Marine Bioactives Research Articles

Bioactives from marine resources as natural health products: A review.

The oceans are a rich source of a myriad of structurally different and unique natural products that are mainly found in invertebrates with potential applications in different disciplines. Microbial infection and cancer are the leading causes of death worldwide. Discovery of new sources of therapy for microbial infections is an urgent requirement due to the emergence of pathogenic microorganisms that are resistant to existing therapies. Marine bioactives have demonstrated to be promising sources for the discovery and development of novel antimicrobial and anticancer compounds. Several marine compounds are confirmed to have antibacterial effects and most marine-based antifungal compounds are cytotoxic. Numerous antitumor marine natural products, derived mainly from sponges or molluscs, and also bryozoans and cyanobacteria, exhibit potent antimitotic activity. In addition, marine biodiversity offers some possible leads or new drugs to treat human immunodeficiency virus (HIV). A majority of marine derived drugs are currently in clinical trials or under preclinical evaluation. Furthermore, marine-based drugs, approved by the US Food and Drug Administration (FDA) are available in the market. This review summarizes the sources, mechanisms of action and potential utilization of marine natural products such as peptides, alkaloids, polyketides, polyphenols, terpenoids and sterols as antifungal, antibacterial, antiviral, and anticancer compounds. Significance Statement Utilization of marine bioactives as natural health products leads to crucial advancement in providing dietary supplements, nutraceuticals, functional foods and pharmaceuticals. Their myriad of application promotes health and plays a role in disease risk reduction. Therapeutic potential of potent compounds from marine organisms and use of their bioactives have promising medicinal value for preventing ailments and advancing pharmaceutical and nutraceutical industries. Their utilization benefits human health globally and contributes to the conservation of marine ecosystem in a transformative / sustainable approach.

Marine Bioactives in Cancer Prevention and Treatment

The twice high incidence risk of cancer in men was the reason for over a million new cases and deaths recorded globally in 2018. The two most frequent cancer-related fatalities are lung and breast cancer. Novel therapies have been made possible by developments in immunotherapy, biology, and pharmaceutical design. Novel cancer prevention and therapy elements are being made possible by technological advancements and studies on marine natural resources. The creation of innovative anticancer medications is utilizing marine-derived natural products (MNPs). Biologically active polyketides, high molecular weight organic sugars, terpenes, bioengineered alkaloids, and marine animal peptides are some examples of these MNPs. Anticancer drugs are also developed with the help of plants, animals, invertebrates, and microbes found on land. The National Cancer Institute is exploring the potential of nutrition and food in cancer prevention despite the absence of preclinical and clinical data. Marine organisms contain bioactive compounds that have potential anticancer effects. Polyphenols, polysaccharides, and alkaloids are some of the active components found in marine species. Polyphenols, found in edible seaweeds like Palmaria palmata, can lower cancer cell division and proliferation, while polysaccharides trigger the innate immune system, causing apoptosis in pancreatic islet cancer and human leukemia cells. Alkaloids, derived from marine sources, can inhibit cancer cell development. Peptides, found in various plant species, have shown cytotoxic effects on several human cell lines, including pancreatic, breast, lung, and bladder cancers. Marine drug approval faces challenges like the possibility of a resurgence of different metabolites due to environmental conditions and limited lead compound availability.

Harnessing the ocean’s pharmacy: marine bioactive compounds as next-generation therapeutics

The ocean’s vast and diverse ecosystem offers a rich reservoir of bioactive compounds with immense clinical potential. Marine organisms produce structurally unique and biologically active compounds, leading to breakthroughs in therapeutic development. Notable examples include anticancer agents like trabectedin and cytarabine, and the analgesic ziconotide. Marine compounds also exhibit potent antimicrobial and antiviral properties, addressing critical challenges like antibiotic resistance and emerging viral infections. Despite the promise, challenges such as sustainable harvesting and complex extraction processes persist. Advances in synthetic biology and metabolic engineering provide solutions for sustainable production, ensuring a stable supply of these valuable compounds. The integration of marine bioactives into modern medicine could revolutionize treatments for cancer, chronic pain, and infectious diseases, underscoring the need for continued investment in marine bioprospecting and biotechnological innovation.

Bioprospecting and marine ‘omics’: surfing the deep blue sea for novel bioactive proteins and peptides

The vast biological and biochemical diversity of the global ocean is the driver behind marine bioprospecting for novel bioproducts. As Marine Biotechnology is gaining momentum as one of the main pillars of the ‘Brue Growth’ revolution, the ability to screen for novel compounds of interest in species with little or no genomic resources is paramount. With this respect, proteins, which are easily metabolised, can be synthetised using convenient DNA recombinant methods and can easily be modified to better meet the needs of human society, making them prized targets. Evidently, proteins that hold natural bioactivity and specificity such as toxins and other venom components, have long captured the focus of biotechnologists, leading to the merger between environmental omics and toxinology termed as ‘venomics’. Indeed, bioactive proteins such as conopeptides, conotoxins, turripeptides and others are long deemed important subjects of research. Even though current mainstream paradigms set the focus on secondary metabolites from marine organisms, transcriptomics and proteomics approaches and their combination are rising strategies for screening for thousands of proteins and peptides in non-conventional biological models, emphasising, but not limited to, marine invertebrate animals due to their abundance, biodiversity and uncanny biochemical strategies to cope with selective pressure in literally every known marine habitat. Untargeted approaches, such as RNA-Seq – based transcriptomics and tandem mass spectrometry – based proteomics, can circumvent limitations related with absent or reduced genomic annotation. The present review will outline the main contributions of ‘omics’ and computational approaches for bioprospecting for proteinaceous marine bioactives. Despite the relatively low number of ‘omics’ studies with the main purpose of discover novel compounds, there is already important literature showcasing pipelines and approaches for revolutionising the exploration of the ocean.

Marine Bioactives and Their Application in the Food Industry: A Review

The structurally diverse bioactive compounds found in marine organisms represent valuable resources for the food and pharmaceutical industries. The marine ecosystem encompasses over half of the world’s biota, providing an extensive range of bioactive compounds that can be extracted from various marine life forms, including marine microorganisms (such as bacteria, cyanobacteria, and actinobacteria), algae (both macroalgae and microalgae), invertebrates (including sponges, mollusks, echinoderms, and crustaceans), and, most importantly, fish. Many of these organisms thrive in extreme marine environments, leading to the production of complex molecules with unique biological functions. Consequently, marine biomolecules, such as lipids (especially polyunsaturated fatty acids), proteins/peptides, polysaccharides, carotenoids, phenolics, and saponins, exhibit a wide range of biological properties and can serve as valuable components in nutraceuticals and functional foods. Nevertheless, most of these biomolecules are susceptible to oxidation and degradation; encapsulation-based technologies tend to preserve them and increase their bioavailability and functions. These biological compounds demonstrate diverse activities, including antioxidant, anticancer, antithrombotic, anticoagulant, anti-inflammatory, antiproliferative, antidiabetic, antimicrobial, and cardioprotective effects, making them promising candidates for applications in the food industry. Despite their numerous health benefits, marine bioactive compounds have remained underutilized, not only in the food industry but also in the pharmaceutical and nutraceutical sectors. Therefore, this review aims to provide an overview of the various sources of marine bioactive compounds and their potential contributions to the food industry.

A comprehensive review of the therapeutic potential of cyanobacterial marine bioactives: Unveiling the hidden treasures of the sea

AbstractMarine cyanobacterial bioactives, due to their diverse chemistry and promising pharmacological properties, hold significant potential as therapeutic agents. Here, we comprehensively review the scientific state‐of‐the‐art relating to marine cyanobacterial bioactives, including bioprospecting, preclinical and clinical studies, mechanisms of action, safety and toxicity considerations, sustainability, and conservation. We discuss challenges in and opportunities for developing marine cyanobacterial bioactives as therapeutics; we underscore their potential in treating life‐threatening health ailments, such as cancer and neurodegenerative, inflammatory and viral diseases. We further articulate the significant potential of marine cyanobacterial bioactives for improving human health, and identify future research directions underpinning their development as therapeutics.

Novel marine bioactives: application in functional foods, nutraceuticals, and pharmaceuticals

Functional food, nutraceutical, and pharmaceutical applications of natural products have gained growing attention as there is increasingly awareness of the association between bioactive compounds and improved health. Recently, food and biomedical scientists have focused more on marine resources to isolate bioactives since the marine ecosystem comprises unexploited resources with a wide range of organisms. Marine species produce a wide range of natural products, such as polysaccharides, peptides, polyunsaturated lipids, phenolic compounds, and pigments, with unique structures and diverse biological activities due to their extreme living environments. These active molecules reduce the risk of chronic disease and improve health by exhibiting antioxidant, anticancer, anti-inflammatory, antimicrobial, antidiabetic, anti-obesity, antihypertensive, cardioprotective, and neuroprotective activities. This review summarizes the recent discoveries of bioactive compounds from marine invertebrates (sponges, cnidarians, echinoderms, molluscs, ascidians, and crustaceans), fishes, seaweeds, and marine microorganisms and their potential for functional foods, nutraceuticals, and pharmaceuticals applications.

HR-LCMS assisted phytochemical screening and an assessment of anticancer activity of Sargassum Squarrossum and Dictyota Dichotoma using in vitro and molecular docking approaches

The research in the area of marine bioactives have substantially improved in the last few decades. The identified marine algae namely Sargassum squarrossum and Dictyota dichotoma were subjected to phytochemical profiling using the most sophisticated High-resolution-LCMS, 1H NMR and revealed the presence of many bioactive compounds.In vitro MTT tests on lung and breast cancer cells revealed that the DCM fractions of Sargassum squarrossum and Dictyota dichotoma have anticancer characteristics, and they also demonstrated significant dose-dependant cytotoxicity on tumour cell lines. In MCF7 cells, the IC50 values for Sargassum squarrossum and Dictyota dichotoma were 139.51 µg/ml and 241.89 µg/ml whereas in A549 the cell line, the IC 50 values for the DCM fractions of Sargassum squarrossum and Dictyota dichotoma were 95.37 µg/ml and 92.09 µg/ml, respectively. Sargassum squarrossum shows potent anticancer activity in MCF7 and A549 whereas Dictyota dichotoma has potent anticancer activity in A549 and moderate activity in MCF7 cell lines.The most prevalent enzymes VEGFR-2 and AXL tyrosine kinase, contribute to the development of cancer. A computational method was used to confirm the anticancer effects of the newly identified compounds targeting the above enzymes. According to the molecular docking studies, most of the detected compounds from marine algae were selectively interacting with AXL and VEGFR receptors with good binding affinity scores. The current work demonstrated the phytochemical assessment of marine algae and showed the ability of marine natural products to provide unique metabolites with significant biological activity.

Cardio-Protective Properties and Health Benefits of Fish Lipid Bioactives; The Effects of Thermal Processing

The beneficial effects of fish-derived lipid bioactives have come to prominence over the last few decades, especially for their utilization in fish oils, supplements, and nutraceuticals. Omega-3 (n-3) polyunsaturated fatty acids (PUFA), lipid vitamins, carotenoids, and polar lipid bioactives from fish have shown to possess a vast range of beneficial effects against a multitude of chronic disorders and especially against inflammation-and cardiovascular disorders (CVD). The observed cardio-protective effects and health benefits are believed to be attributed to the synergy of these fish-derived lipid bioactives. Within the present article the recent findings in the literature on the lipid content of the mainly consumed fish species, their bio-functionality, and cardio-protective benefits is thoroughly reviewed. Moreover, the recovery and valorization of such lipid bioactives from fish by-products and fishing by-catch, in order to reduce waste, while developing useful products containing cardio-protective lipids from the leftover materials of fisheries and aquaculture industries, are also of industrial and environmental interest. Emphasis is also given to the effects of heat treatments during fish processing on the structures and bio-functionality of these marine lipid bioactives, based on the paradigm of different cooking methodologies and thermal processing, while the compounds produced during such treatment(s) with detrimental changes in the fish lipid profile, which can reduce its cardio-protective efficacy, are also reviewed. Novel green extraction technologies and low temperature processing and cooking of fish and fishery by-products are needed to reduce these undesirable effects in a sustainable and environmentally friendly way.

Novel Bioactive Compounds From Marine Sources as a Tool for Functional Food Development

The marine environment is a relatively unexplored source of functional ingredients that can be used in food processing, storage, and fortification in a variety of ways. Marine microorganisms are a possible source of novel bioactive chemicals with potential human utility. Some of these microbes can live in the harsh marine environments, resulting in complex compounds with unique biological properties that can be used in several industrial and biotechnological applications. So far, several marine microorganisms (fungi, myxomycetes, bacteria, and microalgae) have been isolated that produce antioxidant, antibacterial, apoptotic, antitumoral, and antiviral chemicals. Furthermore, it emphasizes the enormous potential for marine microbes to produce very important bioactive chemicals. The main goal of this review is to provide a concise overview of several constituents of marine bioactives. Anticoagulant, anticancer, and hypocholesterolemic effects have been demonstrated for bioactive peptides extracted from fish protein hydrolysates, as well as algal fucans, galactans, and alginates. Furthermore, omega-3 fatty acids are abundant in fish oils and marine microorganisms, while potent antioxidants such as carotenoids and phenolic compounds can be found in crustaceans and seaweeds. This review focuses on the potential use of marine-derived chemicals as functional food ingredients for health maintenance and chronic disease prevention, based on their bioactive qualities.

Seaweed-Derived Proteins and Peptides: Promising Marine Bioactives.

Seaweeds are a typical food of East-Asian cuisine, to which are alleged several beneficial health effects have been attributed. Their availability and their nutritional and chemical composition have favored the increase in its consumption worldwide, as well as a focus of research due to their bioactive properties. In this regard, seaweed proteins are nutritionally valuable and comprise several specific enzymes, glycoproteins, cell wall-attached proteins, red algae phycobiliproteins, lectins, peptides, or mycosporine-like amino acids. This great extent of molecules has been reported to exert significant antioxidant, antimicrobial, anti-inflammatory, antihypertensive, antidiabetic, or antitumoral properties. Hence, knowledge on algae proteins and derived compounds have gained special interest for the potential nutraceutical, cosmetic or pharmaceutical industries based on these bioactivities. Although several molecular mechanisms of action on how these proteins and peptides exert biological activities have been described, many gaps in knowledge still need to be filled. Updating the current knowledge related to seaweed proteins and peptides is of interest to further asses their potential health benefits. This review addresses the characteristics of seaweed protein and protein-derived molecules, their natural occurrence, their studied bioactive properties, and their described potential mechanisms of action.

Alimentary and Pharmaceutical Approach to Natural Antimicrobials against Clostridioides difficile Gastrointestinal Infection.

Incidence of Clostridioides difficile infection (CDI) has been increasing in recent decades due to different factors, namely (i) extended use of broad-spectrum antibiotics, (ii) transmission within asymptomatic and susceptible patients, and (iii) unbalanced gastrointestinal microbiome and collateral diseases that favor C. difficile gastrointestinal domination and toxin production. Although antibiotic therapies have resulted in successful control of CDI in the last 20 years, the development of novel strategies is urged in order to combat the capability of C. difficile to generate and acquire resistance to conventional treatments and its consequent proliferation. In this regard, vegetable and marine bioactives have emerged as alternative and effective molecules to fight against this concerning pathogen. The present review examines the effectiveness of natural antimicrobials from vegetable and algae origin that have been used experimentally in in vitro and in vivo settings to prevent and combat CDI. The aim of the present work is to contribute to accurately describe the prospective use of emerging antimicrobials as future nutraceuticals and preventive therapies, namely (i) as dietary supplement to prevent CDI and reduce CDI recurrence by means of microbiota modulation and (ii) administering them complementarily to other treatments requiring antibiotics to prevent C. difficile gut invasion and infection progression.

From Seabed to Bedside: A Review on Promising Marine Anticancer Compounds.

The marine environment represents an outstanding source of antitumoral compounds and, at the same time, remains highly unexplored. Organisms living in the sea synthesize a wide variety of chemicals used as defense mechanisms. Interestingly, a large number of these compounds exert excellent antitumoral properties and have been developed as promising anticancer drugs that have later been approved or are currently under validation in clinical trials. However, due to the high need for these compounds, new methodologies ensuring its sustainable supply are required. Also, optimization of marine bioactives is an important step for their success in the clinical setting. Such optimization involves chemical modifications to improve their half-life in circulation, potency and tumor selectivity. In this review, we outline the most promising marine bioactives that have been investigated in cancer models and/or tested in patients as anticancer agents. Moreover, we describe the current state of development of anticancer marine compounds and discuss their therapeutic limitations as well as different strategies used to overcome these limitations. The search for new marine antitumoral agents together with novel identification and chemical engineering approaches open the door for novel, more specific and efficient therapeutic agents for cancer treatment.

Second Food Bioactives and Health Conference.

The Food Bioactives and Health Conference has been organized to present and discuss the recent advances in this topic. The first conference took place in Norwich (UK) in 2016 and was organized by Paul Kroon. This meeting was scientifically and technically so successful that in September 2018 Lisbon hosted the 2nd edition of this Conference. More than 250 delegates attended to 8 sessions and flash presentations from 80 speakers on the different topics related to food bioactives and health and 141 posters were presented. Sessions on bioactives effects on neuronal and immune functions, cardiometabolic health, the mechanism of action of plant bioactives and derived metabolites, dietary interventions with bioactives, bioactives functionalization and interactions, marine bioactives, bioactive peptides and proteins, polyphenols and glucosinolates, innovative approaches in bioactives research and novel bioactives, applications and dietary biomarkers were organized. This highlighted issue presents a selection of papers from invited speakers, oral presentations, and posters.

Viral assemblage variation in an Arctic shelf seafloor

UiT The Arctic University of Norway The Centre for Marine Bioactives and Drug Discovery (MABCENT-SFI) Marine Biotechnology in Northern Norway (MABIT).

Novel marine polysaccharides and maternal nutrition to stimulate gut health and performance in post-weaned pigs

Post-weaning complications in piglets are characterised by a reduction in feed intake and growth, atrophy of small-intestine architecture, upregulation of intestinal inflammatory cytokines, alterations in gastrointestinal microflora, diarrhoea and heightened susceptibility to infection. Traditional measures to reduce weaning-associated intestinal dysfunction have centred on dietary inclusion of antibiotic growth promoters in weaning pig diets, or high concentrations of dietary minerals in the form of zinc oxide. However, these strategies are under scrutiny because of their role in promoting multi-drug resistant bacteria and the accumulation of minerals in the environment. Up to recently, the main focus on finding alternatives to in-feed antibiotic growth promoters has been on dietary manipulations post-weaning, through the use of feed additives in the post-weaning diet. However, there are also other strategies that could enhance the growth and health of the newly weaned pig. One of these strategies is the use of maternal nutrition to improve growth and health in her offspring. The development of the immune system begins in utero and is further developed after the colonisation of the gastrointestinal tract with microbiota during birth and post-natal life. The early establishment of this relationship is fundamental to the development and long-term maintenance of gut homeostasis. There are significant efforts being made to identify natural alternatives to support the development of the piglet gastrointestinal tract, in particular during the weaning period. Chemodiversity in nature, including microorganisms, terrestrial plants, seaweeds and marine organisms, offers a valuable source of novel bioactives. This review will discuss the development of the intestinal tract in the pig during gestation, lactation and post-weaning periods and the factors that influence intestinal health post-weaning. It will also discuss how feeding marine bioactives in both the maternal diet and the piglet diet can be used to alleviate the negative effects associated with weaning.

Novel Therapeutic Strategies Against Cancer: Marine-derived Drugs May Be the Answer?

Marine ecosystem represents a wide and untapped reservoir of biologically active metabolites. Most of the sponges, seaweeds, crustaceans, fish species and their associated microorganisms have evolved chemical means in order to defend themselves against predation and to survive in the complex marine environment. Such chemical and biological adaptation produced many bioactive substances with beneficial effects on human health, including potential anticancer agents. With further exploration of sea and ocean environment, several marine bioactives have been identified with promising anticancer activity. More than one hundred novel bioactive compounds with antitumor activity and their synthetic derivative substances displayed in vitro cytotoxic property on neoplastic cell lines and are currently gaining great attention for further evaluations and in vivo applications. This review highlights novel marine molecules and compounds which have been able to inhibit different cancer species in the recent years and aims to describe research on new natural antineoplastic agents obtained from sea world.

Marine bioactives and potential application in sports.

An enriched diet with antioxidants, such as vitamin E, vitamin C, β-carotene and phenolic compounds, has always been suggested to improve oxidative stress, preventing related diseases. In this respect, marine natural product (MNP), such as COX inhibitors, marine steroids, molecules interfering with factors involved in the modulation of gene expression (such as NF-κB), macrolides, many antioxidant agents, thermogenic substances and even substances that could help the immune system and that result in the protection of cartilage, have been recently gaining attention. The marine world represents a reserve of bioactive ingredients, with considerable potential as functional food. Substances, such as chitin, chitosan, n-3 oils, carotenoids, vitamins, minerals and bioactive peptides, can provide several health benefits, such as the reduction of cardiovascular diseases, anti-inflammatory and anticarcinogenic activities. In addition, new marine bioactive substances with potential anti-inflammatory, antioxidant and thermogenic capacity may provide health benefits and performance improvement, especially in those who practice physical activity, because of their increased free radical and Reacting Oxygen Species (ROS) production during exercise, and, particularly, in athletes. The aim of this review is to examine the potential pharmacological properties and application of many marine bioactive substances in sports.

Marketed Marine Natural Products in the Pharmaceutical and Cosmeceutical Industries: Tips for Success

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.

Marine Bioactives: Pharmacological Properties and Potential Applications against Inflammatory Diseases

Inflammation is a hot topic in medical research, because it plays a key role in inflammatory diseases: rheumatoid arthritis (RA) and other forms of arthritis, diabetes, heart diseases, irritable bowel syndrome, Alzheimer’s disease, Parkinson’s disease, allergies, asthma, even cancer and many others. Over the past few decades, it was realized that the process of inflammation is virtually the same in different disorders, and a better understanding of inflammation may lead to better treatments for numerous diseases. Inflammation is the activation of the immune system in response to infection, irritation, or injury, with an influx of white blood cells, redness, heat, swelling, pain, and dysfunction of the organs involved. Although the pathophysiological basis of these conditions is not yet fully understood, reactive oxygen species (ROS) have often been implicated in their pathogenesis. In fact, in inflammatory diseases the antioxidant defense system is compromised, as evidenced by increased markers of oxidative stress, and decreased levels of protective antioxidant enzymes in patients with rheumatoid arthritis (RA). An enriched diet containing antioxidants, such as vitamin E, vitamin C, β-carotene and phenolic substances, has been suggested to improve symptoms by reducing disease-related oxidative stress. In this respect, the marine world represents a largely untapped reserve of bioactive ingredients, and considerable potential exists for exploitation of these bioactives as functional food ingredients. Substances such as n-3 oils, carotenoids, vitamins, minerals and peptides provide a myriad of health benefits, including reduction of cardiovascular diseases, anticarcinogenic and anti-inflammatory activities. New marine bioactives are recently gaining attention, since they could be helpful in combating chronic inflammatory degenerative conditions. The aim of this review is to examine the published studies concerning the potential pharmacological properties and application of many marine bioactives against inflammatory diseases.