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Special Issue "Natural Products from the Beibu Gulf of the South China Sea"

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

Deadline for manuscript submissions: 31 December 2023 | Viewed by 7619

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Dr. Xiaowei Luo

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Guest Editor

Institute of Marine Drugs, Guangxi Key Laboratory of Marine Drugs, Guangxi University of Chinese Medicine, Nanning, China
Interests: marine natural products; secondary metabolites
Special Issues, Collections and Topics in MDPI journals

Prof. Dr. Chenghai Gao
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Guest Editor

Institute of Marine Drugs, Guangxi Key Laboratory of Marine Drugs, Guangxi University of Chinese Medicine, Nanning, China
Interests: marine natural products

Prof. Dr. Xuefeng Zhou

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Guest Editor

Key Laboratory of Tropical Marine Bio-Resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, 164 West Xingang Road, Guangzhou 510301, China
Interests: marine natural product chemistry; drug leads; pharmacological mechanism; marine microorganisms; biotransformation
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The Beibu Gulf (Gulf of Tonkin) is located in the northwestern South China Sea. Vietnam lies to the west of the gulf, while China’s Guangxi Province and Hainan Island lie to the north and east of the gulf, respectively. This gulf harbors four representative marine ecosystems, including a coral reef, a mangrove forest, a seagrass bed, and coastal wetland ecosystems; these are rich in gas, oil, and biological resources, particularly where there is an abundant biodiversity of marine (micro-)organisms. There are few reports (< 150 references) on marine natural product (MNP) research in the Beibu Gulf. To our knowledge, approximately 1200 MNPs, including 500 novel ones, have been obtained from the Beibu Gulf (predominantly polyketides, terpenes, and alkaloids); these untapped and abundant biological resources could attract considerable interest from MNP chemists and marine biologists in the coming decades.

This Special Issue will focus on the investigation of novel and bioactive substances from the Beibu Gulf, including the following aspects:

Structurally new and bioactive natural products from marine macro- and microorganisms;
Structures and functions of marine biomacromolecules;
Efficacy and pharmacological mechanisms of MNPs;
Total synthesis, optimization or biosynthesis of bioactive or novel MNPs;
Marine medicinal biological resources research.

Dr. Xiaowei Luo
Prof. Dr. Chenghai Gao
Prof. Dr. Xuefeng Zhou
Guest Editors

Manuscript Submission Information

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

Beibu Gulf
marine natural products
marine biomacromolecules
marine bioactive compounds
biosynthetic pathway
pharmacological mechanism
marine biological resources

Published Papers (6 papers)

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Research

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Open AccessArticle

Design, Synthesis, and Anticancer Activity of Novel 3,6-Diunsaturated 2,5-Diketopiperazines

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Mar. Drugs 2023, 21(6), 325; https://doi.org/10.3390/md21060325 - 26 May 2023

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Abstract

Based on the marine natural products piperafizine B, XR334, and our previously reported compound 4m, fourteen novel 3,6-diunsaturated 2,5-diketopiperazine (2,5-DKP) derivatives (1, 2, 4–6, 8–16), together with two known ones (3 and 7), were designed and synthesized as anticancer agents against the A549 and Hela cell lines. The MTT assay results showed that the derivatives 6, 8–12, and 14 had moderate to good anticancer capacities, with IC₅₀ values ranging from 0.7 to 8.9 μM. Among them, compound 11, with naphthalen-1-ylmethylene and 2-methoxybenzylidene functions at the 3 and 6 positions of 2,5-DKP ring, respectively, displayed good inhibitory activities toward both A549 (IC₅₀ = 1.2 μM) and Hela (IC₅₀ = 0.7 μM) cancer cells. It could also induce apoptosis and obviously block cell cycle progression in the G2/M phases in both cells at 1.0 μM. The electron-withdrawing functions might not be favorable for the derivatives with high anticancer activities. Additionally, compared to piperafizine B and XR334, these semi-N-alkylated derivatives have high liposolubilities (>1.0 mg mL⁻¹). Compound 11 can be further developed, aiming at the discovery of a novel anticancer candidate. Full article

(This article belongs to the Special Issue Natural Products from the Beibu Gulf of the South China Sea)

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Open AccessArticle

Structural Elucidation of a Glucan from Trichaster palmiferus by Its Degraded Products and Preparation of Its Sulfated Derivative as an Anticoagulant

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Mar. Drugs 2023, 21(3), 148; https://doi.org/10.3390/md21030148 - 24 Feb 2023

Cited by 1 | Viewed by 838

Abstract

Echinoderms have been attracting increasing attention for their polysaccharides, with unique chemical structure and enormous potential for preparing drugs to treat diseases. In this study, a glucan (TPG) was obtained from the brittle star Trichaster palmiferus. Its structure was elucidated by physicochemical analysis and by analyzing its low-molecular-weight products as degraded by mild acid hydrolysis. The TPG sulfate (TPGS) was prepared, and its anticoagulant activity was investigated for potential development of anticoagulants. Results showed that TPG consisted of a consecutive α1,4–linked D-glucopyranose (D-Glcp) backbone together with a α1,4–linked D-Glcp disaccharide side chain linked through C-1 to C-6 of the main chain. The TPGS was successfully prepared with a degree of sulfation of 1.57. Anticoagulant activity results showed that TPGS significantly prolonged activated partial thromboplastin time, thrombin time, and prothrombin time. Furthermore, TPGS obviously inhibited intrinsic tenase, with an EC₅₀ value of 77.15 ng/mL, which was comparable with that of low-molecular-weight heparin (LMWH) (69.82 ng/mL). TPGS showed no AT-dependent anti-FIIa and anti-FXa activities. These results suggest that the sulfate group and sulfated disaccharide side chains play a crucial role in the anticoagulant activity of TPGS. These findings may provide some information for the development and utilization of brittle star resources. Full article

(This article belongs to the Special Issue Natural Products from the Beibu Gulf of the South China Sea)

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Open AccessArticle

Two New Alkaloids and a New Butenolide Derivative from the Beibu Gulf Sponge-Derived Fungus Penicillium sp. SCSIO 41413

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Mar. Drugs 2023, 21(1), 27; https://doi.org/10.3390/md21010027 - 29 Dec 2022

Cited by 3 | Viewed by 1574

Abstract

Marine sponge-derived fungi have been proven to be a prolific source of bioactive natural products. Two new alkaloids, polonimides E (1) and D (2), and a new butenolide derivative, eutypoid F (11), were isolated from the Beibu Gulf sponge-derived fungus, Penicillium sp. SCSIO 41413, together with thirteen known compounds (3–10, 12–16). Their structures were determined by detailed NMR, MS spectroscopic analyses, and electronic circular dichroism (ECD) analyses. Butenolide derivatives 11 and 12 exhibited inhibitory effect against the enzyme PI3K with IC₅₀ values of 1.7 μM and 9.8 μM, respectively. The molecular docking was also performed to understand the inhibitory activity, while 11 and 12 showed obvious protein/ligand-binding effects to the PI3K protein. Moreover, 4 and 15 displayed obvious inhibitory activity against LPS-induced NF-κB activation in RAW264.7 cells at 10 µM. Full article

(This article belongs to the Special Issue Natural Products from the Beibu Gulf of the South China Sea)

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Open AccessArticle

Biological Secondary Metabolites from the Lumnitzera littorea-Derived Fungus Penicillium oxalicum HLLG-13

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Mar. Drugs 2023, 21(1), 22; https://doi.org/10.3390/md21010022 - 27 Dec 2022

Cited by 2 | Viewed by 1358

Abstract

Five new compounds, including two cyclopiane diterpenes conidiogenones J and K (1–2), a steroid andrastin H (5), an alkaloid (Z)-4-(5-acetoxy-N-hydroxy-3-methylpent-2-enamido) butanoate (6), and an aliphatic acid (Z)-5-acetoxy-3-methylpent-2-enoic acid (7), together with ten known compounds (3–4 and 8–15) were isolated from the EtOAc extract of the fermentation broth of the Lumnitzera littorea-derived fungus Penicillium oxalicum HLLG-13. Their structures were elucidated by 1D, 2D NMR, and HR-ESI-MS spectral analyses. The absolute configurations of 1, 2, 5, and 8 were determined by quantum chemical electronic circular dichroism (ECD) calculations, and the absolute configuration of 8 was determined for the first time. Compound 15 was a new natural product, and its NMR data were reported for the first time. Compounds 5 and 9–14 exhibited antibacterial activities against Staphylococcus epidermidis and Candida albicans, with MIC values ranging from 6.25 to 25 μg/ mL. Compounds 1–6 and 9–14 showed significant growth inhibition activities against newly hatched Helicoverpa armigera Hubner larvae, with IC₅₀ values ranging from 50 to 200 μg/mL. Full article

(This article belongs to the Special Issue Natural Products from the Beibu Gulf of the South China Sea)

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Advances in Natural Products from the Marine-Sponge-Associated Microorganisms with Antimicrobial Activity in the Last Decade

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Mar. Drugs 2023, 21(4), 236; https://doi.org/10.3390/md21040236 - 12 Apr 2023

Cited by 2 | Viewed by 3195

Abstract

Microorganisms are the dominating source of food and nutrition for sponges and play an important role in sponge structure, chemical defense, excretion and evolution. In recent years, plentiful secondary metabolites with novel structures and specific activities have been identified from sponge-associated microorganisms. Additionally, as the phenomenon of the drug resistance of pathogenic bacteria is becoming more and more common, it is urgent to discover new antimicrobial agents. In this paper, we reviewed 270 secondary metabolites with potential antimicrobial activity against a variety of pathogenic strains reported in the literature from 2012 to 2022. Among them, 68.5% were derived from fungi, 23.3% originated from actinomycetes, 3.7% were obtained from other bacteria and 4.4% were discovered using the co-culture method. The structures of these compounds include terpenoids (13%), polyketides (51.9%), alkaloids (17.4%), peptides (11.5%), glucosides (3.3%), etc. Significantly, there are 124 new compounds and 146 known compounds, 55 of which have antifungal activity in addition to antipathogenic bacteria. This review will provide a theoretical basis for the further development of antimicrobial drugs. Full article

(This article belongs to the Special Issue Natural Products from the Beibu Gulf of the South China Sea)

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Marine Natural Products from the Beibu Gulf: Sources, Chemistry, and Bioactivities

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Mar. Drugs 2023, 21(2), 63; https://doi.org/10.3390/md21020063 - 19 Jan 2023

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Abstract

Marine natural products (MNPs) play an important role in the discovery and development of new drugs. The Beibu Gulf of South China Sea harbors four representative marine ecosystems, including coral reefs, mangroves, seaweed beds, and coastal wetlands, which are rich in underexplored marine biological resources that produce a plethora of diversified MNPs. In our ongoing efforts to discover novel and biologically active MNPs from the Beibu Gulf, we provide a systematic overview of the sources, chemical structures, and bioactive properties of a total of 477 new MNPs derived from the Beibu Gulf, citing 133 references and covering the literature from the first report in November 2003 up to September 2022. These reviewed MNPs were structurally classified into polyketides (43%), terpenoids (40%), nitrogen-containing compounds (12%), and glucosides (5%), which mainly originated from microorganisms (52%) and macroorganisms (48%). Notably, they were predominantly found with cytotoxic, antibacterial, and anti-inflammatory activities. This review will shed light on these untapped Beibu Gulf-derived MNPs as promising lead compounds for the development of new drugs. Full article

(This article belongs to the Special Issue Natural Products from the Beibu Gulf of the South China Sea)

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