https://pubs.rsc.org/en/content/articlepdf/2019/NP/C8NP00092A

Marine natural products.

The marine environment harbors a number of macro and micro organisms that have developed unique metabolic abilities to ensure their survival in diverse and hostile habitats, resulting in the biosynthesis of an array of secondary metabolites with specific activities. Several of these metabolites are high-value commercial products for the pharmaceutical and cosmeceutical industries. The aim of this review is to outline the paths of marine natural products discovery and development, with a special focus on the compounds that successfully reached the market and particularly looking at the approaches tackled by the pharmaceutical and cosmetic companies that succeeded in marketing those products. The main challenges faced during marine bioactives discovery and development programs were analyzed and grouped in three categories: biodiversity (accessibility to marine resources and efficient screening), supply and technical (sustainable production of the bioactives and knowledge of the mechanism of action) and market (processes, costs, partnerships and marketing). Tips to surpass these challenges are given in order to improve the market entry success rates of highly promising marine bioactives in the current pipelines, highlighting what can be learned from the successful and unsuccessful stories that can be applied to novel and/or ongoing marine natural products discovery and development programs.

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Marketed marine natural products in the pharmaceutical and cosmeceutical industries: tips for success.

Luteolin, a flavonoid, as an anticancer agent: A review.

The peer-reviewed marine pharmacology literature from 2009 to 2011 is presented in this review, following the format used in the 1998–2008 reviews of this series. The pharmacology of structurally-characterized compounds isolated from marine animals, algae, fungi and bacteria is discussed in a comprehensive manner. Antibacterial, antifungal, antiprotozoal, antituberculosis, and antiviral pharmacological activities were reported for 102 marine natural products. Additionally, 60 marine compounds were observed to affect the immune and nervous system as well as possess antidiabetic and anti-inflammatory effects. Finally, 68 marine metabolites were shown to interact with a variety of receptors and molecular targets, and thus will probably contribute to multiple pharmacological classes upon further mechanism of action studies. Marine pharmacology during 2009–2011 remained a global enterprise, with researchers from 35 countries, and the United States, contributing to the preclinical pharmacology of 262 marine compounds which are part of the preclinical pharmaceutical pipeline. Continued pharmacological research with marine natural products will contribute to enhance the marine pharmaceutical clinical pipeline, which in 2013 consisted of 17 marine natural products, analogs or derivatives targeting a limited number of disease categories.

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Marine Pharmacology in 2009–2011: Marine Compounds with Antibacterial, Antidiabetic, Antifungal, Anti-Inflammatory, Antiprotozoal, Antituberculosis, and Antiviral Activities; Affecting the Immune and Nervous Systems, and other Miscellaneous Mechanisms of Action

https://pubs.rsc.org/en/content/articlepdf/2013/np/c3np20106f

Natural product isolation – how to get from biological material to pure compounds

The largely unexplored marine world that presumably harbors the most biodiversity may be the vastest resource to discover novel ‘validated’ structures with novel modes of action that cover biologically relevant chemical space. Several challenges, including the supply problem and target identification, need to be met for successful drug development of these often complex molecules; however, approaches are available to overcome the hurdles. Advances in technologies such as sampling strategies, nanoscale NMR for structure determination, total chemical synthesis, fermentation and biotechnology are all crucial to the success of marine natural products as drug leads. We illustrate the high degree of innovation in the field of marine natural products, which in our view will lead to a new wave of drugs that flow into the market and pharmacies in the future.

https://www.future-science.com/doi/pdf/10.4155/fmc.11.118

Marine natural products: a new wave of drugs?

Pitipeptolides C–F, Antimycobacterial Cyclodepsipeptides from the Marine Cyanobacterium Lyngbya majuscula from Guam

An unusual cyclic depsipeptide, pitiprolamide (1), was isolated from the marine cyanobacterium Lyngbya majuscula collected at Piti Bomb Holes, Guam. The structure was deduced using NMR, MS, X-ray crystallography, and enantioselective HPLC-MS techniques. Remarkably, proline represents half of the residues forming pitiprolamide (1). Other distinctive features include a 4-phenylvaline (dolaphenvaline, Dpv) moiety initially found in dolastatin 16 and the rare 2,2-dimethyl-3-hydroxyhexanoic acid (Dmhha) unit condensed in a unique sequence in one single molecule. Pitiprolamide (1) showed weak cytotoxic activity against HCT116 colon and MCF7 breast cancer cell lines, as well as weak antibacterial activities against Mycobacterium tuberculosis and Bacillus cereus.

Pitiprolamide, a proline-rich dolastatin 16 analogue from the marine cyanobacterium Lyngbya majuscula from Guam.

Malyngamide 3 (1) and cocosamides A (2) and B (3) were isolated from the lipophilic extract of a collection of Lyngbya majuscula from Cocos Lagoon, Guam. The planar structures of compounds 1-3 were determined by spectroscopic methods. The absolute configuration of 1 was determined by modified Mosher's method, NOESY data, and comparison with lyngbic acid (4). The absolute configurations of 2 and 3 were assigned by enantioselective HPLC analysis and comparison with the closely related compound pitipeptolide A (5). Compounds 1-3 showed weak cytotoxicity against MCF7 breast cancer and HT-29 colon cancer cells.

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Malyngamide 3 and cocosamides A and B from the marine cyanobacterium Lyngbya majuscula from Cocos Lagoon, Guam.

Lipids are utilized by diverse organisms, which suggests an evolutionarily conserved role of this class of compounds.[1] Indeed, lipidomics is emerging as a crucial field of research because of the key role of lipid biomolecules in a wide array of physiological functions.[2] Research has also uncovered some vital lipid-protein interactions where lipid molecules can bind to specific protein domains to mediate physiological effects. The endocannabinoid system is a representative example, where two characterized G-protein coupled cannabinoid receptors CB1 and CB2 are modulated by endogenous lipids known as endocannabinoids. Importantly, this system has been implicated in various pathophysiologies, including neurodegenerative diseases, eating disorders, pain, inflammation and cancer.[3–7] Therefore, a better understanding of this system has become of significant interest, and the cannabinoid receptors have been viewed as possible targets for different diseases.[1, 5] The classical concept that all agonists at a given GPCR induce a similar repertoire of downstream events is now uncertain, and the latest experimental evidence supports the existence of ligand-specific functional selectivity at the cannabinoid receptors.[3] Consequently, the identification of new structural scaffolds that can bind to the cannabinoid receptors remains an essential tool to dig further into this complex system.

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Rana Montaser

Papers

Marine natural products: a new wave of drugs?

Pitipeptolides C–F, Antimycobacterial Cyclodepsipeptides from the Marine Cyanobacterium Lyngbya majuscula from Guam

Pitiprolamide, a proline-rich dolastatin 16 analogue from the marine cyanobacterium Lyngbya majuscula from Guam.

Malyngamide 3 and cocosamides A and B from the marine cyanobacterium Lyngbya majuscula from Cocos Lagoon, Guam.

Marine Cyanobacterial Fatty Acid Amides Acting on Cannabinoid Receptors