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Theme Issue Honoring Professor Peter Proksch’s 70th Birthday: Bioactive Compounds from Nature Products

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (31 December 2023) | Viewed by 7962

Special Issue Editors


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Guest Editor
Institute of Pharmaceutical Biology and Biotechnology, Heinrich Heine University, 40225 Düsseldorf, Germany
Interests: structure–activity relationships; anti-inflammatory natural products; drug discovery; molecular pharmacological mechanisms; tumor microenvironment; drug resistance
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Guest Editor
State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China
Interests: bioactive metabolites derived from marine organisms (sponges and corals); marine mangrove plants and their associated microorganisms
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Prof. Dr. Peter Proksch is an eminent biologist in the field of marine natural product chemistry. Throughout his career, he has devoted over 20 years to research and teaching at Heinrich Heine University in Düsseldorf. His research interests cover several aspects of marine natural product chemistry, including marine chemical ecology, bioactive natural compounds with unique structures derived from marine macro- and microorganisms, OSMAC and co-culture of marine-derived fungi to activate silent biosynthetic pathways, and the mode of action of bioactive compounds. He is engaged in the field of bioactive marine natural substances, which have potential for pharmaceutical and agriculture applications. During the early stages of his research career, he focused on marine invertebrates such as sponges and corals, which are regarded to be unique sources of chemical entities with potential bioactivities that could lead to the development of new drug candidates and serve as a powerful chemical defense against a multitude of natural enemies and competitors. His research group is highly productive, having discovered numerous bioactive compounds with structural diversity from benthic organisms inhabiting different ocean locations. Representative works include his discovery of sponge-derived brominated isoxazoline alkaloids and amide dienons that enzymatically converted from aeroplysinin-1 in the wounded sponge, showing pronounced antibiotic activity against many Gram-positive and Gram-negative marine bacteria; brominated bastadins protecting sponges from overgrowth by fouling organisms such as barnacles and mollusks; and dibromohemibastadin (DBHB) preventing fouling by barnacles or mussels through the inhibition of a phenoloxidase in the marine environment. In the last few decades, prior to his retirement, he explored marine-derived fungi as sources of bioactive natural products, due to the fact that many bioactive compounds isolated from sponges or other marine invertebrates are in fact of microbial origin and live within multicellular hosts. He has uncovered several novel, diverse, fungi-derived natural products with potent bioactivities, such as fungus-derived chlorflavonin as a new antibacterial agent and inhibitor of tuberculosis pathogens and multiresistant strains with a new mode of action; phomoxanthone A, provoking apoptosis in various tumor cell lines, including platin-resistant cells; atropisomeric dihydroanthracenones as inhibitors of multiresistant Staphylococcus aureus; and embellicine A as a novel NF-κB inhibitor. Furthermore, he has focused on the effect of microbial cross-talk on natural product accumulation and developed a microbial co-cultivation methodology to induce cryptic natural products. He has also contributed toward the enhancement of constitutive present metabolites compared with axenic cultures. Prof. Proksch has supervised more than 80 international doctoral students and published more than 600 peer-reviewed original publications, review articles, and book chapters.

Prof. Dr. Peter Proksch was born in Leipzig in 1953, and studied biology in Cologne, where he received his doctorate, Master’s degree, and Bachelor’s degree in 1975–1980. After a research stay for two years (1980–1982) as a postdoctoral fellow at the University of California in Irvine (USA), he secured a position as an assistant professor in the field of biology and pharmaceutical biology at the University of Cologne and at the Technical University of Braunschweig in 1982–1989. He was employed as an associate professor for pharmaceutical biology at the University of Würzburg (1990–1999), and then was promoted to full professor and head of the Institute for Pharmaceutical Biology and Biotechnology at Heinrich Heine University Düsseldorf (Germany) until his retirement. Prof. Proksch has participated in international collaborations across a broad range of countries, including China, Indonesia, Vietnam, India, and Nigeria. Based on his excellent contributions to the field of marine natural product science and his international cooperation, he was given the National Friendship Award of the PRC (China) in 2016, the Qilu Friendship Award of Shandong Province (China) in 2014, the Coconut Island Commemorative Award (China) in 2017, an Honorary Doctorate from the University of Abuja (Nigeria) in 2017, a Commemorative Medal of the Vietnamese Academy of Sciences (Vietnam) in 2008, and the First Prize Inventor Award (North-Rhine Westfalia, Germany) in 2008. He has also received Honorary Professorships from both the Three Gorges University (China) (2015) and the Chinese Academy of Tropical Agricultural Science (2016),

Molecules is very pleased to host a Special Issue in honor of Prof. Peter Proksch for his 70th birthday. We invite scientists to submit original contributions to the Special Issue “Bioactive Compounds from Marine-derived Organisms: A Themed Issue in Honor of Professor Peter Proksch's 70th Birthday”. Potential topics include the isolation, structural elucidation, and bioassay of marine-derived compounds; the bio-catalysis and biosynthesis of marine natural products; marine chemoecology; and the synthesis of marine natural products, as well as their bioactivities and modes of action.

Prof. Dr. Nicole Teusch
Prof. Dr. Wenhan Lin
Guest Editors

Manuscript Submission Information

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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. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

  • marine organisms
  • bioactive compounds
  • biosynthesis
  • structure elucidation
  • bioassay

Published Papers (4 papers)

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Research

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14 pages, 3082 KiB  
Article
Structure Elucidation of Two Intriguing Neo-Debromoaplysiatoxin Derivatives from Marine Cyanobacterium Lyngbya sp. Showing Strong Inhibition of Kv1.5 Potassium Channel and Differential Cytotoxicity
by Zijun Chen, Na Chen, Peng Fu, Weiping Wang, Shilin Bian, Huihui Zhang, Sicheng Shen and Bingnan Han
Molecules 2023, 28(6), 2786; https://doi.org/10.3390/molecules28062786 - 20 Mar 2023
Cited by 3 | Viewed by 1498
Abstract
Two aplysiatoxin derivatives, neo-debromoaplysiatoxin I (1) and neo-debromoaplysiatoxin J (2), were isolated from marine cyanobacterium Lyngbya sp. collected from the South China Sea. Their structures including absolute configurations were assigned by spectroscopic analysis, in combination with GIAO NMR shift [...] Read more.
Two aplysiatoxin derivatives, neo-debromoaplysiatoxin I (1) and neo-debromoaplysiatoxin J (2), were isolated from marine cyanobacterium Lyngbya sp. collected from the South China Sea. Their structures including absolute configurations were assigned by spectroscopic analysis, in combination with GIAO NMR shift calculation and DP4+ analysis. Structures of neo-debromoaplysiatoxin I and neo-debromoaplysiatoxin J contained a decahydro-5H-pyrano [2,3,4-de] chromen-5-one 6/6/6 ring skeleton and an intriguing peroxide bridge group, respectively, which are unprecedented structure scaffold and motif in aplysiatoxins. Two compounds displayed comparable inhibitory activities against Kv1.5 K+ channel with IC50 values of 2.59 ± 0.37 μM (1) and 1.64 ± 0.15 μM (2); however, they presented differential cytotoxic effects. It is worth noting that neo-debromoaplysiatoxin J, containing a peroxide bridge, showed remarkable cytotoxicity against four cancer cell lines including SW480, SGC7901, LoVo and PC-9 compared to the human normal cell line. Full article
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17 pages, 4571 KiB  
Article
Monkfish (Lophius litulon) Peptides Ameliorate High-Fat-Diet-Induced Nephrotoxicity by Reducing Oxidative Stress and Inflammation via Regulation of Intestinal Flora
by Xiangyu Ren, Bingtao Miao, Hongjie Cao, Xiaoxiao Tian, Lujia Shen, Zuisu Yang, Falei Yuan and Yaping Ding
Molecules 2023, 28(1), 245; https://doi.org/10.3390/molecules28010245 - 28 Dec 2022
Cited by 9 | Viewed by 2186
Abstract
Background: Renal damage and intestinal flora imbalance due to lipotoxicity are particularly significant in terms of oxidative stress and inflammation, which can be alleviated with bioactive peptides. The monkfish (Lophius litulon) is rich in proteins, which can be used as a [...] Read more.
Background: Renal damage and intestinal flora imbalance due to lipotoxicity are particularly significant in terms of oxidative stress and inflammation, which can be alleviated with bioactive peptides. The monkfish (Lophius litulon) is rich in proteins, which can be used as a source of quality bioactive peptides. This study aimed to examine the protective effect of monkfish peptides on renal injury and their potential role in regulating gut microbiota. Methods: Monkfish meat was hydrolyzed using neutral protease and filtered, and the component with the highest elimination rate of 2,2-diphenyl-1-picrylhydrazyl was named lophius litulon peptides (LPs). Lipid nephrotoxicity was induced via high-fat diet (HFD) feeding for 8 weeks and then treated with LPs. Oxidative stress, inflammatory factors, and intestinal flora were evaluated. Results: LP (200 mg/kg) therapy reduced serum creatinine, uric acid, and blood urea nitrogen levels by 49.5%, 31.6%, and 31.6%, respectively. Renal vesicles and tubules were considerably improved with this treatment. Moreover, the activities of superoxide dismutase, glutathione peroxidase, and total antioxidant capacity increased significantly by 198.7%, 167.9%, 61.5%, and 89.4%, respectively. LPs attenuated the upregulation of HFD-induced Toll-like receptor 4 and phospho-nuclear factor-kappa B and increased the protein levels of heme oxygenase 1, nicotinamide quinone oxidoreductase 1, and nuclear factor erythroid 2-related factor 2. The dysbiosis of intestinal microbiota improved after LP treatment. Conclusions: LPs significantly improve antioxidant activity, reduce inflammatory cytokine levels, and regulate intestinal dysbiosis. Thus, LPs are potential compounds that can alleviate HFD-induced renal lipotoxicity. Full article
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7 pages, 1502 KiB  
Article
Marine-Based Candidates as Potential RSK1 Inhibitors: A Computational Study
by Mousa AlTarabeen, Qosay Al-Balas, Amgad Albohy, Werner Ernst Georg Müller and Peter Proksch
Molecules 2023, 28(1), 202; https://doi.org/10.3390/molecules28010202 - 26 Dec 2022
Cited by 1 | Viewed by 1442
Abstract
Manzamines are chemically related compounds extracted from the methanolic extract of Acanthostrongylophora ingens species. Seven compounds were identified by our research group and are being characterized. As their biological target is unknown, this work is based on previous screening work performed by Mayer [...] Read more.
Manzamines are chemically related compounds extracted from the methanolic extract of Acanthostrongylophora ingens species. Seven compounds were identified by our research group and are being characterized. As their biological target is unknown, this work is based on previous screening work performed by Mayer et al., who revealed that manzamine A could be an inhibitor of RSK1 kinase. Within this work, the RSK1 N-terminal kinase domain is exploited as a target for our work and the seven compounds are docked using Autodock Vina software. The results show that one of the most active compounds, Manzamine A N-oxide (5), with an IC50 = 3.1 μM, displayed the highest docking score. In addition, the compounds with docking scores lower than the co-crystalized ligand AMP-PCP (−7.5 and −8.0 kcal/mol) for ircinial E (1) and nakadomarin A (7) were found to be inferior in activity in the biological assay. The docking results successfully managed to predict the activities of four compounds, and their in silico results were in concordance with their biological data. The β-carboline ring showed noticeable receptor binding, which could explain its reported biological activities, while the lipophilic side of the compound was found to fit well inside the hydrophobic active site. Full article
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Review

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23 pages, 4579 KiB  
Review
Recent Advances of Marine Natural Indole Products in Chemical and Biological Aspects
by Haoyi Sun, Kangping Sun and Jingyong Sun
Molecules 2023, 28(5), 2204; https://doi.org/10.3390/molecules28052204 - 27 Feb 2023
Cited by 11 | Viewed by 2191
Abstract
The ocean has always been one of the important sources of natural products. In recent years, many natural products with different structures and biological activities have been obtained, and their value has been clearly recognized. Researchers have been deeply engaged in the field [...] Read more.
The ocean has always been one of the important sources of natural products. In recent years, many natural products with different structures and biological activities have been obtained, and their value has been clearly recognized. Researchers have been deeply engaged in the field of separation and extraction, derivative synthesis, structural studies, biological evaluation, and other fields of research for marine natural products. Thus, a series of marine indole natural products which have structural and biological prospect have caught our eyes. In this review, we summarize some of these marine indole natural products with relatively good pharmacological activity and research value, and discuss issues concerning chemistry, pharmacological activity, biological evaluation, and synthesis, including monomeric indoles, indole peptides, bis-indoles, and annelated indoles. Most of the compounds have cytotoxic, antiviral, antifungal, or anti-inflammatory activities. Full article
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