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Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery

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

Deadline for manuscript submissions: closed (31 August 2019) | Viewed by 74943

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Dr. Rob Keyzers

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Guest Editor

School of Chemical and Physical Sciences, and Center for Biodiscovery, Victoria University of Wellington, Wellington 6140, New Zealand
Interests: marine invertebrate natural products; bioactive natural products; structure determination of new metabolites; isolation and purification; chemical analysis; analytical chemistry of natural compounds and xenochemicals
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Dear Colleagues,

From the potential human harm caused by the exquisitely potent dinoflagellate cytotoxins, maitotoxin and brevetoxin, through the knowledge gained regarding cellular function and metabolism from the use of latrunculin and laulimalide, right through to new blockbuster anticancer drugs like Eribulin mesylate and Trabectedin, the bioassay-guided isolation of new marine natural products has informed science and helped save many lives over the past half century. The new and exciting molecules sourced from the marine environment are varied in structure and, most importantly, the wide ranging and diverse potent bioactivities they possess. With a significantly greater number of phyla represented in our marine environments than that found on land, the sheer biodiversity found in the oceans, coupled with difficulties, and hence opportunities for obtaining marine organisms, continue to make investigations of marine natural products a lucrative area for medicinal and biochemical research.

Given the great value still waiting to be discovered from the life within our planet’s oceans, as the Guest Editor of this Special Issue of Marine Drugs, I personally invite you to contribute your latest research describing bioassay-guided isolation and identification of novel, bioactive marine natural products, from any marine-based organisms.

Dr. Rob Keyzers
Guest Editor

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Keywords

Biological activity
Phenotypic assay
Enzyme inhibition assay
Mode of action
Isolation
Structural elucidation
Bioassay guided fractionation

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Published Papers (10 papers)

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10 pages, 1381 KB

Open AccessArticle

Asperienes A–D, Bioactive Sesquiterpenes from the Marine-Derived Fungus Aspergillus flavus

by Yun-Feng Liu^1,2, Yu-Fei Yue¹, Li-Xi Feng¹, Hua-Jie Zhu^1,* and Fei Cao^1,2,*

¹ Key Laboratory of Medicinal Chemistry and Molecular Diagnostics of Education Ministry of China, Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding 071002, China

² College of Life Sciences, Hebei University, Baoding 071002, China

Mar. Drugs 2019, 17(10), 550; https://doi.org/10.3390/md17100550 - 26 Sep 2019

Cited by 34 | Viewed by 4493

Abstract

Marine-derived fungi of the genera Aspergillus could produce novel compounds with significant bioactivities. Among these fungi, the strain Aspergillus flavus is notorious for its mutagenic mycotoxins production. However, some minor components with certain toxicities from A. flavus have not been specifically surveyed and might have potent biological activities. Our investigation of the marine-derived fungus Aspergillus flavus CF13-11 cultured in solid medium led to the isolation of four C-6′/C-7′ epimeric drimane sesquiterpene esters, asperienes A–D (1–4). Their absolute configurations were assigned by electronic circular dichroism (ECD) and Snatzke’s methods. This is the first time that two pairs of C-6′/C-7′ epimeric drimane sesquiterpene esters have successfully been separated. Aperienes A–D (1–4) displayed potent bioactivities towards four cell lines with the IC₅₀ values ranging from 1.4 to 8.3 μM. Interestingly, compounds 1 and 4 exhibited lower toxicities than 2 and 3 toward normal GES-1 cells, indicating more potential for development as an antitumor agent in the future. Full article

(This article belongs to the Special Issue Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery)

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27 pages, 18221 KB

Open AccessFeature PaperArticle

Cytotoxic and Antiproliferative Effects of Preussin, a Hydroxypyrrolidine Derivative from the Marine Sponge-Associated Fungus Aspergillus candidus KUFA 0062, in a Panel of Breast Cancer Cell Lines and Using 2D and 3D Cultures

by Fernanda Malhão^1,2

, Alice A. Ramos^1,2, Suradet Buttachon^1,2

, Tida Dethoup³, Anake Kijjoa^1,2

and Eduardo Rocha^1,2,*

¹ Institute of Biomedical Sciences Abel Salazar (ICBAS), Universidade do Porto (U.Porto), Rua de Jorge Viterbo Ferreira n 228, 4050-313 Porto, Portugal

² Interdisciplinary Center for Marine and Environmental Research (CIIMAR), Universidade do Porto (U.Porto), Avenida General Norton de Matos s/n, 4450-208 Matosinhos, Portugal

³ Department of Plant Pathology, Faculty of Agriculture, Kasetsart University, Bangkok 10240, Thailand

Mar. Drugs 2019, 17(8), 448; https://doi.org/10.3390/md17080448 - 30 Jul 2019

Cited by 34 | Viewed by 7121

Abstract

Preussin, a hydroxyl pyrrolidine derivative isolated from the marine sponge-associated fungus Aspergillus candidus KUFA 0062, displayed anticancer effects in some cancer cell lines, including MCF7. Preussin was investigated for its cytotoxic and antiproliferative effects in breast cancer cell lines (MCF7, SKBR3, and MDA-MB-231), representatives of major breast cancers subtypes, and in a non-tumor cell line (MCF12A). Preussin was first tested in 2D (monolayer), and then in 3D (multicellular aggregates), cultures, using a multi-endpoint approach for cytotoxicity (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), resazurin and lactate dehydrogenase (LDH)) and proliferative (5-bromo-2′-deoxyuridine (BrdU)) assays, as well as the analysis of cell morphology by optical/electron microscopy and immunocytochemistry for caspase-3 and ki67. Preussin affected cell viability and proliferation in 2D and 3D cultures in all cell lines tested. The results in the 3D culture showed the same tendency as in the 2D culture, however, cells in the 3D culture were less responsive. The effects were observed at different concentrations of preussin, depending on the cell line and assay method. Morphological study of preussin-exposed cells revealed cell death, which was confirmed by caspase-3 immunostaining. In view of the data, we recommend a multi-endpoint approach, including histological evaluation, in future assays with the tested 3D models. Our data showed cytotoxic and antiproliferative activities of preussin in breast cancer cell lines in 2D and 3D cultures, warranting further studies for its anticancer potential. Full article

(This article belongs to the Special Issue Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery)

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26 pages, 4467 KB

Open AccessFeature PaperReview

Bioactive Compounds Isolated from Marine-Derived Microbes in China: 2009–2018

by Weiwei Sun, Wenhui Wu, Xueling Liu, Diana A. Zaleta-Pinet and Benjamin R. Clark^*

School of Pharmaceutical Science and Technology, Health Science Platform, Tianjin University, 92 Weijin Road, Tianjin 300072, China

Mar. Drugs 2019, 17(6), 339; https://doi.org/10.3390/md17060339 - 6 Jun 2019

Cited by 59 | Viewed by 9762

Abstract

This review outlines the research that was carried out regarding the isolation of bioactive compounds from marine-derived bacteria and fungi by China-based research groups from 2009–2018, with 897 publications being surveyed. Endophytic organisms featured heavily, with endophytes from mangroves, marine invertebrates, and marine algae making up more than 60% of the microbial strains investigated. There was also a strong focus on fungi as a source of active compounds, with 80% of publications focusing on this area. The rapid increase in the number of publications in the field is perhaps most notable, which have increased more than sevenfold over the past decade, and suggests that China-based researchers will play a major role in marine microbial natural products drug discovery in years to come. Full article

(This article belongs to the Special Issue Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery)

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19 pages, 1655 KB

Open AccessArticle

In Vitro and In Silico Approaches to Generating and Identifying Angiotensin-Converting Enzyme I Inhibitory Peptides from Green Macroalga Ulva lactuca

by Marco Garcia-Vaquero^1,*

, Leticia Mora²

and Maria Hayes³

¹ School of Veterinary Medicine, University College Dublin (UCD), Belfield, Dublin 4, Ireland

² Instituto de Agroquímica y Tecnología de Alimentos (CSIC), Avenue Agustín Escardino 7, 46980 Paterna (Valencia), Spain

³ Food Biosciences Department, TEAGASC, Food Research Centre, Ashtown, Dublin 15, Ireland

Mar. Drugs 2019, 17(4), 204; https://doi.org/10.3390/md17040204 - 30 Mar 2019

Cited by 81 | Viewed by 9263

Abstract

A protein extract was generated from the macroalga Ulva lactuca, which was subsequently hydrolysed using the food-grade enzyme papain and angiotensin-converting Enzyme I and renin inhibitory peptides identified using a combination of enrichment strategies employing molecular weight cutoff filtration and mass spectrometry analysis. The generated hydrolysates with the most promising in vitro activity were further purified using preparative RP-HPLC and characterised. The 1 kDa hydrolysate (1 kDa-UFH), purified and collected by preparative RP-HPLC at minutes 41‒44 (Fr41‒44), displayed statistically higher ACE-I inhibitory activities ranging from 96.91% to 98.06%. A total of 48 novel peptides were identified from these four fractions by LC-MS/MS. A simulated gastrointestinal digestion of the identified peptide sequences was carried out using in silico enzyme cleavage simulation tools, resulting in 86 peptide sequences that were further assessed for their potential activity, toxicity and allergenicity using multiple predictive approaches. All the peptides obtained in this study were predicted to be non-toxic. However, 28 out of the 86 novel peptides released after the in silico gastrointestinal digestion were identified as potential allergens. The potential allergenicity of these peptides should be further explored to comply with the current labelling regulations in formulated food products containing U. lactuca protein hydrolysates. Full article

(This article belongs to the Special Issue Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery)

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16 pages, 1811 KB

Open AccessArticle

Antioxidant and Neuroprotective Potential of the Brown Seaweed Bifurcaria bifurcata in an in vitro Parkinson’s Disease Model

by Joana Silva^1,2,*, Celso Alves¹, Rafaela Freitas¹, Alice Martins¹, Susete Pinteus¹

, Joana Ribeiro¹, Helena Gaspar^1,3

, Amparo Alfonso² and Rui Pedrosa^1,*

¹ MARE—Marine and Environmental Sciences Centre, ESTM, Instituto Politécnico de Leiria, 2520-641 Peniche, Portugal

² Department of Pharmacology, Faculty of Veterinary, University of Santiago de Compostela, 27002 Lugo, Spain

³ BioISI-Biosystems & Integrative Sciences Institute, Faculty of Sciences, University of Lisboa, Campo Grande, C8, 1749-016 Lisboa, Portugal

Mar. Drugs 2019, 17(2), 85; https://doi.org/10.3390/md17020085 - 1 Feb 2019

Cited by 80 | Viewed by 7518

Abstract

Bifurcaria bifurcata is a marine brown seaweed mainly found on the Atlantic coast. Herein, we report the antioxidant and neuroprotective activities of seven fractions (F1–F7) obtained by normal phase chromatography from the B. bifurcata dichloromethane extract, as well as of its two major isolated diterpenes. Total phenolic content of fractions was determined by the Folin–Ciocalteu method, while antioxidant activity was evaluated by the DPPH, ORAC, and FRAP assays. Neuroprotective effects were evaluated in a neurotoxic model induced by 6-hydroxydopamine (6-OHDA) in a human neuroblastoma cell line (SH-SY5Y), while the mechanisms associated to neuroprotection were investigated by the determination of mitochondrial membrane potential, H₂O₂ production, Caspase-3 activity, and by observation of DNA fragmentation. Fractions F4 and F5 exhibited the best neuroprotective and antioxidant activities, respectively. F4 fraction prevented changes in mitochondrial potential, and induced a reduction of H₂O₂ levels production and an increase in cell viability, suggesting that it may contain multi-target compounds acting on different pathways. Hence, this fraction was subjected to purification steps, affording the known diterpenes eleganolone and eleganonal. Both compounds exhibited antioxidant potential, being interesting candidates for further neuroprotective studies. Full article

(This article belongs to the Special Issue Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery)

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12 pages, 1745 KB

Open AccessArticle

Anti-Acanthamoeba Activity of Brominated Sesquiterpenes from Laurencia johnstonii

by Sara García-Davis^1,2, Ines Sifaoui³, María Reyes-Batlle³, Ezequiel Viveros-Valdez², José E. Piñero³

, Jacob Lorenzo-Morales³, José J. Fernández^1,4,*

and Ana R. Díaz-Marrero^1,*

¹ Instituto Universitario de Bio-Orgánica Antonio González (IUBO AG), Centro de Investigaciones Biomédicas de Canarias (CIBICAN), Universidad de La Laguna (ULL), Avda. Astrofísico F. Sánchez, 2, 38206 La Laguna, Tenerife, Spain

² Facultad de Ciencias Biológicas, Universidad Autónoma de Nuevo León (UANL), Av. Pedro de Alba s/n, 66450 San Nicolás de los Garza, Nuevo León, Mexico

³ Instituto Universitario de Enfermedades Tropicales y Salud Pública de Islas Canarias, Universidad de La Laguna, Av. Astrofísico Francisco Sánchez s/n, 38206 La Laguna, Tenerife, Spain

⁴ Departamento de Química Orgánica, Universidad de La Laguna (ULL), Avda. Astrofísico F. Sánchez, 2, 38206 La Laguna, Tenerife, Spain

Mar. Drugs 2018, 16(11), 443; https://doi.org/10.3390/md16110443 - 11 Nov 2018

Cited by 30 | Viewed by 5977

Abstract

Focused on our interest to develop novel antiparasistic agents, the present study was aimed to evaluate the biological activity of an extract of Laurencia johnstonii collected in Baja California Sur, Mexico, against an Acantamoeba castellanii Neff strain. Bioassay-guided fractionation allowed us to identify the amoebicidal diastereoisomers α-bromocuparane (4) and α-isobromocuparane (5). Furthermore, bromination of the inactive laurinterol (1) and isolaurinterol (2) yielded four halogenated derivatives, (6)–(9), which improved the activity of the natural sesquiterpenes. Among them, the most active compound was 3α-bromojohnstane (7), a sesquiterpene derivative which possesses a novel carbon skeleton johnstane. Full article

(This article belongs to the Special Issue Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery)

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8 pages, 788 KB

Open AccessArticle

Anti-MRSA Sesquiterpenes from the Semi-Mangrove Plant Myoporum bontioides A. Gray

by Li-Mei Dong^1,†, Li-Lan Huang^2,†, Hang Dai², Qiao-Lin Xu³, Jin-Kui Ouyang¹, Xu-Chao Jia⁴, Wen-Xiang Gu^2,* and Jian-Wen Tan^1,*

¹ State Key Laboratory for Conservation and Utilization of Subtropical Agro-bioresources/Guangdong Key Laboratory for Innovative Development and Utilization of Forest Plant Germplasm, College of Forestry and Landscape Architecture, South China Agricultural University, Guangzhou 510642, China

² College of Materials and Energy, South China Agricultural University, Guangzhou 510642, China

³ Guangdong Provincial Key Laboratory of Bio-control for the Forest Disease and Pest, Guangdong Academy of Forestry, Guangzhou 510520, China

⁴ Key Laboratory of Functional Foods, Ministry of Agriculture/Guangdong Key Laboratory of Agricultural Products Processing/Sericultural & Agri-Food Research Institute, Guangdong Academy of Agricultural Sciences, Guangzhou 510610, China

^† These authors contributed equally to this work.

Mar. Drugs 2018, 16(11), 438; https://doi.org/10.3390/md16110438 - 8 Nov 2018

Cited by 26 | Viewed by 4434

Abstract

The striking rise of methicillin-resistant Staphylococcus aureus (MRSA) infections has become a serious threat to public health worldwide. In an effort to search for new anti-MRSA agents from natural products, a bioassay-guided phytochemical study was conducted on the semi-mangrove plant Myoporum bontioides A. Gray, which led to the isolation of two new sesquiterpene alkaloids (1 and 2) and six known furanosesquiterpenes (3–8). Their structures were elucidated on the basis of extensive analysis of their 1D, 2D NMR and mass spectroscopic data. These two new alkaloids (1 and 2) displayed potent anti-MRSA activity with MIC value of 6.25 μg/mL. This is the first report of sesquiterpene alkaloids from the plants of Myoporum genus and their anti-MRSA activity. Full article

(This article belongs to the Special Issue Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery)

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8 pages, 1445 KB

Open AccessArticle

Cytotoxic Tetrahydroxanthone Dimers from the Mangrove-Associated Fungus Aspergillus versicolor HDN1009

by Guihong Yu¹, Guangwei Wu¹, Zichao Sun¹, Xiaomin Zhang¹, Qian Che¹, Qianqun Gu¹, Tianjiao Zhu^1,2

, Dehai Li^1,2,3

and Guojian Zhang^1,2,*

¹ Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China

² Laboratory for Marine Drugs and Bioproducts of Qingdao Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, China

³ Open Studio for Druggability Research of Marine Natural Products, Qingdao Pilot National Laboratory for Marine Science and Technology, Qingdao 266237, China

Mar. Drugs 2018, 16(9), 335; https://doi.org/10.3390/md16090335 - 14 Sep 2018

Cited by 46 | Viewed by 4584

Abstract

Three new tetrahydroxanthone dimers, 5-epi-asperdichrome (1), versixanthones N (2), and O (3), were isolated from the mangrove-derived fungus Aspergillus versicolor HDN1009. Their structures, including the absolute configurations, were elucidated by NMR, HRMS, and circular dichroism (CD) experiments. Among them, compound 1 was the second example of tetrahydroxanthone dimers, which dimerized by a rare diaryl ether linkage and showed promising antibacterial activities against Vibrio parahemolyticus, Bacillus subtilis, Mycobacterium phlei, and Pseudomonas aeruginosa, with MIC values ranging from 100 μM to 200 μM; whilst compounds 2 and 3 exhibited extensive cytotoxicities against five cancer cell lines (HL-60, K562, H1975, MGC803, and HO-8910), with IC₅₀ values ranging from 1.7 μM to 16.1 μM. Full article

(This article belongs to the Special Issue Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery)

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31 pages, 393 KB

Open AccessReview

Current Screening Methodologies in Drug Discovery for Selected Human Diseases

by Olga Maria Lage^1,2,*, María C. Ramos³, Rita Calisto^1,2, Eduarda Almeida^1,2, Vitor Vasconcelos^1,2

and Francisca Vicente³

¹ Departamento de Biologia, Faculdade de Ciências, Universidade do Porto, Rua do Campo Alegre s/nº 4169-007 Porto, Portugal

² CIIMAR/CIMAR–Centro Interdisciplinar de Investigação Marinha e Ambiental–Universidade do Porto, Terminal de Cruzeiros do Porto de Leixões, Avenida General Norton de Matos, S/N, 4450-208 Matosinhos, Portugal

³ Fundación MEDINA, Centro de Excelencia en Investigación de Medicamentos Innovadores en Andalucía, Parque Tecnológico de Ciencias de la Salud, 18016 Granada, Spain

Mar. Drugs 2018, 16(8), 279; https://doi.org/10.3390/md16080279 - 14 Aug 2018

Cited by 107 | Viewed by 12773

Abstract

The increase of many deadly diseases like infections by multidrug-resistant bacteria implies re-inventing the wheel on drug discovery. A better comprehension of the metabolisms and regulation of diseases, the increase in knowledge based on the study of disease-born microorganisms’ genomes, the development of more representative disease models and improvement of techniques, technologies, and computation applied to biology are advances that will foster drug discovery in upcoming years. In this paper, several aspects of current methodologies for drug discovery of antibacterial and antifungals, anti-tropical diseases, antibiofilm and antiquorum sensing, anticancer and neuroprotectors are considered. For drug discovery, two different complementary approaches can be applied: classical pharmacology, also known as phenotypic drug discovery, which is the historical basis of drug discovery, and reverse pharmacology, also designated target-based drug discovery. Screening methods based on phenotypic drug discovery have been used to discover new natural products mainly from terrestrial origin. Examples of the discovery of marine natural products are provided. A section on future trends provides a comprehensive overview on recent advances that will foster the pharmaceutical industry. Full article

(This article belongs to the Special Issue Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery)

10 pages, 1363 KB

Open AccessArticle

Mycophenolic Acid Derivatives with Immunosuppressive Activity from the Coral-Derived Fungus Penicillium bialowiezense

by Qing Zhang, Beiye Yang, Fengli Li, Mengting Liu, Shuang Lin, Jianping Wang, Yongbo Xue

, Hucheng Zhu, Weiguang Sun^*, Zhengxi Hu^*

and Yonghui Zhang^*

Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China

Mar. Drugs 2018, 16(7), 230; https://doi.org/10.3390/md16070230 - 7 Jul 2018

Cited by 18 | Viewed by 7107

Abstract

Mycophenolic acid (MPA) is a potent inosine-5′-monophosphate dehydrogenase (IMPDH) inhibitor for immunosuppressive chemotherapy. Most importantly, as the 2-morpholinoethyl ester prodrug of MPA, mycophenolate mofetil (MMF) is a well-known immunosuppressant used to prevent rejection in organ transplantations. Nevertheless, due to its frequently occurred side effects, searching for new therapeutic agents is ongoing. In our current work, by virtue of efficient bioassay-guided fractionation and purification, eleven mycophenolic acid derivatives, including five previously unreported metabolites (3–7) and six known compounds (1, 2, and 8–11), were obtained from the coral-derived fungus Penicillium bialowiezense. Their structures were elucidated by means of extensive spectroscopic analyses (including 1D and 2D NMR and HRESIMS data) and comparison of the NMR and other physical data with those reported in the literature in the case of the known compounds. All the isolates 1–11 were evaluated for the immunosuppressive activity, and 1–3 showed potent IMPDH2 inhibitory potency with IC₅₀ values of 0.84–0.95 μM, which were comparable to that of MPA (the positive control), while 4–10 showed significant inhibitory potency with IC₅₀ values of 3.27–24.68 μM. All the MPA derivatives showed promising immunosuppressive activity, endowing them as potential drug leads for organ transplantations and autoimmune related diseases. Full article

(This article belongs to the Special Issue Bioassay-Guided Isolation of Marine Natural Products for Drug Discovery)

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