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Drugs from Marine Sources
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Drugs from Marine Sources

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Chemical and Molecular Sciences".

Deadline for manuscript submissions: closed (30 June 2021) | Viewed by 25475

Printed Edition Available!
A printed edition of this Special Issue is available here.

Special Issue Editors

Dr. Genoveffa Nuzzo

E-Mail Website
Guest Editor
Bio-Organic Chemistry Unit, Institute of Biomolecular Chemistry, Consiglio Nazionale delle Ricerche, Via Campi Flegrei 34, Pozzuoli, 80078 Naples, Italy
Interests: marine natural products; drug disovery; medicinal chemistry; structure elucidation; qualitative and quantitative analysis of organic compounds; lipids
Special Issues, Collections and Topics in MDPI journals
Dr. Carmela Gallo

E-Mail Website
Co-Guest Editor
Institute of Biomolecular Chemistry, Cnr Via Campi Flegrei 34, Comprensorio Olivetti, 80078 Pozzuoli, Italy
Interests: immunology; natural product drug discovery; cell biology; inflammation; microalgae
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Marine natural products represent a unique rich source of new metabolites, with diverse chemical structures, and various bioactivities and molecular characteristics adapted to specific interactions with cellular targets. These compounds, as new leads for drug discovery and development, are attractive targets because they could represent the challenge for the treatment of a high number of diseases that affect human health.

This Special Issue will cover all fields of drugs research from marine natural products, in vitro and/or in vivo biological activities, also including their isolation, structure characterization, mechanisms of action, medicinal applications as well as synthetic approaches towards them and related analogues.

Dr. Genoveffa Nuzzo
Dr. Carmela Gallo
Guest Editors

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Keywords

  • marine natural products
  • bioactive secondary metabolites
  • drug discovery
  • drug carrier
  • drug development
  • nuclear magnetic resonance
  • mass spectrometry
  • biological assay
  • high throughput screening
  • bioassay guided-fractionation

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Published Papers (7 papers)

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Editorial

Jump to: Research, Review

2 pages, 168 KiB  
Editorial
Drugs from Marine Sources
by Carmela Gallo and Genoveffa Nuzzo
Appl. Sci. 2021, 11(24), 12115; https://doi.org/10.3390/app112412115 - 20 Dec 2021
Viewed by 1995
Abstract
Throughout history, natural products have afforded a rich source of compounds that have found many applications in the fields of pharmacology [...] Full article
(This article belongs to the Special Issue Drugs from Marine Sources)

Research

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9 pages, 11966 KiB  
Article
Chemical Investigation of Diketopiperazines and N-Phenethylacetamide Isolated from Aquimarina sp. MC085 and Their Effect on TGF-β-Induced Epithelial–Mesenchymal Transition
by Myong Jin Lee, Geum Jin Kim, Myoung-Sook Shin, Jimin Moon, Sungjin Kim, Joo-Won Nam, Ki Sung Kang and Hyukjae Choi
Appl. Sci. 2021, 11(19), 8866; https://doi.org/10.3390/app11198866 - 23 Sep 2021
Cited by 9 | Viewed by 1953
Abstract
Chemical investigations of Aquimarina sp. MC085, which suppressed TGF-β-induced epithelial–mesenchymal transition (EMT) in A549 human lung cancer cells, led to the isolation of compounds 1–3. Structural characterization using spectroscopic data analyses in combination with Marfey’s analysis revealed that they were [...] Read more.
Chemical investigations of Aquimarina sp. MC085, which suppressed TGF-β-induced epithelial–mesenchymal transition (EMT) in A549 human lung cancer cells, led to the isolation of compounds 1–3. Structural characterization using spectroscopic data analyses in combination with Marfey’s analysis revealed that they were two diketopiperazines [cyclo(l-Pro-l-Leu) (1) and cyclo(l-Pro-l-Ile) (2)] and one N-phenethylacetamide (3). Cyclo(l-Pro-l-Leu) (1) and N-phenethylactamide (3) inhibited the TGF-β/Smad pathway and suppressed the metastasis of A549 cells by affecting TGF-β-induced EMT. However, cyclo(l-Pro-l-Ile) (2) downregulated mesenchymal factors via a non-Smad-mediated signaling pathway. Full article
(This article belongs to the Special Issue Drugs from Marine Sources)
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18 pages, 3115 KiB  
Article
Wound Healing and Antioxidant Evaluations of Alginate from Sargassum ilicifolium and Mangosteen Rind Combination Extracts on Diabetic Mice Model
by Pugar Arga Cristina Wulandari, Zulfa Nailul Ilmi, Saikhu Akhmad Husen, Dwi Winarni, Mochammad Amin Alamsjah, Khalijah Awang, Marco Vastano, Alessandro Pellis, Duncan MacQuarrie and Pratiwi Pudjiastuti
Appl. Sci. 2021, 11(10), 4651; https://doi.org/10.3390/app11104651 - 19 May 2021
Cited by 9 | Viewed by 3811
Abstract
A diabetic foot ulcer is an open wound that can become sore and frequently occurs in diabetic patients. Alginate has the ability to form a hydrophilic gel when in contact with a wound surface in diabetic patients. Xanthones are the main compounds of [...] Read more.
A diabetic foot ulcer is an open wound that can become sore and frequently occurs in diabetic patients. Alginate has the ability to form a hydrophilic gel when in contact with a wound surface in diabetic patients. Xanthones are the main compounds of mangosteen rind and have antibacterial and anti-inflammatory properties. The purpose of this research was to evaluate the wound healing and antioxidants assay with a combination of alginate from S. ilicifolium and mangosteen rind combination extracts on a diabetic mice model. The characterization of alginate was carried out by size exclusion chromatography with multiple angle laser light scattering (SEC-MALLS) and thermogravimetric analysis (TGA). The M/G ratio of alginate was calculated by using proton nuclear magnetic resonance (1H NMR). The antioxidant activity of mangosteen rind and the combination extracts was determined using the DPPH method. The observed parameters were wound width, number of neutrophils, macrophages, fibrocytes, fibroblasts, and collagen densities. The 36 male mice were divided into 12 groups including non-diabetic control (NC), diabetes alginate (DA), alginate–mangosteen (DAM), and diabetes control (DC) groups in three different groups by a histopathology test on skin tissue. The treatment was carried out for 14 days and mice were evaluated on Days 3, 7, and 14. The SEC-MALLS results showed that the molecular weight and dispersity index (Ð) of alginate were 2.77 × 104 Dalton and 1.73, respectively. The M/G ratio of alginate was 0.77 and described as single-stage decomposition based on TGA. Alginate, mangosteen rind extract, and their combination were divided into weak, medium, and strong antioxidant, respectively. The treatment of the DA and DAM groups showed a decrease in wound width and an increase in the number of fibrocytes, fibroblasts, and macrophages. The number of neutrophils decreased while the percentage of collagen densities increased for all the considered groups. Full article
(This article belongs to the Special Issue Drugs from Marine Sources)
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9 pages, 1415 KiB  
Article
UHPLC-MS Method for the Analysis of the Molecular Adjuvant Sulfavant A
by Genoveffa Nuzzo, Emiliano Manzo, Marcello Ziaco, Laura Fioretto, Ana Margarida Campos, Carmela Gallo, Giuliana d’Ippolito and Angelo Fontana
Appl. Sci. 2021, 11(4), 1451; https://doi.org/10.3390/app11041451 - 5 Feb 2021
Cited by 1 | Viewed by 3027
Abstract
A fast and sensitive method that is based on Ultra High Performance Liquid Chromatography coupled with High Resolution Mass Spectrometry (UHPLC-HRMS) for the measurement of Sulfavant A, a molecular adjuvant with a sulfolipid skeleton, is described. The method has been validated over the [...] Read more.
A fast and sensitive method that is based on Ultra High Performance Liquid Chromatography coupled with High Resolution Mass Spectrometry (UHPLC-HRMS) for the measurement of Sulfavant A, a molecular adjuvant with a sulfolipid skeleton, is described. The method has been validated over the linearity range of 2.5–2000 ngmL−1 using a deuterated derivative (d70-Sulfavant A) as internal standard. Chromatographic separation is based on a UHPLC Kinetex® 2.6 µm PS C18 column and a gradient of methanol in 0.32 mM ammonium hydroxide solution buffered at pH 8. The lowest limit of quantification of Sulfavant A was 6.5 ngmL−1. The analytical procedure was tested on an extract of mice lung spiked with 30, 300, and 1500 ng of Sulfavant A. The analysis revealed a precision and accuracy value (as a mean value of all the quality control samples analyzed) of 4.7% and 96% in MeOH and 6.4% and 93.4% in the lung extracts, respectively. Full article
(This article belongs to the Special Issue Drugs from Marine Sources)
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20 pages, 7689 KiB  
Article
Characterization of Alginate from Sargassum duplicatum and the Antioxidant Effect of Alginate–Okra Fruit Extracts Combination for Wound Healing on Diabetic Mice
by Zulfa Nailul Ilmi, Pugar Arga Cristina Wulandari, Saikhu Akhmad Husen, Dwi Winarni, Mochammad Amin Alamsjah, Khalijah Awang, Marco Vastano, Alessandro Pellis, Duncan Macquarrie and Pratiwi Pudjiastuti
Appl. Sci. 2020, 10(17), 6082; https://doi.org/10.3390/app10176082 - 2 Sep 2020
Cited by 15 | Viewed by 4034
Abstract
Diabetes mellitus is a group of metabolic disorders characterized by high blood-glucose levels over a prolonged period that causes complications when an open wound is present. Alginate is an antioxidant and a good absorbent of exudates. Okra fruit contains flavonoids that can act [...] Read more.
Diabetes mellitus is a group of metabolic disorders characterized by high blood-glucose levels over a prolonged period that causes complications when an open wound is present. Alginate is an antioxidant and a good absorbent of exudates. Okra fruit contains flavonoids that can act as antioxidants. The antioxidant properties of extracts combination reduce blood-glucose levels significantly to accelerate the activities of wound-healing processes on diabetic mice. Alginate was characterized by Size Exclusion Chromatography-Multiple Angle Laser Light Scattering (SEC-MALLS), thermal stability and Proton Nuclear Magnetic Resonance (1H-NMR). The evaluation of wound healing on 36 male mice were divided into 12 groups including normal control (NC), diabetics control (DC), alginate (DA) and alginate–okra (DAO) groups in three different times by histopathology test on skin tissue. The results of SEC-MALLS analysis showed that alginate as single and homogeneous polysaccharide. The 1H-NMR spectrum showed that the mannuronate/guluronate ratio of the used alginate was 0.91. Alginate, okra fruit extract and their combination were classified as moderate and strong antioxidants. The numbers of fibrocytes, fibroblasts, collagen densities had significantly increased from three to seven days. In contrast, wound width, neutrophil, macrophages had significantly decreased at 14 days. The administration of extracts combination increased the re-epithelization of the wound area and wound-healing process on diabetic mice. Full article
(This article belongs to the Special Issue Drugs from Marine Sources)
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Review

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17 pages, 1331 KiB  
Review
Mini-Review: Potential of Diatom-Derived Silica for Biomedical Applications
by Angela Sardo, Ida Orefice, Sergio Balzano, Lucia Barra and Giovanna Romano
Appl. Sci. 2021, 11(10), 4533; https://doi.org/10.3390/app11104533 - 16 May 2021
Cited by 21 | Viewed by 6178
Abstract
Diatoms are unicellular eukaryotic microalgae widely distributed in aquatic environments, possessing a porous silica cell wall known as frustule. Diatom frustules are considered as a sustainable source for several industrial applications because of their high biocompatibility and the easiness of surface functionalisation, which [...] Read more.
Diatoms are unicellular eukaryotic microalgae widely distributed in aquatic environments, possessing a porous silica cell wall known as frustule. Diatom frustules are considered as a sustainable source for several industrial applications because of their high biocompatibility and the easiness of surface functionalisation, which make frustules suitable for regenerative medicine and as drug carriers. Frustules are made of hydrated silica, and can be extracted and purified both from living and fossil diatoms using acid treatments or high temperatures. Biosilica frustules have proved to be suitable for biomedical applications, but, unfortunately, they are not officially recognised as safe by governmental food and medical agencies yet. In the present review, we highlight the frustule formation process, the most common purification techniques, as well as advantages and bottlenecks related to the employment of diatom-derived silica for medical purposes, suggesting possible solutions for a large-scale biosilica production. Full article
(This article belongs to the Special Issue Drugs from Marine Sources)
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25 pages, 7758 KiB  
Review
Advances in Purpurin 18 Research: On Cancer Therapy
by Vladimíra Pavlíčková, Jan Škubník, Michal Jurášek and Silvie Rimpelová
Appl. Sci. 2021, 11(5), 2254; https://doi.org/10.3390/app11052254 - 4 Mar 2021
Cited by 10 | Viewed by 3553
Abstract
How to make cancer treatment more efficient and enhance the patient’s outcome? By multimodal therapy, theranostics, or personalized medicine? These are questions asked by scientists and doctors worldwide. However, finding new unique approaches and options for cancer treatment as well as new selective [...] Read more.
How to make cancer treatment more efficient and enhance the patient’s outcome? By multimodal therapy, theranostics, or personalized medicine? These are questions asked by scientists and doctors worldwide. However, finding new unique approaches and options for cancer treatment as well as new selective therapeutics is very challenging. More frequently, researchers “go back in time” and use already known and well-described compounds/drugs, the structure of which further derivatize to “improve” their properties, extend the use of existing drugs to new indications, or even to obtain a completely novel drug. Natural substances, especially marine products, are a great inspiration in the discovery and development of novel anticancer drugs. These can be used in many modern approaches, either as photo- and sonosensitizers in photodynamic and sonodynamic cancer therapy, respectively, or in tumor imaging and diagnosis. This review is focused on a very potent natural product, the chlorophyll metabolite purpurin 18, and its derivatives, which is well suitable for all the mentioned applications. Purpurin 18 can be easily isolated from green plants of all kinds ranging from seaweed to spinach leaves and, thus, it presents an economically feasible source for a very promising anticancer drug. Full article
(This article belongs to the Special Issue Drugs from Marine Sources)
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