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Keywords = Ganoderic acid A

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16 pages, 2264 KiB  
Article
Ethanolic Extract of Ganoderma mexicanum Pat. Mycelium: A Source of Bioactive Compounds with Antiproliferative Activity and Potential PPAR-γ Natural Ligands
by Lucia T. Angulo-Sanchez, Max Vidal-Gutiérrez, Heriberto Torres-Moreno, Martín Esqueda, Aldo Gutiérrez, Georgina Vargas, Juan Luis Monribot-Villanueva, José A. Guerrero-Analco, César Muñoz-Bacasehua and Ramón Enrique Robles-Zepeda
Pharmaceuticals 2025, 18(6), 909; https://doi.org/10.3390/ph18060909 - 18 Jun 2025
Viewed by 623
Abstract
Background/Objective: Ganoderma spp. have long been studied for their bioactive pharmacological properties, and their biomass and extracts have been obtained from various sources. This study adopts a novel approach: enriching a liquid culture of Ganoderma mexicanum with a vineyard pruning waste extract [...] Read more.
Background/Objective: Ganoderma spp. have long been studied for their bioactive pharmacological properties, and their biomass and extracts have been obtained from various sources. This study adopts a novel approach: enriching a liquid culture of Ganoderma mexicanum with a vineyard pruning waste extract to identify bioactive compounds with antiproliferative activity through enriched chromatographic fractions. Methods: The ethanolic extract from a mycelial culture was separated following a partitioning process, and the hexane fraction was subsequently separated in a chromatographic column. The fractions were evaluated for their antiproliferative properties against cancer cell lines. The interactions of the molecules identified with peroxisome proliferator-activated receptor gamma (PPAR-γ) were analyzed via molecular docking. Results: Three chromatographic fractions (FH11–FH13) exhibited antiproliferative activity which was significantly more effective against non-small lung cancer cells (A549). The cells treated with the crude extract and fractions presented a balloon-like morphology. A chemical analysis of the active fractions allowed us to identify four compounds: one fatty acid (9-Hydroxy-10E,12Z-octadecadienoic acid) and three triterpenes (ganoderic acids DM, TQ, and X). These compounds showed interactions with the PPAR-γ receptor through molecular docking. Conclusions: Ganoderma mexicanum is a promising source of compounds with antiproliferative activity that could serve as natural ligands for PPAR-γ and has possible applications in lung cancer therapy. Full article
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19 pages, 1037 KiB  
Review
Evolution and Functional Diversity of GATA Transcription Factors in Filamentous Fungi: Structural Characteristics, Metabolic Regulation and Environmental Response
by Danni Hu, Ruoyu Zhao, Yingxu Lin and Chunmiao Jiang
Microbiol. Res. 2025, 16(6), 120; https://doi.org/10.3390/microbiolres16060120 - 6 Jun 2025
Viewed by 569
Abstract
Filamentous fungi hold critical industrial value for their ability to produce enzymes, antibiotics, organic acids, and food fermentation. GATA transcription factors (TFs) serve as central regulators of nitrogen metabolism, synthesis of secondary metabolites, stress adaptation, and directly influence fungal development and pathogenicity in [...] Read more.
Filamentous fungi hold critical industrial value for their ability to produce enzymes, antibiotics, organic acids, and food fermentation. GATA transcription factors (TFs) serve as central regulators of nitrogen metabolism, synthesis of secondary metabolites, stress adaptation, and directly influence fungal development and pathogenicity in filamentous fungi. In this review, we primarily discuss the structural characterization, different types, and phylogenetic analysis of filamentous fungi GATA TFs in filamentous fungi. Subsequently, we systematically summarize the multifunctions of GATA TFs in the mycelial growth, morphological differentiation, and conidial development of filamentous fungi. In addition, we explore their functions in the synthesis of secondary metabolites such as antibiotics (e.g., cephalosporins, penicillins) and organic acids (e.g., ganoderic acid, fumaric acid) in filamentous fungi. Furthermore, we focus on the key roles of GATA TFs AreA and AreB in nitrogen and carbon metabolism in filamentous fungi and their potential synergistic regulatory relationships. Finally, we review the important roles of GATA TFs in the adaptation of filamentous fungi to environmental changes. This review provides research ideas for the development of genetically engineered strains with optimized growth characteristics, increased target metabolites in the fermentation production process, and enhanced environmental adaptability. Full article
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21 pages, 8241 KiB  
Article
Ganoderic Acid Ameliorates Ulcerative Colitis by Improving Intestinal Barrier Function via Gut Microbiota Modulation
by Yuwei Ye, Abudumijiti Abulizi, Yukun Zhang, Feng Lu, Yongpan An, Chaoqun Ren, Hang Zhang, Yiming Wang, Dongmei Lin, Dan Lu, Min Li and Baoxue Yang
Int. J. Mol. Sci. 2025, 26(6), 2466; https://doi.org/10.3390/ijms26062466 - 10 Mar 2025
Viewed by 1125
Abstract
Ulcerative colitis (UC) is a chronic and recurrent gastrointestinal disease that affects millions of humans worldwide and imposes a huge social and economic burden. It is necessary to find safe and efficient drugs for preventing and treating UC. The aim of this study [...] Read more.
Ulcerative colitis (UC) is a chronic and recurrent gastrointestinal disease that affects millions of humans worldwide and imposes a huge social and economic burden. It is necessary to find safe and efficient drugs for preventing and treating UC. The aim of this study was to determine whether ganoderic acid (GA), the main bioactive components of Ganoderma lucidum, has preventive and therapeutic effect on UC in a dextran sulfate sodium (DSS)-induced UC mouse model. Our experimental results showed that GA significantly ameliorated the body weight loss and disease activity index (DAI) of UC mice. GA significantly restored 11% of the colon length and 69% of the spleen index compared to UC mice. GA significantly decreased the intestinal inflammatory response and improved the barrier function of the intestine by upregulating the tight junction proteins Zonula occludens-1 (ZO-1), occludin and claudin-1. A co-housing experiment showed that gut microbiota accounted for the therapeutic activity of GA on UC, which was confirmed by fecal microbiota transplantation from GA-treated mice to the UC mice. Furthermore, 16S rDNA high-throughput sequencing of fecal bacteria showed that GA significantly enriched the abundance of Lactobacillus, Oscillospira, Odoribacter and Ruminococcus, which were positively correlated with colon length. Furthermore, this study found the functional metabolites, including Indole-3-acetaldehyde (IAAld), Glutamine (Gln) and Glutathione (GSH), reduced barrier damage in the Caco-2 cell model. In conclusion, this study suggests that GA could ameliorate UC by improving intestinal barrier function via modulating gut microbiota and associated metabolites. Full article
(This article belongs to the Section Molecular Microbiology)
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22 pages, 3623 KiB  
Article
In Vitro Antimicrobial Efficacy Assessment of Ethanolic, Aqueous, and Dual Solvent Extracts of Mushroom Ganoderma lucidum: Genomic and Morphological Analysis
by Ewunkem Akamu, Lydia Merrills, Zahirah Williams, Brittany Justice, Uchenna Iloghalu, Vera Williams and Dinesh Singh
Antibiotics 2024, 13(12), 1109; https://doi.org/10.3390/antibiotics13121109 - 21 Nov 2024
Cited by 1 | Viewed by 1991
Abstract
Background: Infectious diseases caused by bacteria are life-threating and are among the major causes of death in the world. Antibiotics have offered humans a new approach to infection control. Antibiotics are reckoned as the “magic bullets” for the fight against bacterial infections, therefore [...] Read more.
Background: Infectious diseases caused by bacteria are life-threating and are among the major causes of death in the world. Antibiotics have offered humans a new approach to infection control. Antibiotics are reckoned as the “magic bullets” for the fight against bacterial infections, therefore increasing life expectancy and decreasing mortality and morbidity. However, the overuse of antibiotics has resulted in the persistent growth of resistant bacterial pathogens. New antimicrobial approaches against resistant pathogens are being examined. Mushrooms seem to be a promising, and possibly more efficient, alternative method to that of conventional antimicrobials. This work aimed to investigate the phytochemical constituents and antimicrobial potential of ethanolic, aqueous, and dual solvent extracts of mushroom Ganoderma lucidum. Methods: The antimicrobial studies were carried out by broth dilution against Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli. The present research work was also carried out to examine genomic changes associated with ethanolic, aqueous, and dual solvent extracts of G. lucidum in S. aureus and E. coli. Results: Our data quantitatively showed that all the extracts of G. lucidum were found to exhibit various degrees of antimicrobial effects against S. aureus and E. coli where the ethanolic extract exhibited the most potent antimicrobial activity. SEM images showed untreated cells with normal cell characteristics while, after treatment with extracts of G. lucidum, cells appeared damaged with irregular cell surfaces and cell wall defacement. The results of HPLC analysis showed that ethanolic and aqueous extract of G. lucidum consisted of beta[1-3] glucans, ganoderic acid, and triterpenoids. Genomic analysis identified selective sweeps in several genes associated with growth, biosynthesis transport, and stress. Conclusions: This study concludes that the extracts of three solvents of G. lucidum have antimicrobial activity against infectious bacteria causing morphological changes and the acquisition of mutations in genes. Therefore, the extracts of G. lucidum may be candidates for preventing infectious diseases in the future. Ganoderma lucidum mushroom is therefore a reliable source of antimicrobial agent that can be used against infectious diseases. Full article
(This article belongs to the Section Antibiotic Therapy in Infectious Diseases)
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17 pages, 8417 KiB  
Review
Research Progress on the Biological Activity of Ganoderic Acids in Ganoderma lucidum over the Last Five Years
by Siyi Wang, Longyu Wang, Jiaolei Shangguan, Ailiang Jiang and Ang Ren
Life 2024, 14(10), 1339; https://doi.org/10.3390/life14101339 - 21 Oct 2024
Cited by 3 | Viewed by 4731
Abstract
Ganoderma lucidum (G. lucidum) is a traditional edible and medicinal mushroom in China. The main bioactive components in G. lucidum include triterpenoids, polysaccharides, steroids, and sterols. Ganoderic acids (GAs) are one of the most abundant triterpenoids found in G. lucidum, [...] Read more.
Ganoderma lucidum (G. lucidum) is a traditional edible and medicinal mushroom in China. The main bioactive components in G. lucidum include triterpenoids, polysaccharides, steroids, and sterols. Ganoderic acids (GAs) are one of the most abundant triterpenoids found in G. lucidum, garnering significant attention from researchers in the fields of medicine and health care. We summarize the extensive studies on the physiological function of GAs in anti-cancer, anti-inflammatory, radiation protection, anti-aging, liver protection, anti-microbial, and neuroprotection areas, among others. This review provides a comprehensive overview of the recent advances in the bioactivities and pharmacological mechanisms of GAs, aiming to delineate the current research directions and the state of the art in this field. This analysis helps to rapidly identify new bioactivities of GAs and understand their mechanisms, leading to more effective treatments for various diseases. Full article
(This article belongs to the Section Pharmaceutical Science)
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18 pages, 4942 KiB  
Article
Distributions of Lanostene-Derived Triterpenoids and Glucan Content in the Fruiting Bodies of the Australian Ganoderma Species
by Aline De Oliveira Campos, Mark D. Harrison, David L. Marshall and Peter James Strong
J. Fungi 2024, 10(10), 723; https://doi.org/10.3390/jof10100723 - 18 Oct 2024
Cited by 2 | Viewed by 1285
Abstract
Lanostene-derived triterpenoids and β-glucans are important metabolites in Ganoderma mushrooms associated with benefits to human health. The medicinal value of the Australian Ganoderma species remains unclear, with no data on triterpenoid distribution or glucan content. In the present study, 22 Australian Ganoderma specimens [...] Read more.
Lanostene-derived triterpenoids and β-glucans are important metabolites in Ganoderma mushrooms associated with benefits to human health. The medicinal value of the Australian Ganoderma species remains unclear, with no data on triterpenoid distribution or glucan content. In the present study, 22 Australian Ganoderma specimens were analyzed for triterpenoid and glucan contents. Thirty-two triterpenoids were identified in the fruiting bodies of 19 of the specimens. Distinct patterns in triterpenoid distribution between laccate and matte fruiting bodies were observed, leading to the classification of four groups of Ganoderma. Most of the glucans in the Ganoderma fruiting bodies were β-glucans (~99%), with a nominal α-glucan content (~1%). The β-glucan content ranged from 19.5 to 43.5% (w/w). A range of antioxidant activities was observed for methanol extracts using the ABTS (1.8 to 8.4 mg GAE.g−1), DPPH (1.7 to 9.4 mg GAE/g−1) and FRAP (24.7 to 111.6 mmol FeSO4.g−1) assays, with four specimens presenting relatively high radical scavenging and reducing activities. For the first time, we demonstrated that Australian Ganoderma mushrooms contain medicinal triterpenoids, including ganoderic acid A, and we established a link between its distribution and the fruiting body morphology. However, further research is required to isolate diploid clones and determine factors that impact triterpenoid and glucan synthesis in these strains. Full article
(This article belongs to the Section Fungal Cell Biology, Metabolism and Physiology)
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14 pages, 31525 KiB  
Article
A Spironolactone-Based Prototype of an Innovative Biomedical Patch for Wound Dressing Applications
by Giovanna Aquino, Gianluca Viscusi, Massimo Christian D’Alterio, Verdiana Covelli, Giuliana Gorrasi, Claudio Pellecchia, Paola Rizzo, Anna Maria D’Ursi, Giacomo Pepe, Chiara Amante, Pasquale Del Gaudio and Manuela Rodriquez
Int. J. Mol. Sci. 2024, 25(17), 9608; https://doi.org/10.3390/ijms25179608 - 5 Sep 2024
Cited by 2 | Viewed by 1253
Abstract
The electrospinning process is an effective technique for creating micro- and nanofibers from synthetic and natural polymers, with significant potential for biomedical applications and drug delivery systems due to their high drug-loading capacity, large surface area, and tunable release times. Poly(L-lactic acid) (PLLA) [...] Read more.
The electrospinning process is an effective technique for creating micro- and nanofibers from synthetic and natural polymers, with significant potential for biomedical applications and drug delivery systems due to their high drug-loading capacity, large surface area, and tunable release times. Poly(L-lactic acid) (PLLA) stands out for its excellent thermo-mechanical properties, biodegradability, and bioabsorbability. Electrospun PLLA nanofibrous structures have been extensively investigated as wound dressings, sutures, drug delivery carriers, and tissue engineering scaffolds. This study aims to create and characterize electrospun PLLA membranes loaded with spironolactone (SP), mimicking active compounds of Ganoderma lucidum (GL), to develop a biodegradable patch for topical wound-healing applications. GL, a medicinal mushroom, enhances dermal wound healing with its bioactive compounds, such as polysaccharides and ganoderic acids. Focusing on GL extracts—obtained through green extraction methods—and innovative drug delivery, we created new fibers for wound-healing potential applications. To integrate complex mixtures of bioactive compounds into the fibers, we developed a prototype using a single pure substance representing the extract mixture. This painstaking work presents the results of the fabricating, wetting, moisture properties, material resilience, and full characterization of the product, providing a robust rationale for the fabrication of fibers imbued with more complex extracts. Full article
(This article belongs to the Section Materials Science)
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21 pages, 7629 KiB  
Article
Synthesis of Ganoderic Acids Loaded Zein-Chitosan Nanoparticles and Evaluation of Their Hepatoprotective Effect on Mice Given Excessive Alcohol
by Yingjia Cao, Yuheng Yang, Zihua Liang, Weiling Guo, Xucong Lv, Li Ni and Youting Chen
Foods 2024, 13(17), 2760; https://doi.org/10.3390/foods13172760 - 29 Aug 2024
Viewed by 1467
Abstract
Ganoderma lucidum, used in East Asia for its health benefits, contains ganoderic acids (GA) which have various pharmacological activities but are limited by poor water solubility and low oral bioaccessibility. This study synthesized and characterized ganoderic acids loaded zein-chitosan nanoparticles (GA-NPs), and [...] Read more.
Ganoderma lucidum, used in East Asia for its health benefits, contains ganoderic acids (GA) which have various pharmacological activities but are limited by poor water solubility and low oral bioaccessibility. This study synthesized and characterized ganoderic acids loaded zein-chitosan nanoparticles (GA-NPs), and investigated its advantages in alleviating alcoholic liver injury (ALI) in mice model. The GA-NPs demonstrated high encapsulation efficiency (92.68%), small particle size (177.20 nm), and a +29.53 mV zeta potential. The experimental results of alcohol-induced liver injury mouse model showed that GA-NPs significantly improved liver metabolic function, reduced alcohol-induced liver oxidative stress in liver by decreasing lactate dehydrogenase activity and malondialdehyde level, while increasing the activities of liver antioxidant enzymes and alcohol dehydrogenase. Moreover, GA-NPs were favorable to ameliorate intestinal microbiota dysbiosis in mice exposed to alcohol by increasing the proportion of probiotics such as Romboutsia, Faecalibaculum, Bifidobacterium and Turicibacter, etc., which were highly correlated with the improvement of liver function. Furthermore, GA-NPs modulated the mRNA expression related to ethanol metabolism, oxidative stress and lipid metabolism. Conclusively, this study revealed that GA-NPs have stronger hepatoprotective effects than non-encapsulated ganoderic acids on alleviating ALI by regulating intestinal microbiota and liver metabolism. Full article
(This article belongs to the Special Issue Functional Foods and Their Benefits for Health Regulation)
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16 pages, 4260 KiB  
Article
Metabolomics Reveals Glycerophospholipids, Peptides, and Flavonoids Contributing to Breast Meat Flavor and Benefit Properties of Beijing-You Chicken
by Jian Zhang, Xia Chen, Jing Cao, Ailian Geng, Qin Chu, Zhixun Yan, Yao Zhang and Huagui Liu
Foods 2024, 13(16), 2549; https://doi.org/10.3390/foods13162549 - 15 Aug 2024
Cited by 3 | Viewed by 1576
Abstract
Unique metabolites contribute to the performance of meat flavor and potential function. In this study, UHPLC-Q Exactive HF-X-based metabolomics and multivariate analysis were applied to explore the characteristic metabolites in the breast meat of Beijing-You chicken (BYC) aged 150, 300, and 450 days [...] Read more.
Unique metabolites contribute to the performance of meat flavor and potential function. In this study, UHPLC-Q Exactive HF-X-based metabolomics and multivariate analysis were applied to explore the characteristic metabolites in the breast meat of Beijing-You chicken (BYC) aged 150, 300, and 450 days (D150, D300, and D450). Based on the criteria of variable importance in the projection (VIP) > 1 and p < 0.05, a total of 154 and 97 differential metabolites (DMs) were screened out compared with D450 (D450 vs. D150, D450 vs. D300), respectively. In general, the relative content of carnosine, L-L-homoglutathione, demethyloleuropein, neohesperidin dihydrochalcone, 7-chloro-2-(3,4-dimethoxyphenyl)-3,5-dihydroxy-6,8-dimethoxy-4H-chromen-4-one, glycerophospholipids, exhibited the highest abundance at D450, while balenine, anserine, L-beta-aspartyl-L-leucine, glutathione, oxidized glutathione, stearoylcarnitine, ganoderic acid alpha, oleuroside, Lysoglycerophospholipid species (LGP) presented a downward trend with age. These 210 DMs were involved in 10 significantly enriched pathways related to the synthesis and metabolism of amino acids, peptides, and glycerophospholipid, such as glutathione metabolism, histidine metabolism, glycerophospholipid metabolism, arginine biosynthesis, tyrosine metabolism, and lysine degradation. In conclusion, this work could not only facilitate a better understanding of the differences of chicken flavor and benefit properties with age, but also provide potential valuable bioactive compounds for further research. Full article
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30 pages, 7686 KiB  
Review
The Biological Activity of Ganoderma lucidum on Neurodegenerative Diseases: The Interplay between Different Active Compounds and the Pathological Hallmarks
by Wenhui Lian, Xu Yang, Qidong Duan, Jie Li, Yuting Zhao, Chunhui Yu, Tianzhu He, Tianxia Sun, Yu Zhao and Weinan Wang
Molecules 2024, 29(11), 2516; https://doi.org/10.3390/molecules29112516 - 26 May 2024
Cited by 8 | Viewed by 5745
Abstract
Neurodegenerative diseases represent a cluster of conditions characterized by the progressive degeneration of the structure and function of the nervous system. Despite significant advancements in understanding these diseases, therapeutic options remain limited. The medicinal mushroom Ganoderma lucidum has been recognized for its comprehensive [...] Read more.
Neurodegenerative diseases represent a cluster of conditions characterized by the progressive degeneration of the structure and function of the nervous system. Despite significant advancements in understanding these diseases, therapeutic options remain limited. The medicinal mushroom Ganoderma lucidum has been recognized for its comprehensive array of bioactive compounds with anti-inflammatory and antioxidative effects, which possess potential neuroprotective properties. This literature review collates and examines the existing research on the bioactivity of active compounds and extracts from Ganoderma lucidum in modulating the pathological hallmarks of neurodegenerative diseases. The structural information and preparation processes of specific components, such as individual ganoderic acids and unique fractions of polysaccharides, are presented in detail to facilitate structure–activity relationship research and scale up the investigation of in vivo pharmacology. The mechanisms of these components against neurodegenerative diseases are discussed on multiple levels and elaborately categorized in different patterns. It is clearly presented from the patterns that most polysaccharides of Ganoderma lucidum possess neurotrophic effects, while ganoderic acids preferentially target specific pathogenic proteins as well as regulating autophagy. Further clinical trials are necessary to assess the translational potential of these components in the development of novel multi-target drugs for neurodegenerative diseases. Full article
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17 pages, 727 KiB  
Review
Exploring the Therapeutic Potential of Ganoderma lucidum in Cancer
by Gabriella Cancemi, Santino Caserta, Sebastiano Gangemi, Giovanni Pioggia and Alessandro Allegra
J. Clin. Med. 2024, 13(4), 1153; https://doi.org/10.3390/jcm13041153 - 18 Feb 2024
Cited by 12 | Viewed by 7237
Abstract
Triterpenoids, such as ganoderic acid, and polysaccharides, including β-D-glucans, α-D-glucans, and α-D-mannans, are the main secondary metabolites of the medicinal fungus Ganoderma lucidum. There is evidence of the effects of ganoderic acid in hematological malignancies, whose mechanisms involve the stimulation of immune [...] Read more.
Triterpenoids, such as ganoderic acid, and polysaccharides, including β-D-glucans, α-D-glucans, and α-D-mannans, are the main secondary metabolites of the medicinal fungus Ganoderma lucidum. There is evidence of the effects of ganoderic acid in hematological malignancies, whose mechanisms involve the stimulation of immune response, the macrophage-like differentiation, the activation of MAP-K pathway, an IL3-dependent cytotoxic action, the induction of cytoprotective autophagy, and the induction of apoptosis. In fact, this compound has been tested in twenty-six different human cancer cell types and has shown an anti-proliferative activity, especially in leukemia, lymphoma, and myeloma lines. Moreover, research clarified the capability of molecules from Ganoderma lucidum to induce mitochondrial damage in acute promyelocytic leukemia cells, without cytotoxic effects in normal mononuclear cells. Active lipids extracted from the spores of this fungus have also been shown to induce apoptosis mediated by downregulation of P-Akt and upregulation of caspases-3, -8, and -9. Among in vivo studies, a study in BALB/c mice injected with WEHI-3 leukemic cells suggested that treatment with Ganoderma lucidum promotes differentiation of T- and B-cell precursors, phagocytosis by PBMCs, and NK cell activity. Our review presents data revealing the possibility of employing Ganoderma lucidum in hematological malignancies and incorporating it into clinical practice. Full article
(This article belongs to the Section Pharmacology)
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42 pages, 19891 KiB  
Review
Progress in Antimelanoma Research of Natural Triterpenoids and Their Derivatives: Mechanisms of Action, Bioavailability Enhancement and Structure Modifications
by Marta Grudzińska, Bogna Stachnik, Agnieszka Galanty, Agnieszka Sołtys and Irma Podolak
Molecules 2023, 28(23), 7763; https://doi.org/10.3390/molecules28237763 - 24 Nov 2023
Cited by 10 | Viewed by 2506
Abstract
Melanoma is one of the most dangerous forms of skin cancer, characterized by early metastasis and rapid development. In search for effective treatment options, much attention is given to triterpenoids of plant origin, which are considered promising drug candidates due to their well [...] Read more.
Melanoma is one of the most dangerous forms of skin cancer, characterized by early metastasis and rapid development. In search for effective treatment options, much attention is given to triterpenoids of plant origin, which are considered promising drug candidates due to their well described anticancer properties and relatively low toxicity. This paper comprehensively summarizes the antimelanoma potential of natural triterpenoids, that are also used as scaffolds for the development of more effective derivatives. These include betulin, betulinic acid, ursolic acid, maslinic acid, oleanolic acid, celastrol and lupeol. Some lesser-known triterpenoids that deserve attention in this context are 22β-hydroxytingenone, cucurbitacins, geoditin A and ganoderic acids. Recently described mechanisms of action are presented, together with the results of preclinical in vitro and in vivo studies, as well as the use of drug delivery systems and pharmaceutical technologies to improve the bioavailability of triterpenoids. This paper also reviews the most promising structural modifications, based on structure–activity observations. In conclusion, triterpenoids of plant origin and some of their semi-synthetic derivatives exert significant cytotoxic, antiproliferative and chemopreventive effects that can be beneficial for melanoma treatment. Recent data indicate that their poor solubility in water, and thus low bioavailability, can be overcome by complexing with cyclodextrins, or the use of nanoparticles and ethosomes, thus making these compounds promising antimelanoma drug candidates for further development. Full article
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16 pages, 3324 KiB  
Article
Metabolomic Insights into the Mechanisms of Ganoderic Acid: Protection against α-Amanitin-Induced Liver Injury
by Chong Zheng, Shaofang Lv, Jianfang Ye, Lu Zou, Kai Zhu, Haichang Li, Yongxi Dong and Lei Li
Metabolites 2023, 13(11), 1164; https://doi.org/10.3390/metabo13111164 - 20 Nov 2023
Cited by 8 | Viewed by 2218
Abstract
α-Amanitin is a representative toxin found in the Amanita genus of mushrooms, and the consumption of mushrooms containing α-Amanitin can lead to severe liver damage. In this study, we conduct toxicological experiments to validate the protective effects of Ganoderic acid A against α-amanitin-induced [...] Read more.
α-Amanitin is a representative toxin found in the Amanita genus of mushrooms, and the consumption of mushrooms containing α-Amanitin can lead to severe liver damage. In this study, we conduct toxicological experiments to validate the protective effects of Ganoderic acid A against α-amanitin-induced liver damage. By establishing animal models with different durations of Ganoderic acid A treatment and conducting a metabolomic analysis of the serum samples, we further confirmed the differences in serum metabolites between the AMA+GA and AMA groups. The analysis of differential serum metabolites after the Ganoderic acid A intervention suggests that Ganoderic acid A may intervene in α-amanitin-induced liver damage by participating in the regulation of retinol metabolism, tyrosine and tryptophan biosynthesis, fatty acid biosynthesis, sphingosine biosynthesis, spermidine and spermine biosynthesis, and branched-chain amino acid metabolism. This provides initial insights into the protective intervention mechanisms of GA against α-amanitin-induced liver damage and offers new avenues for the development of therapeutic drugs for α-Amanitin poisoning. Full article
(This article belongs to the Special Issue Association between Natural Products and the Metabolism in Humans)
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11 pages, 2091 KiB  
Article
Untargeted LC-QTOF-MS Analysis of Metabolites Produced by Penicillium brevicompactum during the Bioconversion of Ganoderic Acid A
by Vizelle Naidoo, Vuyo Mavumengwana, Kudzanai Tapfuma, Ndiwanga F. Rasifudi and Lukhanyo Mekuto
Processes 2023, 11(10), 2963; https://doi.org/10.3390/pr11102963 - 12 Oct 2023
Viewed by 1387
Abstract
The repurposing of expired drugs through bioconversion remains one of the most crucial research milestones, as this practice reduces drug contamination while producing compounds of significance. The present study investigated the bioconversion of ganoderic acid A (GAA) using Penicillium brevicompactum over a period [...] Read more.
The repurposing of expired drugs through bioconversion remains one of the most crucial research milestones, as this practice reduces drug contamination while producing compounds of significance. The present study investigated the bioconversion of ganoderic acid A (GAA) using Penicillium brevicompactum over a period of 3, 6 and 9 days. The GAA intensity reduced from 22,099 cps on day 0 to 11,040, 4700 and 18,126 cps on day 3, 6 and 9, respectively, thus demonstrating the degradation of GAA over time. The produced metabolites that were recovered using ethyl acetate as a solvent were determined using LC-QTOF-MS. P. brevicompactum produced a variety of compounds in the absence of GAA, while in its presence, it was observed that P. brevicompactum was able to convert GAA and produced ganomastenol A/B/D, vitamin E succinate, and aminopregnane on day 3, while on day 6, armillaripin and ganolucidic acid A were produced. After 9 days of operation, vitamin E succinate, ganolucidic acid A and lucilactaene were produced. The present study is the first report on the ability of P. brevicompactum to bioconvert GAA. The identified metabolites have been established to possess bioactivity against various ailments, thus contributing to the discovery of new drugs. Full article
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11 pages, 1643 KiB  
Article
Antiproliferative Activity of Mycelium vs. Fruiting Body: Ganoderma subincrustatum and G. weberianum from Sonora, Mexico
by Damian López-Peña, Heriberto Torres-Moreno, Max Vidal-Gutiérrez, Ramón Enrique Robles-Zepeda, Aldo Gutiérrez and Martín Esqueda
Microbiol. Res. 2023, 14(4), 1534-1544; https://doi.org/10.3390/microbiolres14040105 - 28 Sep 2023
Cited by 3 | Viewed by 2260
Abstract
The genus Ganoderma has been little studied in arid areas worldwide. Ganoderma subincrustatum and Ganoderma weberianum strains were obtained from the Sonoran Desert, Sonora, Mexico. Ganoderma spp. synthesize triterpenoids such as ganoderic acids with antiproliferative activity because they inhibit specific targets, induce apoptosis, [...] Read more.
The genus Ganoderma has been little studied in arid areas worldwide. Ganoderma subincrustatum and Ganoderma weberianum strains were obtained from the Sonoran Desert, Sonora, Mexico. Ganoderma spp. synthesize triterpenoids such as ganoderic acids with antiproliferative activity because they inhibit specific targets, induce apoptosis, and increase the activity of killer cells. Mycelium and fruiting body chloroform extracts from G. subincrustatum and G. weberianum were tested on HeLa, A549, L-929, and RAW 264.7 cell lines. Extracts from the fruiting body present higher antiproliferative activity than mycelium. All extracts induced vesicle and cellular debris formation in all cell lines, being non-selective for cancerous cells. Chloroform extract from G. subincrustatum fruiting bodies presented higher activity against all cell lines. Fractions F7 and F15 from this extract exhibited an IC50 of 37.9 and 41.9 µg/mL on the A549 cell line, respectively; however, chloroform crude extract showed higher activity (IC50 of <25 µg/mL) in all cell lines. Flow cytometry assays of F7 revealed cell death by apoptosis in A549 cells. NMR suggested the presence of ganoderic acids in F7. In future research, it will be interesting to characterize these fractions (metabolites, their bioactivities, and mechanism of action). Full article
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