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Marine Drugs
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Marine Bioactive Compound Discovery through OSMAC Approach
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Marine Bioactive Compound Discovery through OSMAC Approach

A special issue of Marine Drugs (ISSN 1660-3397). This special issue belongs to the section "Marine Biotechnology Related to Drug Discovery or Production".

Deadline for manuscript submissions: 31 August 2024 | Viewed by 7652

Special Issue Editor

Dr. Xiaoling Lu

E-Mail Website
Guest Editor
Department of Biochemistry and Molecular Biology, College of Basic Medical Sciences, Naval Medical University, Shanghai 200433, China
Interests: marine microorganisms; secondary metabolites; anticancer; action mechanism; biosynthetic pathway

Special Issue Information

Dear Colleagues,                

Marine microorganisms have proven to be a source of novel natural products with variety biological activities. However, because of the limitations of the traditional natural product mining methods, the number of gene clusters potentially encoding the production of natural products and the actual number of chemically characterized metabolites for a given microorganism are widely different.

In recent years, with the rapid development of gene sequencing technology and bioinformatics, cryptic metabolic pathways can be accessed using molecular techniques or cultivation-based approaches. The OSMAC approach (one strain—many compounds), based on modification of growth conditions, has proven to be a powerful strategy for the discovery of new cryptic natural products. The addition of chemical elicitors or epigenetic modifiers have also been used to activate silent genes.

This Special Issue invites articles from both molecular techniques or cultivation-based approaches on marine microorganisms with a focus on natural product discovery and characterization. We particularly welcome articles that combine genomic, metabolomic, and epigenetic approaches with OSMAC for the characterization of marine microorganism secondary metabolites.

Dr. Xiaoling Lu
Guest Editor

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

  • marine microorganisms
  • secondary metabolites
  • OSMAC
  • epigenetic
  • cryptic

Published Papers (5 papers)

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Research

10 pages, 678 KiB  
Article
Brominated Depsidones with Antibacterial Effects from a Deep-Sea-Derived Fungus Spiromastix sp.
by Zequan Huang, Dong Liu, Shang Chen, Jinwei Ren, Chenghai Gao, Zhiyong Li, Aili Fan and Wenhan Lin
Mar. Drugs 2024, 22(2), 78; https://doi.org/10.3390/md22020078 - 3 Feb 2024
Viewed by 1490
Abstract
Eleven new brominated depsidones, namely spiromastixones U-Z5 (1–11) along with five known analogues (12–16), were isolated from a deep-sea-derived fungus Spiromastix sp. through the addition of sodium bromide during fermentation. Their structures were elucidated by [...] Read more.
Eleven new brominated depsidones, namely spiromastixones U-Z5 (1–11) along with five known analogues (12–16), were isolated from a deep-sea-derived fungus Spiromastix sp. through the addition of sodium bromide during fermentation. Their structures were elucidated by extensive analysis of the spectroscopic data including high-resolution MS and 1D and 2D NMR data. Compounds 6–10 and 16 exhibited significant inhibition against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VRE) with MIC values ranging from 0.5 to 2.0 μM. Particularly, tribrominated 7 displayed the strongest activity against MRSA and VRE with a MIC of 0.5 and 1.0 μM, respectively, suggesting its potential for further development as a new antibacterial agent. Full article
(This article belongs to the Special Issue Marine Bioactive Compound Discovery through OSMAC Approach)
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15 pages, 2530 KiB  
Article
OSMAC-Based Discovery and Biosynthetic Gene Clusters Analysis of Secondary Metabolites from Marine-Derived Streptomyces globisporus SCSIO LCY30
by Yanqing Li, Naying Gong, Le Zhou, Zhijie Yang, Hua Zhang, Yucheng Gu, Junying Ma and Jianhua Ju
Mar. Drugs 2024, 22(1), 21; https://doi.org/10.3390/md22010021 - 28 Dec 2023
Viewed by 1872
Abstract
The one strain many compounds (OSMAC) strategy is an effective method for activating silent gene clusters by cultivating microorganisms under various conditions. The whole genome sequence of the marine-derived strain Streptomyces globisporus SCSIO LCY30 revealed that it contains 30 biosynthetic gene clusters (BGCs). [...] Read more.
The one strain many compounds (OSMAC) strategy is an effective method for activating silent gene clusters by cultivating microorganisms under various conditions. The whole genome sequence of the marine-derived strain Streptomyces globisporus SCSIO LCY30 revealed that it contains 30 biosynthetic gene clusters (BGCs). By using the OSMAC strategy, three types of secondary metabolites were activated and identified, including three angucyclines, mayamycin A (1), mayamycin B (2), and rabolemycin (3); two streptophenazines (streptophenazin O (4) and M (5)); and a macrolide dimeric dinactin (6), respectively. The biosynthetic pathways of the secondary metabolites in these three families were proposed based on the gene function prediction and structural information. The bioactivity assays showed that angucycline compounds 1–3 exhibited potent antitumor activities against 11 human cancer cell lines and antibacterial activities against a series of Gram-positive bacteria. Mayamycin (1) selectively exhibited potent cytotoxicity activity against triple-negative breast cancer (TNBC) cell lines such as MDA-MB-231, MDA-MB-468, and Bt-549, with IC50 values of 0.60–2.22 μM. Full article
(This article belongs to the Special Issue Marine Bioactive Compound Discovery through OSMAC Approach)
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21 pages, 4160 KiB  
Article
Effects of Epigenetic Modification and High Hydrostatic Pressure on Polyketide Synthase Genes and Secondary Metabolites of Alternaria alternata Derived from the Mariana Trench Sediments
by Qingqing Peng, Yongqi Li, Jiasong Fang and Xi Yu
Mar. Drugs 2023, 21(11), 585; https://doi.org/10.3390/md21110585 - 10 Nov 2023
Cited by 1 | Viewed by 1423
Abstract
The hadal biosphere is the most mysterious ecosystem on the planet, located in a unique and extreme environment on Earth. To adapt to extreme environmental conditions, hadal microorganisms evolve special strategies and metabolisms to survive and reproduce. However, the secondary metabolites of the [...] Read more.
The hadal biosphere is the most mysterious ecosystem on the planet, located in a unique and extreme environment on Earth. To adapt to extreme environmental conditions, hadal microorganisms evolve special strategies and metabolisms to survive and reproduce. However, the secondary metabolites of the hadal microorganisms are poorly understood. In this study, we focused on the isolation and characterization of hadal fungi, screening the potential strains with bioactive natural products. The isolates obtained were detected further for the polyketide synthase (PKS) genes. Two isolates of Alternaria alternata were picked up as the representatives, which had the potential to synthesize active natural products. The epigenetic modifiers were used for the two A. alternata isolates to stimulate functional gene expression in hadal fungi under laboratory conditions. The results showed that the chemical epigenetic modifier, 5-Azacytidine (5-Aza), affected the phenotype, PKS gene expression, production of secondary metabolites, and antimicrobial activity of the hadal fungus A. alternata. The influence of epigenetic modification on natural products was strongest when the concentration of 5-Aza was 50 μM. Furthermore, the modification of epigenetic agents on hadal fungi under high hydrostatic pressure (HHP) of 40 MPa displayed significant effects on PKS gene expression, and also activated the production of new compounds. Our study demonstrates the high biosynthetic potential of cultivable hadal fungi, but also provides evidence for the utility of chemical epigenetic modifiers on active natural products from hadal fungi, providing new ideas for the development and exploitation of microbial resources in extreme environments. Full article
(This article belongs to the Special Issue Marine Bioactive Compound Discovery through OSMAC Approach)
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11 pages, 3609 KiB  
Article
Pimarane-Type Diterpenes with Anti-Inflammatory Activity from Arctic-Derived Fungus Eutypella sp. D-1
by Yaodong Ning, Shi Zhang, Te Zheng, Yao Xu, Song Li, Jianpeng Zhang, Binghua Jiao, Yun Zhang, Zengling Ma and Xiaoling Lu
Mar. Drugs 2023, 21(10), 541; https://doi.org/10.3390/md21100541 - 18 Oct 2023
Cited by 3 | Viewed by 1294
Abstract
The Arctic-derived fungus Eutypella sp. D-1 can produce numerous secondary metabolites, and some compounds exhibit excellent biological activity. Seven pimarane-type diterpenes, including three new compounds eutypellenone F (1), libertellenone Y (2), and libertellenone Z (3), and four [...] Read more.
The Arctic-derived fungus Eutypella sp. D-1 can produce numerous secondary metabolites, and some compounds exhibit excellent biological activity. Seven pimarane-type diterpenes, including three new compounds eutypellenone F (1), libertellenone Y (2), and libertellenone Z (3), and four known compounds (4–7), were isolated from fermentation broth of Eutypella sp. D-1 by the OSMAC strategy of adding ethanol as a promoter in the culture medium. Compound 2 has a rare tetrahydrofuran-fused pimarane diterpene skeleton. The anti-inflammatory activity of all compounds was evaluated. Compounds 3–6 showed a significant inhibitory effect on cell NO release at 10 μmol/L by in vitro experiments, of which 3–5 had inhibitory rates over 60% on nitric oxide (NO) release. Subsequently, the anti-inflammatory activity of 3–5 was evaluated based on a zebrafish model, and the results showed that 3 had a significant inhibitory effect on inflammatory cells migration at 40 μmol/L, while 4 and 5 had a significant inhibitory effect at 20 μmol/L. Moreover, compounds 3–5 have the same conjugated double bond structure, which may be an important group for these compounds to exert anti-inflammatory activity. Full article
(This article belongs to the Special Issue Marine Bioactive Compound Discovery through OSMAC Approach)
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14 pages, 3113 KiB  
Article
Phyllofenones F–M, Scalarane Sesterterpenes from the Marine Sponge Phyllospongia foliascens
by Hao-Bing Yu, Bo Hu, Zhe Ning, Ying He, Xiao-Ling Men, Zi-Fei Yin, Bing-Hua Jiao, Xiao-Yu Liu and Hou-Wen Lin
Mar. Drugs 2023, 21(10), 507; https://doi.org/10.3390/md21100507 - 26 Sep 2023
Viewed by 1198
Abstract
Eight new scalarane sesterterpenes, phyllofenones F–M (1–8), together with two known analogues, carteriofenones B and A (9–10), were isolated from the marine sponge Phyllospongia foliascens collected from the South China Sea. The structures of these [...] Read more.
Eight new scalarane sesterterpenes, phyllofenones F–M (1–8), together with two known analogues, carteriofenones B and A (9–10), were isolated from the marine sponge Phyllospongia foliascens collected from the South China Sea. The structures of these compounds were determined based on extensive spectroscopic and quantum chemical calculation analysis. The antibacterial and cytotoxic activity of these compounds was evaluated. Among them, only compounds 4 and 6 displayed weak inhibitory activity against Staphylococcus aureus and Escherichia coli, with MIC values of 16 μg/mL and 8 μg/mL, respectively. Compounds 1–10 exhibited cytotoxic activity against the HeLa, HCT-116, H460, and SW1990 cancer cell lines, with IC50 values ranging from 3.4 to 19.8 μM. Full article
(This article belongs to the Special Issue Marine Bioactive Compound Discovery through OSMAC Approach)
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