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Marine Carbohydrate-Based Compounds with Medicinal Properties

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A special issue of Marine Drugs (ISSN 1660-3397).

Deadline for manuscript submissions: closed (31 January 2021) | Viewed by 32868

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Special Issue Editors

Prof. Dr. Irina M. Yermak

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Guest Editor

Far Eastern Branch, Russian Academy of Sciences, Vladivostok, Russia
Interests: marine polysaccharides; carrageenans; structure–activity; antiviral; antibacterial; anti-inflamatory; immunostimulating; anticancer activity; drug delivery; mucoadhesive properties; endotoxins; polysaccharide complexes; human health
Special Issues, Collections and Topics in MDPI journals

Dr. Viktoria Davydova

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Guest Editor

G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far-Eastern Branch of the Russian Academy of Sciences, Vladivostok, Russia
Interests: polysaccharides; stucture and bioactivity of polysaccharides; immunostimulating and anti-inflammatory activity of polysaccharides; polyelectrolyte complexes of polysaccharides; physicochemical properties of polysaccharides
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The marine environment is considered one of the most important sources of natural bioactive compounds with extremely rich biodiversity. Marine glycans are remarkable molecules, playing a determinant role in biological processes. Marine сarbohydrate-containing substances have drawn increasing attention in the ﬁeld of biomedicine for their various biological activities, such as antioxidant, antitumor, hypoglycemic, immunomodulatory, and anticoagulant. These compounds obtained from marine sources such as algae, microbes, and animals are usually biodegradable and biocompatible and exhibit biological properties that contribute to the discovery of a wide range of new bioactive substances with special pharmacological properties of interest to medicine. Carbohydrate-based compounds include glycans, glycoproteins, proteoglycans, glycolipids, and low-molecular and complex glycosides of differential origin. All cells, including human cells, have carbohydrates on their surface, known as the glycocalyx. The glycocalyx is a useful target for personalized medicine, including finding new biomarkers for diseases such as cancer, and for patient stratification in clinical trials. The functional studies of carbohydrates concern molecular recognition such as carbohydrate–lectin or glycoside–enzyme interactions, cell recognition (normal and pathological), viral adhesion/penetration, and many other phenomena. Carbohydrate recognition plays a vital role in the activation and function of the immune system.

Production and applications of marine carbohydrate as therapeutic agents are increasingly important topics of intensive researches. A modern study of carbohydrates includes the development of glycotechnologies in the field of diagnosis and therapy of diseases and nutrients. The interest in the study of marine polysaccharides with therapeutic purposes relies in the possibility of developing novel approaches of less invasive and more personalized treatments. Many of these polysaccharides allow loading lower drug dosages, which may lead to a drastic reduction of the side effects caused by the drugs. In addition, the structure of polysaccharides can be relatively easily modiﬁed in order to synthesize derivatives with desirable characteristics for drug delivery. Complexes on the basis of carbohydrates are often prepared to improve their functional properties. This approach allows easily adapting complex characteristics for specific medical applications. Thus, carbohydrate complexes are well-tolerated macroorganism systems and can be used in various fields, such as drug delivery systems, matrices for cell cultivation and enzyme immobilization, materials for the reconstruction of bone, cartilage, cardiac, and dental tissues.

In this Special Issue, we seek to contribute to the discussion of various aspects of marine carbohydrate-containing compounds and provide a unique platform for a new concept for their use in medicine in order to continue to facilitate further research in this area.

We invite researchers to submit reviews and reports of their original recent research that demonstrate or summarize significant advances in the medical use of carbohydrate-containing compounds as well as related biotechnological improvements.

Prof. Dr. Irina M. Yermak
Dr. Viktoria Davydova
Guest Editors

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Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Marine Drugs is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

Marine carbohydrates
Carbohydrate-based compounds
Сarbohydrate–lectin
Glycans in diseases and human health
Glyco immunology
Polysaccharide prevention
Сarbohydrate–protein interaction
Preclinical and clinical studies
Carbohydrate-based diagnosis and therapy
Preclinical and clinical studies
Carbohydrate for drug delivery

Related Special Issue

Marine Carbohydrate-Based Compounds with Medicinal Properties II in Marine Drugs (5 articles)

Published Papers (13 papers)

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Editorial

Jump to: Research

6 pages, 208 KiB

Open AccessEditorial

Current Trend of Marine Carbohydrate-Containing Compounds with Medicinal Properties

by Irina M. Yermak and Viktoria N. Davydova

Mar. Drugs 2021, 19(6), 331; https://doi.org/10.3390/md19060331 - 8 Jun 2021

Cited by 1 | Viewed by 2287

Abstract

Carbohydrates are most abundant biomolecules on Earth and, also, the most complex biomolecules in terms of structure [...] Full article

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

Research

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14 pages, 294 KiB

Open AccessArticle

Effect of Supplementing Seaweed Extracts to Pigs until d35 Post-Weaning on Performance and Aspects of Intestinal Health

by Stafford Vigors, John O’Doherty, Ruth Rattigan and Torres Sweeney

Mar. Drugs 2021, 19(4), 183; https://doi.org/10.3390/md19040183 - 26 Mar 2021

Cited by 15 | Viewed by 2524

Abstract

The objective of this study was to examine the effects of feeding laminarin (LAM) and fucoidan (FUC) enriched seaweed extracts up to d35 post-weaning on measures of animal performance, intestinal microbial and transcriptome profiles. 75 pigs were assigned to one of three groups: (1) basal diet; (2) basal diet + 250 ppm fucoidan; (3) basal diet + 300 ppm laminarin with 7 replicates per treatment group. Measures of performance were collected weekly and animals sacrificed on d35 post-weaning for the sampling of gastrointestinal tissue and digesta. Animal performance was similar between the basal group and the groups supplemented with FUC and LAM (P > 0.05). Pigs fed the basal diet had higher alpha diversity compared to both the LAM and FUC supplemented pigs (P < 0.05). Supplementation with LAM and FUC increased the production of butyric acid compared to basal fed pigs (P < 0.05). At genus level pigs fed the LAM supplemented diet had the greatest abundance of Faecalbacterium, Roseburia and the lowest Campylobacter of the three experimental treatments (P< 0.05). While neither extract had beneficial effects on animal performance, LAM supplementation had a positive influence on intestinal health through alterations in the gastrointestinal microbiome and increased butyrate production. Full article

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

21 pages, 2964 KiB

Open AccessArticle

Antiproliferative Properties of Scandium Exopolysaccharide Complexes on Several Cancer Cell Lines

by Javier Muñoz-Garcia, Mattia Mazza, Cyrille Alliot, Corinne Sinquin, Sylvia Colliec-Jouault, Dominique Heymann and Sandrine Huclier-Markai

Mar. Drugs 2021, 19(3), 174; https://doi.org/10.3390/md19030174 - 23 Mar 2021

Cited by 8 | Viewed by 2631

Abstract

Antimetastatic properties on both murine and human osteosarcoma cell lines (POS-1 and KHOS) have been evidenced using exopolysaccharide (EPS) derivatives, produced by Alteromonas infernus bacterium. These derivatives had no significant effect on the cell cycle neither a pro-apoptotic effect on osteosarcoma cells. Based on this observation, these EPSs could be employed as new drug delivery systems for therapeutic uses. A theranostic approach, i.e., combination of a predictive biomarker with a therapeutic agent, has been developed notably by combining with true pair of theranostic radionuclides, such as scandium ⁴⁷Sc/⁴⁴Sc. However, it is crucial to ensure that, once complexation is done, the biological properties of the vector remain intact, allowing the molecular tropism of the ligand to recognize its molecular target. It is important to assess if the biological properties of EPS evidenced on osteosarcoma cell lines remain when scandium is complexed to the polymers and can be extended to other cancer cell types. Scandium-EPS complexes were thus tested in vitro on human cell lines: MNNG/HOS osteosarcoma, A375 melanoma, A549 lung adenocarcinoma, U251 glioma, MDA231 breast cancer, and Caco2 colon cancer cells. An xCELLigence Real Cell Time Analysis (RTCA) technology assay was used to monitor for 160 h, the proliferation kinetics of the different cell lines. The tested complexes exhibited an anti-proliferative effect, this effect was more effective compared to EPS alone. This increase of the antiproliferative properties was explained by a change in conformation of EPS complexes due to their polyelectrolyte nature that was induced by complexation. Alterations of both growth factor-receptor signaling, and transmembrane protein interactions could be the principal cause of the antiproliferative effect. These results are very promising and reveal that EPS can be coupled to scandium for improving its biological effects and also suggesting that no major structural modification occurs on the ligand. Full article

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

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14 pages, 2969 KiB

Open AccessArticle

Expression and Characterization of a Cold-Adapted Alginate Lyase with Exo/Endo-Type Activity from a Novel Marine Bacterium Alteromonas portus HB161718^T

by Huiqin Huang, Shuang Li, Shixiang Bao, Kunlian Mo, Dongmei Sun and Yonghua Hu

Mar. Drugs 2021, 19(3), 155; https://doi.org/10.3390/md19030155 - 17 Mar 2021

Cited by 24 | Viewed by 2754

Abstract

The alginate lyases have unique advantages in the preparation of alginate oligosaccharides and processing of brown algae. Herein, a gene alg2951 encoding a PL7 family alginate lyase with exo/endo-type activity was cloned from a novel marine bacterium Alteromonas portus HB161718^T and then expressed in Escherichia coli. The recombinant Alg2951 in the culture supernatant reached the activity of 63.6 U/mL, with a molecular weight of approximate 60 kDa. Alg2951 exhibited the maximum activity at 25 °C and pH 8.0, was relatively stable at temperatures lower than 30 °C, and showed a special preference to poly-guluronic acid (polyG) as well. Both NaCl and KCl had the most promotion effect on the enzyme activity of Alg2951 at 0.2 M, increasing by 21.6 and 19.1 times, respectively. The TCL (Thin Layer Chromatography) and ESI-MS (Electrospray Ionization Mass Spectrometry) analyses suggested that Alg2951 could catalyze the hydrolysis of sodium alginate to produce monosaccharides and trisaccharides. Furthermore, the enzymatic hydrolysates displayed good antioxidant activity by assays of the scavenging abilities towards radicals (hydroxyl and ABTS+) and the reducing power. Due to its cold-adapted and dual exo/endo-type properties, Alg2951 can be a potential enzymatic tool for industrial production. Full article

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

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19 pages, 2756 KiB

Open AccessArticle

Potential of Exopolysaccharide from Porphyridium marinum to Contend with Bacterial Proliferation, Biofilm Formation, and Breast Cancer

by Nesrine Gargouch, Fatma Elleuch, Ines Karkouch, Olfa Tabbene, Chantal Pichon, Christine Gardarin, Christophe Rihouey, Luc Picton, Slim Abdelkafi, Imen Fendri and Céline Laroche

Mar. Drugs 2021, 19(2), 66; https://doi.org/10.3390/md19020066 - 27 Jan 2021

Cited by 26 | Viewed by 3242

Abstract

Exopolysaccharide (EPS) from marine microalgae are promising sources of a new generation of drugs. However, lot of them remain to be discovered and tested. In this study, EPS produced by Porphyridium marinum and its oligomers prepared by High Pressure Homogenizer have been tested for different biological activities, i.e., antibacterial, anti-fungal and antibiofilm activities on Candida albicans, as well as for their effects on the viability of murine breast cancer cells. Results have shown that all EPS samples present some biological activity. For antibacterial and antibiofilm activities, the native EPS exhibited a better efficiency with Minimum Inhibitory Concentration (MIC) from 62.5 µg/mL to 1000 µg/mL depending on the bacterial strain. For Candida albicans, the biofilm formation was reduced by about 90% by using only a 31.3 µg/mL concentration. Concerning breast cancer cells, lower molar masses fractions appeared to be more efficient, with a reduction of viability of up to 55%. Finally, analyses of polymers composition and viscosity measurements were conducted on all samples, in order to propose hypotheses involving the activities caused by the intrinsic properties of polymers. Full article

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

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14 pages, 2563 KiB

Open AccessArticle

The Protect Effects of Chitosan Oligosaccharides on Intestinal Integrity by Regulating Oxidative Status and Inflammation under Oxidative Stress

by Ruixia Lan, Qingqing Chang, Linlin Wei and Zhihui Zhao

Mar. Drugs 2021, 19(2), 57; https://doi.org/10.3390/md19020057 - 25 Jan 2021

Cited by 24 | Viewed by 2551

Abstract

The aim of this study was to evaluate the effects of the dietary supplementation of chitosan oligosaccharides (COS) on intestinal integrity, oxidative status, and the inflammation response with hydrogen peroxide (H₂O₂) challenge. In total, 30 rats were randomly assigned to three groups with 10 replications: CON group, basal diet; AS group, basal diet + 0.1% H₂O₂ in drinking water; ASC group, basal diet + 200 mg/kg COS + 0.1% H₂O₂ in drinking water. The results indicated that COS upregulated (p < 0.05) villus height (VH) of the small intestine, duodenum, and ileum; mucosal glutathione peroxidase activity; jejunum and ileum mucosal total antioxidant capacity; duodenum and ileum mucosal interleukin (IL)-6 level; jejunum mucosal tumor necrosis factor (TNF)-α level; duodenum and ileum mucosal IL-10 level; the mRNA expression level of zonula occludens (ZO)-1 in the jejunum and ileum, claudin in the duodenum, nuclear factor-erythroid 2-like 2 in the jejunum, and heme oxygenase-1 in the duodenum and ileum; and the protein expression of ZO-1 and claudin in jejunum; however, it downregulated (p < 0.05) serum diamine oxidase activity and D-lactate level; small intestine mucosal malondialdehyde content; duodenum and ileum mucosal IL-6 level; jejunum mucosal TNF-α level; and the mRNA expression of IL-6 in the duodenum and jejunum, and TNF-α in the jejunum and ileum. These results suggested COS could maintain intestinal integrity under oxidative stress by modulating the intestinal oxidative status and release of inflammatory cytokines. Full article

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

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14 pages, 1321 KiB

Open AccessArticle

Structure of the Polysaccharide Secreted by Vibrio alginolyticus CNCM I-5035 (Epidermist 4.0^TM)

by Sophie Drouillard, Rémi Chambon, Isabelle Jeacomine, Laurine Buon, Claire Boisset, Anthony Courtois, Bertrand Thollas, Pierre-Yves Morvan, Romuald Vallée and William Helbert

Mar. Drugs 2020, 18(10), 509; https://doi.org/10.3390/md18100509 - 9 Oct 2020

Cited by 6 | Viewed by 2435

Abstract

Vibrio alginolyticus (CNCM I-5035) secretes an exopolysaccharide used as ingredient in cosmetic industry under the trademark Epidermist 4.0^TM. It is appreciated for its ability to improve the physical and chemical barrier functions of the skin by notably increasing the keratinocyte differentiation and epidermal renewal. Composition analyses and in depth characterization of the polysaccharides as well as oligosaccharides obtained by mild acid hydrolyses revealed that it was composed of a repetition unit of three residues: d-galactose (d-Gal), d-N-acetylglucosamine (GlcNAc) and l-N-acetylguluronic acid, of which 30% (M/M) was acetylated in position 3. The complete structure of the polysaccharide was resolved giving the repetition unit: [→3)-α-d-Gal-(1→4)-α-l-GulNAcA/α-l-3OAc-GulNAcA-(1→4)-β-d-GlcNAc-(1→]. Full article

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

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13 pages, 2573 KiB

Open AccessArticle

Characterization of Low Molecular Weight Sulfate Ulva Polysaccharide and its Protective Effect against IBD in Mice

by Yuanyuan Li, Han Ye, Ting Wang, Peng Wang, Ruizhi Liu, Yinping Li, Yingying Tian and Jingliang Zhang

Mar. Drugs 2020, 18(10), 499; https://doi.org/10.3390/md18100499 - 29 Sep 2020

Cited by 21 | Viewed by 2840

Abstract

Inflammatory bowel disease (IBD) has been gradually considered a public health challenge worldwide. Sulfated polysaccharides, extracted from seaweed, have been shown to have an anti-inflammatory effect on the disease. In this study, LMW-ulvan, a unique sulfate Ulva polysaccharide with low molecular weight, was prepared using the enzymatic method. The structural characterization of LMW-ulvan and its protective effect on colitis induced by dextran sulfate sodium (DSS) were studied. The results showed that LMW-ulvan with molecular weight of 2.56 kDa consists of 57.23% rhamnose (Rha), 28.76% xylose (Xyl), 7.42% glucuronic acid (GlcA), and 1.77% glucose (Glc). Its backbone contains (1→3,4)-linked Rha, (1→4)-linked Xyl, and (1→4)-linked GlcA with small amounts of (1→4)-linked Rha residues; sulfate substitution was at C-3 of Rha. LMW-ulvan was found to reduce DSS-induced disease activity index, colon shortening, and colonic tissue damage, which were associated with decreased oxidative stresses and inflammation, thus improving the expression of tight junction proteins. These results indicate that LMW-ulvan is able to improve colitis and may be a promising application for IBD. Full article

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

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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 2495

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 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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18 pages, 2845 KiB

Open AccessArticle

Glyceroglycolipid Metabolism Regulations under Phosphate Starvation Revealed by Transcriptome Analysis in Synechococcus elongatus PCC 7942

by Xinrui Xu and Xiaoling Miao

Mar. Drugs 2020, 18(7), 360; https://doi.org/10.3390/md18070360 - 13 Jul 2020

Cited by 6 | Viewed by 3542

Abstract

Glyceroglycolipids, abundant in cyanobacteria’s photosynthetic membranes, present bioactivities and pharmacological activities, and can be widely used in the pharmaceutical industry. Environmental factors could alter the contents and compositions of cyanobacteria glyceroglycolipids, but the regulation mechanism remains unclear. Therefore, the glyceroglycolipids contents and the transcriptome in Synechococcus elongatus PCC 7942 were analyzed under phosphate starvation. Under phosphate starvation, the decrease of monogalactosyl diacylglycerol (MGDG) and increases of digalactosyl diacylglycerol (DGDG) and sulfoquinovosyl diacylglycerol (SQDG) led to a decrease in the MGDG/DGDG ratio, from 4:1 to 5:3, after 12 days of cultivation. However, UDP–sulfoquinovose synthase gene sqdB, and the SQDG synthase gene sqdX, were down-regulated, and the decreased MGDG/DGDG ratio was later increased back to 2:1 after 15 days of cultivation, suggesting the regulation of glyceroglycolipids on day 12 was based on the MGDG/DGDG ratio maintaining glyceroglycolipid homeostasis. There are 12 differentially expressed transcriptional regulators that could be potential candidates related to glyceroglycolipid regulation, according to the transcriptome analysis. The transcriptome analysis also suggested post-transcriptional or post-translational regulations in glyceroglycolipid synthesis. This study provides further insights into glyceroglycolipid metabolism, as well as the scientific basis for glyceroglycolipid synthesis optimization and cyanobacteria glyceroglycolipids utilization via metabolic engineering. Full article

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

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18 pages, 2909 KiB

Open AccessArticle

Inhibitory Effects of Carrageenans on Endotoxin-Induced Inflammation

by Irina M. Yermak, Aleksandra V. Volod’ko, Eleonora I. Khasina, Viktoriya N. Davydova, Evgeniy A. Chusovitin, Dmitry L. Goroshko, Anna O. Kravchenko, Tamara F. Solov’eva and Victor V. Maleev

Mar. Drugs 2020, 18(5), 248; https://doi.org/10.3390/md18050248 - 10 May 2020

Cited by 9 | Viewed by 2753

Abstract

The inhibitory effects of carrageenans (CRGs) on lipopolysaccharide (LPS) induced inflammation in a mouse model of endotoxemia and in complex therapy of patients with enteric infections of Salmonella etiology were studied. The atomic force microscopy (AFM) examination of LPS and its mixture with CRGs showed that the LPS morphology is significantly changed under the action of κ- and κ/β-CRGs. CRGs were able to increase the synthesis of anti-inflammatory interleukin 10 (IL-10) in vitro, and, at low concentrations, their activity in the mixture with LPS was higher. The protective effect of CRGs against Escherichia coli LPS was studied in vivo by monitoring the biochemical and pathomorphological parameters. The κ- and κ/β-CRGs and food supplement “Carrageenan-FE” increased the nonspecific resistance of mice to E. coli LPS at the expense of the inhibition of processes of thymus involution, adrenals hypertrophy, thyroid atrophy, hypercorticoidism, glycogenolysis, and lactate acidosis. The estimation of the therapeutic action of food supplement Carrageenan-FE in complex therapy of patients with enteric infections of Salmonella etiology is given. Carrageenan-FE restores the system of hemostasis and corrects some biochemical indicators and parameters in the immune systems of patients. These results allow us to hope for the practical application of CRGs for lowering the endotoxemia level in patients under the development of the infectious process caused by Gram-negative bacteria. Full article

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

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17 pages, 2235 KiB

Open AccessArticle

Immunostimulatory Effect of Sulfated Galactans from the Green Seaweed Caulerpa cupressoides var. flabellata

by Jefferson da Silva Barbosa, Diego Araújo Sabry, Cynthia Haynara Ferreira Silva, Dayanne Lopes Gomes, Arquimedes Paixão Santana-Filho, Guilherme Lanzi Sassaki and Hugo Alexandre Oliveira Rocha

Mar. Drugs 2020, 18(5), 234; https://doi.org/10.3390/md18050234 - 29 Apr 2020

Cited by 16 | Viewed by 2729

Abstract

Sulfated polysaccharides (SPs) obtained from green seaweeds are structurally heterogeneous molecules with multifunctional bioactivities. In this work, two sulfated and pyruvated galactans were purified from Caulerpa cupressoides var. flabellata (named SP1 and SP2), and their immunostimulatory effect was evaluated using cultured murine macrophage cells. Both SPs equally increased the production of nitric oxide, reactive oxygen species, and the proinflammatory cytokines TNF-α and IL-6. NMR spectroscopy revealed that both galactans were composed primarily of 3)-β-d-Galp-(1→3) units. Pyruvate groups were also found, forming five-membered cyclic ketals as 4,6-O-(1’carboxy)-ethylidene-β-d-Galp residues. Some galactoses are sulfated at C-2. In addition, only SP2 showed some galactose units sulfated at C-4, indicating that sulfation at this position is not essential for the immunomodulatory activity of these galactans. Overall, the data showed that the galactans of C. cupressoides exhibited immunostimulating activity with potential therapeutic applications, which can be used in the development of new biomedical products. Full article

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

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17 pages, 8034 KiB

Open AccessArticle

Chitosan-Gentamicin Conjugate Hydrogel Promoting Skin Scald Repair

by Tingting Yan, Songzhi Kong, Qianqian Ouyang, Chengpeng Li, Tingting Hou, Yu Chen and Sidong Li

Mar. Drugs 2020, 18(5), 233; https://doi.org/10.3390/md18050233 - 29 Apr 2020

Cited by 35 | Viewed by 4067

Abstract

Our earlier research indicated that chitosan-gentamicin conjugate (CS-GT) possesses superior antimicrobial activity and good water solubility. To develop CS-GT-based scald dressings, the antibacterial properties of CS-GT were further studied, and the biosafety of CS-GT and the healing mechanism of CS-GT hydrogel was systematically explored in this article. It was found that cell viability shows a declined inclination with the prolonged culture time and the increased concentration of CS-GT. After three day’s culture, the cell viability could still remain at 79.72% when CS-GT concentration was as high as 1000 μg/mL. On the other hand, the hemolysis rate of CS-GT was lower than 5% when its concentration is 800 μg/mL. Therefore CS-GT has good cytocompatibility and hemocompatibility. A wound-healing experiment has shown that the skin healing rate of CS-GT hydrogel was the highest at 99.61%, followed by the positive control (wet burn ointment) 94.98%, GT hydrogel 87.50%, and matrix 77.39%. The blank control group, however, possessed the lowest healing rate of 75.45%. Further analysis indicated that CS-GT hydrogel could promote the synthesis of total protein (TP) in skin granulation tissue, resulting in the enhanced hydroxyproline (HYP) content, which facilitated collagen fibrogenesis, reduced cytokine expression in an inflammatory response, and, ultimately, accelerated wound healing. To sum up, CS-GT hydrogel is a promising scald dressing. Full article

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

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