Anti-Inflammatory and Antioxidant Advances on Bioactive Compounds Derived from Plants and Foods in Honor of Professor Carlo Franchini on the Occasion of His Retirement

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

Deadline for manuscript submissions: closed (31 January 2022) | Viewed by 49107

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Università degli Studi di Bari, Bari, Italy

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Department of Pharmacy-Pharmaceutical Sciences, Università degli studi Aldo Moro, Bari, Italy
Interests: natural product chemistry
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Special Issue Information

Dear Colleagues,

Antioxidants is delighted to host the Special Issue entitled “Anti-Inflammatory and Antioxidant Advances on Bioactive Compounds Derived from Plants and Foods” honoring the scientific career of Prof. Carlo FRANCHINI on the occasion of his retirement.

He was born in Italy and graduated cum laude both in Pharmacy (1974) and in Chemistry and Pharmaceutical Technology (1975), as second degree, at the University of Bari Aldo Moro, Italy. He spent one year (1979-1980) as Visiting Professor at the McGill University in Montreal in the research group of Prof. B. Belleau. He is still teaching courses on Pharmaceutical and Toxicological Chemistry and Toxicological Environmental and Abuse Drug’s Chemistry at the Department of Pharmacy-Pharmaceutical Sciences at the University of Bari Aldo Moro, Italy.

He was Full Professor in Medicinal Chemistry from March 2000 up today, Director of the School of Specialization in Hospital Pharmacy until 2019; Dean of Drug-Chemistry Department of the Faculty of Pharmacy for six years, President of Apulian Section of Italian Chemical Society, Delegate of the Rector for the Third Mission of the University of Bari and from 2019 until today he is the Coordinator of the PhD School of Pharmaceutical Science.

Moreover, he holds many professional achievements and experiences such as Member of Ethic Committee of the University Hospital Policlinico Consorziale, Bari, Italy (2000-2007), and as a President of the Pharmaceutical-Science School of Ruggieri-Foundation and of the Pharmacist Order of BA-BAT provinces. He also teaches activity for several years at the University of Cosenza, Calabria, Italy.

The research activity of Carlo Franchini started in 1975 after the degree in Medicinal Chemistry at the Faculty of Pharmacy at the University of Bari, Italy. He has been involved in synthesis, chemical characterization, and SAR (structure activity relationships) studies of new chiral compounds, as new candidates as drugs, pro-drugs, and healthy products.

An important part of his research has been on cardiovascular system and related drugs. In particular, he was interested in studying chiral derivatives of Mexiletine and Tocainide, in order to carry out a possible repositioning for the two lead compounds and, at the same time, fully characterize the chemical and toxicological aspects with the aim to discover new antiarrhythmic drugs. Some of these new compounds synthesized in our laboratory, act as potent blockers of Na channels on skeletal or cardiac muscles. They are also active on rare diseases of the nervous system, as myotonia and related pathologies.

Few years ago, he started a second research program on antitumor and antibacterial drugs used in a new synergic way: antibody drugs and natural compound obtained from essential oils of officinal plants. Starting more than ten years ago, he is now also involved in research on Nutraceuticals and Health Food, in particular working on polyphenol molecules contained in the extra virgin olive oil (EVOO), which is the largest agricultural production of the Apulia region, Italy.

His results are reported in more than one hundred fifty original articles published in international journals and he has participated in and addressed more than 100 international meetings.

He has been invited as speaker to a large number of national and international meetings. He has assisted a huge number of students, undergraduate and PhD student, in their research work for thesis and PhD project.

Prof. Franchini has created a large research group supporting the careers of young scientists and, especially women and has been met with approval and respect in all the areas in which he has worked.

Thanking him for the essential contribution he has made to the Pharmaceutical Chemistry and more recently to the Nutraceuticals, in his long career, we wish Prof. Franchini to enjoy life together with his beautiful family.

This Special Issue “Anti-Inflammatory and Antioxidant Advances on Bioactive Compounds Derived from Plants and Foods" in Honor of Professor Carlo Franchini on the occasion of his retirement invites researchers to contribute with original research or review articles related to natural products with antioxidant and inti-inflammatory properties related with Prof. Franchini’s research interests of the last few years.

Keywords

  • Bioactive compounds
  • Medicinal Chemistry
  • Food Technology
  • Biochemistry
  • Molecular Biology
  • Chronic diseases
  • Inflammation
  • Oxidative stress
  • Antioxidant effects

Published Papers (16 papers)

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13 pages, 1134 KiB  
Article
Nutritional Regimes Enriched with Antioxidants as an Efficient Adjuvant for IBD Patients under Infliximab Administration, a Pilot Study
by Marina Liso, Annamaria Sila, Giulio Verna, Aurelia Scarano, Rossella Donghia, Fabio Castellana, Elisabetta Cavalcanti, Pasqua Letizia Pesole, Eduardo Maria Sommella, Antonio Lippolis, Raffaele Armentano, Anna Maria Giudetti, Daniele Vergara, Pietro Campiglia, Rodolfo Sardone, Margherita Curlo, Mauro Mastronardi, Katia Petroni, Chiara Tonelli, Angelo Santino and Marcello Chieppaadd Show full author list remove Hide full author list
Antioxidants 2022, 11(1), 138; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox11010138 - 08 Jan 2022
Cited by 10 | Viewed by 3194
Abstract
Antioxidants are privileged candidates for the development of adjuvants able to improve the efficiency of pharmacological therapies, particularly for chronic inflammatory syndromes. During the last 20 years, anti-TNFα (tumor necrosis factor alpha) monoclonal antibodies infusion has been the biological therapy most frequently administered [...] Read more.
Antioxidants are privileged candidates for the development of adjuvants able to improve the efficiency of pharmacological therapies, particularly for chronic inflammatory syndromes. During the last 20 years, anti-TNFα (tumor necrosis factor alpha) monoclonal antibodies infusion has been the biological therapy most frequently administered but there is still large space for improvement in disease remission rates and maintenance. In this context, nutritional bioactive compounds contained in dietary patterns or included as supplements, may act as adjuvants for the induction and maintenance of IBD (inflammatory bowel diseases) remission. To verify this possibility, a single-center preliminary study (SI-CURA, Soluzioni Innovative per la gestione del paziente e il follow up terapeutico della Colite UlceRosA) was designed and carried out to evaluate whether a daily administration of purple corn supplement could improve the response to Infliximab (IFX) infusion of IBD patients with both Crohn’s disease (CD) and ulcerative colitis (UC). A cohort of 47 patients was enrolled in the study. Biological samples were collected before the first and the third IFX infusion. All patients received nutritional guidelines, 27 of them received commercial red fruit tea with low anthocyanins content, while 20 received a purple corn supplement with a high anthocyanin content. Results show that the administration of an antioxidant-enriched purple corn supplement could improve IFX-mediated disease remission in terms of circulating inflammatory markers. Comparison between CD and UC patients revealed that, at this anthocyanin dosage, the purple corn extract administration improved the IFX response in CD but not in UC patients. Our results may pave the way for a new metacentric study of CD patients, recruiting a wider cohort and followed-up over a longer observational time. Full article
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17 pages, 8213 KiB  
Article
Commiphora myrrh Supplementation Protects and Cures Ethanol-Induced Oxidative Alterations of Gastric Ulceration in Rats
by Mohamed A. Lebda, Rabab E. Mostafa, Nabil M. Taha, Eman M. Abd El-Maksoud, Hossam G. Tohamy, Soad K. Al Jaouni, Ali H. El-Far and Mohamed S. Elfeky
Antioxidants 2021, 10(11), 1836; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10111836 - 19 Nov 2021
Cited by 14 | Viewed by 2280
Abstract
Gastric ulceration is a multifactorial disease defined as a defect in the gastric wall that extends through the muscularis mucosae into the deeper layers of the wall. The most common cause of gastric ulceration is alcohol consumption. In the current study, rats were [...] Read more.
Gastric ulceration is a multifactorial disease defined as a defect in the gastric wall that extends through the muscularis mucosae into the deeper layers of the wall. The most common cause of gastric ulceration is alcohol consumption. In the current study, rats were gavaged by ethanol to investigate the protective (before ethanol) and curative (after ethanol) ability of Commiphora myrrh (myrrh) oil and extract against gastric ulcer oxidative alterations induced by ethanol. Myrrh significantly improved ulcer index, histomorphology, and periodic acid Schiff (PAS) impaired by ethanol. In addition, myrrh improved the antioxidant potential of gastric mucosa through enhancement of nuclear factor related to erythroid 2 (Nrf2), total glutathione (GSH), reduced GSH, and oxidized glutathione (GSSG), along with significant reduction in malondialdehyde (MDA) levels. Amelioration of gastric oxidative stress by myrrh enables gastric mucosa to counteract the ethanol’s inflammatory and apoptotic processes leading to improved gastric proliferation and healing. Interestingly, myrrh extract showed better protective and curative effects than myrrh oil against gastric ulceration. Full article
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25 pages, 7952 KiB  
Article
Exploring the Chemical Profiles and Biological Values of Two Spondias Species (S. dulcis and S. mombin): Valuable Sources of Bioactive Natural Products
by Kouadio Ibrahime Sinan, Gokhan Zengin, Dimitrina Zheleva-Dimitrova, Reneta Gevrenova, Marie Carene Nancy Picot-Allain, Stefano Dall’Acqua, Tapan Behl, Bey Hing Goh, Patrick Tang Siah Ying and Mohamad Fawzi Mahomoodally
Antioxidants 2021, 10(11), 1771; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10111771 - 05 Nov 2021
Cited by 6 | Viewed by 2238
Abstract
Spondias species have been used in traditional medicine for different human ailments. In this study, the effect of different solvents (ethyl acetate, methanol, and water) and extraction methods (infusion, maceration, and Soxhlet extraction) on the enzyme inhibitory activity against acetylcholinesterase, butyrylcholinesterase, tyrosinase, α-amylase, [...] Read more.
Spondias species have been used in traditional medicine for different human ailments. In this study, the effect of different solvents (ethyl acetate, methanol, and water) and extraction methods (infusion, maceration, and Soxhlet extraction) on the enzyme inhibitory activity against acetylcholinesterase, butyrylcholinesterase, tyrosinase, α-amylase, α-glucosidase, and antioxidant properties of S. mombin and S. dulcis leaves and stem bark were evaluated. Ultra-high-performance liquid chromatography–high resolution mass spectrometry (UHPLC-HRMS) yield in the identification and/or annotation of 98 compounds showing that the main secondary metabolites of the plant are gallic and ellagic acids and their derivatives, ellagitannins, hydroxybenzoic, hydroxycinnamic, acylquinic acids and flavonols, flavanones, and flavanonols. The leaves infusion of both Spondias species showed highest inhibition against acetylcholinesterase (AChE) (10.10 and 10.45 mg galantamine equivalent (GALAE)/g, for S. dulcis and S. mombin, respectively). The ethyl acetate extracts of the stem bark of S. mombin and S. dulcis actively inhibited α-glucosidase. Methanolic extracts of the leaves and stem bark exhibited highest tyrosinase inhibitory action. Antioxidant activity and higher levels of phenolics were observed for the methanolic extracts of Spondias. The results suggested that the Spondias species could be considered as natural phyto-therapeutic agents in medicinal and cosmeceutical applications. Full article
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17 pages, 11792 KiB  
Article
Albumin from Erythrina edulis (Pajuro) as a Promising Source of Multifunctional Peptides
by Cleni Palma-Albino, Arturo Intiquilla, Karim Jiménez-Aliaga, Nathaly Rodríguez-Arana, Estela Solano, Eduardo Flores, Amparo Iris Zavaleta, Víctor Izaguirre and Blanca Hernández-Ledesma
Antioxidants 2021, 10(11), 1722; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10111722 - 28 Oct 2021
Cited by 6 | Viewed by 2855
Abstract
Multifunctional peptides, capable of acting on different body systems through multiple mechanisms of action, offer many advantages over monofunctional peptides, including lower adverse side effects and costs. Erythrina edulis (pajuro) is a legume with a large number of high-quality proteins, of which their [...] Read more.
Multifunctional peptides, capable of acting on different body systems through multiple mechanisms of action, offer many advantages over monofunctional peptides, including lower adverse side effects and costs. Erythrina edulis (pajuro) is a legume with a large number of high-quality proteins, of which their potential as a source of antioxidant peptides has been recently reported. In this study, the behavior of these proteins under a sequential enzymatic hydrolysis with digestive and microbial enzymes was investigated by evaluating the multi-functionality of the hydrolyzates. The albumin hydrolyzates obtained after the action of pepsin, pancreatin, and Alcalase showed antioxidant, angiotensin-converting enzyme (ACE), α-amylase, α-glucosidase, and dipeptidyl peptidase (DPP)-IV inhibitory activities. The radical scavenging properties of the hydrolyzate could be responsible for the potent protective effects observed in FeSO4-induced neuroblastoma cells. The findings support the role of pajuro protein as an ingredient of functional foods or nutraceuticals for health promotion and the prevention of oxidative stress, hypertension, and metabolic alteration-associated chronic diseases. Full article
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17 pages, 894 KiB  
Article
Phenolic Analysis and In Vitro Biological Activity of Red Wine, Pomace and Grape Seeds Oil Derived from Vitis vinifera L. cv. Montepulciano d’Abruzzo
by Adriano Mollica, Giuseppe Scioli, Alice Della Valle, Angelo Cichelli, Ettore Novellino, Marta Bauer, Wojciech Kamysz, Eulogio J. Llorent-Martínez, Maria Luisa Fernández-de Córdova, R. Castillo-López, Gunes Ak, Gokhan Zengin, Stefano Pieretti and Azzurra Stefanucci
Antioxidants 2021, 10(11), 1704; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10111704 - 27 Oct 2021
Cited by 51 | Viewed by 3704
Abstract
Grape pomace is commonly considered a waste product of monovarietal red wine production. Methods: HPLC-DAD analysis was performed to determine the polyphenol and flavonoid contents of all the extracts obtained from Montepulciano d’Abruzzo red wine and grape skins whereas, GC-MS was applied to [...] Read more.
Grape pomace is commonly considered a waste product of monovarietal red wine production. Methods: HPLC-DAD analysis was performed to determine the polyphenol and flavonoid contents of all the extracts obtained from Montepulciano d’Abruzzo red wine and grape skins whereas, GC-MS was applied to the determination of fatty acid composition in grape seeds oil. Biological characterization involves antioxidant and antimicrobial assays for all the extracts and seeds oil; Their ability to inhibit α-glucosidase, α-amylase, α-tyrosinase, and ChE enzymes was also detected, together with anti-inflammatory activity on wine, grape skin extracts, and seeds oil by lipoxygenase (5-LOX) and LPS-stimulated macrophage release assays. Data indicate significative polyphenols content (199.31 ± 7.21 mgGAE/g), antioxidant (CUPRAC assay (1036.98 mgTE/g)), enzymatic inhibition (α-tyrosinase: 151.30 ± 1.20 mgKAE/g) and anti-inflammatory activities for wine-organic extract 2, while the antimicrobial activity of grape skin decoction is higher than those reported by wine extracts on three bacterial strains. Interestingly only dealcoholized wine and wine-aqueous extract exerts inhibitory effects on α-glucosidase (20.62 ± 0.23 mmolACAE/g and 19.81 ± 0.03 mmolACAE/g, respectively), while seeds oil is rich in oleic and linoleic acids. These results confirm the strong antioxidant properties of Montepulciano d’Abruzzo grape pomace, suggesting the potential use of this waste product as functional food supplements in the human diet and in cosmeceutics. Full article
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21 pages, 5303 KiB  
Article
LC-MS Based Analysis and Biological Properties of Pseudocedrela kotschyi (Schweinf.) Harms Extracts: A Valuable Source of Antioxidant, Antifungal, and Antibacterial Compounds
by Kouadio Ibrahime Sinan, Stefano Dall’Acqua, Irene Ferrarese, Adriano Mollica, Azzurra Stefanucci, Jasmina Glamočlija, Marina Sokovic, Marija Nenadić, Abdurrahman Aktumsek and Gokhan Zengin
Antioxidants 2021, 10(10), 1570; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10101570 - 02 Oct 2021
Cited by 20 | Viewed by 2336
Abstract
The impact of two extraction solvents on the phenolic composition, antioxidant, and enzymes inhibitory and antimicrobial activities of two parts (leaves and stem bark) of P. kotschyi was studied. Two different LC-DAD-MSn approaches were used to identify and quantify the bioactive compounds [...] Read more.
The impact of two extraction solvents on the phenolic composition, antioxidant, and enzymes inhibitory and antimicrobial activities of two parts (leaves and stem bark) of P. kotschyi was studied. Two different LC-DAD-MSn approaches were used to identify and quantify the bioactive compounds in the different extracts. A total of thirty-two compounds were quantified, being the procyanidin the most abundant in stem bark while catechin and flavonoids are most abundant in leaves. Overall, the stem bark extraction using methanol showed higher amounts of total phenolic (131.83 ± 1.81 mg GAE/g) and flavanol (14.14 ± 0.11 mg CE/g) while the leaves extraction using water exhibited stronger levels of total flavonoid (44.95 ± 0.38 mg RE/g) and phenolic acid (63.58 ± 2.00 mg CAE/g). As regards the antioxidant assays, methanol stem bark extracts were characterized by the highest antioxidant activities (DPPH: 1.94 ± 0.01 mmol TE/g, ABTS: 3.31 ± 0.01 mmol TE/g, FRAP: 2.86 ± 0.02 mmol TE/g, CUPRAC: 5.09 ± 0.08 mmol TE/g, phosphomolybdenum: 5.16 ± 0.23 mmol TE/g and metal chelating: 17.12 ± 0.46 mg EDTAE/g). In addition, the methanolic extracts of stem bark had highest impact on acetylcholinesterase (2.54 mg GALAE/g), butyrylcholinesterase (5.48 mg GALAE/g). In contrast, the methanolic extracts of leaves was potent against tyrosinase (77.39 ± 0.21 mg KAE/g) and α-glucosidase (0.97 ± 0.01 mmol ACAE/g), while a higher anti-α–amylase (0.97 ± 0.01 mmol ACAE/g) was observed for water extracts of the same part. All of the tested extracts showed inhibitory effects on elastase, except methanolic leaves extracts. Additionally, the extracts exhibited appreciable antifungal toward A. ochraceus, A. fumigatus, P. ochrochloron, T. viride, and P. funiculosum and promising antibacterial activity against M. flavus, S. aureus, L. monocytogenes, E. coli, P. aeruginosa, E. cloacae, and S. typhimurium. Taken together, the outcomes demonstrated P. kotschyi as a novel source of bioactive molecules of interest with an evident therapeutic value. Full article
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22 pages, 4475 KiB  
Article
Noble 3,4-Seco-triterpenoid Glycosides from the Fruits of Acanthopanax sessiliflorus and Their Anti-Neuroinflammatory Effects
by Bo-Ram Choi, Hyoung-Geun Kim, Wonmin Ko, Linsha Dong, Dahye Yoon, Seon Min Oh, Young-Seob Lee, Dong-Sung Lee, Nam-In Baek and Dae Young Lee
Antioxidants 2021, 10(9), 1334; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10091334 - 24 Aug 2021
Cited by 8 | Viewed by 2249
Abstract
Acanthopanax sessiliflorus (Araliaceae) have been reported to exhibit many pharmacological activities. Our preliminary study suggested that A. sessiliflorus fruits include many bioactive 3,4-seco-triterpenoids. A. sessiliflorus fruits were extracted in aqueous EtOH and fractionated into EtOAc, n-BuOH, and H2O fractions. Repeated [...] Read more.
Acanthopanax sessiliflorus (Araliaceae) have been reported to exhibit many pharmacological activities. Our preliminary study suggested that A. sessiliflorus fruits include many bioactive 3,4-seco-triterpenoids. A. sessiliflorus fruits were extracted in aqueous EtOH and fractionated into EtOAc, n-BuOH, and H2O fractions. Repeated column chromatographies for the organic fractions led to the isolation of 3,4-seco-triterpenoid glycosides, including new compounds. Ultra-high-performance liquid chromatography (UPLC) mass spectrometry (MS) systems were used for quantitation and quantification. BV2 and RAW264.7 cells were induced by LPS, and the levels of pro-inflammatory cytokines and mediators and their underlying mechanisms were measured by ELISA and Western blotting. NMR, IR, and HR-MS analyses revealed the chemical structures of the nine noble 3,4-seco-triterpenoid glycosides, acanthosessilioside G–O, and two known ones. The amounts of the compounds were 0.01–2.806 mg/g, respectively. Acanthosessilioside K, L, and M were the most effective in inhibiting NO, PGE2, TNF-α, IL-1β, and IL-6 production and reducing iNOS and COX-2 expression. In addition, it had inhibitory effects on the LPS-induced p38 and ERK MAPK phosphorylation in both BV2 and RAW264.7 cells. Nine noble 3,4-seco-triterpenoid glycosides were isolated from A. sessiliflorus fruits, and acanthosessilioside K, L, and M showed high anti-inflammatory and anti-neuroinflammatory effects. Full article
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15 pages, 2047 KiB  
Article
Lupinus angustifolius Protein Hydrolysates Reduce Abdominal Adiposity and Ameliorate Metabolic Associated Fatty Liver Disease (MAFLD) in Western Diet Fed-ApoE−/− Mice
by Guillermo Santos-Sánchez, Ivan Cruz-Chamorro, Ana Isabel Álvarez-Ríos, José María Fernández-Santos, María Victoria Vázquez-Román, Beatriz Rodríguez-Ortiz, Nuria Álvarez-Sánchez, Ana Isabel Álvarez-López, María del Carmen Millán-Linares, Francisco Millán, Justo Pedroche, María Soledad Fernández-Pachón, Patricia Judith Lardone, Juan Miguel Guerrero, Ignacio Bejarano and Antonio Carrillo-Vico
Antioxidants 2021, 10(8), 1222; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10081222 - 29 Jul 2021
Cited by 16 | Viewed by 2901
Abstract
Metabolic-associated fatty liver disease (MAFLD) is the most important cause of liver disease worldwide. It is characterized by the accumulation of fat in the liver and is closely associated with abdominal obesity. In addition, oxidative stress and inflammation are significant features involved in [...] Read more.
Metabolic-associated fatty liver disease (MAFLD) is the most important cause of liver disease worldwide. It is characterized by the accumulation of fat in the liver and is closely associated with abdominal obesity. In addition, oxidative stress and inflammation are significant features involved in MAFLD. Recently, our group demonstrated that lupin protein hydrolysates (LPHs) had lipid lowering, antioxidant, and anti-inflammatory effects. Sixty male mice fed with a Western diet were intragastrically treated with LPHs (or vehicle) for 12 weeks. Liver and adipose tissue lipid accumulation and hepatic inflammatory and oxidant status were evaluated. A significant decrease in steatosis was observed in LPHs-treated mice, which presented a decreased gene expression of CD36 and LDL-R, crucial markers in MAFLD. In addition, LPHs increased the hepatic total antioxidant capacity and reduced the hepatic inflammatory status. Moreover, LPHs-treated mice showed a significant reduction in abdominal adiposity. This is the first study to show that the supplementation with LPHs markedly ameliorates the generation of the steatotic liver caused by the intake of a Western diet and reduces abdominal obesity in ApoE−/− mice. Future clinical trials should shed light on the effects of LPHs on MAFLD. Full article
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15 pages, 4523 KiB  
Article
Hidrox® and Chronic Cystitis: Biochemical Evaluation of Inflammation, Oxidative Stress, and Pain
by Ramona D’Amico, Angela Trovato Salinaro, Marika Cordaro, Roberta Fusco, Daniela Impellizzeri, Livia Interdonato, Maria Scuto, Maria Laura Ontario, Roberto Crea, Rosalba Siracusa, Salvatore Cuzzocrea, Rosanna Di Paola and Vittorio Calabrese
Antioxidants 2021, 10(7), 1046; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10071046 - 29 Jun 2021
Cited by 17 | Viewed by 3353
Abstract
Interstitial cystitis/painful bladder syndrome (IC/PBS) is a chronic bladder condition characterized by frequent urination, inflammation, oxidative stress, and pain. The aim of the study was to evaluate the anti-inflammatory and antioxidant effects of an oral administration of Hidrox® (10 mg/kg) in the [...] Read more.
Interstitial cystitis/painful bladder syndrome (IC/PBS) is a chronic bladder condition characterized by frequent urination, inflammation, oxidative stress, and pain. The aim of the study was to evaluate the anti-inflammatory and antioxidant effects of an oral administration of Hidrox® (10 mg/kg) in the bladder and spinal cord in a rodent model of IC/BPS. The chronic animal model of cystitis was induced by repeated intraperitoneal injections of cyclophosphamide (CYP) for five consecutive days. Treatment with Hidrox® began on the third day of the CYP injection and continued until the 10th day. CYP administration caused macroscopic and histological bladder changes, inflammatory infiltrates, increased mast cell numbers, oxidative stress, decreased expression of the tight endothelial junction (e.g., zonula occludens-1 (ZO-1) and occludin), and bladder pain. Treatment with Hidrox® was able to improve CYP-induced inflammation and oxidative stress via the nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase 1 (HO-1) pathway. It was also able to reduce bladder pain which was aggravated by the activation of neuroinflammation in the central nervous system. In particular, Hidrox® reduced the brain-derived neurotrophic factor (BDNF), as well as the activation of astrocytes and microglia, consequently reducing mechanical allodynia. These results indicate that nutritional consumption of Hidrox® can be considered as a new therapeutic approach for human cystitis, increasing the conceivable potential of a significant improvement in the quality of life associated with a lowering of symptom intensity in patients with IC/BPS. Full article
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18 pages, 3297 KiB  
Article
Salvigenin, a Trimethoxylated Flavone from Achillea Wilhelmsii C. Koch, Exerts Combined Lipid-Lowering and Mitochondrial Stimulatory Effects
by Elena Serino, Azam Chahardoli, Nadia Badolati, Carmina Sirignano, Fereshteh Jalilian, Mahdi Mojarrab, Zahra Farhangi, Daniela Rigano, Mariano Stornaiuolo, Yalda Shokoohinia and Orazio Taglialatela-Scafati
Antioxidants 2021, 10(7), 1042; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10071042 - 29 Jun 2021
Cited by 11 | Viewed by 3381
Abstract
Phytochemical analysis of the Iranian plant Achillea wilhelmsii led to the isolation of 17 pure secondary metabolites belonging to the classes of sesquiterpenoids and phenolics. Two of these compounds, named wilhemsin (7) and wilhelmsolide (9), are new sesquiterpenoids, and [...] Read more.
Phytochemical analysis of the Iranian plant Achillea wilhelmsii led to the isolation of 17 pure secondary metabolites belonging to the classes of sesquiterpenoids and phenolics. Two of these compounds, named wilhemsin (7) and wilhelmsolide (9), are new sesquiterpenoids, and the first shows undescribed structural features. Their structures were elucidated through extensive spectroscopic analysis, mainly based on 1D and 2D NMR, and chemical derivatization. Starting from plant traditional use and previous reports on the activity of the plant extracts, all the pure compounds were evaluated on endpoints related to the treatment of metabolic syndrome. The sesquiterpene hanphyllin (8) showed a selective cholesterol-lowering activity (−12.7% at 30 µM), santoflavone (13) stimulated glucose uptake via the GLUT transporter (+16.2% at 30 µM), while the trimethoxylated flavone salvigenin (14) showed a dual activity in decreasing lipid levels (−22.5% palmitic acid biosynthesis at 30 µM) and stimulating mitochondrial functionality (+15.4% at 30 µM). This study further confirms that, in addition to the antioxidants vitexin, isovitexin, and isoschaftoside, A. wilhelmsii extracts contain molecules that can act at different levels on the metabolic syndrome symptoms. Full article
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17 pages, 3579 KiB  
Article
Cardamonin Attenuates Inflammation and Oxidative Stress in Interleukin-1β-Stimulated Osteoarthritis Chondrocyte through the Nrf2 Pathway
by Yi-Jen Peng, Jeng-Wei Lu, Chian-Her Lee, Herng-Sheng Lee, You-Hsiang Chu, Yi-Jung Ho, Feng-Cheng Liu, Chun-Jung Huang, Chia-Chun Wu and Chih-Chien Wang
Antioxidants 2021, 10(6), 862; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10060862 - 27 May 2021
Cited by 27 | Viewed by 3426
Abstract
Osteoarthritis (OA) is a chronic degenerative joint disease characterized by the deterioration of articular cartilage. The progression of OA leads to an increase in inflammatory mediators in the joints, thereby promoting the destruction of the cartilage matrix. Recent studies have reported on the [...] Read more.
Osteoarthritis (OA) is a chronic degenerative joint disease characterized by the deterioration of articular cartilage. The progression of OA leads to an increase in inflammatory mediators in the joints, thereby promoting the destruction of the cartilage matrix. Recent studies have reported on the anti-inflammatory and antioxidant properties of cardamonin, which also appears to interact with cellular targets, such as nuclear erythroid 2-related factor 2 (Nrf2), extracellular signal-regulated kinase (ERK), and mammalian target of rapamycin (mTOR) during the progression of tumors. To date, few studies have investigated the effects of cardamonin on chondrocyte inflammation. In the current study, we determined that treating interleukin-1 beta (IL-1β-stimulated chondrocyte cells) with cardamonin significantly reduced the release of nitric oxide (NO) and prostaglandin E2 (PGE2) and significantly inhibited the expression of pro-inflammatory proteins, including inducible nitric oxide synthase (iNOS) and cyclooxygenase 2 (COX2). Cardamonin was also shown to: (1) inhibit the activation and production of matrix metalloproteinases (MMPs), (2) suppress the nuclear factor-κB (NF-κB) signaling pathway, (3) suppress the expression of toll-like receptor proteins, (4) activate the Nrf2 signaling pathway, and (5) increase the levels of antioxidant proteins heme oxygenase-1 (HO-1) and NAD(P)H:quinone oxidoreductase 1 (NQO1). The increase in antioxidant proteins led to corresponding antioxidant effects (which were abolished by Nrf2 siRNA). Our findings identify cardamonin as a candidate Nrf2 activator for the treatment and prevention of OA related to inflammation and oxidative stress. Full article
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26 pages, 51158 KiB  
Article
The Antioxidant Carrichtera annua DC. Ethanolic Extract Counteracts Cisplatin Triggered Hepatic and Renal Toxicities
by Enas E. Eltamany, Sameh S. Elhady, Mohamed S. Nafie, Haidy A. Ahmed, Dina M. Abo-Elmatty, Safwat A. Ahmed, Jihan M. Badr and Asmaa R. Abdel-Hamed
Antioxidants 2021, 10(6), 825; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10060825 - 21 May 2021
Cited by 11 | Viewed by 2884
Abstract
Cisplatin is a powerful anti-neoplastic drug that displays multi-organ toxicity, especially to the liver and kidneys. Consumption of phytomedicines is a promising strategy to overcome the side effects of chemotherapy. Carrichtera annua extract proved to possess potent antioxidant activity. Its protective potential against [...] Read more.
Cisplatin is a powerful anti-neoplastic drug that displays multi-organ toxicity, especially to the liver and kidneys. Consumption of phytomedicines is a promising strategy to overcome the side effects of chemotherapy. Carrichtera annua extract proved to possess potent antioxidant activity. Its protective potential against cisplatin-induced hepato–nephrotoxicity was scrutinized. Moreover, a phytochemical study was conducted on C. annua ethyl acetate fraction which led to the isolation of five known phenolic compounds. Structure determination was achieved utilizing 1H- and 13C-NMR spectral analyses. The isolated phytochemicals were trans-ferulic acid (1), kaempferol (2), p-coumaric acid (3), luteolin (4) and quercetin (5). Regarding our biological study, C. annua has improved liver and kidney deteriorated functions caused by cisplatin administration and attenuated the histopathological injury in their tissues. Serum levels of ALT, AST, blood urea nitrogen and creatinine were significantly decreased. C. annua has modulated the oxidative stress mediated by cisplatin as it lowered MDA levels while enhanced reduced-GSH concentrations. More importantly, the plant has alleviated cisplatin triggered inflammation, apoptosis via reduction of INFγ, IL-1β and caspase-3 production. Moreover, mitochondrial injury has been ameliorated as remarkable increase of mtDNA was noted. Furthermore, the MTT assay proved the combination of cisplatin—C. annua extract led to growth inhibition of MCF-7 cells in a notable additive way. Additionally, we have investigated the binding affinity of C. annua constituents with caspase-3 and IFN-γ proteins using molecular simulation. All the isolated compounds exhibited good binding affinities toward the target proteins where quercetin possessed the most auspicious caspase-3 and IFN-γ inhibition activities. Our results put forward that C. annua is a promising candidate to counteract chemotherapy side effects and the observed activity could be attributed to the synergism between its phytochemicals. Full article
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25 pages, 3948 KiB  
Article
Enhanced Recovery of Phenolic and Tocopherolic Compounds from Walnut (Juglans Regia L.) Male Flowers Based on Process Optimization of Ultrasonic Assisted-Extraction: Phytochemical Profile and Biological Activities
by Anca Pop, Ionel Fizeșan, Laurian Vlase, Marius Emil Rusu, Julien Cherfan, Mihai Babota, Ana-Maria Gheldiu, Ioan Tomuta and Daniela-Saveta Popa
Antioxidants 2021, 10(4), 607; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10040607 - 15 Apr 2021
Cited by 34 | Viewed by 3129
Abstract
The extraction of bioactive compounds present in walnut (Juglans regia L.) male flowers (WMFs) was performed based on an experimental design using ultrasonic-assisted extraction. Solvent nature, extraction time, and water content were selected as experimental variables, and phenolic, flavonoidic, and condensed tannins [...] Read more.
The extraction of bioactive compounds present in walnut (Juglans regia L.) male flowers (WMFs) was performed based on an experimental design using ultrasonic-assisted extraction. Solvent nature, extraction time, and water content were selected as experimental variables, and phenolic, flavonoidic, and condensed tannins contents and antioxidant properties were evaluated. Acetone was the solvent with the highest extraction performance, with the extracts obtained using this solvent displaying an increased concentration of bioactive compounds and increased antioxidant activities. For several extracts with high bioactive content, individual polyphenolic and tocopherolic compounds were evaluated by means of LC-MS and LC-MS/MS. The best extraction conditions for polyphenolic (2.86 mg gallic acid equivalents/g WMF) and tocopherolic compounds (29.4 µg/g WMF) were acetone with 40% water content (N20) and acetone with 20% water content (N15), respectively. Although the total tocopherol concentrations were lower than in other Juglans regia parts, most of the total tocopherol quantity was provided by the highly biologically active δ-tocopherol (84%). Significant quantities of quercetin (101.9 µg/g), hyperoside (2662.9 µg/g), quercitrin (405.7 µg/g), and isoquercitrin (1293.7 µg/g) were determined in WMF (N20). Both extracts inhibited the enzymatic activity of α-glucosidase and tyrosinase; however, an increased inhibition was observed for N20, the extract with the higher polyphenolic content. Conversely, N15 had higher anticancerous activity on the cell lines used, with a moderate selectivity towards the cancerous phenotype being observed for both extracts. At non-cytotoxic concentrations, both extracts displayed good antioxidant activities in cellular cultures, decreasing basal and H2O2-induced oxidative stress. This is the first characterization of both hydrophilic and lipophilic phytochemicals in WMF extracts. The outcomes of our study reveal that walnut male flowers have strong biological activities, thus justifying further research to demonstrate their usefulness in the food, pharmaceutical, and/or cosmetic industries. Full article
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15 pages, 3578 KiB  
Article
Efficacy of Alpinumisoflavone Isolated from Maclura tricuspidata Fruit in Tumor Necrosis Factor-α-Induced Damage of Human Dermal Fibroblasts
by Sullim Lee, Giang Do Hoang, Daeyoung Kim, Ho Sueb Song, Sungyoul Choi, Dongho Lee and Ki Sung Kang
Antioxidants 2021, 10(4), 514; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10040514 - 25 Mar 2021
Cited by 8 | Viewed by 2775
Abstract
The skin is an important organ in the human body that protects the body from environmentally hazardous substances. Reactive oxygen species (ROS) cause inflammatory reactions and degradation of the extracellular matrix leading to skin aging and various cutaneous lesions. This study evaluated the [...] Read more.
The skin is an important organ in the human body that protects the body from environmentally hazardous substances. Reactive oxygen species (ROS) cause inflammatory reactions and degradation of the extracellular matrix leading to skin aging and various cutaneous lesions. This study evaluated the potential of isoflavones isolated from Maclura tricuspidata fruit to prevent TNF-α-induced skin inflammation in normal human dermal fibroblasts (HDFs). It focused on alpinumisoflavone (AIF) that suppressed the accumulation of ROS and nitric oxide (NO) in tumor necrosis factor-alpha (TNF-α)-treated HDFs. AIF inhibited the TNF-α-induced increase in matrix metalloproteinase-1, decreased procollagen I α1, and suppressed pro-inflammatory mediators and pro-inflammatory cytokines, including NO synthase, cyclooxygenase-2, interleukin (IL)-1β, IL-6, and IL-8 that trigger inflammatory responses. AIF inhibited nuclear factor-κB and activating protein 1 mitogen-activated protein kinases that were increased by TNF-α stimulation. These results suggest that AIF may protect skin from aging and various cutaneous lesions. Full article
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14 pages, 3272 KiB  
Article
Synthesis of Short-Chain-Fatty-Acid Resveratrol Esters and Their Antioxidant Properties
by You-Lin Tain, Sam K. C. Chang, Jin-Xian Liao, Yu-Wei Chen, Hung-Tse Huang, Yu-Lun Li and Chih-Yao Hou
Antioxidants 2021, 10(3), 420; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox10030420 - 10 Mar 2021
Cited by 24 | Viewed by 4092
Abstract
To expand the applications and enhance the stability and bioactivity of resveratrol (RE), and to simultaneously include the potential health benefits of short chain fatty acids (SCFA) esters of RE were prepared by Steglich reactions with acetic, propionic, and butyric acids, respectively. RE [...] Read more.
To expand the applications and enhance the stability and bioactivity of resveratrol (RE), and to simultaneously include the potential health benefits of short chain fatty acids (SCFA) esters of RE were prepared by Steglich reactions with acetic, propionic, and butyric acids, respectively. RE and the esterified RE-SCFA products (including RAE, RPE, and RBE) were analyzed using nuclear magnetic resonance (NMR), Fourier-transform infrared (FTIR) spectroscopy, thermogravimetric analysis (TGA), differential thermal analysis (DTA), and liquid chromatography–mass spectrometry (LC–MS). The FTIR and 13C NMR spectra of the esterified products included ester-characteristic peaks at 1751 cm−1 and 171 ppm, respectively. Moreover, the peaks in the range of 1700 to 1600 cm−1 in the FTIR spectra of the esterified products indicated that the esterification of RE-SCFA was successful. The TGA results revealed that the RE-SCFA esters decomposed at lower temperatures than RE. The peaks in the LC–MS profiles of the esterified products indicated the formation of mono- and diesters, and the calculated monoester synthesis rates ranged between 45.81 and 49.64%. The RE esters inhibited the Cu2+-induced low-density lipoprotein oxidation reaction, exhibited antioxidant activity in bulk oil, and effectively inhibited the hydroxyl radical-induced DNA scission. Moreover, the RE-SCFA esters had better hydrogen peroxide scavenging activity than RE. Our results are the first in the literature to successfully including short chain fatty acids in the esters of resveratrol, and the products could be used as a functional food ingredient in processed foods or can be used as dietary supplements to promote health. Full article
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Review

Jump to: Research

11 pages, 1398 KiB  
Review
Correlation between Chemical Characterization and Biological Activity: An Urgent Need for Human Studies Using Extra Virgin Olive Oil
by Stefania De Santis, Maria Lisa Clodoveo and Filomena Corbo
Antioxidants 2022, 11(2), 258; https://0-doi-org.brum.beds.ac.uk/10.3390/antiox11020258 - 28 Jan 2022
Cited by 12 | Viewed by 2147
Abstract
Extra virgin olive oil (EVOO) is one of the most important functional foods from the Mediterranean Diet due to its beneficial effect on human health in terms of prevention and/or adjuvant treatment of different pathological conditions. The positive effects linked to EVOO consumption [...] Read more.
Extra virgin olive oil (EVOO) is one of the most important functional foods from the Mediterranean Diet due to its beneficial effect on human health in terms of prevention and/or adjuvant treatment of different pathological conditions. The positive effects linked to EVOO consumption are not only due to its major (monounsaturated fatty acids), but also to its minor components (phenolics), whose roles were greatly re-evaluated in the last years. Notwithstanding the huge number of studies demonstrating the antioxidant, anti-inflammatory and anti-cancer properties of EVOO’s phenolic compounds, only their antioxidant ability was supported by a Health Claim. However, to bear the claim, a specific phenolic composition is needed, thus reinforcing the need to correlate the characterization of the phenolic compounds to their biological activity. In fact, although the chemical characterization of VOO’s phenolic compounds was extensively studied, its correlation with biological effects is only partially investigated; this is especially true for human studies. This review aims to study the correlation between the chemical characterization of EVOO’s phenolics and the biological effects in terms of antioxidant/anti-inflammatory potentials, with a focus on the human studies and the relative concern on getting a specific Health Claim. Full article
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