Bioactive Compounds from Natural Sources with Antioxidant and Anti-Inflammatory Potential

A special issue of Antioxidants (ISSN 2076-3921). This special issue belongs to the section "Natural and Synthetic Antioxidants".

Deadline for manuscript submissions: 31 May 2026 | Viewed by 1513

Special Issue Editor


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Guest Editor
National Institute of Complementary Medicine (NICM), Western Sydney University, Penrith, NSW 2751, Australia
Interests: anti-inflammatory; antioxidant; anticancer; bioactive compounds; plant extracts; pharmacology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are pleased to announce a Special Issue of Antioxidants, focusing on “Bioactive Compounds from Natural Sources with Antioxidant and Anti-Inflammatory Potential”.

Oxidative stress and chronic inflammation are key underlying mechanisms in many diseases, including metabolic disorders, cancer, musculoskeletal diseases, and neurodegenerative conditions. Natural bioactive compounds derived from plants, marine organisms, microbes, and other biological sources have been extensively studied, with some being found to display notable anti-inflammatory and antioxidant properties showing promising therapeutic potential. This Special Issue aims to highlight cutting-edge research on the discovery, mechanisms, and applications of natural bioactive compounds with antioxidant and anti-inflammatory properties.

We invite submissions of original research articles and quality reviews within the following scope/topics:

Discovery and Characterization:

Isolation and structural elucidation of novel antioxidant and anti-inflammatory compounds from natural sources;

Biosynthesis, modification, biological activity, and sustainable production of active natural products.

Mechanistic Insights and Applications:

Molecular mechanisms, e.g., dual ROS-scavenging and NF-κB inhibition properties;

Synergistic effects of multi-component natural compounds and extracts; 

Pharmacodynamics and pharmacokinetics of natural antioxidant and anti-inflammatory compounds;

Clinical studies on active natural compounds in diseases;

Applications in functional foods, nutraceuticals, and cosmeceuticals.

Methodological Advances:

Formulation strategies for enhanced bioavailability (e.g., nano-delivery systems);

Innovative extraction and analytical techniques (e.g., metabolomics, bioassay-guided fractionation, online assays) and delivery methods.

Prof. Dr. Chun Guang Li
Guest Editor

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Keywords

  • antioxidant
  • anti-inflammatory
  • natural compounds
  • isolation
  • extraction
  • molecular mechanism
  • synergistic effect
  • clinical trial
  • bioavailability
  • analytical method
  • pharmacodynamics
  • pharmacokinetics

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Published Papers (4 papers)

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Research

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20 pages, 4328 KB  
Article
Spider Venom-Derived Peptide Exhibits Dual Anti-Inflammatory and Antioxidative Activities in LPS-Stimulated BEAS-2B Cells
by Jin Wook Oh, Min Kyoung Shin, Hye-Ran Park, Sukin Jeong, Minho Lee, Ji Hyuk Ko, Jae Young Lee, Seung-Cheol Jee and Jung-Suk Sung
Antioxidants 2025, 14(12), 1485; https://doi.org/10.3390/antiox14121485 - 11 Dec 2025
Viewed by 128
Abstract
Most respiratory diseases are driven by excessive airway inflammation and oxidative stress, yet current therapies often lack durable efficacy or are unsafe. Host-defense peptides, commonly enriched in animal venoms, offer diverse, target-selective scaffolds for new therapeutics. In this study, we aimed to discover [...] Read more.
Most respiratory diseases are driven by excessive airway inflammation and oxidative stress, yet current therapies often lack durable efficacy or are unsafe. Host-defense peptides, commonly enriched in animal venoms, offer diverse, target-selective scaffolds for new therapeutics. In this study, we aimed to discover a novel bioactive peptide with therapeutic potential on respiratory tract damage by utilizing Nephila clavata venom gland transcriptome. Using in silico analysis and machine learning-based functional prediction, we designed a peptide, NC-CV, expected to have dual anti-inflammatory and antioxidant activities with low cytotoxicity. In experimental validation, NC-CV improved human bronchial epithelial BEAS-2B cell viability under lipopolysaccharide (LPS) exposure while reducing LPS-induced pro-inflammatory cytokine expression and intracellular reactive oxygen species (ROS) generation. Mechanistic studies and molecular docking simulations indicated that NC-CV prevents toll-like receptor 4 signaling activation, suppressing nuclear factor κB and mitogen-activated protein kinase pathways. Moreover, the antioxidant activity of NC-CV was primarily based on direct intracellular ROS scavenging rather than the induction of endogenous antioxidant enzymes. Collectively, these findings demonstrated that the venom-derived peptide NC-CV disrupts the self-reinforcing cycle involving inflammatory signaling and oxidative stress in airway epithelium, highlighting its promise as a therapeutic candidate for respiratory disease. Full article
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18 pages, 2819 KB  
Article
Dual Antioxidant Activity: Preventive and Scavenger Effects of Wild and Cultivated P. nebrodensis Extracts Against ROS and SOX in Human Keratinocytes
by Daniela Ratto, Maria Teresa Venuti, Anthea Desiderio, Ilenia Cicero, Gaetano Balenzano, Elena Savino, Giuseppe Venturella, Maria Letizia Gargano and Paola Rossi
Antioxidants 2025, 14(12), 1439; https://doi.org/10.3390/antiox14121439 - 28 Nov 2025
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Abstract
Pleurotus nebrodensis, a rare endemic Sicilian mushroom with notable gastronomic and medicinal value, attracts interest for its potential antioxidant properties, though data on its biological effects in skin models are lacking. This study evaluated the antioxidant activities of several aqueous extracts from [...] Read more.
Pleurotus nebrodensis, a rare endemic Sicilian mushroom with notable gastronomic and medicinal value, attracts interest for its potential antioxidant properties, though data on its biological effects in skin models are lacking. This study evaluated the antioxidant activities of several aqueous extracts from wild (1a, 2a, 3a, 1b, 2b, and 3b) and cultivated (CAN1 °F, 3A, 2B(II), and CAN2 °F) P. nebrodensis basidiomes in human keratinocytes (HaCaT cells). Extracts were characterized through DPPH radical scavenging assay, MTT viability assay, and intracellular ROS and mitochondrial SOX quantification by DCFH-DA and MitoSOX Red fluorescence analyses. The methodology specifically included two approaches in keratinocytes: co-treatment of extracts and H2O2 to investigate direct scavenger activity, and pre-treatment to assess the preventive activity on oxidative stress modulation. This analysis demonstrated that selected extracts (1b and CAN2 °F) exert a dual action, combining anti-intracellular ROS and anti-mitochondrial SOX preventive effect with a direct free radical scavenging activity in human keratinocytes. In particular, CAN2 °F exerts its activity predominantly through prevention (modulation of cellular defenses), while 1b primarily functions as a direct intracellular ROS and mitochondrial SOX scavenger. Notably, glucan quantification revealed a correlation between β-glucan content and the overall antioxidant activity. These findings provide the first evidence of P. nebrodensis’s anti-ROS and anti-SOX efficacy in human keratinocytes, highlighting its potential as a source of natural bioactives for cosmeceutical and dermatological applications. Full article
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15 pages, 8882 KB  
Article
Ovatifolin Purified from Leptocarpha rivularis Induces Cell Death in A375 and A2058 Melanoma Cancer Cells
by Viviana Burgos, Nicole Cortez, Rocío Aguilera-Paillán, Sofía Bravo-Bouchat, Bernd Schmidt, Eric Sperlich, Rebeca Pérez, Nelia M. Rodriguez, Leandro Ortiz, Jaime R. Cabrera-Pardo, Cecilia Villegas and Cristian Paz
Antioxidants 2025, 14(12), 1392; https://doi.org/10.3390/antiox14121392 - 21 Nov 2025
Viewed by 631
Abstract
Skin cancer is increasing worldwide, with melanoma being its most aggressive and lethal form due to its high metastatic potential. Despite therapeutic advances, drug resistance remains a challenge, highlighting the need to explore new anticancer agents. Leptocarpha rivularis is a native plant of [...] Read more.
Skin cancer is increasing worldwide, with melanoma being its most aggressive and lethal form due to its high metastatic potential. Despite therapeutic advances, drug resistance remains a challenge, highlighting the need to explore new anticancer agents. Leptocarpha rivularis is a native plant of Chile, locally called “Palo negro”, and is traditionally used in medicine by the Mapuche people. L. rivularis produces bioactive germacrene sesquiterpenoids with cytotoxic, antioxidant, anti-inflammatory and anti-angiogenic properties. This study reports for the first time the isolation of ovatifolin from aerial parts of L. rivularis and its identification by NMR and X-ray diffraction, together with its antiproliferative activity against two melanoma cell lines. The results show that ovatifolin has cytotoxic activity against the cell lines A2058 and A375, with an IC50 of 27.6 (90.2 µM) and 18.4 µg/mL (60.1 µM), respectively, evaluated by live-cell IncuCyte® analysis. Moreover, ovatifolin arrests colony formation in a clonogenic assay, with an IC50 of 3.26 (10.6 μM) and 3.65 µg/mL (11.9 μM) in these same cell lines. Therefore, ovatifolin increased intracellular ROS and decreased the mitochondrial membrane potential (ΔΨ m). Cell death studies using Annexin V showed that its cytotoxic activity is partially caused by non-specific apoptosis, which was corroborated by the caspase inhibitor Z-VAD with an incomplete recovery of the cell death process. Full article
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Review

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17 pages, 333 KB  
Review
Effectiveness of Common Extraction Solvents in Obtaining Antioxidant Compounds from African Medicinal Plants
by Khayelihle Ncama, Joseph Malele, Dhiren Munsami Govender, Thagen Anumanthoo and Mack Moyo
Antioxidants 2025, 14(12), 1498; https://doi.org/10.3390/antiox14121498 (registering DOI) - 13 Dec 2025
Abstract
The efficacy of phytoextracts is equally affected by the extraction solvent and the extraction method. Details of the solvent type, concentration, density, and other characteristics are associated with the quality of the resultant extract. Some solvents have been found to be effective only [...] Read more.
The efficacy of phytoextracts is equally affected by the extraction solvent and the extraction method. Details of the solvent type, concentration, density, and other characteristics are associated with the quality of the resultant extract. Some solvents have been found to be effective only on specific parts of plants. Industry has shown a growing interest in eco-friendly plant extracts for the formulation of medication, food additives, cosmetics, and agricultural products. This interest is aligned with the proven necessity of sustainability, marketability, and regulation of manufactured products in value chains. In this review, the literature on antioxidant compounds and activity of extracts from African medicinal plants is reviewed. Findings indicate that the use of ethanol, methanol, water, and to a lesser extent, acetone as solvents for the extraction of antioxidant compounds is common. The use of these solvents is supported by decisive selection of procedure, ideal temperature, duration, solvent pH, and the extracted plant parts. Fermentation enhances the antioxidant activity of aqueous extracts but reduces that of alcohol extracts. This is particularly essential in continents such as Africa, where water is available but alcohol is scarce. “Green” extraction technologies are not as successful as solvent extractions for use with African medicinal plants. There is a financial hurdle that results in a mismatch between academic research innovations and societal transmission to new technologies, as most communities are dominated by small-to-medium enterprises. Further studies on the extraction of antioxidants from African medicinal plants are recommended to guide the research and link it to ordinary African societies. Full article
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