Marine Drugs

14 pages, 2926 KiB

Open AccessArticle

Brasilterpenes A–E, Bergamotane Sesquiterpenoid Derivatives with Hypoglycemic Activity from the Deep Sea-Derived Fungus Paraconiothyrium brasiliense HDN15-135

by Wenxue Wang, Yeqin Shi, Yuanyuan Liu, Yundong Zhang, Jiajin Wu, Guojian Zhang, Qian Che, Tianjiao Zhu, Mingyu Li and Dehai Li

Mar. Drugs 2022, 20(5), 338; https://doi.org/10.3390/md20050338 - 23 May 2022

Cited by 6 | Viewed by 2500

Abstract

Five bergamotane sesquiterpenoid derivatives, brasilterpenes A–E (1–5), bearing an unreported spiral 6/4/5 tricyclic ring system, were isolated from the deep sea-derived ascomycete fungus Paraconiothyrium brasiliense HDN15-135. Their structures, including absolute configurations, were established by extensive spectroscopic methods complemented by [...] Read more.

Five bergamotane sesquiterpenoid derivatives, brasilterpenes A–E (1–5), bearing an unreported spiral 6/4/5 tricyclic ring system, were isolated from the deep sea-derived ascomycete fungus Paraconiothyrium brasiliense HDN15-135. Their structures, including absolute configurations, were established by extensive spectroscopic methods complemented by single-crystal X-ray diffraction analyses, electronic circular dichroism (ECD), and density-functional theory (DFT) calculations of nuclear magnetic resonance (NMR) data including DP4+ analysis. The hypoglycemic activity of these compounds was assessed using a diabetic zebrafish model. Brasilterpenes A (1) and C (3) significantly reduced free blood glucose in hyperglycemic zebrafish in vivo by improving insulin sensitivity and suppressing gluconeogenesis. Moreover, the hypoglycemic activity of compound 3 was comparable to the positive control, anti-diabetes drug rosiglitazone. These results suggested brasilterpene C (3) had promising anti-diabetes potential. Full article

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18 pages, 3194 KiB

Open AccessReview

Secondary Metabolites Isolated from Chilean Marine Algae: A Review

by Dioni Arrieche, Héctor Carrasco, Andrés F. Olea, Luis Espinoza, Aurelio San-Martín and Lautaro Taborga

Mar. Drugs 2022, 20(5), 337; https://doi.org/10.3390/md20050337 - 23 May 2022

Cited by 3 | Viewed by 2342

Abstract

Chile is in the extreme southwestern part of America, and it has an extreme length, of approximately 4300 km that increases to 8000 km considering the Chilean Antarctic Territory. Despite the large extent of its coastal territory and the diversity of geographic environments [...] Read more.

Chile is in the extreme southwestern part of America, and it has an extreme length, of approximately 4300 km that increases to 8000 km considering the Chilean Antarctic Territory. Despite the large extent of its coastal territory and the diversity of geographic environments and climates associated with Chilean coasts, the research on marine resources in Chile has been rather scarce. From marine organisms found in Chilean coastal waters, algae have been the most studied, since they contain a wide range of interesting secondary metabolites that have some structural traits that make them unique and uncharacteristic. Thus, a wide structural variety of natural products including terpenoids (monoterpenes, sesquiterpenes, diterpenes, and meroterpenoids), furanones, and C₁₅-acetogenins have been isolated and identified. This review describes the existing literature on bioprospecting and exploration of secondary metabolites from Chilean coasts. Full article

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43 pages, 7687 KiB

Open AccessReview

Exopolysaccharides from Microalgae and Cyanobacteria: Diversity of Strains, Production Strategies, and Applications

by Céline Laroche

Mar. Drugs 2022, 20(5), 336; https://doi.org/10.3390/md20050336 - 21 May 2022

Cited by 44 | Viewed by 4624

Abstract

Microalgae and cyanobacteria are photosynthetic organisms that can produce/accumulate biomolecules with industrial interest. Among these molecules, EPSs are macromolecular polysaccharidic compounds that present biological activities and physico-chemical properties, allowing to consider their valorization in diverse commercial markets, such as cosmetic, therapeutic, nutraceutic, or [...] Read more.

Microalgae and cyanobacteria are photosynthetic organisms that can produce/accumulate biomolecules with industrial interest. Among these molecules, EPSs are macromolecular polysaccharidic compounds that present biological activities and physico-chemical properties, allowing to consider their valorization in diverse commercial markets, such as cosmetic, therapeutic, nutraceutic, or hydrocolloids areas. The number of microalgae and cyanobacteria strains described to produce such EPSs has increased in recent years as, among the 256 producing strains gathered in this review, 86 were published in the last 10 years (~33%). Moreover, with the rise of research on microalgae EPSs, a variety of monosaccharides compositions have been discovered, highlighting the versatility of these organisms. If some production strategies can be applied to increase EPS production yields, it appears that case by case studies are needed to promote EPS synthesis by a strain, as many responses exist. This paper proposes an up-to-date state of the art of the diversity of microalgae and cyanobacteria EPS-producing strains, associated to the variability of compositions. The strategies for the production and extraction of the polymers are also discussed. Finally, an overview of the biological activities and physico-chemical properties allow one to consider their use on several commercial markets. Full article

(This article belongs to the Special Issue Marine Exopolysaccharides: Health Potential and Other Industrial Applications)

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42 pages, 2499 KiB

Open AccessReview

Multiple Roles of Chitosan in Mucosal Drug Delivery: An Updated Review

by Paola Mura, Francesca Maestrelli, Marzia Cirri and Natascia Mennini

Mar. Drugs 2022, 20(5), 335; https://doi.org/10.3390/md20050335 - 20 May 2022

Cited by 42 | Viewed by 5216

Abstract

Chitosan (CS) is a linear polysaccharide obtained by the deacetylation of chitin, which, after cellulose, is the second biopolymer most abundant in nature, being the primary component of the exoskeleton of crustaceans and insects. Since joining the pharmaceutical field, in the early 1990s, [...] Read more.

Chitosan (CS) is a linear polysaccharide obtained by the deacetylation of chitin, which, after cellulose, is the second biopolymer most abundant in nature, being the primary component of the exoskeleton of crustaceans and insects. Since joining the pharmaceutical field, in the early 1990s, CS attracted great interest, which has constantly increased over the years, due to its several beneficial and favorable features, including large availability, biocompatibility, biodegradability, non-toxicity, simplicity of chemical modifications, mucoadhesion and permeation enhancer power, joined to its capability of forming films, hydrogels and micro- and nanoparticles. Moreover, its cationic character, which renders it unique among biodegradable polymers, is responsible for the ability of CS to strongly interact with different types of molecules and for its intrinsic antimicrobial, anti-inflammatory and hemostatic activities. However, its pH-dependent solubility and susceptibility to ions presence may represent serious drawbacks and require suitable strategies to be overcome. Presently, CS and its derivatives are widely investigated for a great variety of pharmaceutical applications, particularly in drug delivery. Among the alternative routes to overcome the problems related to the classic oral drug administration, the mucosal route is becoming the favorite non-invasive delivery pathway. This review aims to provide an updated overview of the applications of CS and its derivatives in novel formulations intended for different methods of mucosal drug delivery. Full article

(This article belongs to the Special Issue Pharmaceutical Formulation of Marine Drugs)

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16 pages, 1982 KiB

Open AccessArticle

Bioactivity-Guided Screening of Antimicrobial Secondary Metabolites from Antarctic Cultivable Fungus Acrostalagmus luteoalbus CH-6 Combined with Molecular Networking

by Ting Shi, Xiang-Qian Li, Ze-Min Wang, Li Zheng, Yan-Yan Yu, Jia-Jia Dai and Da-Yong Shi

Mar. Drugs 2022, 20(5), 334; https://doi.org/10.3390/md20050334 - 19 May 2022

Cited by 3 | Viewed by 2189

Abstract

With the increasingly serious antimicrobial resistance, discovering novel antibiotics has grown impendency. The Antarctic abundant microbial resources, especially fungi, can produce unique bioactive compounds for adapting to the hostile environment. In this study, three Antarctic fungi, Chrysosporium sp. HSXSD-11-1, Cladosporium sp. HSXSD-12 and [...] Read more.

With the increasingly serious antimicrobial resistance, discovering novel antibiotics has grown impendency. The Antarctic abundant microbial resources, especially fungi, can produce unique bioactive compounds for adapting to the hostile environment. In this study, three Antarctic fungi, Chrysosporium sp. HSXSD-11-1, Cladosporium sp. HSXSD-12 and Acrostalagmus luteoalbus CH-6, were found to have the potential to produce antimicrobial compounds. Furthermore, the crude extracts of CH-6 displayed the strongest antimicrobial activities with 72.3–84.8% growth inhibition against C. albicans and Aeromonas salmonicida. The secondary metabolites of CH-6 were researched by bioactivity tracking combined with molecular networking and led to the isolation of two new α-pyrones, acrostalapyrones A (1) and B (2), along with one known analog (3), and three known indole diketopiperazines (4–6). The absolute configurations of 1 and 2 were identified through modified Mosher’s method. Compounds 4 and 6 showed strong antimicrobial activities. Remarkably, the antibacterial activity of 6 against A. salmonicida displayed two times higher than that of the positive drug Ciprofloxacin. This is the first report to discover α-pyrones from the genus Acrostalagmus, and the significant antimicrobial activities of 4 and 6 against C. albicans and A. salmonicida. This study further demonstrates the great potential of Antarctic fungi in the development of new compounds and antibiotics. Full article

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28 pages, 11828 KiB

Open AccessReview

Approaches to Configuration Determinations of Flexible Marine Natural Products: Advances and Prospects

by Zong-Qing Huo, Feng Zhu, Xing-Wang Zhang, Xiao Zhang, Hong-Bao Liang, Jing-Chun Yao, Zhong Liu, Gui-Min Zhang, Qing-Qiang Yao and Guo-Fei Qin

Mar. Drugs 2022, 20(5), 333; https://doi.org/10.3390/md20050333 - 19 May 2022

Cited by 8 | Viewed by 2918

Abstract

Flexible marine natural products (MNPs), such as eribulin and bryostatin, play an important role in the development of modern marine drugs. However, due to the multiple chiral centers and geometrical uncertainty of flexible systems, configuration determinations of flexible MNPs face great challenges, which, [...] Read more.

Flexible marine natural products (MNPs), such as eribulin and bryostatin, play an important role in the development of modern marine drugs. However, due to the multiple chiral centers and geometrical uncertainty of flexible systems, configuration determinations of flexible MNPs face great challenges, which, in turn, have led to obstacles in druggability research. To resolve this issue, the comprehensive use of multiple methods is necessary. Additionally, configuration assignment methods, such as X-ray single-crystal diffraction (crystalline derivatives, crystallization chaperones, and crystalline sponges), NMR-based methods (JBCA and Mosher’s method), circular dichroism-based methods (ECCD and ICD), quantum computational chemistry-based methods (NMR calculations, ECD calculations, and VCD calculations), and chemical transformation-based methods should be summarized. This paper reviews the basic principles, characteristics, and applicability of the methods mentioned above as well as application examples to broaden the research and applications of these methods and to provide a reference for the configuration determinations of flexible MNPs. Full article

(This article belongs to the Special Issue Configurational and Conformational Studies on the Structures of Marine Natural Products)

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17 pages, 10917 KiB

Open AccessFeature PaperArticle

by Yuqi Lin, Jiajia Yang, Lianxiang Luo, Xiaoyong Zhang, Shengyu Deng, Xiaodan Chen, Yiyang Li, Alaa El-Din A. Bekhit, Baojun Xu and Riming Huang

Mar. Drugs 2022, 20(5), 332; https://doi.org/10.3390/md20050332 - 19 May 2022

Cited by 10 | Viewed by 2723

Abstract

Marine fungi represent an important and sustainable resource, from which the search for novel biological substances for application in the pharmacy or food industry offers great potential. In our research, novel polysaccharide (AUM-1) was obtained from marine Aureobasidium melanogenum SCAU-266 were obtained and [...] Read more.

Marine fungi represent an important and sustainable resource, from which the search for novel biological substances for application in the pharmacy or food industry offers great potential. In our research, novel polysaccharide (AUM-1) was obtained from marine Aureobasidium melanogenum SCAU-266 were obtained and the molecular weight of AUM-1 was determined to be 8000 Da with 97.30% of glucose, 1.9% of mannose, and 0.08% galactose, owing to a potential backbone of α-D-Glcp-(1→2)-α-D-Manp-(1→4)-α-D-Glcp-(1→6)-(SO₃⁻)-4-α-D-Glcp-(1→6)-1-β-D-Glcp-1→2)-α-D-Glcp-(1→6)-β-D-Glcp-1→6)-α-D-Glcp-1→4)-α-D-Glcp-6→1)-[α-D-Glcp-4]₂₆→1)-α-D-Glcp and two side chains that consisted of α-D-Glcp-1 and α-D-Glcp-(1→6)-α-D-Glcp residues. The immunomodulatory effect of AUM-1 was identified. Then, the potential molecular mechanism by which AUM-1 may be connected to ferroptosis was indicated by metabonomics, and the expression of COX2, SLC7A11, GPX4, ACSL4, FTH1, and ROS were further verified. Thus, we first speculated that AUM-1 has a potential effect on the ferroptosis-related immunomodulatory property in RAW 264.7 cells by adjusting the expression of GPX4, regulated glutathione (oxidative), directly causing lipid peroxidation owing to the higher ROS level through the glutamate metabolism and TCA cycle. Thus, the ferroptosis related immunomodulatory effect of AUM-1 was obtained. Full article

(This article belongs to the Special Issue Poly- and Oligosaccharides from Marine Origins)

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16 pages, 1991 KiB

Open AccessArticle

Cyclodepsipeptides: Isolation from Endophytic Fungi of Sarcophyton ehrenbergi and Verification of Their Larvicidal Activity via In-Vitro and In-Silico Studies

by Abdel Nasser B. Singab, Nada M. Mostafa, Yasmin A. Elkhawas, Eman Al-Sayed, Mokhtar M. Bishr, Ahmed M. Elissawy, Mohamed S. Elnaggar, Iten M. Fawzy, Osama M. Salama, Yi-Hong Tsai and Fang-Rong Chang

Mar. Drugs 2022, 20(5), 331; https://doi.org/10.3390/md20050331 - 18 May 2022

Cited by 15 | Viewed by 2315

Abstract

Culex pipiens mosquitoes are vectors to many viruses and can transmit diseases such as filariasis and avian malaria. The present study evaluated the larvicidal activity of marine-derived endophytic fungi Aspergillus nomius and Aspergillus flavus from the soft coral Sarcophyton ehrenbergi along with two [...] Read more.

Culex pipiens mosquitoes are vectors to many viruses and can transmit diseases such as filariasis and avian malaria. The present study evaluated the larvicidal activity of marine-derived endophytic fungi Aspergillus nomius and Aspergillus flavus from the soft coral Sarcophyton ehrenbergi along with two known cyclodepsipeptide compounds, scopularide A (1) and B (2), isolated from A. flavus extract, against third-instar larvae of C. pipiens, using distilled water as a negative control and toosenedanin as a positive control. The structures of the isolated compounds were confirmed by various spectroscopic analyses. The lethal concentrations (LC₅₀ and LC₉₀) were calculated by probit analysis. Scopularide A was the most potent after 96 h treatment, with LC₅₀ and LC₉₀ values of 58.96 and 994.31 ppm, respectively, and with 82.66% mortality at a concentration of 300 ppm. To unravel the biochemical mechanism of the tested extracts and compounds, their effects against protease, chitinase, phenoloxidases and lipase enzymes from the whole-body tissue of C. pipiens were evaluated after 72 h treatment at LC₅₀ dose. Superior activity was observed for A. flavus extract against all tested enzymes. A molecular docking study was conducted for scopularide A and B on the four tested enzymes, to further verify the observed activity. Results revealed good binding affinities for both compounds as compared to the docked ligands, mainly via a number of hydrogen bonds. This was the first study to report the isolation of endophytic fungi A. flavus and A. nomius from the marine soft coral S. ehrenbergi. The endophytic fungal extract of A. flavus was found to be a promising source for a natural larvicidal agent against C. pipiens populations. Full article

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23 pages, 713 KiB

Open AccessReview

The Role of Seawater and Saline Solutions in Treatment of Upper Respiratory Conditions

by Danijela Štanfel, Livije Kalogjera, Sergej V. Ryazantsev, Kristina Hlača, Elena Y. Radtsig, Rashidov Teimuraz and Pero Hrabač

Mar. Drugs 2022, 20(5), 330; https://doi.org/10.3390/md20050330 - 17 May 2022

Cited by 7 | Viewed by 5618

Abstract

The history of saline nasal irrigation (SNI) is indeed a long one, beginning from the ancient Ayurvedic practices and gaining a foothold in the west at the beginning of the 20th century. Today, there is a growing number of papers covering the effects [...] Read more.

The history of saline nasal irrigation (SNI) is indeed a long one, beginning from the ancient Ayurvedic practices and gaining a foothold in the west at the beginning of the 20th century. Today, there is a growing number of papers covering the effects of SNI, from in vitro studies to randomized clinical trials and literature overviews. Based on the recommendations of most of the European and American professional associations, seawater, alone or in combination with other preparations, has its place in the treatment of numerous conditions of the upper respiratory tract (URT), primarily chronic (rhino)sinusitis, allergic rhinitis, acute URT infections and postoperative recovery. Additionally, taking into account its multiple mechanisms of action and mounting evidence from recent studies, locally applied seawater preparations may have an important role in the prevention of viral and bacterial infections of the URT. In this review we discuss results published in the past years focusing on seawater preparations and their use in clinical and everyday conditions, since such products provide the benefits of additional ions vs. saline, have an excellent safety profile and are recommended by most professional associations in the field of otorhinolaryngology. Full article

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27 pages, 5494 KiB

Open AccessReview

A Medicinal Halophyte Ipomoea pes-caprae (Linn.) R. Br.: A Review of Its Botany, Traditional Uses, Phytochemistry, and Bioactivity

by Ganiyu Akinniyi, Jeonghee Lee, Hiyoung Kim, Joon-Goo Lee and Inho Yang

Mar. Drugs 2022, 20(5), 329; https://doi.org/10.3390/md20050329 - 17 May 2022

Cited by 7 | Viewed by 4560

Abstract

Ipomoea pes-caprae (Linn.) R. Br. (Convolvulaceae) is a halophytic plant that favorably grows in tropical and subtropical countries in Asia, America, Africa, and Australia. Even though this plant is considered a pan-tropical plant, I. pes-caprae has been found to occur in inland habitats [...] Read more.

Ipomoea pes-caprae (Linn.) R. Br. (Convolvulaceae) is a halophytic plant that favorably grows in tropical and subtropical countries in Asia, America, Africa, and Australia. Even though this plant is considered a pan-tropical plant, I. pes-caprae has been found to occur in inland habitats and coasts of wider areas, such as Spain, Anguilla, South Africa, and Marshall Island, either through a purposeful introduction, accidentally by dispersal, or by spreading due to climate change. The plant parts are used in traditional medicine for treating a wide range of diseases, such as inflammation, gastrointestinal disorders, pain, and hypertension. Previous phytochemical analyses of the plant have revealed pharmacologically active components, such as alkaloids, glycosides, steroids, terpenoids, and flavonoids. These phytoconstituents are responsible for the wide range of biological activities possessed by I. pes-caprae plant parts and extracts. This review arranges the previous reports on the botany, distribution, traditional uses, chemical constituents, and biological activities of I. pes-caprae to facilitate further studies that would lead to the discovery of novel bioactive natural products from this halophyte. Full article

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13 pages, 1880 KiB

Open AccessArticle

An Octopus-Derived Peptide with Antidiuretic Activity in Rats

by Ye-Ji Kim, Jei Ha Lee, Seung-Hyun Jung, Ki Hyun Kim, Chang-Hoon Choi, Seonmi Jo and Dong Ho Woo

Mar. Drugs 2022, 20(5), 328; https://doi.org/10.3390/md20050328 - 17 May 2022

Viewed by 2377

Abstract

Discovering new drug candidates with high efficacy and few side effects is a major challenge in new drug development. The two evolutionarily related peptides oxytocin (OXT) and arginine vasopressin (AVP) are known to be associated with a variety of physiological and psychological processes [...] Read more.

Discovering new drug candidates with high efficacy and few side effects is a major challenge in new drug development. The two evolutionarily related peptides oxytocin (OXT) and arginine vasopressin (AVP) are known to be associated with a variety of physiological and psychological processes via the association of OXT with three types of AVP receptors. Over decades, many synthetic analogs of these peptides have been designed and tested for therapeutic applications; however, only a few studies of their natural analogs have been performed. In this study, we investigated the bioactivity and usefulness of two natural OXT/AVP analogs that originate from the marine invertebrate Octopus vulgaris, named octopressin (OTP) and cephalotocin (CPT). By measuring the intracellular Ca²⁺ or cyclic AMP increase in each OXT/AVP receptor subtype–overexpressing cell, we found that CPT, but not OTP, acts as a selective agonist of human AVP type 1b and 2 receptors. This behavior is reminiscent of desmopressin, the most widely prescribed antidiuretic drug in the world. Similar to the case for desmopressin, a single intravenous tail injection of CPT into Sprague-Dawley rats reduced urine output and increased urinary osmolality. In conclusion, we suggest that CPT has a significant antidiuretic effect and that CPT might be beneficial for treating urological conditions such as nocturia, enuresis, and diabetes insipidus. Full article

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27 pages, 2931 KiB

Open AccessReview

Humic Substances as Microalgal Biostimulants—Implications for Microalgal Biotechnology

by Daria Gabriela Popa, Carmen Lupu, Diana Constantinescu-Aruxandei and Florin Oancea

Mar. Drugs 2022, 20(5), 327; https://doi.org/10.3390/md20050327 - 16 May 2022

Cited by 15 | Viewed by 3176

Abstract

Humic substances (HS) act as biostimulants for terrestrial photosynthetic organisms. Their effects on plants are related to specific HS features: pH and redox buffering activities, (pseudo)emulsifying and surfactant characteristics, capacity to bind metallic ions and to encapsulate labile hydrophobic molecules, ability to adsorb [...] Read more.

Humic substances (HS) act as biostimulants for terrestrial photosynthetic organisms. Their effects on plants are related to specific HS features: pH and redox buffering activities, (pseudo)emulsifying and surfactant characteristics, capacity to bind metallic ions and to encapsulate labile hydrophobic molecules, ability to adsorb to the wall structures of cells. The specific properties of HS result from the complexity of their supramolecular structure. This structure is more dynamic in aqueous solutions/suspensions than in soil, which enhances the specific characteristics of HS. Therefore, HS effects on microalgae are more pronounced than on terrestrial plants. The reported HS effects on microalgae include increased ionic nutrient availability, improved protection against abiotic stress, including against various chemical pollutants and ionic species of potentially toxic elements, higher accumulation of value-added ingredients, and enhanced bio-flocculation. These HS effects are similar to those on terrestrial plants and could be considered microalgal biostimulant effects. Such biostimulant effects are underutilized in current microalgal biotechnology. This review presents knowledge related to interactions between microalgae and humic substances and analyzes the potential of HS to enhance the productivity and profitability of microalgal biotechnology. Full article

(This article belongs to the Special Issue Biotechnology Applications of Microalgae)

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23 pages, 2211 KiB

Open AccessArticle

Metabolic Profiling and In Vitro Assessment of the Biological Activities of the Ethyl Acetate Extract of Penicillium chrysogenum “Endozoic of Cliona sp. Marine Sponge” from the Red Sea (Egypt)

by Muneera S. M. Al-Saleem, Wafaa H. B. Hassan, Zeinab I. El Sayed, Mahmoud M. Abdel-Aal, Wael M. Abdel-Mageed, Eman Abdelsalam and Sahar Abdelaziz

Mar. Drugs 2022, 20(5), 326; https://doi.org/10.3390/md20050326 - 15 May 2022

Cited by 6 | Viewed by 2868

Abstract

Marine sponge-derived endozoic fungi have been gaining increasing importance as promising sources of numerous and unique bioactive compounds. This study investigates the phytochemical profile and biological activities of the ethyl acetate extract of Penicillium chrysogenum derived from Cliona sp. sponge. Thirty-six compounds were [...] Read more.

Marine sponge-derived endozoic fungi have been gaining increasing importance as promising sources of numerous and unique bioactive compounds. This study investigates the phytochemical profile and biological activities of the ethyl acetate extract of Penicillium chrysogenum derived from Cliona sp. sponge. Thirty-six compounds were tentatively identified from P. chrysogenum ethyl acetate extract along with the kojic acid (KA) isolation. The UPLC-ESI-MS/MS positive ionization mode was used to analyze and identify the extract constituents while 1D and 2D NMR spectroscopy were used for kojic acid (KA) structure confirmation. The antimicrobial, antioxidant, and cytotoxic activities were assessed in vitro. Both the extract and kojic acid showed potent antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa with MIC 250 ± 0.82 µg/mL. Interestingly, the extract showed strong antifungal activity against Candida albicans and Cryptococcus neoformans with MIC 93.75 ± 0.55 and 19.53 ± 0.48 µg/mL, respectively. Furthermore, KA showed the same potency against Fusarium oxysporum and Cryptococcus neoformans with MIC 39.06 ± 0.85 and 39.06 ± 0.98 µg/mL, respectively. Ultimately, KA showed strong antioxidant activity with IC₅₀ 33.7 ± 0.8 µg/mL. Moreover, the extract and KA showed strong cytotoxic activity against colon carcinoma (with IC₅₀ 22.6 ± 0.8 and 23.4 ± 1.4 µg/mL, respectively) and human larynx carcinoma (with equal IC₅₀ 30.8 ± 1.3 and ± 2.1 µg/mL, respectively), respectively. The current study represents the first insights into the phytochemical profile and biological properties of P. chrysoenum ethyl acetate extract, which could be a promising source of valuable secondary metabolites with potent biological potentials. Full article

(This article belongs to the Special Issue Marine Compounds and Research of the Middle East)

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20 pages, 5284 KiB

Open AccessArticle

Novel Antioxidant Collagen Peptides of Siberian Sturgeon (Acipenserbaerii) Cartilages: The Preparation, Characterization, and Cytoprotection of H₂O₂-Damaged Human Umbilical Vein Endothelial Cells (HUVECs)

by Yan Sheng, Yi-Ting Qiu, Yu-Mei Wang, Chang-Feng Chi and Bin Wang

Mar. Drugs 2022, 20(5), 325; https://doi.org/10.3390/md20050325 - 14 May 2022

Cited by 53 | Viewed by 4031

Abstract

For making full use of aquatic by-products to produce high value-added products, Siberian sturgeon (Acipenser baerii) cartilages were degreased, mineralized, and separately hydrolyzed by five kinds of proteases. The collagen hydrolysate (SCH) generated by Alcalase showed the strongest 2,2-diphenyl-1-picrylhydrazyl radical (DPPH·) [...] Read more.

For making full use of aquatic by-products to produce high value-added products, Siberian sturgeon (Acipenser baerii) cartilages were degreased, mineralized, and separately hydrolyzed by five kinds of proteases. The collagen hydrolysate (SCH) generated by Alcalase showed the strongest 2,2-diphenyl-1-picrylhydrazyl radical (DPPH·) and hydroxide radical (HO·) scavenging activity. Subsequently, thirteen antioxidant peptides (SCP1-SCP3) were isolated from SCH, and they were identified as GPTGED, GEPGEQ, GPEGPAG, VPPQD, GLEDHA, GDRGAEG, PRGFRGPV, GEYGFE, GFIGFNG, PSVSLT, IELFPGLP, LRGEAGL, and RGEPGL with molecular weights of 574.55, 615.60, 583.60, 554.60, 640.64, 660.64, 885.04, 700.70, 710.79, 602.67, 942.12, 714.82, and 627.70 Da, respectively. GEYGFE, PSVSLT, and IELFPGLP showed the highest scavenging activity on DPPH· (EC₅₀: 1.27, 1.05, and 1.38 mg/mL, respectively) and HO· (EC₅₀: 1.16, 0.97, and 1.63 mg/mL, respectively), inhibiting capability of lipid peroxidation, and protective functions on H₂O₂-damaged plasmid DNA. More importantly, GEYGFE, PSVSLT, and IELFPGLP displayed significant cytoprotection on HUVECs against H₂O₂ injury by regulating the endogenous antioxidant enzymes of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) to decrease the contents of reactive oxygen species (ROS) and malondialdehyde (MDA). Therefore, the research provided better technical assistance for a higher-value utilization of Siberian sturgeon cartilages and the thirteen isolated peptides—especially GEYGFE, PSVSLT, and IELFPGLP—which may serve as antioxidant additives for generating health-prone products to treat chronic diseases caused by oxidative stress. Full article

(This article belongs to the Special Issue Marine Bioactive Peptides—Structure, Function, and Application)

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15 pages, 2120 KiB

Open AccessArticle

The Impact of Natural Deep Eutectic Solvents and Extraction Method on the Co-Extraction of Trace Metals from Fucus vesiculosus

by Alexander N. Shikov, Ekaterina D. Obluchinskaya, Elena V. Flisyuk, Inna I. Terninko, Yulia E. Generalova and Olga N. Pozharitskaya

Mar. Drugs 2022, 20(5), 324; https://doi.org/10.3390/md20050324 - 13 May 2022

Cited by 15 | Viewed by 2555

Abstract

In recent years, natural deep eutectic solvents (NADES) have been widely investigated for the extraction of food and medicinal plants as well as seaweeds. However, the ability of NADES for trace elements co-extraction from natural sources is not well investigated. The aim of [...] Read more.

In recent years, natural deep eutectic solvents (NADES) have been widely investigated for the extraction of food and medicinal plants as well as seaweeds. However, the ability of NADES for trace elements co-extraction from natural sources is not well investigated. The aim of this study was to investigate the ability of common NADES for trace elements co-extraction from Fucus vesiculosus. All of the tested NADES did not recover As and Co (concentration <LOQ). Moreover, all of the tested NADES provided a low recovery (<9%) of Ba, Ca, Fe, Mg, Mn, Sr, and Zn. The method of extraction had not shown a statistically significant effect on the co-extraction of all elements (excluding Ba and Ca). In contrast, the water content in NADES was significantly affected on the recovery of Ba, Ca, Mg, Mn, Sr, and Zn. The recovery of Al and Cr was relatively high and considerably varied (from 1.5 to 59.9%). NADES comprising lactic acid:glucose:H₂O (5:3:1) provided the lowest contents of all elements, and the highest extracted amounts were obtained employing water contents of 60–80%. The calculated daily intake of all the elements contained in NADES extracts were less than the daily dose risk estimators. The hazard quotients, hazard indexes, and carcinogenic risk calculated for all trace elements and their combination were considerably less than 1. This evidences no health risk, and carcinogenic risk after topical application of all studied NADES. For the first time, the results of the current study demonstrated that NADES extracts of F. vesiculosus contain a lower amount of trace metals and are safer than the extracts obtained with water and 70% acetone. This indicates a significant advantage for NADES compared with the other solvents. Full article

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19 pages, 6526 KiB

Open AccessArticle

Effects of Formulation on the Palatability and Efficacy of In-Feed Praziquantel Medications for Marine Finfish Aquaculture

by Edith K. Y. Tang, Gavin J. Partridge, Lindsey D. Woolley, Luke Pilmer and Lee Yong Lim

Mar. Drugs 2022, 20(5), 323; https://doi.org/10.3390/md20050323 - 13 May 2022

Cited by 1 | Viewed by 2059

Abstract

Praziquantel (PZQ) provides an effective treatment against monogenean parasitic infestations in finfish. However, its use as an in-feed treatment is challenging due to palatability issues. In this study, five formulations of PZQ beads (1–4 mm) were developed using marine-based polymers, with allicin added [...] Read more.

Praziquantel (PZQ) provides an effective treatment against monogenean parasitic infestations in finfish. However, its use as an in-feed treatment is challenging due to palatability issues. In this study, five formulations of PZQ beads (1–4 mm) were developed using marine-based polymers, with allicin added as a flavouring agent. All formulations attained PZQ loading rates ≥74% w/w, and the beads were successfully incorporated into fish feed pellets at an active dietary inclusion level of 10 g/kg. When tested for palatability and digestibility in small yellowtail kingfish, the PZQ-loaded beads produced with alginate-chitosan, alginate-Cremophor^® RH40, and agar as carriers resulted in high consumption rates of 99–100% with no digesta or evidence of beads in the gastrointestinal tract (GIT) of fish fed with diets containing either formulation. Two formulations produced using chitosan-based carriers resulted in lower consumption rates of 68–75%, with undigested and partly digested beads found in the fish GIT 3 h post feeding. The PZQ-loaded alginate-chitosan and agar beads also showed good palatability in large (≥2 kg) yellowtail kingfish infected with gill parasites and were efficacious in removing the parasites from the fish, achieving >90% reduction in mean abundance relative to control fish (p < 0.001). The two effective formulations were stable upon storage at ambient temperature for up to 18 months, showing residual drug content >90% compared with baseline levels. Overall, the palatability, efficacy and stability data collected from this study suggest that these two PZQ particulate formulations have potential applications as in-feed anti-parasitic medications for the yellowtail kingfish farming industry. Full article

(This article belongs to the Special Issue Alginate-Based Biomaterials and Drug Delivery)

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10 pages, 1487 KiB

Open AccessArticle

Homo/Hetero-Dimers of Aromatic Bisabolane Sesquiterpenoids with Neuroprotective Activity from the Fungus Aspergillus versicolor A18 from South China Sea

by Han-Zhuang Weng, Jun-Yu Zhu, Fang-Yu Yuan, Zhuo-Ya Tang, Xiao-Qing Tian, Ye Chen, Cheng-Qi Fan, Gui-Hua Tang and Sheng Yin

Mar. Drugs 2022, 20(5), 322; https://doi.org/10.3390/md20050322 - 13 May 2022

Cited by 13 | Viewed by 3488

Abstract

Chromatographic fractionation of the EtOH extracts of the marine-derived fungus Aspergillus versicolor A18 has led to the isolation of 11 homo/hetero-dimers of aromatic bisabolane sesquiterpenoids including eight diphenyl ether-coupled aromatic bisabolanes (1a/1b and 5–10) and three [...] Read more.

Chromatographic fractionation of the EtOH extracts of the marine-derived fungus Aspergillus versicolor A18 has led to the isolation of 11 homo/hetero-dimers of aromatic bisabolane sesquiterpenoids including eight diphenyl ether-coupled aromatic bisabolanes (1a/1b and 5–10) and three homodimers (2–4), together with their monomers including three aromatic bisabolanes (11–13) and two diphenyl ethers (14 and 15). Their structures and absolute configurations were elucidated by extensive spectroscopic analysis including HRESIMS, 1D/2D NMR, calculated ECD, and the optical rotatory data. Among the four new compounds, (+/−)-asperbisabol A (1a/1b), asperbisabol B (2), and asperbisabol C (3), the enantiomers 1a and 1b represent an unprecedented skeleton of diphenyl ether-coupled aromatic bisabolane sesquiterpenoids with a spiroketal core moiety. The neuroprotective effects of selected compounds against sodium nitroprusside (SNP)-induced injury were evaluated in PC12 cells by the MTT assay. Five compounds (1a, 6, and 8–10) showed remarkable neuroprotective activities at 10 μM, being more active than the positive control edaravone. Full article

(This article belongs to the Special Issue Bioactive Compounds from the Deep-Sea-Derived Microorganisms)

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19 pages, 2746 KiB

Open AccessArticle

Taxonomic and Bioactivity Characterizations of Mameliella alba Strain LZ-28 Isolated from Highly Toxic Marine Dinoflagellate Alexandrium catenella LZT09

by Cheng-Zhe Ren, Hui-Min Gao, Jun Dai, Wen-Zhuo Zhu, Fei-Fei Xu, Yun Ye, Xiao-Ling Zhang and Qiao Yang

Mar. Drugs 2022, 20(5), 321; https://doi.org/10.3390/md20050321 - 12 May 2022

Cited by 5 | Viewed by 2177

Abstract

Microalgae host varied microbial consortium harboring cross-kingdom interactions with fundamental ecological significance in aquatic ecosystems. Revealing the complex biofunctions of the cultivable bacteria of phycosphere microbiota is one vital basis for deeply understanding the mechanisms governing these dynamic associations. In this study, a [...] Read more.

Microalgae host varied microbial consortium harboring cross-kingdom interactions with fundamental ecological significance in aquatic ecosystems. Revealing the complex biofunctions of the cultivable bacteria of phycosphere microbiota is one vital basis for deeply understanding the mechanisms governing these dynamic associations. In this study, a new light-yellow pigmented bacterial strain LZ-28 was isolated from the highly-toxic and harmful algal bloom-forming dinoflagellate Alexandrium catenella LZT09. Collective phenotypic and genotypic profiles were obtained to confidently identify this strain as a new Mameliellaalba member. Comparative genomic analysis showed that strain LZ-28 shared highly similar functional features with other four marine algae-derived M. alba strains in spite of their distinctive isolation sources. Based on the bioactivity assaying, the mutual growth-promoting effects between bacterial strain LZ-28 and algal strain LZT09 were observed. After the culture conditions were optimized, strain LZ-28 demonstrated an extraordinary production ability for its bioflocculanting exopolysaccharides (EPS). Moreover, the portions of two monosaccharides glucose and fucose of the EPS were found to positively contribute to the bioflocculanting capacity. Therefore, the present study sheds light on the similar genomic features among the selected M. alba strains, and it also reveals the potential pharmaceutical, environmental and biotechnological implications of active EPS produced by this new Mameliella alba strain LZ-28 recovered from toxic bloom-forming marine dinoflagellate. Full article

(This article belongs to the Special Issue Marine Glycomics)

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34 pages, 1933 KiB

Open AccessReview

Application of MS-Based Metabolomic Approaches in Analysis of Starfish and Sea Cucumber Bioactive Compounds

by Roman S. Popov, Natalia V. Ivanchina and Pavel S. Dmitrenok

Mar. Drugs 2022, 20(5), 320; https://doi.org/10.3390/md20050320 - 12 May 2022

Cited by 11 | Viewed by 3495

Abstract

Today, marine natural products are considered one of the main sources of compounds for drug development. Starfish and sea cucumbers are potential sources of natural products of pharmaceutical interest. Among their metabolites, polar steroids, triterpene glycosides, and polar lipids have attracted a great [...] Read more.

Today, marine natural products are considered one of the main sources of compounds for drug development. Starfish and sea cucumbers are potential sources of natural products of pharmaceutical interest. Among their metabolites, polar steroids, triterpene glycosides, and polar lipids have attracted a great deal of attention; however, studying these compounds by conventional methods is challenging. The application of modern MS-based approaches can help to obtain valuable information about such compounds. This review provides an up-to-date overview of MS-based applications for starfish and sea cucumber bioactive compounds analysis. While describing most characteristic features of MS-based approaches in the context of starfish and sea cucumber metabolites, including sample preparation and MS analysis steps, the present paper mainly focuses on the application of MS-based metabolic profiling of polar steroid compounds, triterpene glycosides, and lipids. The application of MS in metabolomics studies is also outlined. Full article

(This article belongs to the Special Issue Echinoderms Metabolites: Structure, Functions and Biomedical Perspectives II)

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22 pages, 6680 KiB

Open AccessArticle

The Inhibitors of CDK4/6 from a Library of Marine Compound Database: A Pharmacophore, ADMET, Molecular Docking and Molecular Dynamics Study

by Lianxiang Luo, Qu Wang and Yinglin Liao

Mar. Drugs 2022, 20(5), 319; https://doi.org/10.3390/md20050319 - 12 May 2022

Cited by 7 | Viewed by 2544

Abstract

Background: CDK4/6 (Cyclin-dependent kinases 4/6) are the key promoters of cell cycle transition from G1 phase to S phase. Thus, selective inhibition of CDK4/6 is a promising cancer treatment. Methods: A total of 52,765 marine natural products were screened for CDK4/6. To screen [...] Read more.

Background: CDK4/6 (Cyclin-dependent kinases 4/6) are the key promoters of cell cycle transition from G1 phase to S phase. Thus, selective inhibition of CDK4/6 is a promising cancer treatment. Methods: A total of 52,765 marine natural products were screened for CDK4/6. To screen out better natural compounds, pharmacophore models were first generated, then the absorption, distribution, metabolism, elimination, and toxicity (ADMET) were tested, followed by molecular docking. Finally, molecular dynamics simulation was carried out to verify the binding characteristics of the selected compounds. Results: Eighty-seven marine small molecules were screened based on the pharmacophore model. Then, compounds 41369 and 50843 were selected according to the ADMET and molecular docking score for further kinetic simulation evaluation. Finally, through molecular dynamics analysis, it was confirmed that compound 50843 maintained a stable conformation with the target protein, so it has the opportunity to become an inhibitor of CDK4/6. Conclusion: Through structure-based pharmacophore modeling, ADMET, the molecular docking method and molecular dynamics (MD) simulation, marine natural compound 50843 was proposed as a promising marine inhibitor of CDK4/6. Full article

(This article belongs to the Special Issue Marine Drug Research in China: Selected Papers from the 15-NASMD Conference)

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23 pages, 1547 KiB

Open AccessArticle

In Vivo Nutritional Assessment of the Microalga Nannochloropsis gaditana and Evaluation of the Antioxidant and Antiproliferative Capacity of Its Functional Extracts

by Rosario Martínez, Alejandro García-Beltrán, Garyfallia Kapravelou, Cristina Mesas, Laura Cabeza, Gloria Perazzoli, Palmira Guarnizo, Alberto Rodríguez-López, Roberto Andrés Vallejo, Milagros Galisteo, Pilar Aranda, Jose Prados, María López-Jurado, Consolación Melguizo and Jesus M. Porres

Mar. Drugs 2022, 20(5), 318; https://doi.org/10.3390/md20050318 - 11 May 2022

Cited by 7 | Viewed by 2613

Abstract

Nannochloropsis gaditana is a microalga with interesting nutritional and functional value due to its high content of protein, polyunsaturated fatty acids, and bioactive compounds. However, the hardness of its cell wall prevents accessibility to these components. This work aimed to study the effect [...] Read more.

Nannochloropsis gaditana is a microalga with interesting nutritional and functional value due to its high content of protein, polyunsaturated fatty acids, and bioactive compounds. However, the hardness of its cell wall prevents accessibility to these components. This work aimed to study the effect of a treatment to increase the fragility of the cell wall on the bioavailability of its nutrients and functional compounds. The antioxidant and antiproliferative capacity of functional extracts from treated and untreated N. gaditana was assessed, and the profile of bioactive compounds was characterized. Furthermore, to study the effect of treatment on its nutrient availability and functional capacity, an in vivo experiment was carried out using a rat experimental model and a 20% dietary inclusion level of microalgae. Functional extracts from treated N. gaditana exhibited higher antioxidant activity than the untreated control. Furthermore, the treated microalga induced hypoglycemic action, higher nitrogen digestibility, and increased hepatic antioxidant activity. In conclusion, N. gaditana has interesting hepatoprotective, antioxidant, and anti-inflammatory potential, thus proving itself an ideal functional food candidate, especially if the microalga is treated to increase the fragility of its cell wall before consumption. Full article

(This article belongs to the Special Issue In Vitro and In Vivo Approaches to Study Potential Marine Drugs II)

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16 pages, 1207 KiB

Open AccessReview

Bioactive Peptides from Algae: Traditional and Novel Generation Strategies, Structure-Function Relationships, and Bioinformatics as Predictive Tools for Bioactivity

by Jack O’Connor, Marco Garcia-Vaquero, Steve Meaney and Brijesh Kumar Tiwari

Mar. Drugs 2022, 20(5), 317; https://doi.org/10.3390/md20050317 - 10 May 2022

Cited by 18 | Viewed by 5088

Abstract

Over the last decade, algae have been explored as alternative and sustainable protein sources for a balanced diet and more recently, as a potential source of algal-derived bioactive peptides with potential health benefits. This review will focus on the emerging processes for the [...] Read more.

Over the last decade, algae have been explored as alternative and sustainable protein sources for a balanced diet and more recently, as a potential source of algal-derived bioactive peptides with potential health benefits. This review will focus on the emerging processes for the generation and isolation of bioactive peptides or cryptides from algae, including: (1) pre-treatments of algae for the extraction of protein by physical and biochemical methods; and (2) methods for the generation of bioactive including enzymatic hydrolysis and other emerging methods. To date, the main biological properties of the peptides identified from algae, including anti-hypertensive, antioxidant and anti-proliferative/cytotoxic effects (for this review, anti-proliferative/cytotoxic will be referred to by the term anti-cancer), assayed in vitro and/or in vivo, will also be summarized emphasizing the structure–function relationship and mechanism of action of these peptides. Moreover, the use of in silico methods, such as quantitative structural activity relationships (QSAR) and molecular docking for the identification of specific peptides of bioactive interest from hydrolysates will be described in detail together with the main challenges and opportunities to exploit algae as a source of bioactive peptides. Full article

(This article belongs to the Special Issue Novel Applications and Technologies for the Industrial Exploitation of Algal Derived Marine Bioactives as Nutraceuticals or Pharmaceuticals)

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10 pages, 2214 KiB

Open AccessArticle

Inhibition of Lipopolysaccharide-Induced Inflammatory Signaling by Soft Coral-Derived Prostaglandin A₂ in RAW264.7 Cells

by Osamu Ohno, Eika Mizuno, Junichiro Miyamoto, Tomoyuki Hoshina, Takuya Sano and Kenji Matsuno

Mar. Drugs 2022, 20(5), 316; https://doi.org/10.3390/md20050316 - 09 May 2022

Cited by 1 | Viewed by 2063

Abstract

Lipopolysaccharide (LPS) is a component of the outer membrane of Gram-negative bacteria and causes inflammatory diseases. We searched MeOH extracts of collected marine organisms for inhibitors of LPS-induced nitric oxide (NO) production in RAW264.7 cells and identified prostaglandin A₂ (PGA₂) [...] Read more.

Lipopolysaccharide (LPS) is a component of the outer membrane of Gram-negative bacteria and causes inflammatory diseases. We searched MeOH extracts of collected marine organisms for inhibitors of LPS-induced nitric oxide (NO) production in RAW264.7 cells and identified prostaglandin A₂ (PGA₂) as an active compound from the MeOH extract of the soft coral Lobophytum sp. PGA₂ inhibited the production of NO and reduced the expression of inducible NO synthase (iNOS) in LPS-stimulated RAW264.7 cells. Although short preincubation with PGA₂ did not inhibit LPS-induced degradation and resynthesis of IκBα, the suppressive effect of PGA₂ was observed only after a prolonged incubation period prior to LPS treatment. In addition, PGA₂-inhibited NO production was negated by the addition of the EP4 antagonist L161982. Thus, PGA₂ was identified as an inhibitor of LPS-induced inflammatory signaling in RAW264.7 cells. Full article

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21 pages, 6084 KiB

Open AccessArticle

BDDE-Inspired Chalcone Derivatives to Fight Bacterial and Fungal Infections

by Ana Jesus, Fernando Durães, Nikoletta Szemerédi, Joana Freitas-Silva, Paulo Martins da Costa, Eugénia Pinto, Madalena Pinto, Gabriella Spengler, Emília Sousa and Honorina Cidade

Mar. Drugs 2022, 20(5), 315; https://doi.org/10.3390/md20050315 - 08 May 2022

Cited by 6 | Viewed by 3701

Abstract

The growing number of infectious diseases around the world threatens the effective response of antibiotics, contributing to the increase in antibiotic resistance seen as a global health problem. Currently, one of the main challenges in antimicrobial drug discovery is the search for new [...] Read more.

The growing number of infectious diseases around the world threatens the effective response of antibiotics, contributing to the increase in antibiotic resistance seen as a global health problem. Currently, one of the main challenges in antimicrobial drug discovery is the search for new compounds that not only exhibit antimicrobial activity, but can also potentiate the antimicrobial activity and revert antibiotics’ resistance, through the interference with several mechanisms, including the inhibition of efflux pumps (EPs) and biofilm formation. Inspired by macroalgae brominated bromophenol BDDE with antimicrobial activity, a series of 18 chalcone derivatives, including seven chalcones (9–15), six dihydrochalcones (16–18, and 22–24) and five diarylpropanes (19–21, and 25 and 26), was prepared and evaluated for its antimicrobial activity and potential to fight antibiotic resistance. Among them, chalcones 13 and 14 showed promising antifungal activity against the dermatophyte clinical strain of Trichophyton rubrum, and all compounds reversed the resistance to vancomycin in Enterococcus faecalis B3/101, with 9, 14, and 24 able to cause a four-fold decrease in the MIC of vancomycin against this strain. Compounds 17–24 displayed inhibition of EPs and the formation of biofilm by S. aureus 272123, suggesting that these compounds are inhibiting the EPs responsible for the extrusion of molecules involved in biofilm-related mechanisms. Interestingly, compounds 17–24 did not show cytotoxicity in mouse embryonic fibroblast cell lines (NIH/3T3). Overall, the results obtained suggest the potential of dihydrochalcones 16–18 and 22–24, and diarylpropanes 19–21, 25 and 26, as hits for bacterial EPs inhibition, as they are effective in the inhibition of EPs, but present other features that are important in this matter, such as the lack of antibacterial activity and cytotoxicity. Full article

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

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38 pages, 4439 KiB

Open AccessReview

Marine Biopolymers as Bioactive Functional Ingredients of Electrospun Nanofibrous Scaffolds for Biomedical Applications

by Konstantina Iliou, Stefanos Kikionis, Efstathia Ioannou and Vassilios Roussis

Mar. Drugs 2022, 20(5), 314; https://doi.org/10.3390/md20050314 - 05 May 2022

Cited by 21 | Viewed by 4147

Abstract

Marine biopolymers, abundantly present in seaweeds and marine animals, feature diverse structures and functionalities, and possess a wide range of beneficial biological activities. Characterized by high biocompatibility and biodegradability, as well as unique physicochemical properties, marine biopolymers are attracting a constantly increasing interest [...] Read more.

Marine biopolymers, abundantly present in seaweeds and marine animals, feature diverse structures and functionalities, and possess a wide range of beneficial biological activities. Characterized by high biocompatibility and biodegradability, as well as unique physicochemical properties, marine biopolymers are attracting a constantly increasing interest for the development of advanced systems for applications in the biomedical field. The development of electrospinning offers an innovative technological platform for the production of nonwoven nanofibrous scaffolds with increased surface area, high encapsulation efficacy, intrinsic interconnectivity, and structural analogy to the natural extracellular matrix. Marine biopolymer-based electrospun nanofibrous scaffolds with multifunctional characteristics and tunable mechanical properties now attract significant attention for biomedical applications, such as tissue engineering, drug delivery, and wound healing. The present review, covering the literature up to the end of 2021, highlights the advancements in the development of marine biopolymer-based electrospun nanofibers for their utilization as cell proliferation scaffolds, bioadhesives, release modifiers, and wound dressings. Full article

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11 pages, 1500 KiB

Open AccessArticle

Balenine, Imidazole Dipeptide Promotes Skeletal Muscle Regeneration by Regulating Phagocytosis Properties of Immune Cells

by Min Yang, Luchuanyang Sun, Yasunosuke Kawabata, Fumihito Murayama, Takahiro Maegawa, Takeshi Nikawa and Katsuya Hirasaka

Mar. Drugs 2022, 20(5), 313; https://doi.org/10.3390/md20050313 - 05 May 2022

Cited by 1 | Viewed by 2661

Abstract

Balenine is one of the endogenous imidazole dipeptides derived from marine products. It is composed of beta-alanine and 3-methyl-L-histidine, which exist mainly in the muscles of marine organisms. The physiological functions of dietary balenine are not well-known. In this study, we investigated whether [...] Read more.

Balenine is one of the endogenous imidazole dipeptides derived from marine products. It is composed of beta-alanine and 3-methyl-L-histidine, which exist mainly in the muscles of marine organisms. The physiological functions of dietary balenine are not well-known. In this study, we investigated whether the supplementation of dietary balenine was associated with muscle function in a cardiotoxin-indued muscle degeneration/regeneration model. Through morphological observation, we found that the supplementation of balenine-enriched extract promoted the regeneration stage. In addition, the expression of regeneration-related myogenic marker genes, such as paired box protein 7, MyoD1, myogenin, and Myh3, in a group of mice fed a balenine-enriched extract diet was higher than that in a group fed a normal diet. Moreover, the supplementation of balenine-enriched extract promoted the expression of anti-inflammatory cytokines as well as pro-inflammatory cytokines at the degeneration stage. Interestingly, phagocytic activity in the balenine group was significantly higher than that in the control group in vitro. These results suggest that balenine may promote the progress of muscle regeneration by increasing the phagocytic activity of macrophages. Full article

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17 pages, 6281 KiB

Open AccessArticle

Monkfish Peptides Mitigate High Fat Diet-Induced Hepatic Steatosis in Mice

by Jiena Ye, Xiaoxiao Tian, Qiongfen Wang, Jiawen Zheng, Yanzhuo Yang, Baogui Xu, Shuai Zhang, Falei Yuan and Zuisu Yang

Mar. Drugs 2022, 20(5), 312; https://doi.org/10.3390/md20050312 - 05 May 2022

Cited by 12 | Viewed by 2796

Abstract

Non-alcoholic fatty liver disease (NAFLD) is a hepatic metabolic syndrome usually accompanied by fatty degeneration and functional impairment. The aim of the study was to determine whether monkfish peptides (LPs) could ameliorate high-fat diet (HFD)-induced NAFLD and its underlying mechanisms. NAFLD was induced [...] Read more.

Non-alcoholic fatty liver disease (NAFLD) is a hepatic metabolic syndrome usually accompanied by fatty degeneration and functional impairment. The aim of the study was to determine whether monkfish peptides (LPs) could ameliorate high-fat diet (HFD)-induced NAFLD and its underlying mechanisms. NAFLD was induced in mice by giving them an HFD for eight weeks, after which LPs were administered in various dosages. In comparison to the HFD control group: body weight in the LP-treated groups decreased by 23–28%; triacylglycerol levels in the blood decreased by 16–35%; and low-density lipoproteins levels in the blood decreased by 23–51%. Additionally, we found that LPs elevated the activity of hepatic antioxidant enzymes and reduced the inflammatory reactions within fatty liver tissue. Investigating the effect on metabolic pathways, we found that in LP-treated mice: the levels of phospho-AMP-activated protein kinase (p-AMPK), and phospho-acetyl CoA carboxylase (p-ACC) in the AMP-activated protein kinase (AMPK) pathway were up-regulated and the levels of downstream sterol regulatory element-binding transcription factor 1 (SREBP-1) were down-regulated; lipid oxidation increased and free fatty acid (FFA) accumulation decreased (revealed by the increased carnitine palmitoyltransferase-1 (CPT-1) and the decreased fatty acid synthase (FASN) expression, respectively); the nuclear factor erythroid-2-related factor 2 (Nrf2) antioxidant pathway was activated; and the levels of heme oxygenase-1 (HO-1) and nicotinamide quinone oxidoreductase 1 (NQO1) were increased. Overall, all these findings demonstrated that LPs can improve the antioxidant capacity of liver to alleviate NAFLD progression mainly through modulating the AMPK and Nrf2 pathways, and thus it could be considered as an effective candidate in the treatment of human NAFLD. Full article

(This article belongs to the Special Issue Marine Bioactive Peptides—Structure, Function, and Application)

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2 pages, 434 KiB

Open AccessEditorial

Chasing Chances in a Changing Sea

by Ernesto Mollo

Mar. Drugs 2022, 20(5), 311; https://doi.org/10.3390/md20050311 - 03 May 2022

Cited by 1 | Viewed by 1662

Abstract

Bioactive marine natural products (BMNPs) of interest for applications as drugs, antimicrobials, cosmetics, nutraceuticals, or antifoulants, are often present in traces in producer organisms and often occur in threatened or endangered species, or in organisms playing key ecological roles [...] Full article

(This article belongs to the Special Issue Marine Invasive Species and Their Bioactive Metabolites)

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24 pages, 3249 KiB

Open AccessReview

Biodegradation and Prospect of Polysaccharide from Crustaceans

by Shuting Qiu, Shipeng Zhou, Yue Tan, Jiayao Feng, Yan Bai, Jincan He, Hua Cao, Qishi Che, Jiao Guo and Zhengquan Su

Mar. Drugs 2022, 20(5), 310; https://doi.org/10.3390/md20050310 - 02 May 2022

Cited by 10 | Viewed by 3329

Abstract

Marine crustacean waste has not been fully utilized and is a rich source of chitin. Enzymatic degradation has attracted the wide attention of researchers due to its unique biocatalytic ability to protect the environment. Chitosan (CTS) and its derivative chitosan oligosaccharides (COSs) with [...] Read more.

Marine crustacean waste has not been fully utilized and is a rich source of chitin. Enzymatic degradation has attracted the wide attention of researchers due to its unique biocatalytic ability to protect the environment. Chitosan (CTS) and its derivative chitosan oligosaccharides (COSs) with various biological activities can be obtained by the enzymatic degradation of chitin. Many studies have shown that chitosan and its derivatives, chitosan oligosaccharides (COSs), have beneficial properties, including lipid-lowering, anti-inflammatory and antitumor activities, and have important application value in the medical treatment field, the food industry and agriculture. In this review, we describe the classification, biochemical characteristics and catalytic mechanisms of the major degrading enzymes: chitinases, chitin deacetylases (CDAs) and chitosanases. We also introduced the technology for enzymatic design and modification and proposed the current problems and development trends of enzymatic degradation of chitin polysaccharides. The discussion on the characteristics and catalytic mechanism of chitosan-degrading enzymes will help to develop new types of hydrolases by various biotechnology methods and promote their application in chitosan. Full article

(This article belongs to the Special Issue Marine Oligosaccharides and Polysaccharides 2.0)

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18 pages, 1202 KiB

Open AccessArticle

Valorization of Side Stream Products from Sea Cage Fattened Bluefin Tuna (Thunnus thynnus): Production and In Vitro Bioactivity Evaluation of Enriched ω-3 Polyunsaturated Fatty Acids

by Concetta Maria Messina, Rosaria Arena, Simona Manuguerra, Laura La Barbera, Eleonora Curcuraci, Giuseppe Renda and Andrea Santulli

Mar. Drugs 2022, 20(5), 309; https://doi.org/10.3390/md20050309 - 30 Apr 2022

Cited by 7 | Viewed by 2456

Abstract

The valorization of side streams from fishery and aquaculture value-chains is a valuable solution to address one of the challenges of the circular economy: turning wastes into profit. Side streams produced after filleting of sea cage fattened bluefin tuna (Thunnus thynnus) [...] Read more.

The valorization of side streams from fishery and aquaculture value-chains is a valuable solution to address one of the challenges of the circular economy: turning wastes into profit. Side streams produced after filleting of sea cage fattened bluefin tuna (Thunnus thynnus) were analyzed for proximate composition and fatty acid profile to evaluate the possibility of producing tuna oil (TO) as a valuable source of ω-3 polyunsaturated fatty acids (PUFA) and testing its bioactivity in vitro. Ethyl esters of total fatty acids (TFA), obtained from TO, were pre-enriched by urea complexation (PUFA-Ue) and then enriched by short path distillation (SPD) up to almost 85% of the PUFA fraction (PUFA-SPe). The bioactivity of TFA, PUFA-SPe, and ethyl esters of depleted PUFA (PUFA-SPd) were tested in vitro, through analysis of lipid metabolism genes, in gilthead sea bream (Sparus aurata) fibroblast cell line (SAF-1) exposed to oils. TFA and PUFA-SPd upregulated transcription factors (pparβ and pparγ) and lipid metabolism-related genes (D6D, fas, fabp, fatp1, and cd36), indicating the promotion of adipogenesis. PUFA-SPe treated cells were similar to control. PUFA-SPe extracted from farmed bluefin tuna side streams could be utilized in fish feed formulations to prevent excessive fat deposition, contributing to improving both the sustainability of aquaculture and the quality of its products. Full article

(This article belongs to the Special Issue Fishery Discards, Processing Waste and Marine By-Products Valorization in the Era of Zero Waste: From Discovery to Profit 2.0)

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Mar. Drugs, Volume 20, Issue 5 (May 2022) – 66 articles

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