Antioxidant and Chemopreventive Activity of Natural Compounds

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 March 2022) | Viewed by 50530

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Guest Editor
Department of Biochemistry and Biotechnology, University of Thessaly, Larissa, Greece
Interests: antioxidant activity of plant extracts, plant polyphenols and other natural products; physiological adaptive mechanisms of human organism to oxidative stress conditions; chemopreventive (anticarcinogenic) activity of plant extracts, plant polyphenols and other natural products; anti-angiogenic activity of chemical compounds (natural or synthetic); biochemical and physiological role of human aldehyde dehydrogenases
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Special Issue Information

Dear Colleagues,

An important strategy for fighting cancer is chemoprevention. Chemoprevention is defined as the use of natural or synthetic chemical agents to reverse, suppress or prevent carcinogenic progression to invasive cancer. Many chemopreventive agents are phytochemicals, namely, non-nutritive plant chemicals that have protective or disease preventive properties. Moreover, natural compounds exert chemoprevention through modulation of the cells’ redox status. In several cases, these changes in the cellular redox environment may lead to completely different outcomes. For example, some phytochemicals may act as antioxidants and protect from ROS-induced DNA damage, thus preventing mutagenesis and initiation of carcinogenesis. On the other hand, there are natural compounds inducing apoptosis of cancer cells by acting as pro-oxidants. We invite you to submit your latest research findings or a review article to this Special Issue which will bring together current research focused on critical thinking on the complex and interesting interplay between the antioxidant/pro-oxidant and chemopreventive activity of compounds of natural origin. The natural compounds may be individual substances or chemical mixtures derived from either terrestrial or marine sources.

Dr. Dimitrios Stagos
Guest Editor

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Keywords

  • Antioxidants
  • Chemoprevention
  • Natural compounds
  • Anticancer
  • Oxidative stress

Published Papers (13 papers)

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Research

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17 pages, 5602 KiB  
Article
Phytochemical Characterization of Taxus baccata L. Aril with Emphasis on Evaluation of the Antiproliferative and Pro-Apoptotic Activity of Rhodoxanthin
by Daria-Antonia Dumitraş, Andrea Bunea, Dan Cristian Vodnar, Daniela Hanganu, Emoke Pall, Mihai Cenariu, Adrian Florin Gal and Sanda Andrei
Antioxidants 2022, 11(6), 1039; https://doi.org/10.3390/antiox11061039 - 24 May 2022
Cited by 10 | Viewed by 2395
Abstract
Taxus baccata L., an evergreen tree, was known until recently due to its high concentration of toxic compounds. The purpose of the present study was to focus on the only non-poisonous part, the red arils, which have recently been described as an important [...] Read more.
Taxus baccata L., an evergreen tree, was known until recently due to its high concentration of toxic compounds. The purpose of the present study was to focus on the only non-poisonous part, the red arils, which have recently been described as an important source of various bioactive constituents. To establish total phenolic, flavonoid, and carotenoid content, antioxidant capacity, and cytotoxic properties, two types of extracts were obtained. The chemical profile of the ethanolic extract was evaluated using chromatographic (HPLC-DAD-ESI+) and spectral (UV-Vis) methods, and the antioxidant activity of the ethanolic extract was assessed using DPPH and FRAP assays, yielding moderate results. In the second type of extract (methanol: ethyl acetate: petroleum ether (1:1:1, v/v/v)) we identified three carotenoids using open column chromatography and RP–PAD–HPLC, with rhodoxanthin being the most abundant. Considering the above and mainly because of the lack of information in the literature about this pigment and its biological effects, we decided to further investigate the cytotoxic activity of rhodoxanthin, the main carotenoid presented in aril, and its protective effect against H2O2-induced oxidative stress using two cell lines: human HaCaT keratinocytes and B16F10 murine malignant melanoma. The MTT and Annexin-V Apoptosis assays showed a substantial cytotoxic potential expressed in a dose-dependent manner towards the melanoma cell line, however, no obvious cytotoxic effects on human keratinocytes were noticed. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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18 pages, 2707 KiB  
Article
Flaxseed Ethanol Extracts’ Antitumor, Antioxidant, and Anti-Inflammatory Potential
by Elisabeta Ioana Chera, Raluca Maria Pop, Marcel Pârvu, Olga Sorițău, Ana Uifălean, Florinela Adriana Cătoi, Andra Cecan, Andrada Gabriela Negoescu, Patriciu Achimaș-Cadariu and Alina Elena Pârvu
Antioxidants 2022, 11(5), 892; https://doi.org/10.3390/antiox11050892 - 30 Apr 2022
Cited by 8 | Viewed by 2707
Abstract
The antitumoral, antioxidant, and anti-inflammatory effects of flaxseed ethanol extract was screened. Phytochemical analysis was performed by measuring the total phenolic content and by HPLC-DAD-ESI MS. In vitro antiproliferative activity was appreciated by MMT test of four adenocarcinomas and two normal cell lines. [...] Read more.
The antitumoral, antioxidant, and anti-inflammatory effects of flaxseed ethanol extract was screened. Phytochemical analysis was performed by measuring the total phenolic content and by HPLC-DAD-ESI MS. In vitro antiproliferative activity was appreciated by MMT test of four adenocarcinomas and two normal cell lines. In vitro, antioxidant activity was evaluated by DPPH, FRAP, H2O2, and NO scavenging tests. The in vivo growth inhibitory activity against Ehrlich ascites carcinoma (EAC) in female BALB/c mice was determined using the trypan blue test. In EAC mice serum and ascites total oxidative status, total antioxidant reactivity, oxidative stress index, malondialdehyde, total thiols, total nitrites, 3-nitrotyrosine, and NFkB were measured. The phytochemical analysis found an significant content of phenols, with lignans having the highest concentration. The extract had an significant in vitro antioxidant effect and different inhibitory effects on different cell lines. After treatment of EAC mice with flaxseeds extract, body weight, ascites volume and viable tumour cell count, serum and ascites oxidative stress, and inflammatory markers decreased significantly. The ethanol flaxseeds extract has potential antiproliferative activity against some ovary and endometrial malignant cells and EAC. This effect can be attributed to the phenols content, and its antioxidant and anti-inflammatory activity. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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18 pages, 7691 KiB  
Article
Antioxidant and Anticancer Activities of Synthesized Methylated and Acetylated Derivatives of Natural Bromophenols
by Hui Dong, Li Wang, Meng Guo, Dimitrios Stagos, Antonis Giakountis, Varvara Trachana, Xiukun Lin, Yankai Liu and Ming Liu
Antioxidants 2022, 11(4), 786; https://doi.org/10.3390/antiox11040786 - 15 Apr 2022
Cited by 3 | Viewed by 2101
Abstract
Natural bromophenols are important secondary metabolites in marine algae. Derivatives of these bromophenol are potential candidates for the drug development due to their biological activities, such as antioxidant, anticancer, anti-diabetic and anti-inflammatory activity. In our present study, we have designed and synthesized a [...] Read more.
Natural bromophenols are important secondary metabolites in marine algae. Derivatives of these bromophenol are potential candidates for the drug development due to their biological activities, such as antioxidant, anticancer, anti-diabetic and anti-inflammatory activity. In our present study, we have designed and synthesized a series of new methylated and acetylated bromophenol derivatives from easily available materials using simple operation procedures and evaluated their antioxidant and anticancer activities on the cellular level. The results showed that 2.,3-dibromo-1-(((2-bromo-4,5-dimethoxybenzyl)oxy)methyl)-4,5-dimethoxybenzene (3b-9) and (oxybis(methylene))bis(4-bromo-6-methoxy-3,1-phenylene) diacetate (4b-3) compounds ameliorated H2O2-induced oxidative damage and ROS generation in HaCaT keratinocytes. Compounds 2.,3-dibromo-1-(((2-bromo-4,5-dimethoxybenzyl)oxy)methyl)-4,5-dimethoxybenzene (3b-9) and (oxybis(methylene) )bis(4-bromo-6-methoxy-3,1-phenylene) diacetate (4b-3) also increased the TrxR1 and HO-1 expression while not affecting Nrf2 expression in HaCaT. In addition, compounds (oxybis(methylene)bis(2-bromo-6-methoxy-4,1-phenylene) diacetate (4b-4) inhibited the viability and induced apoptosis of leukemia K562 cells while not affecting the cell cycle distribution. The present work indicated that some of these bromophenol derivatives possess significant antioxidant and anticancer potential, which merits further investigation. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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14 pages, 17808 KiB  
Article
Luteolin Synergistically Enhances Antitumor Activity of Oxaliplatin in Colorectal Carcinoma via AMPK Inhibition
by Chan Ho Jang, Nayoung Moon, Jinkyung Lee, Min Jeong Kwon, Jisun Oh and Jong-Sang Kim
Antioxidants 2022, 11(4), 626; https://doi.org/10.3390/antiox11040626 - 24 Mar 2022
Cited by 15 | Viewed by 2636
Abstract
Luteolin is a naturally-occurring polyphenolic compound that is known to have antioxidative and antitumor activities in vitro. This study aimed to examine the in vivo anticancer efficacy of luteolin in conjunction with oxaliplatin treatment using a colorectal carcinoma xenograft mouse model. HCT116 human [...] Read more.
Luteolin is a naturally-occurring polyphenolic compound that is known to have antioxidative and antitumor activities in vitro. This study aimed to examine the in vivo anticancer efficacy of luteolin in conjunction with oxaliplatin treatment using a colorectal carcinoma xenograft mouse model. HCT116 human colorectal carcinoma cells were subcutaneously implanted into BALB/c nude mice, followed by the intraperitoneal administration of luteolin at a dose of 50 mg/kg body weight (BW)/day with or without oxaliplatin at a dose of 10 mg/kg BW/day three times per week for a total of 3 weeks. The combined luteolin and oxaliplatin treatment resulted in the synergistic suppression of the growth of HCT116 xenograft tumors when compared to treatment with luteolin or oxaliplatin alone. In addition, the combined treatment significantly increased the expression of cleaved PARP and p53 in the xenograft tumors compared with the vehicle control, but only marginally affected the level of heme oxygenase-1 (HO-1). These results indicated that luteolin treatment retarded oxaliplatin-induced tumor growth by facilitating apoptotic cell death and inhibiting HO-1-mediated cytoprotection. Therefore, these findings suggest the synergistic potential of dietary luteolin in conjunction with conventional chemotherapy for the treatment of colorectal cancer. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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10 pages, 2085 KiB  
Article
Medicarpin Increases Antioxidant Genes by Inducing NRF2 Transcriptional Level in HeLa Cells
by Jung-Hwan Kim, Dong-Min Kang, Young-Jin Cho, Jin-Won Hyun and Mi-Jeong Ahn
Antioxidants 2022, 11(2), 421; https://doi.org/10.3390/antiox11020421 - 18 Feb 2022
Cited by 13 | Viewed by 2217
Abstract
The nuclear factor erythroid-derived 2-related factor 2 (NRF2) plays a pivotal role in the regulation of genes involved in oxidative stress and drug detoxification. Therefore, it is important to find NRF2 inducers to protect cells from excessive oxidative damage. Here, we investigated the [...] Read more.
The nuclear factor erythroid-derived 2-related factor 2 (NRF2) plays a pivotal role in the regulation of genes involved in oxidative stress and drug detoxification. Therefore, it is important to find NRF2 inducers to protect cells from excessive oxidative damage. Here, we investigated the effect of medicarpin isolated from the root of Robinia pseudoacacia L. on the activity of NRF2 in HeLa cells. Medicarpin significantly induced the antioxidant response elements (ARE)-luciferase activity in a concentration-dependent manner. Furthermore, medicarpin not only induced HO-1, GCLC, and NQO1 mRNA by translocating NRF2 to the nucleus but also induced the mRNA level of NRF2. To verify the NRF2 induction mechanism by medicarpin, ~2 kb of NRF2 promoter-luciferase assay was executed. As a result, medicarpin significantly induced NRF2-luciferase activity. Moreover, medicarpin strongly inhibited the ubiquitin-dependent proteasomal degradation of NRF2. Thus, medicarpin might protect cells by promoting the NRF2 transcriptional activity. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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26 pages, 6785 KiB  
Article
Vulnerability of Triple-Negative Breast Cancer to Saponin Formosanin C-Induced Ferroptosis
by Hsin-Chih Chen, Han-Hsuan Tang, Wei-Hsiang Hsu, Shan-Ying Wu, Wen-Hsing Cheng, Bao-Yuan Wang and Chun-Li Su
Antioxidants 2022, 11(2), 298; https://doi.org/10.3390/antiox11020298 - 31 Jan 2022
Cited by 18 | Viewed by 4090
Abstract
Targeting ferritin via autophagy (ferritinophagy) to induce ferroptosis, an iron- and reactive oxygen species (ROS)-dependent cell death, provides novel strategies for cancer therapy. Using a ferroptosis-specific inhibitor and iron chelator, the vulnerability of triple-negative breast cancer (TNBC) MDA-MB-231 cells to ferroptosis was identified [...] Read more.
Targeting ferritin via autophagy (ferritinophagy) to induce ferroptosis, an iron- and reactive oxygen species (ROS)-dependent cell death, provides novel strategies for cancer therapy. Using a ferroptosis-specific inhibitor and iron chelator, the vulnerability of triple-negative breast cancer (TNBC) MDA-MB-231 cells to ferroptosis was identified and compared to that of luminal A MCF-7 cells. Saponin formosanin C (FC) was revealed as a potent ferroptosis inducer characterized by superior induction in cytosolic and lipid ROS formation as well as GPX4 depletion in MDA-MB-231 cells. The FC-induced ferroptosis was paralleled by downregulation of ferroportin and xCT expressions. Immunoprecipitation and electron microscopy demonstrated the involvement of ferritinophagy in FC-treated MDA-MB-231 cells. The association of FC with ferroptosis was strengthened by the results that observed an enriched pathway with differentially expressed genes from FC-treated cells. FC sensitized cisplatin-induced ferroptosis in MDA-MB-231 cells. Through integrated analysis of differentially expressed genes and pathways using the METABRIC patients’ database, we confirmed that autophagy and ferroptosis were discrepant between TNBC and luminal A and that TNBC was hypersensitive to ferroptosis. Our data suggest a therapeutic strategy by ferroptosis against TNBC, an aggressive subtype with a poor prognosis. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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12 pages, 3007 KiB  
Article
Fisetin Protects HaCaT Human Keratinocytes from Fine Particulate Matter (PM2.5)-Induced Oxidative Stress and Apoptosis by Inhibiting the Endoplasmic Reticulum Stress Response
by Ilandarage Menu Neelaka Molagoda, Mirissa Hewage Dumindu Kavinda, Yung Hyun Choi, Hyesook Lee, Chang-Hee Kang, Mi-Hwa Lee, Chang-Min Lee and Gi-Young Kim
Antioxidants 2021, 10(9), 1492; https://doi.org/10.3390/antiox10091492 - 18 Sep 2021
Cited by 12 | Viewed by 3148
Abstract
Fine particulate matter (PM2.5) originates from the combustion of coal and is found in the exhaust of fumes of diesel vehicles. PM2.5 readily penetrates the skin via the aryl hydrocarbon receptor, causing skin senescence, inflammatory skin diseases, DNA damage, and [...] Read more.
Fine particulate matter (PM2.5) originates from the combustion of coal and is found in the exhaust of fumes of diesel vehicles. PM2.5 readily penetrates the skin via the aryl hydrocarbon receptor, causing skin senescence, inflammatory skin diseases, DNA damage, and carcinogenesis. In this study, we investigated whether fisetin, a bioactive flavonoid, prevents PM2.5-induced apoptosis in HaCaT human keratinocytes. The results demonstrated that fisetin significantly downregulated PM2.5-induced apoptosis at concentrations below 10 μM. Fisetin strongly inhibited the production of reactive oxygen species (ROS) and the expression of pro-apoptotic proteins. The PM2.5-induced apoptosis was associated with the induction of the endoplasmic reticulum (ER) stress response, mediated via the protein kinase R-like ER kinase (PERK)–eukaryotic initiation factor 2α (eIF2α)–activating transcription factor 4 (ATF4)–CCAAT-enhancer-binding protein (C/EBP) homologous protein (CHOP) axis. Additionally, the cytosolic Ca2+ levels were markedly increased following exposure to PM2.5. However, fisetin inhibited the expression of ER stress-related proteins, including 78 kDa glucose-regulated protein (GRP78), phospho-eIF2α, ATF4, and CHOP, and reduced the cytosolic Ca2+ levels. These data suggest that fisetin inhibits PM2.5-induced apoptosis by inhibiting the ER stress response and production of ROS. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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12 pages, 2905 KiB  
Article
Bromophenol Bis (2,3,6-Tribromo-4,5-dihydroxybenzyl) Ether Protects HaCaT Skin Cells from Oxidative Damage via Nrf2-Mediated Pathways
by Hui Dong, Mingfei Liu, Li Wang, Yankai Liu, Xuxiu Lu, Dimitrios Stagos, Xiukun Lin and Ming Liu
Antioxidants 2021, 10(9), 1436; https://doi.org/10.3390/antiox10091436 - 9 Sep 2021
Cited by 9 | Viewed by 2327
Abstract
Excessive reactive oxygen species (ROS) promotes the oxidative stress of keratinocytes, eventually causing cell damage. The natural bromophenol bis (2,3,6-tribromo-4,5-dihydroxybenzyl) ether (BTDE) from marine red algae has been reported to have a varied bioactivity; however, its antioxidant effect has yet to be investigated [...] Read more.
Excessive reactive oxygen species (ROS) promotes the oxidative stress of keratinocytes, eventually causing cell damage. The natural bromophenol bis (2,3,6-tribromo-4,5-dihydroxybenzyl) ether (BTDE) from marine red algae has been reported to have a varied bioactivity; however, its antioxidant effect has yet to be investigated systemically. Our present work aimed to explore the antioxidant effect of BTDE both on the molecular and cellular models and also to illustrate the antioxidant mechanisms. Our results showed that BTDE could effectively scavenge ABTS free radicals and protect HaCaT cells from damage induced by H2O2. Mechanism studies in HaCaT cells demonstrated that BTDE attenuated hydrogen peroxide (H2O2)-induced ROS production, reduced the malondialdehyde (MDA) level, decreased the oxidized glutathione (GSSG)/glutathione (GSH) ratio, and increased the antioxidant enzyme superoxide dismutase (SOD). Moreover, BTDE could inhibit the expression of Kelch-like epichlorohydrin-associated protein 1 (Keap1) and increase the expression of both nuclear factor erythroid 2-related factor 2 (Nrf2) and its downstream proteins TrXR1, HO-1, and NQO1. BTDE also activated the upstream signaling pathway of Nrf2 such as AKT pathway, while not activating the ERK or AMPKα pathways. In general, BTDE is a promising antioxidant to protect HaCaT cells against oxidative damage via Nrf2-mediated pathways. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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16 pages, 1510 KiB  
Article
Microalgal Co-Cultivation Prospecting to Modulate Vitamin and Bioactive Compounds Production
by Luigi Pistelli, Angelo Del Mondo, Arianna Smerilli, Federico Corato, Concetta Piscitelli, Paola Pellone, Dora Allegra Carbone, Clementina Sansone and Christophe Brunet
Antioxidants 2021, 10(9), 1360; https://doi.org/10.3390/antiox10091360 - 26 Aug 2021
Cited by 7 | Viewed by 2256
Abstract
Microalgal biotechnology is gaining importance. However, key issues in the pipeline from species selection towards large biomass production still require improvements to maximize the yield and lower the microalgal production costs. This study explores a co-cultivation strategy to improve the bioactive compounds richness [...] Read more.
Microalgal biotechnology is gaining importance. However, key issues in the pipeline from species selection towards large biomass production still require improvements to maximize the yield and lower the microalgal production costs. This study explores a co-cultivation strategy to improve the bioactive compounds richness of the harvested microalgal biomass. Based on their biotechnological potential, two diatoms (Skeletonema marinoi, Cyclotella cryptica) and one eustigmatophyte (Nannochloropsis oceanica) were grown alone or in combination. Concentrations of ten vitamins (A, B1, B2, B6, B12, C, D2, D3, E and H), carotenoids and polyphenols, together with total flavonoids, sterols, lipids, proteins and carbohydrates, were compared. Moreover, antioxidant capacity and chemopreventive potential in terms inhibiting four human tumor-derived and normal cell lines proliferation were evaluated. Co-cultivation can engender biomass with emergent properties regarding bioactivity or bioactive chemical profile, depending on the combined species. The high vitamin content of C. cryptica or N. oceanica further enhanced (until 10% more) when co-cultivated, explaining the two-fold increase of the antioxidant capacity of the combined C. cryptica and N. oceanica biomass. Differently, the chemopreventive activity was valuably enhanced when coupling the two diatoms C. cryptica and S. marinoi. The results obtained in this pilot study promote microalgal co-cultivation as a valuable strategy aiming to boost their application in eco-sustainable biotechnology. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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14 pages, 2736 KiB  
Article
Protective Effects of Fucoxanthin Dampen Pathogen-Associated Molecular Pattern (PAMP) Lipopolysaccharide-Induced Inflammatory Action and Elevated Intraocular Pressure by Activating Nrf2 Signaling and Generating Reactive Oxygen Species
by Shiu-Jau Chen, Tzer-Bin Lin, Hsien-Yu Peng, Cheng-Hsien Lin, An-Sheng Lee, Hsiang-Jui Liu, Chun-Chieh Li and Kuang-Wen Tseng
Antioxidants 2021, 10(7), 1092; https://doi.org/10.3390/antiox10071092 - 7 Jul 2021
Cited by 16 | Viewed by 2747
Abstract
Inflammation and oxidative stress are closely related processes in the pathogenesis of various ocular diseases. Uveitis is a disorder of the uvea and ocular tissues that causes extreme pain, decreases visual acuity, and can eventually lead to blindness. The pharmacological functions of fucoxanthin, [...] Read more.
Inflammation and oxidative stress are closely related processes in the pathogenesis of various ocular diseases. Uveitis is a disorder of the uvea and ocular tissues that causes extreme pain, decreases visual acuity, and can eventually lead to blindness. The pharmacological functions of fucoxanthin, isolated from brown algae, induce a variety of therapeutic effects such as oxidative stress reduction and repression of inflammation reactions. However, the specific anti-inflammatory effects of fucoxanthin on pathogen-associated molecular pattern (PAMP) lipopolysaccharide-induced uveitis have yet to be extensively described. Therefore, the aim of present study was to investigate the anti-inflammatory effects of fucoxanthin on uveitis in rats. The results showed that fucoxanthin effectively enhanced the expression of nuclear factor erythroid 2-related factor 2 (Nrf2) in ocular tissues. Furthermore, fucoxanthin significantly increased the ocular activities of superoxide dismutase and decreased the levels of malondialdehyde stimulated by PAMP-induced uveitis. Ocular hypertension and the levels of inflammatory cells and proinflammatory cytokine tumor necrosis factor-alpha in the aqueous humor were alleviated with fucoxanthin treatment. Consequently, compared to the observed effects in lipopolysaccharide groups, fucoxanthin treatment significantly preserved iris sphincter innervation and pupillary function. Additionally, PAMP-induced corneal endothelial disruption was significantly inhibited by fucoxanthin treatment. Overall, these findings suggest that fucoxanthin may protect against inflammation from PAMP-induced uveitis by promoting the Nrf2 pathway and inhibiting oxidative stress. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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16 pages, 2574 KiB  
Article
LC-ESI/MS-Phytochemical Profiling with Antioxidant, Antibacterial, Antifungal, Antiviral and In Silico Pharmacological Properties of Algerian Asphodelus tenuifolius (Cav.) Organic Extracts
by Ayoub Khalfaoui, Emira Noumi, Soumia Belaabed, Kaïss Aouadi, Bouslama Lamjed, Mohd Adnan, Andrea Defant, Adel Kadri, Mejdi Snoussi, Mushtaq Ahmad Khan and Ines Mancini
Antioxidants 2021, 10(4), 628; https://doi.org/10.3390/antiox10040628 - 20 Apr 2021
Cited by 13 | Viewed by 4019
Abstract
Asphodelus tenuifolius Cav. (A. tenuifolius) is a medicinal plant with a long history of traditional use to treat ailments. In this study, total phenolic and flavonoid content evaluation using LC-ESI/MS analysis and various biological activities (antioxidant, antibacterial, antifungal, antiviral and cytotoxicity) [...] Read more.
Asphodelus tenuifolius Cav. (A. tenuifolius) is a medicinal plant with a long history of traditional use to treat ailments. In this study, total phenolic and flavonoid content evaluation using LC-ESI/MS analysis and various biological activities (antioxidant, antibacterial, antifungal, antiviral and cytotoxicity) of organic extracts from the aerial parts of A. tenuifolius were analyzed. ADME tools were used to predict the potential of the identified compounds from the most potent extract as specific drugs. As shown, LC-ESI/MS results of chloroformic extract allowed the tentative identification of 12 compounds. Chloroformic extract was rich in polyphenols and flavonoids and exhibited the highest antioxidant activity given by DPPH (IC50 = 25 µg/mL) as compared to the BHT standard (11.5 µg/mL) and β-carotene bleaching assays (IC50 = 95.692 µg/mL). Antibacterial activity results showed that chloroformic extract has a highest activity against Gram-positive and -negative bacteria, especially against Salmonella Typhimurium DT104 (IZ = 19.3 mm, MIC = 18.75 mg/mL, MBC = 37.5 mg/mL). The MBC/MIC ratio was evaluated to interpret the activity that was bacteriostatic rather than bactericidal. Conversely, weaker antifungal activity was registered, and no antiviral activity was observed for all extracts against Herpes Simplex Virus type 2 and Coxsakievirus B-3 viruses. Cytotoxic activity on VERO cell line results revealed that butanol extract was not toxic, with CC50 value of 1430 µg/mL, while chloroformic extract showed moderate cytotoxicity. Additionally, in silico studies performed proved promising pharmacokinetic and drug-likeness properties of the main compounds from the chloroformic extract. Taken together, this work highlights the potent bioactivity and acceptable drug-likeness of this plant, which supports its further preclinical development. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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14 pages, 3883 KiB  
Article
Physalis peruviana-Derived Physapruin A (PHA) Inhibits Breast Cancer Cell Proliferation and Induces Oxidative-Stress-Mediated Apoptosis and DNA Damage
by Tzu-Jung Yu, Yuan-Bin Cheng, Li-Ching Lin, Yi-Hong Tsai, Bo-Yi Yao, Jen-Yang Tang, Fang-Rong Chang, Chia-Hung Yen, Fu Ou-Yang and Hsueh-Wei Chang
Antioxidants 2021, 10(3), 393; https://doi.org/10.3390/antiox10030393 - 5 Mar 2021
Cited by 20 | Viewed by 3190
Abstract
Breast cancer expresses clinically heterogeneous characteristics and requires multipurpose drug development for curing the different tumor subtypes. Many withanolides have been isolated from Physalis species showing anticancer effects, but the anticancer function of physapruin A (PHA) has rarely been investigated. In this study, [...] Read more.
Breast cancer expresses clinically heterogeneous characteristics and requires multipurpose drug development for curing the different tumor subtypes. Many withanolides have been isolated from Physalis species showing anticancer effects, but the anticancer function of physapruin A (PHA) has rarely been investigated. In this study, the anticancer properties of PHA in breast cancer cells were examined by concentration and time-course experiments. In terms of cellular ATP content, PHA inhibited the proliferation of three kinds of breast cancer cells: MCF7 (estrogen receptor (ER)+, progesterone receptor (PR)+/−, human epidermal growth factor receptor 2 (HER2)−), SKBR3 (ER−/PR−/HER2+), and MDA-MB-231 (triple-negative). Moreover, PHA induced G2/M arrest in MCF7 and MDA-MB-231 cells. In terms of flow cytometry, PHA induced the generation of reactive oxygen species (ROS), the generation of mitochondrial superoxide, mitochondrial membrane potential depletion, and γH2AX-detected DNA damage in breast cancer MCF7 and MDA-MB-231 cells, which were suppressed by the ROS inhibitor N-acetylcysteine (NAC). In terms of flow cytometry and Western blotting, PHA induced apoptotic expression (annexin V, and intrinsic and extrinsic apoptotic signaling), which was suppressed by NAC and an apoptosis inhibitor (Z-VAD-FMK), in breast cancer cells. Therefore, PHA is a potential anti-breast-cancer natural product that modulates the oxidative-stress response, cell-cycle disturbance, apoptosis, and γH2AX-detected DNA damage. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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23 pages, 69553 KiB  
Review
Role of Phytochemicals in Cancer Chemoprevention: Insights
by Blassan P. George, Rahul Chandran and Heidi Abrahamse
Antioxidants 2021, 10(9), 1455; https://doi.org/10.3390/antiox10091455 - 14 Sep 2021
Cited by 109 | Viewed by 14773
Abstract
Cancer is a condition where the body cells multiply in an uncontrollable manner. Chemoprevention of cancer is a broad term that describes the involvement of external agents to slow down or suppress cancer growth. Synthetic and natural compounds are found useful in cancer [...] Read more.
Cancer is a condition where the body cells multiply in an uncontrollable manner. Chemoprevention of cancer is a broad term that describes the involvement of external agents to slow down or suppress cancer growth. Synthetic and natural compounds are found useful in cancer chemoprevention. The occurrence of global cancer type varies, depending on many factors such as environmental, lifestyle, genetic etc. Cancer is often preventable in developed countries with advanced treatment modalities, whereas it is a painful death sentence in developing and low-income countries due to the lack of modern therapies and awareness. One best practice to identify cancer control measures is to study the origin and risk factors associated with common types. Based on these factors and the health status of patients, stage, and severity of cancer, type of treatment is decided. Even though there are well-established therapies, cancer still stands as one of the major causes of death and a public health burden globally. Research shows that most cancers can be prevented, treated, or the incidence can be delayed. Phytochemicals from various medicinal plants were reported to reduce various risk factors associated with different types of cancer through their chemopreventive role. This review highlights the role of bioactive compounds or natural products from plants in the chemoprevention of cancer. There are many plant based dietary factors involved in the chemoprevention process. The review discusses the process of carcinogenesis and chemoprevention using plants and phytocompounds, with special reference to five major chemopreventive phytocompounds. The article also summarizes the important chemopreventive mechanisms and signaling molecules involved in the process. Since the role of antioxidants in chemoprevention is inevitable, an insight into plant-based antioxidant compounds that fight against this dreadful disease at various stages of carcinogenesis and disease progression is discussed. This will fill the research gap in search of chemopreventive natural compounds and encourage scientists in clinical trials of anticancer agents from plants. Full article
(This article belongs to the Special Issue Antioxidant and Chemopreventive Activity of Natural Compounds)
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