Search Results (37)

The discovery of bioactive natural compounds from microbes holds promise for regenerative medicine. In this study, we identified and characterized a steroid-like compound, 3,12-dioxochola-4,6-dien-24-oic acid (DOCDA), from a crude extract of Rhodococcus sp. DOCDA significantly promoted wound healing by enhancing HaCaT cell invasion and migration. It upregulated key growth factors (EGF, VEGF-A, IGF, TGF-β, and HGF), indicating the activation of regenerative signaling. Additionally, DOCDA increased the expression of genes related to focal adhesion and cytoskeletal regulation (ITGB1, ITGA4, FAK, SRC, RHOA, CDC42, RAC1, and paxillin), supporting enhanced cellular motility and remodeling. Notably, DOCDA promoted stem-like properties in HaCaT cells, as shown by increased spheroid formation and elevated levels of the stemness markers ALDH1 and CD44. Target prediction and molecular docking identified the glucocorticoid receptor (GR) as the primary target of DOCDA, with a docking score of −7.7 kcal/mol. Network and pathway enrichment analysis revealed that GR-linked pathways were significantly associated with wound healing, including steroid hormone signaling, inflammation, immune responses, and cell migration. In vivo, the topical application of DOCDA led to over 70% wound closure in mice by day 5. These findings suggest that DOCDA is a steroid-like compound that accelerates wound healing and may serve as a potential agent in regenerative therapy. Full article

The expanding field of nutraceuticals and functional food science is increasingly turning to marine-derived bioactive compounds, particularly saponins, for their diverse pharmacological properties. These so-called thalassochemicals display distinctive structural features—such as sulfated glycosidic moieties and amphiphilic backbones—that underpin potent antitumor, hypolipidemic, antioxidant, and antimicrobial activities. In contrast to their terrestrial analogs, marine saponins remain underexplored, and their complexity poses analytical and functional challenges. This review provides a critical and integrative synthesis of recent advances in the structural elucidation, biological function, and technological application of marine saponins. Special emphasis is placed on the unresolved limitations in their isolation, characterization, and structural validation, including coelution of isomers, adduct formation in MS spectra, and lack of orthogonal techniques such as NMR or FTIR. We illustrate these limitations through original MS/MS data and propose experimental workflows to improve compound purity and identification fidelity. In addition to discussing known structure–activity relationships (SARs) and mechanisms of action, we extend the scope by integrating recent developments in computational modeling, including machine learning, molecular descriptors, and quantitative structure–activity relationship (QSAR) models. These tools offer new avenues for predicting saponin bioactivity, despite current limitations in available high-quality datasets. Furthermore, we include a classification and comparison of steroidal and triterpenoid saponins from marine versus terrestrial sources, complemented by detailed chemical schematics. We also address the impact of processing techniques, delivery systems, and bioavailability enhancements using encapsulation and nanocarriers. Finally, this review contextualizes these findings within the regulatory and sustainability frameworks that shape the future of saponin commercialization. By bridging analytical chemistry, computational biology, and food technology, this work establishes a roadmap for the targeted development of marine saponins as next-generation nutraceuticals and functional food ingredients. 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

Five novel 2-methyl-4-(1-glycerol)furan (MGF) dimers, namely nocardifuran A (1), 13-acetyl-nocardifuran A (2), 15-epi-nocardifuran A (3), nocardifuran B (4), and nocardifuran C (5), were isolated from the Gause liquid fermentation of the marine-derived Nocardiopsis sp. ZSN1. Their structures were elucidated through HRESIMS, 1D and 2D NMR spectroscopic data analysis, and ECD calculations. Compounds 1–4 were identified as derivatives of MGF with its rearrangement of furan or pyran derivatives, while compound 5 was identified as the derivative of MGF with an indole derivative. These MGF dimers, representing a new structural class, were isolated from a marine microorganism for the first time, thereby enhancing chemical diversity. Screening for farnesoid X receptor (FXR) agonistic activity revealed that MGF dimers could activate FXR. Furthermore, bioactivity evaluations demonstrated that these types of compounds exhibited lipid-lowering activity with lower cytotoxicity in vitro. Consequently, our findings not only contribute to the chemical diversity of marine-derived MGF-type natural products but also offer potential insights into the development of MGF dimers as lead compounds for FXR agonists in the dysregulation of hepatic lipid metabolism. 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

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

Fusarium species are commonly found in soil, water, plants, and animals. A variety of secondary metabolites with multiple biological activities have been recently isolated from Fusarium species, making Fusarium fungi a treasure trove of bioactive compounds. This mini-review comprehensively highlights the newly isolated secondary metabolites produced by Fusarium species and their various biological activities reported from 2019 to October 2024. About 276 novel metabolites were revealed from at least 21 Fusarium species in this period. The main metabolites were nitrogen-containing compounds, polyketides, terpenoids, steroids, and phenolics. The Fusarium species mostly belonged to plant endophytic, plant pathogenic, soil-derived, and marine-derived fungi. The metabolites mainly displayed antibacterial, antifungal, phytotoxic, antimalarial, anti-inflammatory, and cytotoxic activities, suggesting their medicinal and agricultural applications. This mini-review aims to increase the diversity of Fusarium metabolites and their biological activities in order to accelerate their development and applications. Full article

Inflammation is considered as one of the most primary protective innate immunity responses, closely related to the body’s defense mechanism for responding to chemical, biological infections, or physical injuries. Furthermore, prolonged inflammation is undesirable, playing an important role in the development of various diseases, such as heart disease, diabetes, Alzheimer’s disease, atherosclerosis, rheumatoid arthritis, and even certain cancers. Marine-derived fungi represent promising sources of structurally novel bioactive natural products, and have been a focus of research for the development of anti-inflammatory drugs. This review covers secondary metabolites with anti-inflammatory activities from marine-derived fungi, over the period spanning August 2018 to July 2024. A total of 285 anti-inflammatory metabolites, including 156 novel compounds and 11 with novel skeleton structures, are described. Their structures are categorized into five categories: terpenoids, polyketides, nitrogen-containing compounds, steroids, and other classes. The biological targets, as well as the in vitro and in vivo screening models, were surveyed and statistically summarized. This paper aims to offer valuable insights to researchers in the exploration of natural products and the discovery of anti-inflammatory drugs. Full article

This article presents a comprehensive overview of recent discoveries and advancements in the field of steroid chemistry, highlighting the isolation and characterization of various steroidal compounds from natural sources. This paper discusses a wide range of steroids, including pregnane steroids, steroidal alkaloids, ketosteroids, and novel triterpenoids, derived from marine organisms, fungi, and plants. Significant findings include the isolation of bioactive compounds such as the cytotoxic erectsterates from microorganisms, soft corals, the unusual tetracyclic steroid penicillitone from a fungal culture, and innovative steroidal derivatives with potential anti-inflammatory and anticancer activities. The synthesis of steroids from microorganisms as a tool for pharmaceutical development is also explored, showcasing the role of microbial biotransformation in generating steroidal drugs. Additionally, this paper emphasizes the ecological and medicinal relevance of these compounds, which are often used in traditional medicine and have potential therapeutic applications in treating diseases like cancer and microbial infections. This article serves as a vital resource for researchers interested in the chemical diversity of steroids and their applications in drug discovery and development. Full article

Cladosporium, a genus of ascomycete fungi in the Dematiaceae family, is primarily recognized as a widespread environmental saprotrophic fungus or plant endophyte. Further research has shown that the genus is distributed in various environments, particularly in marine ecosystems, such as coral reefs, mangroves and the polar region. Cladosporium, especially the marine-derived Cladosporium, is a highly resourceful group of fungi whose natural products have garnered attention due to their diverse chemical structures and biological activities, as well as their potential as sources of novel leads to compounds for drug production. This review covers the sources, distribution, bioactivities, biosynthesis and structural characteristics of compounds isolated from Cladosporium in the period between January 2000 and December 2022, and conducts a comparative analysis of the Cladosporium isolated compounds derived from marine and terrestrial sources. Our results reveal that 34% of Cladosporium-derived natural products are reported for the first time. And 71.79% of the first reported compounds were isolated from marine-derived Cladosporium. Cladosporium-derived compounds exhibit diverse skeletal chemical structures, concentrating in the categories of polyketides (48.47%), alkaloids (19.21%), steroids and terpenoids (17.03%). Over half of the natural products isolated from Cladosporium have been found to have various biological activities, including cytotoxic, antibacterial, antiviral, antifungal and enzyme-inhibitory activities. These findings testify to the tremendous potential of Cladosporium, especially the marine-derived Cladosporium, to yield novel bioactive natural products, providing a structural foundation for the development of new drugs. Full article

This article explores the diverse array of biologically active compounds derived from microbial symbionts, particularly focusing on the isolation and characterization of diepoxides, highly oxygenated triterpenoids, secosteroids, ergostane-type steroids, and meroterpenoids from various marine and plant-derived fungi. We highlight significant discoveries such as vitamin D variants from fungal species, unique sesterterpenoids from mangrove endophytic fungi, and secosteroids with potential medicinal applications. The study delves into the structural uniqueness and bioactivities of these compounds, including their anti-inflammatory, antibacterial, antifungal, antiviral, and cytotoxic effects. Notable findings include the isolation of compounds with significant activity against cancer cell lines, the inhibition of acetylcholinesterase, and promising antifouling properties. This work underscores the potential of microbial symbionts as a rich source of novel bioactive compounds with diverse therapeutic applications, highlighting the importance of marine and fungal biodiversity in drug discovery and development. Full article

COVID-19 patients with comorbid DM face more severe outcomes, indicating that hyperglycemic conditions exacerbate SARS-CoV-2 infection. Negative side effects from existing hyperglycemia treatments have urged the need for safer compounds. Therefore, sourcing potential compounds from marine resources becomes a new potential approach. Algal lipids are known to possess beneficial activities for human health. However, due to limitations in analyzing large amounts of potential anti-hyperglycemic and anti-COVID-19-related marine metabolites, there is an increasing need for new approaches to reduce risks and costs. Therefore, the main aim of this study was to identify potential compounds in macroalgae Sargassum cristaefolium, Tricleocarpa cylindrica, and Ulva lactuca lipophilic extracts for treating DM and COVID-19 by an integrated approach utilizing in vitro anti-oxidant, in vivo anti-hyperglycemic, and metabolomic-integrated in silico approaches. Among them, S. cristaefolium and T. cylindrica showed potential anti-hyperglycemic activity, with S. cristaefolium showing the highest anti-oxidant activity. A GC-MS-based untargeted metabolomic analysis was used to profile the lipophilic compounds in the extracts followed by an in silico molecular docking analysis to examine the binding affinity of the compounds to anti-DM and anti-COVID-19 targets, e.g., α-amylase, α-glucosidase, ACE2, and TMPRSS2. Notably, this study reveals for the first time that steroid-derived compounds in the macroalgae T. cylindrica had higher binding activity than known ligands for all the targets mentioned. Studies on drug likeliness indicate that these compounds possess favorable drug properties. These findings suggest the potential for these compounds to be further developed to treat COVID-19 patients with comorbid DM. The information in this study would be a basis for further in vitro and in vivo analysis. It would also be useful for the development of these candidate compounds into drug formulations. Full article

This review explores the biological activity and structural diversity of steroids and related isoprenoid lipids, with a particular focus on compounds containing an oxirane ring. These natural compounds are derived from fungi, fungal endophytes, as well as extracts of plants, algae, and marine invertebrates. To evaluate their biological activity, an extensive examination of refereed literature sources was conducted, including in vivo and in vitro studies and the utilization of the QSAR method. Notable properties observed among these compounds include strong anti-inflammatory, antineoplastic, antiproliferative, anti-hypercholesterolemic, antiparkinsonian, diuretic, anti-eczematic, anti-psoriatic, and various other activities. Throughout this review, 3D graphs illustrating the activity of individual steroids are presented, accompanied by images of selected terrestrial or marine organisms. Furthermore, this review provides explanations for specific types of biological activity associated with these compounds. The data presented in this review are of scientific interest to the academic community and carry practical implications in the fields of pharmacology and medicine. By analyzing the biological activity and structural diversity of steroids and related isoprenoid lipids, this review offers valuable insights that contribute to both theoretical understanding and applied research. This review draws upon data from various authors to compile information on the biological activity of natural steroids containing an oxirane ring. Full article

This review delves into the investigation of the biological activity and structural diversity of steroids and related isoprenoid lipids. The study encompasses various natural compounds, such as steroids with aromatic ring(s), steroid phosphate esters derived from marine invertebrates, and steroids incorporating halogen atoms (I, Br, or Cl). These compounds are either produced by fungi or fungal endophytes or found in extracts of plants, algae, or marine invertebrates. To assess the biological activity of these natural compounds, an extensive examination of referenced literature sources was conducted. The evaluation encompassed in vivo and in vitro studies, as well as the utilization of the QSAR method. Numerous compounds exhibited notable properties such as strong anti-inflammatory, anti-neoplastic, anti-proliferative, anti-hypercholesterolemic, anti-Parkinsonian, diuretic, anti-eczematic, anti-psoriatic, and various other activities. Throughout the review, 3D graphs illustrating the activity of individual steroids are presented alongside images of selected terrestrial or marine organisms. Additionally, the review provides explanations for specific types of biological activity associated with these compounds. The data presented in this review hold scientific interest for academic science as well as practical implications in the fields of pharmacology and practical medicine. The analysis of the biological activity and structural diversity of steroids and related isoprenoid lipids provides valuable insights that can contribute to advancements in both theoretical understanding and applied research. Full article