Antioxidant and Anti-Inflammatory Activities of Plant Extracts and Phytochemicals

A special issue of Plants (ISSN 2223-7747). This special issue belongs to the section "Phytochemistry".

Deadline for manuscript submissions: 30 June 2025 | Viewed by 16637

Special Issue Editor

Special Issue Information

Dear Colleagues,

We are pleased to invite you to contribute a Special Issue of the journal Plants focused on “Antioxidant and Anti-inflammatory Activities of Plant Extracts and Phytochemicals.” Oxidation and Inflammation are critical processes for normal cellular function and immune responses. Moreover, oxidative stress can trigger inflammation, vice versa, creating a positive feedback loop. Consequently, an imbalance or dysregulation of these processes can contribute to the development and progression of various chronic diseases, including allergies, diabetes, cardiovascular disease, neurodegenerative diseases, and cancer. Therefore, understanding the interconnected nature of oxidation and inflammation is essential for the development of effective strategies for disease prevention and treatment. Targeting both processes represents a promising therapeutic approach for managing these pathological conditions.

Plants serves as a rich source of complex and highly structurally diverse chemical compounds. These compounds often serve as the starting point for drug discovery and development, having provided us with a plethora of clinically useful drugs, including paclitaxel, artemisinin, galantamine, and morphine. Notably, acetylsalicylic acid (aspirin), a nonsteroidal anti-inflammatory drug derived from salicylic acid found in willow and other salicylate-rich plants, has been employed to treat fever and pain for thousands of years. However, many natural compounds beneficial for human health remain undiscovered, particularly with regard to addressing oxidative stress and inflammation-associated diseases. In this context, this Special Issue aims to provide a comprehensive platform for researchers, scientists, and practitioners to share their latest research findings and insights related to the crucial role that plant extracts and phytochemicals play in combating oxidative stress and inflammation. We welcome submissions of original research articles, reviews, and short communications that explore plant extracts and phytochemicals, their antioxidant and/or anti-inflammatory activities, and their pharmacological potential in addressing oxidative stress- and inflammation-associated diseases.  

Prof. Dr. Seok-Geun Lee
Guest Editor

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Keywords

  • plants
  • phytochemicals
  • drug discovery
  • bioactive compounds
  • biochemometrics
  • metabolomics
  • molecular network analysis
  • oxidative stress
  • inflammation
  • oxidative stress or/and inflammation-associated diseases

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Published Papers (10 papers)

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Research

Jump to: Review

14 pages, 634 KiB  
Article
Chemical Composition and Biological Activity of Hypericum Species—H. hirsutum, H. barbatum, H. rochelii
by Jovan Baljak, Mirjana Bogavac, Maja Karaman, Branislava Srđenović Čonić, Biljana Vučković, Goran Anačkov and Nebojša Kladar
Plants 2024, 13(20), 2905; https://doi.org/10.3390/plants13202905 - 17 Oct 2024
Viewed by 736
Abstract
St. John’s wort (Hypericum perforatum, Hypericaceae) is the most well-known species in the genus Hypericum, which comprises several hundred species. This study investigates the biological and phytochemical potential of the under-researched Hypericum species, H. hirsutum, H. barbatum, and [...] Read more.
St. John’s wort (Hypericum perforatum, Hypericaceae) is the most well-known species in the genus Hypericum, which comprises several hundred species. This study investigates the biological and phytochemical potential of the under-researched Hypericum species, H. hirsutum, H. barbatum, and H. rochelii. A high level of similarity between the chemical profiles of H. hirsutum and H. barbatum and the official source of the herbal drug (H. perforatum) was shown, but a higher content of quercetin and rutin was also found in all three evaluated species (116–230 µg/g dry herb). The highest amount of phenolics (195 mg GAE/g) was recorded in H. hirsutum extract, while the highest amount of flavonoids (47 mg QE/g) was recorded in H. barbatum extract. The evaluated species were excellent scavengers of DPPH, OH, and NO radicals, as well as strong ferric ion reducers in the FRAP test. Prominent monoamine oxidase A and α-glucosidase inhibition was observed, compared to modest inhibition of monoamine oxidase B, α-amylase, and acetylcholinesterase. High activity against Gram-positive MRSA S. aureus was demonstrated for the tested species, with MIC/MBC values recorded at 12.5 µg/mL. Antifungal activity against Candida strains was not observed. The obtained results emphasize the need for further investigation of species of the genus Hypericum to discover potentially new sources of biologically active compounds. Full article
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18 pages, 2991 KiB  
Article
Aqueous Extracts of Rhus trilobata Inhibit the Lipopolysaccharide-Induced Inflammatory Response In Vitro and In Vivo
by Alejandra Jazmín Rodríguez-Castillo, Susana Aideé González-Chávez, Ismael Portillo-Pantoja, Eunice Cruz-Hermosillo, César Pacheco-Tena, David Chávez-Flores, Ma. Carmen E. Delgado-Gardea, Rocío Infante-Ramírez, José Juan Ordaz-Ortiz and Blanca Sánchez-Ramírez
Plants 2024, 13(20), 2840; https://doi.org/10.3390/plants13202840 - 10 Oct 2024
Viewed by 1086
Abstract
Chronic noncommunicable diseases (NCDs) are responsible for approximately 74% of deaths globally. Medicinal plants have traditionally been used to treat NCDs, including diabetes, cancer, and rheumatic diseases, and are a source of anti-inflammatory compounds. This study aimed to evaluate the anti-inflammatory effects of [...] Read more.
Chronic noncommunicable diseases (NCDs) are responsible for approximately 74% of deaths globally. Medicinal plants have traditionally been used to treat NCDs, including diabetes, cancer, and rheumatic diseases, and are a source of anti-inflammatory compounds. This study aimed to evaluate the anti-inflammatory effects of Rhus trilobata (Rt) extracts and fractions in lipopolysaccharide (LPS)-induced inflammation models in vitro and in vivo. The aqueous extract (RtAE) and five fractions (F2 to F6) were obtained via C18 solid-phase separation and tested in murine LPS-induced J774.1 macrophages. Key inflammatory markers, such as IL-1β, IL-6, TNF-α, and COX-2 gene expression were measured using RT-qPCR, and PGE2 production was assessed via HPLC-DAD. The in vivo effects were tested in an LPS-induced paw edema model in Wistar rats. Results showed that RtAE at 15 μg/mL significantly decreased IL-1β and IL-6 gene expression in vitro. Fraction F6 further reduced IL-1β, TNF-α, and IL-6 gene expression, COX-2 expression, and PGE2 production. In vivo, F6 significantly reduced LPS-induced paw edema, inflammatory infiltration, and IL-1β and COX-2 protein expression. Chemical characterization of F6 by UPLC/MS-QTOF revealed at least eight compounds with anti-inflammatory activity. These findings support the anti-inflammatory potential of RtAE and F6, reinforcing the medicinal use of Rt. Full article
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17 pages, 3138 KiB  
Article
Antioxidant Active Phytochemicals in Ternstroemia lineata Explained by Aquaporin Mechanisms
by Nahim Salgado-Medrano, César Millán-Pacheco, Verónica Rodríguez-López, Lucía Corona-Sánchez, François Mesnard, Roland Molinié, Eleazar León-Álvarez, María Luisa Villarreal and Alexandre Toshirrico Cardoso-Taketa
Plants 2024, 13(16), 2223; https://doi.org/10.3390/plants13162223 - 10 Aug 2024
Cited by 1 | Viewed by 1055
Abstract
The antioxidant action of terngymnoside C (1) and hydroxytyrosol-1-glucoside (2), isolated for the first time from the flower buds of Ternstroemia lineata, as well as katsumadin (3), obtained from the seedless fruits, was evaluated using ABTS [...] Read more.
The antioxidant action of terngymnoside C (1) and hydroxytyrosol-1-glucoside (2), isolated for the first time from the flower buds of Ternstroemia lineata, as well as katsumadin (3), obtained from the seedless fruits, was evaluated using ABTS•+ and H2O2Saccharomyces cerevisiae models. In silico docking analysis of 1, 2, and 3 determined their affinity forces to the aquaporin monomers of the modeled S. cerevisiae protein 3 (AQP3) and human protein 7 (AQP7) channels that regulate the H2O2 cell transport. The ABTS•+ antiradical capacity of these compounds showed IC50 values of 22.00 μM (1), 47.64 μM (2), and 73.93 μM (3). The S. cerevisiae antioxidant assay showed that at 25 µM (1) and 50 µM (2 and 3), the cells were protected from H2O2-oxidative stress. These compounds, together with quercetin and vitamin C, were explored through the modeled S. cerevisiae AQP3 and human AQP7 by molecular docking analysis. To explain these results, an antioxidant mechanism for the isolated compounds was proposed through blocking H2O2 passage mediated by aquaporin transport. On the other hand, 1, 2, and 3 were not cytotoxic in a panel of three cancer cell lines. Full article
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13 pages, 3017 KiB  
Article
Cancer Chemopreventive Effect of 2′,4′-Dihydroxy-6′-methoxy-3′,5′-dimethylchalcone on Diethylnitrosamine-Induced Early Stages of Hepatocarcinogenesis in Rats
by Sirinya Taya, Charatda Punvittayagul, Puttinan Meepowpan and Rawiwan Wongpoomchai
Plants 2024, 13(14), 1975; https://doi.org/10.3390/plants13141975 - 19 Jul 2024
Viewed by 2527
Abstract
2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone (DMC) is a major compound in Cleistocalyx nervosum seed extract (CSE), which has been reported to have various biological activities, including anti-cancer activity. Therefore, this study attempted to evaluate whether DMC is a chemopreventive compound in CSE. Moreover, the preventive mechanisms of [...] Read more.
2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone (DMC) is a major compound in Cleistocalyx nervosum seed extract (CSE), which has been reported to have various biological activities, including anti-cancer activity. Therefore, this study attempted to evaluate whether DMC is a chemopreventive compound in CSE. Moreover, the preventive mechanisms of CSE and DMC in the DEN-induced early stages of hepatocarcinogenesis in rats were investigated. Male Wistar rats were intraperitoneally injected with DEN 50 mg/kg bw once a week for 8 weeks. Rats received CSE and DMC orally throughout the experiment. The number of glutathione S-transferase placental form (GST-P)-positive foci in the liver was measured. Furthermore, the preventive mechanisms of CSE and DMC on DEN-induced HCC, including cell proliferation and apoptosis, were investigated. Administering CSE at a dosage of 400 mg/kg bw and DMC at a dosage of 10 mg/kg bw significantly decreased the number and size of GST-P-positive foci and GST-P expression. In addition, DMC inhibited the development of preneoplastic lesions by decreasing cell proliferation and causing cell apoptosis; however, CSE inhibited the development of preneoplastic lesions by inducing cell apoptosis. In conclusion, DMC exhibited a cancer chemopreventive effect on the early stages of hepatocarcinogenesis by increasing cell apoptosis and reducing cell proliferation. Full article
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14 pages, 280 KiB  
Article
The Potential of Hemp Extracts to Modify the Course of Oxidative-Stress Related Conditions
by Katarina Bijelić, Branislava Srdjenović Čonić, Blagoje Prpa, Vladimir Pilija, Saša Vukmirović and Nebojša Kladar
Plants 2024, 13(12), 1630; https://doi.org/10.3390/plants13121630 - 13 Jun 2024
Cited by 1 | Viewed by 969
Abstract
The leaves of industrial hemp, which have long been considered as a waste product, have been proven to contain numerous compounds that possess potential biological activity. One of the most interesting groups of compounds present are polyphenolic compounds, which, due to their specific [...] Read more.
The leaves of industrial hemp, which have long been considered as a waste product, have been proven to contain numerous compounds that possess potential biological activity. One of the most interesting groups of compounds present are polyphenolic compounds, which, due to their specific structure, have a pronounced antioxidant and antihyperglycemic potential. This study aimed to detect biological activity, including antioxidant and antihyperglycemic potential, of water and water–alcoholic extracts of five commercially available hemp teas, followed by phytochemical profiling. Hemp aqueous and ethanolic extracts demonstrate potent antioxidant properties. Ethanol extracts are better scavengers of DPPH• and OH•, while aqueous extracts neutralize NO• better. Both types of extracts exhibit antioxidant potential in the catalase test and moderate XOD inhibition. Furthermore, aqueous extracts are potent α-amylase inhibitors, while ethanolic extracts demonstrate stronger anti-α-glucosidase activity, suggesting therapeutic potential for chronic diseases like insulin resistance or diabetes. Further detailed chemical characterization and in vivo studies are needed to validate these findings. Full article
22 pages, 2668 KiB  
Article
Pharmaceutical Potential Evaluation of Damask Rose By-Products from Volatile Oil Extraction
by Nutthawut Charoimek, Piyachat Sunanta, Tibet Tangpao, Ratchuporn Suksathan, Wisinee Chanmahasathien, Sasithorn Sirilun, Kuo-Feng Hua, Hsiao-Hang Chung, Sarana Rose Sommano and Taepin Junmahasathien
Plants 2024, 13(12), 1605; https://doi.org/10.3390/plants13121605 - 9 Jun 2024
Cited by 1 | Viewed by 2008
Abstract
Despite its well-known fragrance in cosmetics and medicine, a complete understanding of the phytochemical properties within by-products generated during commercial extraction of Damask rose remains elusive. Cultivated in Thailand for their essential oil, Damask rose varieties, including Mon Dang Prasert, Mon Klai Kangwon, [...] Read more.
Despite its well-known fragrance in cosmetics and medicine, a complete understanding of the phytochemical properties within by-products generated during commercial extraction of Damask rose remains elusive. Cultivated in Thailand for their essential oil, Damask rose varieties, including Mon Dang Prasert, Mon Klai Kangwon, and Bishop’s Castle, share phenylethyl alcohol (57.62–61.11%) as the dominant component, which is responsible for their characteristic floral, sweet, rosy, and bready aroma. Through a circular hydro-distillation process, three different by-product fractions, including distilled water (D), hydrosol (H), and rose dreg (R), were recovered. Subsequently, we assessed their pharmaceutical potential, including the antioxidant, antimicrobial, anti-inflammatory, and anti-melanogenesis properties of these residual substances. The H fraction displayed the highest total phenolics (10.56 mgGAE/g) and flavonoids (6.93 mgCE/g) and significant antioxidant activity (IC50, 0.67–0.97 µg/mL). While the H fraction inhibited melanin formation at 50 μg/mL, the R fraction of MK (100 μg/mL) surprisingly promoted melanin production in B16-F10 cells. Nevertheless, the antimicrobial assay against Staphylococcus aureus, Cutibacterium acnes, Staphylococcus epidermidis, Pseudomonas aeruginosa, Escherichia coli, and Candida albicans revealed no antimicrobial activity in any fraction. Murine macrophage stimulation (J774A.1) with lipopolysaccharide revealed no anti-inflammatory effects from the by-products, as measured by IL-1β production. In summary, the H fraction exhibited the highest level of phenolic and flavonoid contents, as well as antioxidant and anti-melanogenesis activities. Therefore, this by-product is a desirable choice for the development of value-added products such as functional food, cosmetics, and pharmaceutical products. Full article
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14 pages, 4356 KiB  
Article
Interaction of Norsecurinine-Type Oligomeric Alkaloids with α-Tubulin: A Molecular Docking Study
by Gérard Vergoten and Christian Bailly
Plants 2024, 13(9), 1269; https://doi.org/10.3390/plants13091269 - 3 May 2024
Viewed by 1013
Abstract
The medicinal plant Securinega virosa (Roxb ex. Willd) Baill., also known as Flueggea virosa (Roxb. ex Willd.) Royle, is commonly used in traditional medicine in Africa and Asia for the management of diverse pathologies, such as parasite infections, diabetes, and gastrointestinal diseases. Numerous [...] Read more.
The medicinal plant Securinega virosa (Roxb ex. Willd) Baill., also known as Flueggea virosa (Roxb. ex Willd.) Royle, is commonly used in traditional medicine in Africa and Asia for the management of diverse pathologies, such as parasite infections, diabetes, and gastrointestinal diseases. Numerous alkaloids have been isolated from the twigs and leaves of the plant, notably a variety of oligomeric indolizidine alkaloids derived from the monomers securinine and norsecurinine which both display anticancer properties. The recent discovery that securinine can bind to tubulin and inhibit microtubule assembly prompted us to investigate the potential binding of two series of alkaloids, fluevirosines A–H and fluevirosinine A–J, with the tubulin dimer by means of molecular modeling. These natural products are rare high-order alkaloids with tri-, tetra-, and pentameric norsecurinine motifs. Despite their large size (up to 2500 Å3), these alkaloids can bind easily to the large drug-binding cavity (about 4800 Å3) on α-tubulin facing the β-tubulin unit. The molecular docking analysis suggests that these hydrophobic macro-alkaloids can form stable complexes with α/β-tubulin. The tubulin-binding capacity varies depending on the alkaloid size and structure. Structure-binding relationships are discussed. The docking analysis identifies the trimer fluevirosine D, tetramer fluevirosinine D, and pentamer fluevirosinine H as the most interesting tubulin ligands in the series. This study is the first to propose a molecular target for these atypical oligomeric Securinega alkaloids. Full article
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16 pages, 3028 KiB  
Article
Bioassay-Guided Fractionation of Pittosporum angustifolium and Terminalia ferdinandiana with Liquid Chromatography Mass Spectroscopy and Gas Chromatography Mass Spectroscopy Exploratory Study
by Janice Mani, Joel Johnson, Holly Hosking, Luke Schmidt, Ryan Batley, Ryan du Preez, Daniel Broszczak, Kerry Walsh, Paul Neilsen and Mani Naiker
Plants 2024, 13(6), 807; https://doi.org/10.3390/plants13060807 - 12 Mar 2024
Viewed by 1597
Abstract
Bioprospecting native Australian plants offers the potential discovery of latent and novel bioactive compounds. The promising cytotoxic and antibacterial activity of methanolic extracts of Pittosporum angustifolium and Terminalia ferdinandiana led to further fractionation and isolation using our laboratory’s bioassay-guided fractionation protocol. Hence, the [...] Read more.
Bioprospecting native Australian plants offers the potential discovery of latent and novel bioactive compounds. The promising cytotoxic and antibacterial activity of methanolic extracts of Pittosporum angustifolium and Terminalia ferdinandiana led to further fractionation and isolation using our laboratory’s bioassay-guided fractionation protocol. Hence, the aim of this study was to further evaluate the bioactivity of the fractions and subfractions and characterize bioactive compounds using liquid chromatography mass spectroscopy (LC-MS/MS) and gas chromatography MS (GC-MS). Compounds tentatively identified in P. angustifolium Fraction 1 using LC-ESI-QTOF-MS/MS were chlorogenic acid and/or neochlorogenic acid, bergapten, berberine, 8′-epitanegool and rosmarinic acid. GC-MS analysis data showed the presence of around 100 compounds, mainly comprising carboxylic acids, sugars, sugar alcohols, amino acids and monoalkylglycerols. Furthermore, the fractions obtained from T. ferdinandiana flesh extracts showed no cytotoxicity, except against HT29 cell lines, and only Fraction 2 exhibited some antibacterial activity. The reduced bioactivity observed in the T. ferdinandiana fractions could be attributed to the potential loss of synergy as compounds become separated within the fractions. As a result, the further fractionation and separation of compounds in these samples was not pursued. However, additional dose-dependent studies are warranted to validate the bioactivity of T. ferdinandiana flesh fractions, particularly since this is an understudied species. Moreover, LC-MS/GC-MS studies confirm the presence of bioactive compounds in P. angustifolium Fraction 1/subfractions, which helps to explain the significant acute anticancer activity of this plant. The screening process designed in this study has the potential to pave the way for developing scientifically validated phytochemical/bioactivity information on ethnomedicinal plants, thereby facilitating further bioprospecting efforts and supporting the discovery of novel drugs in modern medicine. Full article
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13 pages, 3633 KiB  
Article
In Vitro and In Vivo Anti-Inflammatory Potential of Cannabichromene Isolated from Hemp
by Min Hong, Jong-Hui Kim, Joon-Hee Han, Byeong-Ryeol Ryu, Young-Seok Lim, Jung-Dae Lim, Sang-Hyuck Park, Chang-Hyeug Kim, Soo-Ung Lee and Tae-Hyung Kwon
Plants 2023, 12(23), 3966; https://doi.org/10.3390/plants12233966 - 25 Nov 2023
Cited by 7 | Viewed by 3039
Abstract
Cannabichromene (CBC), a non-psychoactive cannabinoid found in Cannabis sativa, has recently been shown to possess several medicinal properties. However, how CBC produces anti-inflammatory effects and the mechanisms of this remain poorly studied. Therefore, we extracted and purified the CBC from the Cannabis [...] Read more.
Cannabichromene (CBC), a non-psychoactive cannabinoid found in Cannabis sativa, has recently been shown to possess several medicinal properties. However, how CBC produces anti-inflammatory effects and the mechanisms of this remain poorly studied. Therefore, we extracted and purified the CBC from the Cannabis sativa cv. pink pepper (hemp cultivar). The efficacy of CBC in reducing inflammation in RAW 264.7 macrophages and a λ-carrageenan-induced mouse model was then evaluated. CBC had no cytotoxicity up to a concentration of 20 μM and inhibited nitric oxide production by approximately 50% at a concentration of 20 μM. In addition, CBC treatment significantly inhibited causes of inflammation such as inducible nitric oxide synthase (iNOS), interleukin-1β (IL-1β), IL-6, and tumor necrosis factor-α (TNF-α) at both the mRNA and protein levels. Moreover, CBC suppressed LPS-stimulated inflammation in RAW 264.7 cells by downregulating the nuclear factor kappa B (NF-kB) and mitogen-activated protein kinase pathways (MAPK). Furthermore, our in vivo experiments confirmed that the λ-carrageenan-induced increase in the levels of the cytokines iNOS, IL-1β, and IL-6 was abrogated following treatment with CBC. Therefore, CBC has potential anti-inflammatory effects and may be useful for preventing or treating inflammation. Full article
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Review

Jump to: Research

16 pages, 2176 KiB  
Review
Fissistigma oldhamii (Hemsl.) Merr.: Ethnomedicinal, Phytochemistry, and Pharmacological Aspects
by Christian Bailly
Plants 2023, 12(24), 4094; https://doi.org/10.3390/plants12244094 - 7 Dec 2023
Cited by 1 | Viewed by 1585
Abstract
The species Fissistigma oldhamii (Hemsl.) Merr. (Annonaceae) has long been used as a traditional herbal medicine in China to treat diverse human diseases. Decoctions from the roots of the plant (Guā Fù Mù) are used to treat body pain and inflammatory pathologies, such [...] Read more.
The species Fissistigma oldhamii (Hemsl.) Merr. (Annonaceae) has long been used as a traditional herbal medicine in China to treat diverse human diseases. Decoctions from the roots of the plant (Guā Fù Mù) are used to treat body pain and inflammatory pathologies, such as rheumatic syndromes, sciatica, and osteoarthritis. The phytochemical content of the plant and the associated pharmacological activities have been analyzed. Seventy natural products were identified in the different parts of the plants, namely, the roots, stems, leaves, fruits, and seeds. The compounds comprise many tri- and tetracyclic alkaloids (aporphine-type), anthraquinones, terpenoids, flavonoids, and others. The pharmacological properties of these molecules were analyzed to point out the anti-inflammatory, antioxidant, anticancer, and/or antimicrobial effects, together with the underlying modulated pathways and molecular targets in some cases. The panel of phytoconstituents present in F. oldhamii extracts is large, with the majority of bioactive products identified in the roots and stems. Multiple molecules can contribute to the anti-inflammatory properties of the extracts. Network pharmacology analyses of the phytoconstituents are needed to better delineate the effective components and their targets. Full article
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