Detection of pharmacologically active natural products using ecology. Selected examples from Indopacific marine invertebrates and sponge-derived fungi

2003 ◽  
Vol 75 (2-3) ◽  
pp. 343-352 ◽  
Author(s):  
P. Proksch ◽  
R. Ebel ◽  
R. A. Edrada ◽  
P. Schupp ◽  
W. H. Lin ◽  
...  
Keyword(s):  
Natural Products ◽  
Marine Invertebrates ◽  
Marine Sponges ◽  
Bioactive Metabolites ◽  
Marine Biodiversity ◽  
Marine Microorganisms ◽  
Bioactive Constituents ◽  
Isolation And Identification ◽  
Bioactive Natural Products ◽  
Pharmacologically Active

This review article presents our group's recent research findings with regard to bioactive natural products from marine sponges and tunicates, as well as from sponge derived fungi. The organisms discussed originate in the Indopacific region, which has an exceptionally rich marine biodiversity. Major topics that are covered in our review include the chemical ecology of sponges, focusing on defense against fishes, as well as the isolation and identification of new bioactive constituents from sponges and tunicates. Sponge derived fungi are introduced as an emerging source for new bioactive metabolites, reflecting the currently growing interest in natural products from marine microorganisms.

scholarly journals Cytotoxic activity of marine sponge extracts from the sub-Antarctic Islands and the Southern Ocean

2016 ◽  
Vol Volume 112 (Number 11/12) ◽  
Author(s):  
Elisabeth K. Olsen ◽  
Christopher K. de Cerf ◽  
Godwin A. Dziwornu ◽  
Eleonora Puccinelli ◽  
Isabelle J. Ansorge ◽  
...  
Keyword(s):  
Natural Products ◽  
Southern Ocean ◽  
Cytotoxic Activity ◽  
Marine Invertebrates ◽  
Cold Water ◽  
Research Effort ◽  
Benthic Invertebrate ◽  
Marine Sponges ◽  
Bioactive Natural Products ◽  
Prince Edward Islands

Abstract Over the past 50 years, marine invertebrates, especially sponges, have proven to be a valuable source of new and/or bioactive natural products that have the potential to be further developed as lead compounds for pharmaceutical applications. Although marine benthic invertebrate communities occurring off the coast of South Africa have been explored for their biomedicinal potential, the natural product investigation of marine sponges from the sub-Antarctic Islands in the Southern Ocean for the presence of bioactive secondary metabolites has been relatively unexplored thus far. We report here the results for the biological screening of both aqueous and organic extracts prepared from nine specimens of eight species of marine sponges, collected from around Marion Island and the Prince Edward Islands in the Southern Ocean, for their cytotoxic activity against three cancer cell lines. The results obtained through this multidisciplinary collaborative research effort by exclusively South African institutions has provided an exciting opportunity to discover cytotoxic compounds from sub-Antarctic sponges, whilst contributing to our understanding of the biodiversity and geographic distributions of these cold-water invertebrates. Therefore, we acknowledge here the various contributions of the diverse scientific disciplines that played a pivotal role in providing the necessary platform for the future natural products chemistry investigation of these marine sponges from the sub- Antarctic Islands and the Southern Ocean.

scholarly journals Novel Natural Product Discovery from Marine Sponges and their Obligate Symbiotic Organisms

2014 ◽  
Author(s):  
Regina Monaco ◽  
Rena Quinlan
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Marine Invertebrates ◽  
Quinone Reductase ◽  
Marine Sponges ◽  
Bioactive Molecules ◽  
Channel Blockers ◽  
Terrestrial Plants ◽  
Technological Advances ◽  
Pharmacologically Active

Abstract: Discovery of novel natural products is an accepted method for the elucidation of pharmacologically active molecules and drug leads. Best known sources for such discovery have been terrestrial plants and microbes, accounting for about 85% of the approved natural products in pharmaceutical use (1), and about 60% of approved pharmaceuticals and new drug applications annually (2). Discovery in the marine environment has lagged due to the difficulty of exploration in this ecological niche. Exploration began in earnest in the 1950’s, after technological advances such as scuba diving allowed collection of marine organisms, primarily at a depth to about 15m. Natural products from filter feeding marine invertebrates and in particular, sponges, have proven to be a rich source of structurally unique pharmacologically active compounds, with over 16,000 molecules isolated thus far (3, 1) and a continuing pace of discovery at hundreds of novel bioactive molecules per year. All classes of pharmaceuticals have been represented in this discovery process, including antiprotazoals, pesticides, TGF-beta inhibitors, cationic channel blockers, anticancer, cytotoxic, antiviral, anti-inflammatory and antibacterial compounds. Important biosynthetic pathways found in sponges which give rise to these compounds include the terpenoid (4), fatty acid, polyketoid, quinone reductase, alkaloid, isoprenoid (5), and non-ribosomal protein synthase pathways. Keywords: natural products; marine sponges; drug discovery; terpenoids; carotenoids; polyketides; marine drug discovery

Novel natural product discovery from obligate symbiotic organisms of marine sponges

2018 ◽  
Vol 1 (1) ◽  
Author(s):  
Regina R. Monaco ◽  
Rena F. Quinlan
Keyword(s):  
Natural Products ◽  
Marine Invertebrates ◽  
Quinone Reductase ◽  
Marine Sponges ◽  
Rich Source ◽  
Bioactive Molecules ◽  
Channel Blockers ◽  
Terrestrial Plants ◽  
Technological Advances ◽  
Pharmacologically Active

A rich source for the discovery of novel, pharmacologically active natural products has been terrestrial plants and microbes, accounting for about 85% of the approved natural products in pharmaceutical use (1), and about 60% of approved pharmaceuticals and new drug applications annually (2). Discovery in the marine environment has lagged due to the difficulty of exploration in this ecological niche. Such exploration began in the 1950’s, after technological advances such as scuba diving allowed collection of marine organisms, primarily to a depth of about 15m, which was the limit of that technology.Natural products from filter feeding marine invertebrates and in particular, sponges, have proven to be a rich source of structurally unique pharmacologically active compounds, with over 16,000 molecules isolated thus far (3, 1) and a continuing pace of discovery at hundreds of novel bioactive molecules per year. All classes of pharmaceuticals have been represented in this discovery process, including antiprotozoals, pesticides, TGF-beta inhibitors, cationic channel blockers, anticancer, cytotoxic, antiviral, anti-inflammatory and antibacterial compounds. Important biosynthetic pathways found in sponges which give rise to these compounds include the terpenoid (4), fatty acid, polyketoid, quinone reductase, alkaloid, isoprenoid (5), and non-ribosomal protein synthase pathways.

scholarly journals Mori Ramulus (Chin.Ph.)—the Dried Twigs of Morus alba L./Part 1: Discovery of Two Novel Coumarin Glycosides from the Anti-Hyperuricemic Ethanol Extract

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 629
Author(s):  
Jianbiao Yao ◽  
Houhong He ◽  
Jin Xue ◽  
Jianfang Wang ◽  
Huihui Jin ◽  
...  
Keyword(s):  
Natural Products ◽  
Ethanol Extract ◽  
Accurate Method ◽  
Morus Alba ◽  
Strongly Correlated ◽  
Bioactive Constituents ◽  
Antiplatelet Aggregation ◽  
Pharmacologically Active ◽  
First Time ◽  
Tof Ms

In Traditional Chinese Medicine (TCM), Mori ramulus (Chin.Ph.)—the dried twigs of Morus alba L.—is extensively used as an antirheumatic agent and also finds additional use in asthma therapy. As a pathological high xanthine oxidase (XO, EC 1.1.3.22) activity is strongly correlated to hyperuricemy and gout, standard anti-hyperuremic therapy typically involves XO inhibitors like allopurinol, which often cause adverse effects by inhibiting other enzymes involved in purine metabolism. Mori ramulus may therefore be a promissing source for the development of new antirheumatic therapeutics with less side effects. Coumarins, one of the dominant groups of bioactive constituents of M. alba, have been demonstrated to possess anti-inflammatory, antiplatelet aggregation, antitumor, and acetylcholinesterase (AChE) inhibitory activities. The combination of HPLC (DAD) and Q-TOF technique could give excellent separating and good structural characterization abilities which make it suitable to analyze complex multi-herbal extracts in TCM. The aim of this study was to develop a HPLC (DAD)/ESI-Q-TOF-MS/MS method for the identification and profiling of pharmacologically active coumarin glycosides in Mori ramulus refined extracts for used in TCM. This HPLC (DAD)/ESI-Q-TOF-MS/MS method provided a rapid and accurate method for identification of coumarin glycosides—including new natural products described here for the first time—in the crude extract of M. alba L. In the course of this project, two novel natural products moriramulosid A (umbelliferone-6-β-d-apiofuranosyl-(1→6)-β-d-glucopyranoside) and moriramulosid B (6-[[6-O-(6-deoxy-α-l-mannopyranosyl)-β-d-glucopyranosyl]oxy]-2H-1-benzopyran-1-one) were newly discovered and the known natural product Scopolin was identified in M. alba L. for the first time.

scholarly journals Secondary metabolites from marine microorganisms

2002 ◽  
Vol 74 (1) ◽  
pp. 151-170 ◽  
Author(s):  
ALPHONSE KELECOM
Keyword(s):  
Secondary Metabolites ◽  
Cyclic Peptides ◽  
Marine Invertebrates ◽  
Indole Alkaloids ◽  
Marine Sponges ◽  
Annual Reports ◽  
Marine Microorganisms ◽  
Mature Field ◽  
Bacteria And Fungi ◽  
New Metabolites

After 40 years of intensive research, chemistry of marine natural products has become a mature field. Since 1995, there are signals of decreased interest in the search of new metabolites from traditional sources such as macroalgae and octocorals, and the number of annual reports on marine sponges stabilized. On the contrary, metabolites from microorganisms is a rapidly growing field, due, at least in part, to the suspicion that a number of metabolites obtained from algae and invertebrates may be produced by associated microorganisms. Studies are concerned with bacteria and fungi, isolated from seawater, sediments, algae, fish and mainly from marine invertebrates such as sponges, mollusks, tunicates, coelenterates and crustaceans. Although it is still to early to define tendencies, it may be stated that the metabolites from microorganisms are in most cases quite different from those produced by the invertebrate hosts. Nitrogenated metabolites predominate over acetate derivatives, and terpenes are uncommon. Among the latter, sesquiterpenes, diterpenes and carotenes have been isolated; among nitrogenated metabolites, amides, cyclic peptides and indole alkaloids predominate.

scholarly journals New Antibacterial Bagremycins F and G from the Marine-Derived Streptomyces sp. ZZ745

Marine Drugs ◽  
2018 ◽  
Vol 16 (9) ◽  
pp. 330 ◽  
Author(s):  
Di Zhang ◽  
Chenyan Shu ◽  
Xiaoyuan Lian ◽  
Zhizhen Zhang
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Natural Products ◽  
Spectroscopic Analysis ◽  
Optical Rotation ◽  
Marine Microorganisms ◽  
Streptomyces Sp ◽  
Bioactive Natural Products ◽  
Marine Actinomycete

As part of our research to discover novel bioactive natural products from marine microorganisms, five bagremycin analogues, including the previously unreported bagremycins F (1) and G (2), were isolated from a marine actinomycete Streptomyces sp. ZZ745. The structures of these compounds were determined by means of NMR spectroscopic analysis, HRESIMS data, and optical rotation. Both bagremycins F (1) and G (2) showed antibacterial activity against Escherichia coli, with MIC values of 41.8 and 61.7 μM, respectively.

scholarly journals Integration of high-content screening and untargeted metabolomics for comprehensive functional annotation of natural product libraries

2015 ◽  
Vol 112 (39) ◽  
pp. 11999-12004 ◽  
Author(s):  
Kenji L. Kurita ◽  
Emerson Glassey ◽  
Roger G. Linington
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Chemical Properties ◽  
Untargeted Metabolomics ◽  
Bioactive Metabolites ◽  
Discovery Process ◽  
Bioactive Constituents ◽  
Modes Of Action ◽  
New Family ◽  
Natural Products Discovery

Traditional natural products discovery using a combination of live/dead screening followed by iterative bioassay-guided fractionation affords no information about compound structure or mode of action until late in the discovery process. This leads to high rates of rediscovery and low probabilities of finding compounds with unique biological and/or chemical properties. By integrating image-based phenotypic screening in HeLa cells with high-resolution untargeted metabolomics analysis, we have developed a new platform, termed Compound Activity Mapping, that is capable of directly predicting the identities and modes of action of bioactive constituents for any complex natural product extract library. This new tool can be used to rapidly identify novel bioactive constituents and provide predictions of compound modes of action directly from primary screening data. This approach inverts the natural products discovery process from the existing ‟grind and find” model to a targeted, hypothesis-driven discovery model where the chemical features and biological function of bioactive metabolites are known early in the screening workflow, and lead compounds can be rationally selected based on biological and/or chemical novelty. We demonstrate the utility of the Compound Activity Mapping platform by combining 10,977 mass spectral features and 58,032 biological measurements from a library of 234 natural products extracts and integrating these two datasets to identify 13 clusters of fractions containing 11 known compound families and four new compounds. Using Compound Activity Mapping we discovered the quinocinnolinomycins, a new family of natural products with a unique carbon skeleton that cause endoplasmic reticulum stress.

ChemInform Abstract: Bioactive Natural Products from Papua New Guinea Marine Sponges

ChemInform ◽  
2013 ◽  
Vol 44 (2) ◽  
pp. no-no
Author(s):  
Jeffrey C. Noro ◽  
John A. Kalaitzis ◽  
Brett A. Neilan
Keyword(s):  
Natural Products ◽  
Papua New Guinea ◽  
New Guinea ◽  
Marine Sponges ◽  
Bioactive Natural Products

scholarly journals A Study on the Phytotoxic Potential of the Seasoning Herb Marjoram (Origanum majorana L.) Leaves

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3356
Author(s):  
Antonio Cala ◽  
José R. Salcedo ◽  
Ascensión Torres ◽  
Rosa M. Varela ◽  
José M. G. Molinillo ◽  
...  
Keyword(s):  
Natural Products ◽  
Weed Control ◽  
Isolation And Identification ◽  
Edible Plant ◽  
Bioactive Natural Products ◽  
Mediterranean Countries ◽  
Extraction Processes ◽  
Therapeutic Properties ◽  
Origanum Majorana ◽  
First Time

In the search of new alternatives for weed control, spices appear as an option with great potential. They are rich in bioactive natural products and edible, which might minimize toxicity hazard. Marjoram (Origanum majorana L.) is an aromatic herb that has been widely employed as a seasoning herb in Mediterranean countries. Although marjoram boasts a plethora of therapeutic properties (painkiller, antibiotic, treatment for intestinal disorders, etc.), the potential for its extracts for weed control is still to be more thoroughly explored. In order to determine their phytotoxic potential, marjoram leaves were subjected to different bioguided extraction processes, using water, ethyl acetate, acetone or methanol. The most active extract (acetone) was sequentially fractionated to identify its most active compounds. This fractionation led to the isolation and identification of 25 compounds that were classified as monoterpenes, diterpenes or flavonoids. Among them, a new compound named majoradiol and several compounds are described in marjoram for the first time. The phytotoxicity of the major compounds to etiolated wheat coleoptiles was compared against that of the commercial herbicide (Logran®), with similar or higher activity in some cases. These results confirm the extraordinary potential of the extracts from this edible plant to develop safer and more environmentally friendly herbicides.

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