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Antioxidants
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Bioactive Compounds: Antioxidant, Antibacterial, and Anti-Inflammatory Modulation—2nd Edition
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Bioactive Compounds: Antioxidant, Antibacterial, and Anti-Inflammatory Modulation—2nd Edition

A Special Issue of Antioxidants (ISSN 2076-3921) belonging to the section "Natural and Synthetic Antioxidants".

Deadline for manuscript submissions: 31 January 2027 | Viewed by 6291

Editors

Dr. Raquel Bridi

E-Mail Website
Guest Editor
Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago 8380000, Chile
Interests: natural products; bioactive compounds; secondary metabolites; phytochemistry; medicinal plants; bee products; phenolic compounds; antioxidants; bioaccessibility
Special Issues, Collections and Topics in MDPI journals
Dr. Christian Espinosa-Bustos

E-Mail Website1 Website2
Guest Editor
Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Santiago 7820436, Chile
Interests: bioactive compounds; organic synthesis; medicinal chemistry; neurodegeneration; anti-cancer compounds; nuclear magnetic resonance; natural products; antioxidants
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Bioactive compounds derived from natural sources continue to attract significant scientific attention due to their multifaceted biological properties and potential applications in health and disease prevention. Among them, phenolic acids, flavonoids, terpenes, alkaloids, peptides, fatty acids, and other secondary metabolites exhibit potent antioxidant activities that play a fundamental role in mitigating oxidative stress—an underlying factor in inflammation, infection, and chronic degenerative disorders. Their chemical structures enable them to scavenge free radicals, neutralize reactive oxygen and nitrogen species, and chelate transition metals, thereby preserving cellular homeostasis.

Emerging evidence also highlights the complex interplay between oxidative stress and inflammatory or antibacterial responses, demonstrating that modulation of redox balance can influence immune signaling pathways and microbial resistance mechanisms. Moreover, advances in analytical chemistry, biochemistry, and synthetic strategies are enabling the identification, isolation, and structural modification of these compounds, expanding their potential for pharmaceutical, nutraceutical, and functional food development.

This second edition aims to present cutting-edge research and comprehensive reviews addressing the antioxidant, antibacterial, and anti-inflammatory modulation exerted by bioactive compounds from natural, semi-synthetic, or synthetic sources inspired by nature. We particularly welcome studies focusing on mechanistic insights, innovative extraction or characterization approaches, and novel applications contributing to the understanding and valorization of bioactive compounds for health promotion.

Dr. Raquel Bridi
Dr. Christian Espinosa-Bustos
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 250 words) can be sent to the Editorial Office for assessment.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-anonymized peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Antioxidants is an international peer-reviewed open access monthly journal published by MDPI.

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

  • bioactive compounds
  • antioxidants
  • anti-inflammatory activity
  • antibacterial properties
  • reactive oxygen species
  • oxidative stress
  • phytochemicals

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Published Papers (6 papers)

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Research

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28 pages, 19859 KB  
Article
Comprehensive Phytopharmacological Profiling of Polygonum aviculare L.: Antioxidant, Anti-Inflammatory, and α-Glucosidase Inhibitory Activities of Bioactive Constituents with Molecular Docking and In Silico Drug-Likeness Analysis
by Yuen-Sing Lee, Sin-Min Li, Hui-Ju Chen and Jih-Jung Chen
Antioxidants 2026, 15(8), 947; https://doi.org/10.3390/antiox15080947 - 29 Jul 2026
Viewed by 582
Abstract
This study investigated the extracts and bioactive constituents of the aerial parts of Polygonum aviculare L., a well-known traditional medicine for inflammation and diuresis, through bioactivity-guided investigation and molecular docking analysis. Solvent extracts demonstrated significant antioxidant, anti-α-glucosidase, and anti-inflammatory activities, supporting their value [...] Read more.
This study investigated the extracts and bioactive constituents of the aerial parts of Polygonum aviculare L., a well-known traditional medicine for inflammation and diuresis, through bioactivity-guided investigation and molecular docking analysis. Solvent extracts demonstrated significant antioxidant, anti-α-glucosidase, and anti-inflammatory activities, supporting their value for further pharmacological investigation. Among the isolated compounds, gallic acid (1), quercetin (3), myricetin (4), avicularin (6), and isorhamnetin (7) exhibited excellent antioxidant activity in the DPPH assay (SC50 ≤ 6.50 μM) and were stronger than the positive control BHT (SC50 = 36.99 μM). Kaempferol (9) (IC50 of 4.50 µM) demonstrated the highest α-glucosidase inhibition, surpassing that of the clinically used acarbose (IC50 = 519.7 µM). Additionally, gallic acid and quercetin demonstrated significantly stronger NO inhibition than apigenin, while kaempferol showed comparable activity (IC50 = 15.06 ± 1.50 μM vs. 16.08 ± 1.86 μM for apigenin). Molecular docking analyses supported favorable interactions between the active compounds and α-glucosidase and inducible nitric oxide synthase (iNOS). Kaempferol reduced the expression of iNOS and COX-2 in LPS-stimulated RAW 264.7 macrophages and was associated with increased KLF4 and Arg-1 expression and decreased phosphorylation of p38 MAPK and IκBα, suggesting a potential role in promoting an anti-inflammatory M2-like macrophage phenotype. Structure–activity relationship analysis indicated that flavonoid aglycones and specific hydroxylation patterns contribute to the observed biological activities. Collectively, these findings identify quercetin and kaempferol as highly active constituents of P. aviculare and support their potential for further pharmacological investigation. Full article
(This article belongs to the Special Issue Bioactive Compounds: Antioxidant, Antibacterial, and Anti-Inflammatory Modulation—2nd Edition)
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22 pages, 4838 KB  
Article
In Vitro Regeneration of Ludwigia octovalvis via Indirect Organogenesis and Evaluation of Its Bioactive Properties
by Stephany Abigail Tadeo-Cuenca, Silvia Marquina-Bahena, Gabriel Alfonso Gutiérrez-Rebolledo, María Crystal Columba-Palomares, Araceli Guerrero-Alonso, Valeri Domínguez-Villegas, Francisco Cruz-Sosa and Mariana Sánchez-Ramos
Antioxidants 2026, 15(7), 810; https://doi.org/10.3390/antiox15070810 - 28 Jun 2026
Viewed by 375
Abstract
Due to Ludwigia octovalvis’ aquatic habitat’s vulnerability to climate change, this study developed an in vitro regeneration system using indirect organogenesis to ensure sustainable production of biomass and secondary metabolites. Treatment T16 (0.1 mg/L BAP and 1.0 mg/L NAA) was identified as the [...] Read more.
Due to Ludwigia octovalvis’ aquatic habitat’s vulnerability to climate change, this study developed an in vitro regeneration system using indirect organogenesis to ensure sustainable production of biomass and secondary metabolites. Treatment T16 (0.1 mg/L BAP and 1.0 mg/L NAA) was identified as the optimal hormonal regimen for callus induction and shoot differentiation. Phytochemical analysis by GC-MS revealed that seedlings regenerated under treatment T16 exhibited a diverse profile of 18 phytoconstituents, enhancing the accumulation of phytosterols, terpenes, and tocopherols. In vitro biological evaluation demonstrated that T16 extract possesses significant antibacterial activity (MIC < 62.5 µg/mL) against methicillin-resistant Staphylococcus aureus, and moderate antioxidant capacity. T16 extract showed anti-inflammatory effects superior to indomethacin at a low quantity (0.5 mg/ear) in adult CD1 mice of both sexes. In conclusion, the indirect organogenesis of L. octovalvis not only conserves the species but also optimizes its pharmacological potential, consolidating it as an efficient biotechnological platform for the development of advanced phytopharmaceuticals. Full article
(This article belongs to the Special Issue Bioactive Compounds: Antioxidant, Antibacterial, and Anti-Inflammatory Modulation—2nd Edition)
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17 pages, 14638 KB  
Article
Astragaloside IV Alleviates Trueperella pyogenes-Induced Endometritis via the Nrf2/HO-1 Signaling Pathway
by Chunyang Gou, Hetian Mu, Yueting Wang, Yanan Liu, Ziqi Peng, Yun Li, Mingwei Xing and Maozhen Qi
Antioxidants 2026, 15(2), 271; https://doi.org/10.3390/antiox15020271 - 22 Feb 2026
Viewed by 1158
Abstract
The increasing antimicrobial resistance of T. pyogenes, one of the principal pathogens associated with endometritis, presents a formidable challenge in veterinary medicine. Astragaloside IV (AS-IV) is a triterpene saponin compound isolated from the traditional Chinese medicine Astragalus membranaceus. While recognized as the [...] Read more.
The increasing antimicrobial resistance of T. pyogenes, one of the principal pathogens associated with endometritis, presents a formidable challenge in veterinary medicine. Astragaloside IV (AS-IV) is a triterpene saponin compound isolated from the traditional Chinese medicine Astragalus membranaceus. While recognized as the primary bioactive constituent of Astragalus membranaceus with diverse pharmacological properties, its potential to counteract T. pyogenes-induced endometritis has yet to be elucidated. In the current study, T. pyogenes infection models were successfully established in both mouse uteri and cultured goat endometrial epithelial cells (gEECs). Integrating histopathology, molecular biology and transcriptomic technology, this study characterized the multifaceted biological effects of AS-IV. Transcriptomic analysis indicates that the regulatory effects of AS-IV on T. pyogenes-induced infection are primarily associated with the enrichment of signaling pathways related to inflammation, apoptosis, and oxidative stress. Subsequent validation demonstrated that AS-IV treatment effectively alleviated T. pyogenes-induced endometrial damage by suppressing inflammation, apoptosis, and oxidative stress. These effects were mediated through Nrf2 and its downstream target HO-1, a mechanism further confirmed by the loss of protection upon Nrf2 inhibition. In summary, AS-IV protects the endometrium against T. pyogenes-induced inflammatory and oxidative damage by activating the Nrf2/HO-1 signaling pathway. Full article
(This article belongs to the Special Issue Bioactive Compounds: Antioxidant, Antibacterial, and Anti-Inflammatory Modulation—2nd Edition)
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21 pages, 2513 KB  
Article
Experimental and In Silico Studies to Unravel the Antioxidant and Antibacterial Properties of Lichen Metabolites from Pseudocyphellaria compar and Pseudocyphellaria nudata
by Mauricio A. Cuellar, Jessica Mejía, Helena Quintero-Pertuz, Alejandro Castro-Álvarez, Marco Mellado, Waleska Vera-Quezada, Gloria Montenegro, Christian Espinosa-Bustos, Raquel Bridi and Cristian O. Salas
Antioxidants 2026, 15(1), 34; https://doi.org/10.3390/antiox15010034 - 25 Dec 2025
Cited by 1 | Viewed by 1575
Abstract
Lichens are a source of diverse compounds with a wide range of biological activities, making them of significant interest for novel drug development. In this study, metabolites were extracted from Lobariaceae lichens, and their antioxidant and antibacterial properties were experimentally investigated and explained [...] Read more.
Lichens are a source of diverse compounds with a wide range of biological activities, making them of significant interest for novel drug development. In this study, metabolites were extracted from Lobariaceae lichens, and their antioxidant and antibacterial properties were experimentally investigated and explained using various computational approaches. Specifically, four lichen metabolites were analyzed using three methods to assess their antioxidant capacity. Antibacterial activity assays were conducted against four pathogens, and the minimum inhibitory concentrations (MICs) of the most promising compounds were determined. Ab initio studies were performed to evaluate radical stability. A pharmacological target responsible for the antibacterial effect was identified, and possible binding sites and modes were studied in silico. Metabolite IX, physciosporin, exhibited the highest antioxidant activity, which was associated with the theoretical stability of the radical. Additionally, IX exhibited an MIC of 0.97 μg/mL against S. pyogenes, surpassing the potency of streptomycin. The RecA protein was identified as a potential target, and a possible binding site and pattern of interactions at that site were described. Finally, IX showed low cytotoxicity in human cancer cell lines and was predicted to have favorable oral absorption properties, supporting its potential as a promising antioxidant and antibacterial agent against S. pyogenes. Full article
(This article belongs to the Special Issue Bioactive Compounds: Antioxidant, Antibacterial, and Anti-Inflammatory Modulation—2nd Edition)
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Review

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23 pages, 457 KB  
Review
Multi-Target Modulation of Interconnected Pathogenetic Pathways by Natural Bioactive Compounds in Endometriosis
by Kamila Pokorska-Niewiada, Małgorzata Szczuko, Khasan Kayumov and Katarzyna Janda-Milczarek
Antioxidants 2026, 15(8), 1003; https://doi.org/10.3390/antiox15081003 - 13 Aug 2026
Viewed by 342
Abstract
Background: Endometriosis is a chronic estrogen-dependent disease characterized by the presence of endometrial-like tissue outside the uterine cavity. Its pathogenesis involves interactions between inflammatory, angiogenic, hormonal, oxidative stress-related, and cell survival-associated pathways, contributing to lesion development and persistence. Current treatment options are often [...] Read more.
Background: Endometriosis is a chronic estrogen-dependent disease characterized by the presence of endometrial-like tissue outside the uterine cavity. Its pathogenesis involves interactions between inflammatory, angiogenic, hormonal, oxidative stress-related, and cell survival-associated pathways, contributing to lesion development and persistence. Current treatment options are often limited by adverse effects, incomplete symptom control, and high recurrence rates. Methods: This integrative review summarizes the molecular mechanisms involved in endometriosis and the potential role of natural bioactive compounds in their modulation. A literature search was conducted using PubMed, Scopus, and Web of Science, and evidence from experimental, animal, and clinical studies was reviewed. Results: Natural compounds such as curcumin, resveratrol, quercetin, EGCG (epigallocatechin-3 gallate) and genistein have been reported to modulate multiple pathways involved in endometriosis. Their biological activity includes modulation of inflammatory signaling, angiogenesis, estrogen-dependent processes, epithelial–mesenchymal transition, oxidative stress, and apoptosis. While some compounds influence several interconnected pathways, others appear to exert more selective effects. Conclusions: The findings summarized in this review suggest that natural bioactive compounds may influence several interconnected mechanisms involved in endometriosis. Although clinical evidence remains limited, these compounds warrant further investigation as potential adjuncts to current therapeutic approaches. Full article
(This article belongs to the Special Issue Bioactive Compounds: Antioxidant, Antibacterial, and Anti-Inflammatory Modulation—2nd Edition)
37 pages, 4369 KB  
Review
Potential of Native Brazilian Fruits in Modulating Oxidative Stress and Inflammation: A Focused Review
by Maria Carolina Zsigovics Alfino, Geni Rodrigues Sampaio, Adriano Costa de Camargo and Elizabeth Aparecida Ferraz da Silva Torres
Antioxidants 2026, 15(6), 677; https://doi.org/10.3390/antiox15060677 - 28 May 2026
Viewed by 1362
Abstract
Chronic non-communicable diseases are closely linked to low-grade inflammation and oxidative stress. Native Brazilian fruits, rich in bioactive compounds such as polyphenols and carotenoids, have recognized antioxidant, anti-inflammatory, and neuroprotective properties. Mechanisms of action included inhibition of NF-κB signaling, downregulation of pro-inflammatory cytokines, [...] Read more.
Chronic non-communicable diseases are closely linked to low-grade inflammation and oxidative stress. Native Brazilian fruits, rich in bioactive compounds such as polyphenols and carotenoids, have recognized antioxidant, anti-inflammatory, and neuroprotective properties. Mechanisms of action included inhibition of NF-κB signaling, downregulation of pro-inflammatory cytokines, modulation of oxidative biomarkers, and improvement of metabolic parameters. Several studies demonstrate protective effects against insulin resistance, hepatic steatosis, cardiovascular alterations, and neuroinflammation, alongside modulation of gut microbiota. Most evidence is from animal or cell models, with scarce clinical trials, limiting translational applicability. Overall, native Brazilian fruits represent promising dietary sources of bioactive compounds that may contribute to the modulation of oxidative stress and chronic inflammation. Challenges include variability in phytochemical content due to species, maturity, processing, a lack of standardized extraction and dosage protocols, and limited bioavailability data. Although preclinical findings are robust, further controlled human trials are necessary to confirm their efficacy and clarify their role in the clinical management of inflammatory and neurodegenerative diseases. Full article
(This article belongs to the Special Issue Bioactive Compounds: Antioxidant, Antibacterial, and Anti-Inflammatory Modulation—2nd Edition)
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