article

(This article belongs to the Special Issue Genetics and Genomics of Marine Secondary Metabolite Gene Clusters and Their Biotechnological and Pharmaceutical Applications)

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13 pages, 4796 KiB

Open AccessArticle

Marine Fungus Aspergillus chevalieri TM2-S6 Extract Protects Skin Fibroblasts from Oxidative Stress

by Sophia Letsiou, Artemis Bakea, Géraldine Le Goff, Philippe Lopes, Konstantinos Gardikis, Michal Weis, Yehuda Benayahu and Jamal Ouazzani

Mar. Drugs 2020, 18(9), 460; https://doi.org/10.3390/md18090460 - 8 Sep 2020

Cited by 15 | Viewed by 4070

Abstract

The strain Aspergillus chevalieri TM2-S6 was isolated from the sponge Axinella and identified according to internal transcribed spacer (ITS) molecular sequence homology with Aspergillus species from the section Restricti. The strain was cultivated 9 days on potato dextrose broth (PDB), and the [...] Read more.

The strain Aspergillus chevalieri TM2-S6 was isolated from the sponge Axinella and identified according to internal transcribed spacer (ITS) molecular sequence homology with Aspergillus species from the section Restricti. The strain was cultivated 9 days on potato dextrose broth (PDB), and the medium evaluated as antioxidant on primary normal human dermal fibroblasts (NHDF). The cultivation broth was submitted to sterile filtration, lyophilized and used without any further processing to give the Aspergillus chevalieri TM2-S6 cultivation broth ingredient named ACBB. ACCB contains two main compounds: tetrahydroauroglaucin and flavoglaucin. Under oxidative stress, ACCB showed a significant promotion of cell viability. To elucidate the mechanism of action, the impact on a panel of hundreds of genes involved in fibroblast physiology was evaluated. Thus, ACCB stimulates cell proliferation (VEGFA, TGFB3), antioxidant response (GPX1, SOD1, NRF2), and extracellular matrix organization (COL1A1, COL3A1, CD44, MMP14). ACCD also reduced aging (SIRT1, SIRT2, FOXO3). These findings indicate that Aspergillus chevalieri TM2-S6 cultivation broth exhibits significant in vitro skin protection of human fibroblasts under oxidative stress, making it a potential cosmetic ingredient. Full article

(This article belongs to the Special Issue Marine-Derived Ingredients for Cosmeceuticals)

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22 pages, 3031 KiB

Open AccessReview

Astaxanthin and other Nutrients from Haematococcus pluvialis—Multifunctional Applications

by Malwina Mularczyk, Izabela Michalak and Krzysztof Marycz

Mar. Drugs 2020, 18(9), 459; https://doi.org/10.3390/md18090459 - 7 Sep 2020

Cited by 120 | Viewed by 15172

Abstract

Bioactive compounds of natural origin are gaining increasing popularity. High biological activity and bioavailability, beneficial effects on health and safety of use are some of their most desirable features. Low production and processing costs render them even more attractive. Microorganisms have been used [...] Read more.

Bioactive compounds of natural origin are gaining increasing popularity. High biological activity and bioavailability, beneficial effects on health and safety of use are some of their most desirable features. Low production and processing costs render them even more attractive. Microorganisms have been used in the food, medicinal, cosmetic and energy industries for years. Among them, microalgae have proved to be an invaluable source of beneficial compounds. Haematococcus pluvialis is known as the richest source of natural carotenoid called astaxanthin. In this paper, we focus on the cultivation methods of this green microalga, its chemical composition, extraction of astaxanthin and analysis of its antioxidant, anti-inflammatory, anti–diabetic and anticancer activities. H. pluvialis, as well as astaxanthin can be used not only for the treatment of human and animal diseases, but also as a valuable component of diet and feed. Full article

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15 pages, 967 KiB

Open AccessArticle

The Comparative Immunotropic Activity of Carrageenan, Chitosan and Their Complexes

by Viktoriya N. Davydova, Irina V. Sorokina, Aleksandra V. Volod’ko, Ekaterina V. Sokolova, Marina S. Borisova and Irina M. Yermak

Mar. Drugs 2020, 18(9), 458; https://doi.org/10.3390/md18090458 - 4 Sep 2020

Cited by 9 | Viewed by 2955

Abstract

The immunotropic activity of polyelectrolyte complexes (PEC) of κ-carrageenan (κ-CGN) and chitosan (CH) of various compositions was assessed in comparison with the initial polysaccharides in comparable doses. For this, two soluble forms of PEC, with an excess of CH (CH:CGN mass ratios of [...] Read more.

The immunotropic activity of polyelectrolyte complexes (PEC) of κ-carrageenan (κ-CGN) and chitosan (CH) of various compositions was assessed in comparison with the initial polysaccharides in comparable doses. For this, two soluble forms of PEC, with an excess of CH (CH:CGN mass ratios of 10:1) and with an excess of CGN (CH: CGN mass ratios of 1:10) were prepared. The ability of PEC to scavenge NO depended on the content of the κ-CGN in the PEC. The ability of the PEC to induce the synthesis of pro-inflammatory (tumor necrosis factor-α (TNF-α)) and anti-inflammatory (interleukine-10 (IL-10)) cytokines in peripheral blood mononuclear cell was determined by the activity of the initial κ-CGN, regardless of their composition. The anti-inflammatory activity of PEC and the initial compounds was studied using test of histamine-, concanavalin A-, and sheep erythrocyte immunization-induced inflammation in mice. The highest activity of PEC, as well as the initial polysaccharides κ-CGN and CH, was observed in a histamine-induced exudative inflammation, directly related to the activation of phagocytic cells, i.e., macrophages and neutrophils. Full article

(This article belongs to the Special Issue Marine Carbohydrate-Based Compounds with Medicinal Properties)

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28 pages, 4662 KiB

Open AccessReview

Natural Products Repertoire of the Red Sea

by Ebaa M. El-Hossary, Mohammad Abdel-Halim, Eslam S. Ibrahim, Sheila Marie Pimentel-Elardo, Justin R. Nodwell, Heba Handoussa, Miada F. Abdelwahab, Ulrike Holzgrabe and Usama Ramadan Abdelmohsen

Mar. Drugs 2020, 18(9), 457; https://doi.org/10.3390/md18090457 - 4 Sep 2020

Cited by 29 | Viewed by 8123

Abstract

Marine natural products have achieved great success as an important source of new lead compounds for drug discovery. The Red Sea provides enormous diversity on the biological scale in all domains of life including micro- and macro-organisms. In this review, which covers the [...] Read more.

Marine natural products have achieved great success as an important source of new lead compounds for drug discovery. The Red Sea provides enormous diversity on the biological scale in all domains of life including micro- and macro-organisms. In this review, which covers the literature to the end of 2019, we summarize the diversity of bioactive secondary metabolites derived from Red Sea micro- and macro-organisms, and discuss their biological potential whenever applicable. Moreover, the diversity of the Red Sea organisms is highlighted as well as their genomic potential. This review is a comprehensive study that compares the natural products recovered from the Red Sea in terms of ecological role and pharmacological activities. Full article

(This article belongs to the Special Issue Bioactive Natural Products from the Red Sea)

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