Search Results (303)

Microorganisms serve as a vital source of natural anticancer agents, with many of their secondary metabolites already employed in clinical oncology. In recent years, salt-adapted microbes, including halophilic and halotolerant species from marine, salt lake, and other high-salinity environments, have gained significant attention. Their unique adaptation mechanisms and diverse secondary metabolites offer promising potential for novel anticancer drug discovery. This review consolidated two decades of research alongside current global cancer statistics to evaluate the therapeutic potential of salt-adapted microorganisms. Halophilic and halotolerant species demonstrate significant promise, with their bioactive metabolites exhibiting potent inhibitory effects against major cancer cell lines, particularly in lung and breast cancer. Evidence reveals structurally unique secondary metabolites displaying enhanced cytotoxicity compared to conventional anticancer drugs. Collectively, salt-adapted microorganisms represent an underexplored yet high-value resource for novel anticancer agents, offering potential solutions to chemotherapy resistance and treatment-related toxicity. Full article

Tetracyclic bis-piperidine alkaloids (TcBPAs) are structurally complex natural products primarily isolated from marine sponges of the order Haplosclerida. Distinguished by their intricate architecture, TcBPAs feature two central piperidine units linked by dual macrocyclic rings. These unique structural motifs contribute significantly to their biological activities. For example, TcBPAs exhibit antiproliferative activities at low micromolar concentrations across various cancer cell lines, including leukemia, melanoma, breast, colon, fibrosarcoma, and glioblastoma. Despite this promising therapeutic profile, the structural intricacy of TcBPAs has posed considerable challenges to the development of efficient synthetic methodologies, thereby limiting comprehensive exploration and potential clinical advancement. This review highlights recent progress and persisting challenges in the synthesis, structural analysis, and biological evaluation of TcBPAs, underscoring their therapeutic potential in anticancer drug discovery. Full article

The purpose of this study was to investigate the taxonomic and phylogenomic placement of the proposed genus ‘Solwaraspora’ within the context of other marine genera using a dual-omics approach. Initially, we isolated bacteria from marine tunicates, squirts, and sponges, which were morphologically similar to an emerging genus (identified as ‘Micromonospora_E’ by the GTDB-tk2 database using whole genome sequence data) by colony shape, size, and clustering pattern, but only found five strains in our dataset belonging to this distinction. Due to the minimally explored nature of this genus, we sought to identify more bacterial strains with similar morphology to Micromonospora‘Micromonospora_E’ by whole genome sequencing (WGS). Within our collection, we noted 35 strains that met this criterion and extracted genomic information to perform WGS on these strains. With this information, we studied taxonomic and phylogenomic relationships among these organisms. Using the data gathered from WGS, we were able to identify an additional five strains labeled by the GTDB-tk2 database as Micromonospora‘Micromonospora_E’, as well as construct phylogenomic trees to examine the evolutionary relationships between these strains. ANI values were calculated between strains from our dataset and type strains of Micromonospora and Plantactinospora as well as against an outgroup Streptomyces strain. No type strains are available for ‘Solwaraspora’. Using MALDI-TOF MS, we positively identified ‘Solwaraspora’, which was supported by the phylogenomic tree showing Micromonospora’Micromonospora_E’ (‘Solwaraspora’) in a distinct clade from Plantactinospora and Micromonospora. Additionally, we discovered gene cluster families (GCFs) in alignment with genera, as well as a large representation of biosynthetic gene clusters (BGCs) coming from the ‘Solwaraspora’ strains. These findings suggest significant potential to discover novel chemistry from ‘Solwaraspora’, adding to the importance of investigating this new genus of bacteria. Full article

Algal polysaccharides are a kind of bioactive compound with diverse pharmacological applications, yet their structure–activity relationships and therapeutic potential in chronic disease management remain systematically underexplored. This review comprehensively analyzes the structural characteristics of brown, red, and green algal polysaccharides, revealing how specific structural features—such as glycosidic linkage patterns and sulfate group positioning—dictate their biological activities. We also demonstrated their multifaceted roles in diabetes, cancer, and cardiovascular diseases through distinct mechanisms, including gut microbiota modulation via short-chain fatty acid production, antioxidant enzyme activation, and targeted inhibition of pathological signaling pathways like mTOR and JAK-STAT3. The work further evaluates extraction methodologies, highlighting the advantages of emerging techniques such as enzyme-assisted and ultrasonic extraction for preserving bioactive integrity. By integrating fundamental research with practical applications in functional foods, this synthesis provides critical insights for harnessing algal polysaccharides in precision nutrition and sustainable biomedicine, while identifying key challenges in standardization and environmental safety that warrant future investigation. Full article

Marine-derived Penicillium spp., including Penicillium citrinum, Penicillium chrysogenum, and Penicillium sclerotiorum, have emerged as prolific producers of structurally diverse secondary metabolites with cytotoxic activity. This review systematically categorizes 177 bioactive compounds isolated from marine Penicillium spp. between 2018 and 2024, derived from diverse marine environments such as sediments, animals, plants, and mangroves. These compounds, classified into polyketides, alkaloids, terpenoids, and steroids, exhibit a wide range of cytotoxic activities. Their potency is categorized as potent (<1 μM or <0.5 μg/mL), notable (1–10 μM or 0.5–5 μg/mL), moderate (10–30 μM or 5–15 μg/mL), mild (30–50 μM or 15–25 μg/mL), and negligible (>50 μM or >25 μg/mL). The current review highlights the promising role of marine Penicillium spp. as a rich repository for the discovery of anticancer agents and the advancement of marine-inspired drug development. Full article

Steroids have been pivotal in medicine and biology, with research into their therapeutic potential accelerating over the past few decades. This review examines recent steroid discoveries from marine and terrestrial sources, highlighting both novel compounds and those with newly identified biological activities. The structural diversity of these steroids contributes to their wide range of biological activity, including anticancer, antimicrobial, antidiabetic, anti-inflammatory, and immunomodulatory properties. Particular emphasis is placed on steroids derived from marine invertebrates, fungi, and medicinal plants, which have shown promising therapeutic potential. Advances in analytical techniques such as NMR spectroscopy and mass spectrometry have facilitated the identification of these compounds. These findings emphasize the growing importance of steroids in addressing pressing global health issues, particularly antibiotic resistance and cancer, where new therapeutic strategies are urgently needed. Although many newly identified steroids exhibit potent bioactivity, challenges remain in translating these findings into clinical therapies. Ongoing exploration of natural sources, along with the application of modern synthetic and computational methods, will be crucial in unlocking the full therapeutic potential of steroid-based compounds. Full article

Bioactive components of abalone and other marine organisms have attracted significant attention owing to their functional performance. The development of peptides with bioactivity like angiotensin-converting enzyme inhibitory (ACEi) and antioxidant properties is of great significance for chronic disease management and drug discovery. In this study, according to the issues of low utilization rate and bioactive content from the hydrolysate of abalone, single-factor and orthogonal experiments were designed to improve the utilization rate of abalone protein, and step hydrolysis with specific proteases was used to improve the overall biological activity of the hydrolysate. A total of 1937 peptide sequences were obtained from the highly bioactive components after separation and peptidomic analysis. Through virtual screening and molecular docking, 14 peptides exhibiting ACEi activity were identified and synthesized for experimental verification, with IC₅₀ values ranging from 0.05 to 0.54 mg/mL. Notably, nine of these peptides were powerful antioxidants. The developed step enzymatic hydrolysis and in silico screening-assisted preparation also provided a feasible and efficient method for exploring more bioactive peptides from diverse biomasses. Full article

Diterpenoids from marine-derived organisms represent a prolific source of secondary metabolites, characterized by their exceptionally promising chemical structures and pronounced pharmacological properties. In recent years, marine diterpenoids have garnered considerable attention and are regarded as a prominent area of scientific research. As a vital class of metabolites, diterpenoids show diverse biological activities, encompassing antibacterial, antifungal, antiviral, anti-inflammatory, inhibitory, and cytotoxic activities, among others. With the rapid advancement of equipment and identified technology, there has been a tremendous surge in the discovery rate of novel diterpenoid skeletons and bioactivities derived from marine fungi over the past decade. The present review compiles the reported diterpenoids from marine fungal sources mainly generated from January 2000 to December 2024. In this paper, 515 diterpenoids from marine organisms are summarized. Among them, a total of 281 structures from various fungal species are included, comprising 55 from sediment, 39 from marine animals (predominantly invertebrates, including 17 from coral and 22 from sponges), and 53 from marine plants (including 34 from algae and 19 from mangrove). Diverse biological activities are exhibited in 244 compounds, and among these, 112 compounds showed great anti-tumor activity (45.90%) and 110 metabolites showed remarkable cytotoxicity (45.08%). Furthermore, these compounds displayed a range of diverse bioactivities, including potent anti-oxidant activity (2.87%), promising anti-inflammatory activity (1.64%), great anti-bacterial activity (1.64%), notable anti-thrombotic activity (1.23%), etc. Moreover, the diterpenoids’ structural characterization and biological activities are additionally elaborated upon. The present critical summary provides a comprehensive overview of the reported knowledge regarding diterpenoids derived from marine fungi, invertebrates, and aquatic plants. The systematic review presented herein offers medical researchers an extensive range of promising lead compounds for the development of marine drugs, thereby furnishing novel and valuable pharmaceutical agents. Full article

Voltage-gated sodium (Nav) channels play a crucial role in initiating and propagating action potentials throughout the heart, muscles and nervous systems, making them targets for a number of drugs and toxins. While patch-clamp electrophysiology is considered the gold standard for measuring ion channel activity, its labor-intensive and time-consuming nature highlights the need for fast screening strategies to facilitate a preliminary selection of potential drugs or hazards. In this study, a high-throughput and cost-effective biosensing method was developed to rapidly identify specific agonists and inhibitors targeting the human Nav1.1 (hNav1.1) channel. It combines a red fluorescent dye sensitive to transmembrane potentials with CHO cells stably expressing the hNav1.1 α-subunit (hNav1.1-CHO). In the initial screening mode, the tested compounds were mixed with pre-equilibrated hNav1.1-CHO cells and dye to detect potential agonist effects via fluorescence enhancement. In cases where no fluorescence enhancement was observed, the addition of a known agonist veratridine allowed the indication of inhibitor candidates by fluorescence reduction, relative to the veratridine control without test compounds. Potential agonists or inhibitors identified in the initial screening were further evaluated by measuring concentration–response curves to determine EC₅₀/IC₅₀ values, providing semi-quantitative estimates of their binding strength to hNav1.1. This robust, high-throughput biosensing assay was validated through comparisons with the patch-clamp results and tested with 12 marine toxins, yielding consistent results. It holds promise as a low-cost, rapid, and long-term stable approach for drug discovery and non-target screening of neurotoxins. Full article

Cone snails are carnivorous marine predators that prey on mollusks, worms, or fish. They purposefully inject a highly diversified and peptide-rich venom, which can vary according to the predatory or defensive intended use. Previous studies have shown some correlations between the predation- and defense-evoked venoms and specific sections of the venom gland. In this study, we focus on the characterization of the venom of Cylinder canonicus, a molluscivorous species collected from Mayotte Island. Integrated proteomics and transcriptomics studies allowed for the identification of 108 conotoxin sequences from 24 gene superfamilies, with the most represented sequences belonging to the O1, O2, M, and conkunitzin superfamilies. A comparison of the predatory injected venom and the distal, central, and proximal sections of the venom duct suggests mostly distal origin. Identified conotoxins will contribute to a better understanding of venom–ecology relationships in cone snails and provide a novel resource for potential drug discovery. Full article

In recent years, marine natural products have continued to serve as a pivotal resource for novel drug discovery. Globally, the number of studies focusing on Porifera has been on the rise, underscoring their considerable importance and research value. Marine sponges are prolific producers of a vast array of bioactive compounds, including terpenes, alkaloids, peptides, and numerous secondary metabolites. Over the past fifteen years, a substantial number of sponge-derived terpenes have been identified, exhibiting extensive structural diversity and notable biological activities. These terpenes have been isolated from marine sponges or their associated symbiotic microorganisms, with several demonstrating multifaceted biological activities, such as anti-inflammatory, antibacterial, cytotoxic, anticancer, and antioxidant properties. In this review, we summarize 997 novel terpene metabolites, detailing their structures, sources, and activities, from January 2009 to December 2024. The structural features and structure-activity relationship (SAR) of different types of terpenes are broadly analyzed and summarized. This systematic and comprehensive review will contribute to the summary of and speculation on the taxonomy, activity profiles, and SAR of terpenes and the development of sponge-derived terpenes as potential lead drugs. Full article

It is widely recognized that prostate cancer is a multifaceted illness that is the second most common cause of cancer-related fatalities among males. Natural sources from both plants and marine organisms have long been used in treating various diseases and in the discovery of new pharmaceutical compounds. Medicinal plants, in particular, provide bioactive substances like alkaloids, phenolic compounds, terpenes, and steroids. In addition, marine natural products play a crucial role in the search for novel cancer treatments. A substantial number of anticancer drugs have been derived from natural sources, including plants, marine organisms, and microorganisms. In fact, over the past 60 years, 80% of new chemical entities have originated from natural sources, which are generally considered safer than synthetic compounds. This review seeks to emphasize the role of phytochemical compounds derived from both plant and marine sources in prostate cancer, highlighting their potential therapeutic impact. It is also intended to support global researchers working on the identification of natural-based treatments for prostate cancer. Full article

Under physiological conditions, the inflammatory response acts as a biological defense against tissue damage or infection, and is rapidly resolved once the infection is cleared. However, chronic inflammatory diseases, including inflammatory bowel disease (IBD), have become increasingly widespread in the last decades, placing a burden on the quality of life of affected people and on healthcare systems worldwide. Available drug therapies are often ineffective due to the chronic nature of these diseases, and prolonged administration of drugs can result in severe side effects for the patient or a lack of efficacy. In addition, there is the growing problem of bacterial resistance to synthetic antibiotics. Together, these factors have led to a strong research focus on the discovery of natural products capable of treating IBD. Recently, there has been a growing interest in compounds derived from marine sources, mainly algae, due to their bioactive secondary metabolites with anti-inflammatory properties well known in the literature. Based on this evidence, this review aimed to evaluate the anti-inflammatory potential of algae-derived biomolecules in IBD. In particular, interesting species from green algae (e.g., Chlorella vulgaris and Ulva pertusa), brown algae (e.g., Macrocystis pyrifera and Ecklonia cava) and red algae (e.g., Porphyra tenera and Grateloupia turuturu) are included in this review due to their proven anti-inflammatory properties. For this purpose, an extensive literature search was conducted using several databases. The results suggest that both macroalgae and microalgae have remarkable potential for IBD therapy due to the anti-inflammatory and antioxidant activities of their bioactive compounds. However, while the preclinical evidence is encouraging, further and long-term clinical studies are needed to better understand their mechanisms of action in order to determine the true efficacy of marine algae in the treatment of IBD. Full article

Echinoderms, a diverse group of marine invertebrates including starfish, sea urchins, and sea cucumbers, have been recognized as prolific sources of structurally diverse natural products. In the past five years, remarkable progress has been made in the isolation, structural elucidation, and pharmacological assessment of these bioactive compounds. These metabolites, including polysaccharides, triterpenoids, steroids, and peptides, demonstrate potent bioactivities such as anticancer, anti-inflammatory, antiviral, and antimicrobial effects, providing valuable insights and scaffolds for drug discovery. This review highlights the structural diversity and biological activities of natural products derived from echinoderms over the last five years, with a particular focus on their structure–activity relationships and therapeutic potential. It also outlines the prospects and challenges for future research, aiming to stimulate further exploration in marine drug discovery. Full article

The increase in cancer incidence in recent years necessitates urgent exploration of novel and alternative sources of natural bioactives for targeted cancer therapy. Approximately 75% of the Earth’s surface is covered by oceans, which are thought to harbor untapped physiologically active compounds with potential efficacy against cancer. Recently, a growing focus has been on isolating and investigating novel bioactive compounds derived from marine sources. Bioactive metabolites with diverse chemical structures, isolated from various marine species such as algae, mollusks, and actinomycetes, demonstrate potential efficacy against a wide range of cancers. To our knowledge, this is one of the articles that has reviewed recent papers on the application of marine-derived bioactives in targeted cancer therapy. This study aims to showcase some of the most current developments in targeted cancer therapy with various bioactives that have been identified from marine sources. Full article