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Pharmaceuticals
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Natural Products Derived from Fungi and Their Biological Activities
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Natural Products Derived from Fungi and Their Biological Activities

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (25 May 2025) | Viewed by 8533

Special Issue Editor

Dr. Katarzyna J. Kała

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Guest Editor
Department of Pharmaceutical Botany, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland
Interests: medicinal mushrooms; mycelial cultures; biotechnology; bioactive compounds; pro-health activity
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Medicinal fungi are products that have been present in human life for centuries. On the one hand, mushrooms were appreciated for their flavor, aroma, and nutritional potential, while on the other hand they were a source of bioactive substances and were used as medicines. In recent years, due to the development of analytical techniques, more and more properties of fungi are being recognized and their specific mechanisms of action are being determined. It has been proven that fungi exhibit a number of activities, including antioxidant, immunostimulating, antimicrobial, anti-atherosclerotic, or anti-inflammatory effects. Despite the numerous reports on fungi, there is a constant need for new works on a broad and comprehensive analysis of such natural products, so that they can be used in the prevention and treatment of diseases.

This Special Issue covers any aspect connected to medicinal fungi, brief reports, communications, research articles, as well as reviews.

Dr. Katarzyna J. Kała
Guest Editor

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • fungi
  • medicinal fungi
  • fruiting bodies
  • mycelial cultures
  • bioactive compounds
  • pro-health activity
  • mushroom products
  • natural therapy
  • natural medicines

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Published Papers (6 papers)

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Research

21 pages, 3499 KiB  
Article
Auricularia auricula’s Exopolysaccharide Mitigates DSS-Induced Colitis Through Dectin–1-Mediated Immunomodulation and Microbiota Remodeling
by Luísa Coutinho Coelho, Luísa Dan Favilla, Thais Bergmann de Castro, Maria Carolina B. Di Medeiros Leal, Christian Hoffmann and Anamélia Lorenzetti Bocca
Pharmaceuticals 2025, 18(8), 1085; https://doi.org/10.3390/ph18081085 - 22 Jul 2025
Abstract
Background/Objectives: Ulcerative colitis (UC) is characterized by the interplay between immune responses and dysbiosis in disease development. Aiming to provide additional insights into disease development and potential treatment strategies, the present study investigates the local effect of oral treatment with polysaccharides obtained from [...] Read more.
Background/Objectives: Ulcerative colitis (UC) is characterized by the interplay between immune responses and dysbiosis in disease development. Aiming to provide additional insights into disease development and potential treatment strategies, the present study investigates the local effect of oral treatment with polysaccharides obtained from Auricularia auricula’s submerged culture in an experimental model of DSS-induced colitis and its impact on lesion resolution. Methods: The structure and monosaccharide composition of Auricularia polysaccharides were characterized through Nuclear Magnetic Resonance (NMR). To evaluate the effect of this polysaccharide on the murine model, wild-type and Dectin-1 knockout mice were treated or not with the exopolysaccharide (EPS) while under DSS consumption. During the experimental period, feces samples were collected to evaluate microbial shifts during disease development, and, finally, the colonic tissue was analyzed to assess the inflammatory process and cytokine production. Results: The EPS composition showed a polymeric mixture of glucans and fucogalactomannans. The treatment of the wild-type DSS-induced colitis group improved the inflammatory response by increasing gut–homeostatic cytokines, such as interleukin-10 (IL-10) and tumor necrosis factor-alpha (TNF-α). The Dectin-1 KO mice group did not show the same enhancement after EPS treatment. The microbiome analysis revealed a difference in the genotype, and the treatment modified the DSS microbiome modulation, with nine and four ASVs in WT and Dectin-1 KO mice, respectively. Conclusions: The EPS treatment demonstrated therapeutic potential in treating inflammatory intestinal diseases by modulating cytokine secretion and microbiota composition, which is dependent on the Dectin-1 receptor’s carbohydrate recognition. Full article
(This article belongs to the Special Issue Natural Products Derived from Fungi and Their Biological Activities)
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20 pages, 6229 KiB  
Article
Integrating Network Pharmacology and Experimental Validation to Explore the Effect and Mechanism of Inonotus obliquus Polysaccharide in the Treatment of Rheumatoid Arthritis
by Yuan Fu, Tianyi Jiang, Xizhu Fang, Yifang Chen, Jiawei Li, Shengnan Huang, Fangfang Li and Dan Jin
Pharmaceuticals 2025, 18(7), 1017; https://doi.org/10.3390/ph18071017 - 8 Jul 2025
Viewed by 415
Abstract
Background/Objectives: Rheumatoid arthritis (RA) is a chronic, systemic, and progressive autoimmune–inflammatory disease primarily affecting small joints. Inonotus obliquus polysaccharide (IOP) is the main component of the parasitic fungus obliquus, which has anti-tumor, anti-inflammatory, and antioxidant effects. However, whether IOP has a therapeutic effect [...] Read more.
Background/Objectives: Rheumatoid arthritis (RA) is a chronic, systemic, and progressive autoimmune–inflammatory disease primarily affecting small joints. Inonotus obliquus polysaccharide (IOP) is the main component of the parasitic fungus obliquus, which has anti-tumor, anti-inflammatory, and antioxidant effects. However, whether IOP has a therapeutic effect on RA is still unclear. Thus, this study aimed to reveal the effect of IOP on MH7A cells and collagen-induced arthritis (CIA) rats and to investigate the molecular mechanism of IOP in RA. Methods: In this study, network pharmacology was used to identify the key signaling pathways in IOP treatment of RA. The effect of IOP was verified in rats with CIA. We performed CCK-8, EdU, colony formation assay, cell apoptosis, cell migration and invasion, Western blot analysis, and immunofluorescence to elucidate the effect of IOP on the proliferation, apoptosis, migration and invasion of MH7A cells and revealed its modulation of the NF-κB and NLRP3 inflammasome signaling pathways. Results: IOP treatment of CIA rats significantly alleviated joint swelling, synovial tissue proliferation and erosion, and reduced the expression of inflammatory factors TNF-α, IL-6, IL-1β and IL-18. In vitro, IOP significantly inhibited the proliferation, migration, and invasion abilities of TNF-α-stimulated MH7A cells and promoted their apoptosis. Mechanistically, IOP inhibited the NF-κB and NLRP3 inflammasome activation. Conclusions: This study revealed that IOP exerts anti-RA effects by downregulating the NF-κB and NLRP3 inflammasome signaling pathways, promoting cell apoptosis, and inhibiting the expression of inflammatory cytokines, representing a promising therapeutic option for RA. Full article
(This article belongs to the Special Issue Natural Products Derived from Fungi and Their Biological Activities)
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18 pages, 2696 KiB  
Article
Isolation of Ten New Sesquiterpenes and New Abietane-Type Diterpenoid with Immunosuppressive Activity from Marine Fungus Eutypella sp.
by Nina Wang, Chunmei Chen, Qin Li, Qiqiang Liang, Yingjie Liu, Zongze Shao, Xiupian Liu and Qun Zhou
Pharmaceuticals 2025, 18(5), 737; https://doi.org/10.3390/ph18050737 - 16 May 2025
Viewed by 378
Abstract
Background: Ten new sesquiterpenes, including eight eremophilane-type sesquiterpenes (1–8) and two compounds (9–10) with a cyclopentane ring, representing an undescribed subtype of sesquiterpene, along with a new abietane-type diterpenoid (11), were isolated [...] Read more.
Background: Ten new sesquiterpenes, including eight eremophilane-type sesquiterpenes (1–8) and two compounds (9–10) with a cyclopentane ring, representing an undescribed subtype of sesquiterpene, along with a new abietane-type diterpenoid (11), were isolated and identified from a deep-sea-derived fungus: Eutypella sp. Methods: Their structures were elucidated on the basis of various spectroscopic analyses, mainly including nuclear magnetic resonance (NMR) and high-resolution electrospray ionization mass spectrometry (HRESIMS) data, 13C NMR calculations with DP4+ probability analyses, electronic circular dichroism (ECD) calculations, and single-crystal X-ray diffraction experiments. Results: Furthermore, compound 11 exhibited potent immunosuppressive activity with IC50 values of 8.99 ± 1.08 μM in a lipopolysaccharide (LPS) model and 5.39 ± 0.20 μM in a concanavalin A (ConA) model. Full article
(This article belongs to the Special Issue Natural Products Derived from Fungi and Their Biological Activities)
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16 pages, 3535 KiB  
Article
Identification of Novel Progesterone Receptor (PR) Inhibitors (Homo sapiens) from Metabolites of Biotransformation Fungal: A Bioinformatics Approach
by Janaína de Araújo E. Dourado, Samuel Q. Lopes, David Esteban Q. Jimenez, Ryan S. Ramos and Irlon M. Ferreira
Pharmaceuticals 2025, 18(2), 136; https://doi.org/10.3390/ph18020136 - 21 Jan 2025
Viewed by 1058
Abstract
Background/Objectives: Steroids have demonstrated selective cytotoxic properties against tumor cells. The pro-gesterone receptor (PR) plays a vital role in the proliferation, cell differentiation, and maintenance of female reproductive tissue, and its malfunction can lead to breast cancer. The use of the biocatalytic [...] Read more.
Background/Objectives: Steroids have demonstrated selective cytotoxic properties against tumor cells. The pro-gesterone receptor (PR) plays a vital role in the proliferation, cell differentiation, and maintenance of female reproductive tissue, and its malfunction can lead to breast cancer. The use of the biocatalytic method by filamentous fungi has sparked interest in the obtained of steroids due to the advantages of the process. Methods: Pharmacokinetic and toxicological properties (rat and mouse), molecular docking simulation studies, and prediction of the spectrum of biological activity were performed to select molecules with the potential for PR inhibition, from 155 biotransformed products of the progesterone. Subsequently, the chemical structures were subjected to an evaluation of their pharmacokinetic and toxicological properties and, with the application of ADMET filters. Results: Androstenedione, 17α-hydroxyprogesterone, and dihydrotestosterone, obtained by the process of biotransformation of PR by different filamentous fungi, showed good pharmacokinetic profiles and low toxicity compared to the control groups. The in-silico data associated with molecular docking studies revealed the best binding affinity and similarity in the interactions of these molecules against the human progesterone receptor target. Thus, the results of biological activity spectrum prediction highlight the great potential to investigate the role of molecular descriptors in the attribution of anti-cancer activities. Conclusions: The biocatalytic process, by filamentous fungi, can provide important molecules as a product of progesterone biotransformation, such as androstenedione, 17α-hydroxyprogesterone, and dihydrotestosterone. In this study we showed that these molecules have good pharmacokinetic profiles and low toxicity for antineoplastic activity (breast cancer). Full article
(This article belongs to the Special Issue Natural Products Derived from Fungi and Their Biological Activities)
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27 pages, 18799 KiB  
Article
Effect of Mn(II) and Co(II) on Anti-Candida Metabolite Production by Aspergillus sp. an Endophyte Isolated from Dizygostemon riparius (Plantaginaceae)
by Anne Karoline Maiorana Santos, Bianca Araújo dos Santos, Josivan Regis Farias, Sebastião Vieira de Morais, Cleydlenne Costa Vasconcelos, Rosane Nassar Meireles Guerra, Edson Rodrigues-Filho, Alberto Jorge Oliveira Lopes and Antônio José Cantanhede Filho
Pharmaceuticals 2024, 17(12), 1678; https://doi.org/10.3390/ph17121678 - 12 Dec 2024
Cited by 1 | Viewed by 850
Abstract
Background/Objectives: This study evaluates the effect of Mn(II) and Co(II) ions on the production of anti-Candida metabolites by the endophytic fungus Aspergillus sp., isolated from Dizygostemon riparius. The objective was to identify metal-induced secondary metabolites with antifungal potential against drug-resistant [...] Read more.
Background/Objectives: This study evaluates the effect of Mn(II) and Co(II) ions on the production of anti-Candida metabolites by the endophytic fungus Aspergillus sp., isolated from Dizygostemon riparius. The objective was to identify metal-induced secondary metabolites with antifungal potential against drug-resistant Candida species. Methods: Aspergillus sp. was cultivated in Czapek agar supplemented with MnCl₂ (400 µM) or CoCl₂ (200 µM). Metabolite profiles were analyzed using UHPLC-DAD and LC-ESI-HRMS, followed by structural elucidation via NMR. Antifungal and biofilm inhibition activities were tested against Candida albicans and Candida parapsilosis. Toxicity was assessed using Tenebrio molitor larvae. Results: Key metabolites, including pyrophen, penicillquei B, and fonsecinone B, demonstrated antifungal activity with MIC values of 4.37–280.61 µg/mL. Fonsecinone B exhibited superior biofilm inhibition, surpassing fluconazole in reducing biofilm biomass and viability. In vivo assays showed low toxicity, with survival rates above 80% at 2× MIC/kg. Conclusions: Mn(II) and Co(II) significantly modulated the production of antifungal metabolites in Aspergillus sp. Fonsecinone B emerged as a promising candidate for antifungal therapy due to its potent activity and low toxicity. These findings support further investigation into the therapeutic potential of metal-induced fungal metabolites for combating drug-resistant Candida infections. Full article
(This article belongs to the Special Issue Natural Products Derived from Fungi and Their Biological Activities)
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14 pages, 681 KiB  
Article
Coffee with Cordyceps militaris and Hericium erinaceus Fruiting Bodies as a Source of Essential Bioactive Substances
by Katarzyna Kała, Małgorzata Cicha-Jeleń, Kamil Hnatyk, Agata Krakowska, Katarzyna Sułkowska-Ziaja, Agnieszka Szewczyk, Jan Lazur and Bożena Muszyńska
Pharmaceuticals 2024, 17(7), 955; https://doi.org/10.3390/ph17070955 - 17 Jul 2024
Cited by 2 | Viewed by 4779
Abstract
Drinking coffee is a daily routine for many people. Supplement manufacturers have proposed adding powdered Cordyceps militaris, known for its ergogenic and immunostimulating properties, and Hericium erinaceus, known for its nerve growth factor (NGF)-stimulating properties, to coffee. The aim of this [...] Read more.
Drinking coffee is a daily routine for many people. Supplement manufacturers have proposed adding powdered Cordyceps militaris, known for its ergogenic and immunostimulating properties, and Hericium erinaceus, known for its nerve growth factor (NGF)-stimulating properties, to coffee. The aim of this work was to compare the bioactive substances in three types of coffee: machine-brewed, instant, and traditionally brewed, prepared with the addition of H. erinaceus and C. militaris fruiting bodies. The analysis of bioactive substances was performed using AAS and RP-HPLC methods. Among the control samples of coffee, traditionally brewed coffee was the best source of bioelements. Considering the mushroom species tested, the best additional source of Mg, Zn, Cu, Na, K, and Ca was C. militaris. A slightly higher Fe content was determined for H. erinaceus. With the addition of C. militaris, the amounts of 4-feruloylquinic acid (18.6 mg/200 mL) and 3,5-di-caffeoylquinic acid (3.76 mg/200 mL) also increased. In conclusion, the C. militaris species has been proven to be a better source of bioactive substances as a coffee additive in the daily diet. The combination of brewed coffee and the tested mushrooms seems to be the most beneficial in terms of health-promoting effects. Full article
(This article belongs to the Special Issue Natural Products Derived from Fungi and Their Biological Activities)
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