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Bioactive Compounds: From Diet to Therapeutic Use

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (20 October 2022) | Viewed by 36732

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Special Issue Editors

Prof. Dr. Federica Pessina

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Department of Molecular and Developmental Medicine, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy
Interests: the biological effects of natural bioactive compounds; antinflammatory; antioxidant; analgesic and wound healing properties; hypoxia and oxidative stress
Special Issues, Collections and Topics in MDPI journals

Prof. Dr. Antonella Brizzi

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Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy
Interests: organic synthesis of bio-inspired molecules; small libraries of compounds; design and synthesis of new small molecules and/or modification/hybridization of natural compounds
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Bioactive compounds naturally present in foods are substances which help people to maintain their physiological functions and prevent multiple diseases. There are different classifications of biologically active compounds depending on their origin, chemical structure, as well as biological activity, and their influence on human health.

This Special Issue aims to cover aspects on either isolated bioactive or synthesized bioinspired compounds, as well as bioactive derivatives, with applications on cellular functions in physiology and diseases, which could potentially be exploited for the development of pharmaceuticals and nutraceuticals. Contributions to this Issue may be original research or review articles and short communications on any kind of health topic and diseases related to biological targets.

Prof. Dr. Federica Pessina
Prof. Dr. Antonella Brizzi
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

bioactive compounds
health
physiological functions
diseases
natural compounds
antioxidants
diet
topical usage
aging

Published Papers (12 papers)

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12 pages, 678 KiB

Open AccessArticle

Effect of Dietary Geranylgeraniol and Green Tea Polyphenols on Glucose Homeostasis, Bone Turnover Biomarkers, and Bone Microstructure in Obese Mice

by Chwan-Li Shen, Jannette M. Dufour, Jonathan M. Miranda, Gurvinder Kaur, Eunhee Chung, Latha Ramalingam, Naima Moustaid-Moussa and Jay J. Cao

Int. J. Mol. Sci. 2023, 24(2), 979; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24020979 - 04 Jan 2023

Cited by 1 | Viewed by 1887

Abstract

Previously, we demonstrated that the administration of either geranylgeraniol (GGOH) or green tea polyphenols (GTP) improved bone health. This study examined the combined effects of GGOH and GTP on glucose homeostasis in addition to bone remodeling in obese mice. We hypothesized that GGOH and GTP would have an additive or synergistic effect on improving glucose homeostasis and bone remodeling possibly in part via suppression of proinflammatory cytokines. Forty-eight male C57BL/6J mice were assigned to a high-fat diet (control), HFD + 400 mg GGOH/kg diet (GG), HFD + 0.5% GTP water (TP), or HFD + GGOH + GTP (GGTP) diet for 14 weeks. Results demonstrated that GTP supplementation improved glucose tolerance in obese mice. Neither GGOH nor GTP affected pancreas insulin or bone formation procollagen type I intact N-terminal, bone volume at the lumbar vertebrae, or bone parameters at the trabecular bone and cortical bone of the femur. There was an interactive effect for serum bone resorption collagen type 1 cross-linked C-telopeptide concentrations, resulting in no-GGOH and no-GTP groups having the highest values. GGOH increased trabecular number and decreased trabecular separation at the lumbar vertebrae. GTP increased trabecular thickness at lumbar vertebrae. The GG group produced the greatest connectivity density and the lowest structure model index. Only GTP, not GGOH, decreased adipokines concentrations (resistin, leptin, monocyte chemoattractant protein-1, and interleukin-6). In an obese male mouse model, individual GGOH and GTP supplementation improved glucose homeostasis, serum CTX, and trabecular microstructure of LV-4. However, the combined GGOH and GTP supplementation compromises such osteoprotective effects on serum CTX and trabecular bone of obese mice. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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13 pages, 1978 KiB

Open AccessArticle

Cycloartenyl Ferulate Is the Predominant Compound in Brown Rice Conferring Cytoprotective Potential against Oxidative Stress-Induced Cytotoxicity

by Hongyan Wu, Toshiyuki Nakamura, Yingnan Guo, Riho Matsumoto, Shintaro Munemasa, Yoshiyuki Murata and Yoshimasa Nakamura

Int. J. Mol. Sci. 2023, 24(1), 822; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24010822 - 03 Jan 2023

Cited by 2 | Viewed by 4161

Abstract

Since brown rice extract is a rich source of biologically active compounds, the present study is aimed to quantify the major compounds in brown rice and to compare their cytoprotective potential against oxidative stress. The content of the main hydrophobic compounds in brown rice followed the order of cycloartenyl ferulate (CAF) (89.00 ± 8.07 nmol/g) >> α-tocopherol (αT) (19.73 ± 2.28 nmol/g) > γ-tocotrienol (γT3) (18.24 ± 1.41 nmol/g) > α-tocotrienol (αT3) (16.02 ± 1.29 nmol/g) > γ-tocopherol (γT) (3.81 ± 0.40 nmol/g). However, the percent contribution of CAF to the radical scavenging activity of one gram of whole brown rice was similar to those of αT, αT3, and γT3 because of its weaker antioxidant activity. The CAF pretreatment displayed a significant cytoprotective effect on the hydrogen peroxide-induced cytotoxicity from 10 µM, which is lower than the minimal concentrations of αT and γT required for a significant protection. CAF also enhanced the nuclear factor erythroid 2-related factor 2 (Nrf2) nuclear translocation coincided with the enhancement of the heme oxygenase-1 (HO-1) mRNA level. An HO-1 inhibitor, tin protoporphyrin IX (SnPP), significantly impaired the cytoprotection of CAF. The cytoprotective potential of CAF is attributable to its cycloartenyl moiety besides the ferulyl moiety. These results suggested that CAF is the predominant cytoprotector in brown rice against hydrogen peroxide-induced cytotoxicity. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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14 pages, 1656 KiB

Open AccessArticle

Lipoic/Capsaicin-Related Amides: Synthesis and Biological Characterization of New TRPV1 Agonists Endowed with Protective Properties against Oxidative Stress

by Antonella Brizzi, Samuele Maramai, Francesca Aiello, Maria Camilla Baratto, Federico Corelli, Claudia Mugnaini, Marco Paolino, Francesco Scorzelli, Carlo Aldinucci, Luciano De Petrocellis, Cinzia Signorini and Federica Pessina

Int. J. Mol. Sci. 2022, 23(21), 13580; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232113580 - 05 Nov 2022

Cited by 4 | Viewed by 1326

Abstract

α-Lipoic acid is a sulfur-containing nutrient endowed with pleiotropic actions and a safe biological profile selected to replace the unsaturated alkyl acid of capsaicin with the aim of obtaining lipoic amides potentially active as a TRPV1 ligand and with significant antioxidant properties. Thus, nine compounds were obtained in good yields following a simple synthetic procedure and tested for their functional TRPV1 activity and radical-scavenger activity. The safe biological profile together with the protective effect against hypoxia damage as well as the in vitro antioxidant properties were also evaluated. Although less potent than capsaicin, almost all lipoic amides were found to be TRPV1 agonists and, specifically, compound 4, the lipoic analogue of capsaicin, proved to be the best ligand in terms of efficacy and potency. EPR experiments and in vitro biological assays suggested the potential protective role against oxidative stress of the tested compounds and their safe biological profile. Compounds 4, 5 and 9 significantly ameliorated the mitochondrial membrane potential caused by hypoxia condition and decreased F2-isoprostanes, known markers of oxidative stress. Thus, the experimental results encourage further investigation of the therapeutic potential of these lipoic amides. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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12 pages, 1354 KiB

Open AccessArticle

Anti-Leukemic Activity of Brassica-Derived Bioactive Compounds in HL-60 Myeloid Leukemia Cells

by María Ángeles Núñez-Sánchez, María Antonia Martínez-Sánchez, Marina Verdejo-Sánchez, Paula García-Ibáñez, Alba Oliva Bolarín, Bruno Ramos-Molina, Diego A. Moreno and Antonio J. Ruiz-Alcaraz

Int. J. Mol. Sci. 2022, 23(21), 13400; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232113400 - 02 Nov 2022

Cited by 1 | Viewed by 1713

Abstract

Acute myeloid leukemia (AML) is a cancer of the myeloid blood cells mainly treated with chemotherapy for cancer remission, but this non-selective treatment also induces numerous side effects. Investigations with bioactive compounds from plant-derived foods against cancer have increased in the last years because there is an urgent need to search for new anti-leukemic agents possessing higher efficacy and selectivity for AML cells and fewer negative side effects. In this study, we analyzed the anti-leukemic activity of several phytochemicals that are representative of the major classes of compounds present in cruciferous foods (glucosinolates, isothiocyanates, hydroxycinnamic acids, flavonols, and anthocyanins) in the human acute myeloid leukemia cell line HL-60. Our results revealed that among the different Brassica-derived compounds assayed, sulforaphane (SFN) (an aliphatic isothiocyanate) showed the most potent anti-leukemic activity with an IC₅₀ value of 6 µM in dose-response MTT assays after 48 h of treatment. On the other hand, chlorogenic acid (a hydroxycinnamic acid) and cyanidin-3-glucoside (an anthocyanin) also displayed anti-leukemic potential, with IC₅₀ values of 7 µM and 17 µM after 48 h of incubation, respectively. Importantly, these compounds did not show significant cell toxicity in macrophages-like differentiated cells at 10 and 25 µM, indicating that their cytotoxic effects were specific to AML cancer cells. Finally, we found that these three compounds were able to induce the NRF2/KEAP1 signaling pathway in a dose-dependent manner, highlighting SFN as the most potent NRF2 activator. Overall, the present evidence shed light on the potential for using foods and ingredients rich in anticancer bioactive phytochemicals from Brassica spp. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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17 pages, 2503 KiB

Open AccessArticle

Betula alba Bark Extract and Empetrum nigrum Fruit Juice, a Natural Alternative to Niacinamide for Skin Barrier Benefits

by Sandra Smiljanic, Cyril Messaraa, Virginie Lafon-Kolb, Nina Hrapovic, Nahid Amini, Christina Osterlund and Lene Visdal-Johnsen

Int. J. Mol. Sci. 2022, 23(20), 12507; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232012507 - 19 Oct 2022

Cited by 3 | Viewed by 2749

Abstract

The Scandinavian region is home to a unique biome with endemic plant species. The aim of this study was to explore this natural diversity and identify plant extracts providing positive skin barrier effects. Six plant extracts were identified as starting material. Following biochemical screening, two candidates outperformed the rest: Betula alba (BA) and Empetrum nigrum (EN). Quantitative PCR analysis showed that BA and EN upregulated barrier genes, when used individually and in combination. Betula alba increased AQP3 and OCLN protein expression, something niacinamide was incapable of. Additionally, the skin barrier was strengthened, evidenced by inhibition of KLK5 and hyaluronidase and showed strong antioxidant and anti-inflammatory activity through DPPH and COX2 inhibition, respectively. A first split-face clinical study was conducted using the combination of extracts versus placebo. There was a significantly better skin restructuring effect and corneocyte cohesion on the side treated with combined extracts. A second split-face clinical study assessed the combined extracts versus 3% niacinamide. Significant variations in skin hydration and TEWL were observed in favor of the extract treated side. In conclusion, we identified a natural alternative to niacinamide for improving skin barrier health, in Scandinavian plant extracts, which yield strong performance, but at a lower concentration. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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19 pages, 5286 KiB

Open AccessArticle

Comparison of Cytotoxic, Genotoxic, and DNA-Protective Effects of Skyrin on Cancerous vs. Non-Cancerous Human Cells

by Terézia Zajičková, Eva Horváthová, Stanislav Kyzek, Eva Šályová, Eva Túryová, Andrea Ševčovičová and Eliška Gálová

Int. J. Mol. Sci. 2022, 23(10), 5339; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23105339 - 10 May 2022

Cited by 1 | Viewed by 1539

Abstract

Secondary metabolites as a potential source of anticancer therapeutics have been the subject of many studies. Since hypericin, a metabolite isolated from Hypericum perforatum L., shows several biomedical properties applicable in oncology, the aim of our study was to investigate its potential precursor skyrin in terms of genotoxic and DNA-protective effects. These skyrin effects were analyzed by cell-free methods, and cytotoxicity was estimated by an MTT assay and by a trypan blue exclusion test, while the genotoxic/antigenotoxic potential was examined by comet assay using non-cancerous human lymphocytes and the HepG2 cancer cell line. Skyrin did not show DNA-damaging effects but rather exhibited DNA-protectivity using a DNA-topology assay. However, we observed only weak antioxidant and chelating skyrin properties in other cell-free methods. Regarding the cytotoxic activity of skyrin, HepG2 cells were more prone to skyrin-induced death in comparison to human lymphocytes. Skyrin in non-cytotoxic concentrations did not exhibit elevated genotoxicity in both cell types. On the other hand, skyrin displayed moderate DNA-protective effects that were more noticeable in the case of non-cancerous human lymphocytes. The potential genotoxic effects of skyrin were not observed, and its DNA-protective capacity was more prominent in non-cancerous cells. Therefore, skyrin might be a promising agent used in anticancer therapy. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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20 pages, 2445 KiB

Open AccessArticle

RNA-Seq, Bioinformatic Identification of Potential MicroRNA-like Small RNAs in the Edible Mushroom Agaricus bisporus and Experimental Approach for Their Validation

by Francisco R. Marin, Alberto Dávalos, Dylan Kiltschewskij, Maria C. Crespo, Murray Cairns, Eduardo Andrés-León and Cristina Soler-Rivas

Int. J. Mol. Sci. 2022, 23(9), 4923; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23094923 - 28 Apr 2022

Cited by 4 | Viewed by 3144

Abstract

Although genomes from many edible mushrooms are sequenced, studies on fungal micro RNAs (miRNAs) are scarce. Most of the bioinformatic tools are designed for plants or animals, but the processing and expression of fungal miRNAs share similarities and differences with both kingdoms. Moreover, since mushroom species such as Agaricus bisporus (A. bisporus, white button mushroom) are frequently consumed as food, controversial discussions are still evaluating whether their miRNAs might or might not be assimilated, perhaps within extracellular vesicles (i.e., exosomes). Therefore, the A. bisporus RNA-seq was studied in order to identify potential de novo miRNA-like small RNAs (milRNAs) that might allow their later detection in diet. Results pointed to 1 already known and 37 de novo milRNAs. Three milRNAs were selected for RT-qPCR experiments. Precursors and mature milRNAs were found in the edible parts (caps and stipes), validating the predictions carried out in silico. When their potential gene targets were investigated, results pointed that most were involved in primary and secondary metabolic regulation. However, when the human transcriptome is used as the target, the results suggest that they might interfere with important biological processes related with cancer, infection and neurodegenerative diseases. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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17 pages, 2912 KiB

Open AccessArticle

A Novel Selenium Polysaccharide Alleviates the Manganese (Mn)-Induced Toxicity in Hep G2 Cells and Caenorhabditis elegans

by Tao Chen, Xiaoju Wang, Xinchen Yan, Yali Dai, Tao Liang, Lijun Zhou, Shiling Feng, Ming Yuan, Hongyu Yang and Chunbang Ding

Int. J. Mol. Sci. 2022, 23(8), 4097; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23084097 - 07 Apr 2022

Cited by 4 | Viewed by 2023

Abstract

Manganese (Mn) is now known to have a variety of toxicities, particularly when exposed to it in the workplace. However, there are still ineffective methods for reducing Mn’s hazardous effects. In this study, a new selenium polysaccharide (Se-PCS) was developed from the shell of Camellia oleifera to reduce Mn toxicity in vitro and in vivo. The results revealed that Se-PCS may boost cell survival in Hep G2 cells exposed to Mn and activate antioxidant enzyme activity, lowering ROS and cell apoptosis. Furthermore, after being treated with Se-PCS, Caenorhabditis elegans survived longer under Mn stress. daf-16, a tolerant critical gene, was turned on. Moreover, the antioxidant system was enhanced as the increase in strong antioxidant enzyme activity and high expression of the sod-3, ctl-2, and gst-1 genes. A variety of mutations were also used to confirm that Se-PCS downregulated the insulin signaling pathway. These findings showed that Se-PCS protected Hep G2 cells and C. elegans via the insulin/IGF-1 signaling pathway and that it could be developed into a promising medication to treat Mn toxicity. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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16 pages, 3270 KiB

Open AccessArticle

A Novel Mechanism of Macrophage Activation by the Natural Yolkin Polypeptide Complex from Egg Yolk

by Wioletta Kazana, Dominika Jakubczyk, Katarzyna Pacyga-Prus, Katarzyna Leszczyńska, Sabina Górska, Jakub Siednienko, Józefa Macała, Grażyna Piechowiak and Agnieszka Zabłocka

Int. J. Mol. Sci. 2022, 23(6), 3125; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23063125 - 14 Mar 2022

Cited by 4 | Viewed by 2776

Abstract

Ageing is accompanied by the inevitable changes in the function of the immune system. It provides increased susceptibility to chronic infections that have a negative impact on the quality of life of older people. Therefore, rejuvenating the aged immunity has become an important research and therapeutic goal. Yolkin, a polypeptide complex isolated from hen egg yolks, possesses immunoregulatory and neuroprotective activity. Considering that macrophages play a key role in pathogen recognition and antigen presentation, we evaluated the impact of yolkin on the phenotype and function of mouse bone marrow-derived macrophages of the BMDM cell line. We determined yolkin bioavailability and the surface co-expression of CD80/CD86 using flow cytometry and IL-6, IL-10, TGF-β and iNOS mRNA expression via real-time PCR. Additionally, the impact of yolkin on the regulation of cytokine expression by MAPK and PI3K/Akt kinases was determined. The stimulation of cells with yolkin induced significant changes in cell morphology and an increase in CD80/CD86 expression. Using pharmaceutical inhibitors of ERK, JNK and PI3K/Akt, we have shown that yolkin is able to activate these kinases to control cytokine mRNA expression. Our results suggest that yolkin is a good regulator of macrophage activity, priming mainly the M1 phenotype. Therefore, it is believed that yolkin possesses significant therapeutic potential and represents a promising possibility for the development of novel immunomodulatory medicine. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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26 pages, 42940 KiB

Open AccessArticle

Mechanisms of the Cytotoxic Effect of Selenium Nanoparticles in Different Human Cancer Cell Lines

by Elena G. Varlamova, Mikhail V. Goltyaev, Valentina N. Mal’tseva, Egor A. Turovsky, Ruslan M. Sarimov, Alexander V. Simakin and Sergey V. Gudkov

Int. J. Mol. Sci. 2021, 22(15), 7798; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22157798 - 21 Jul 2021

Cited by 48 | Viewed by 3502

Abstract

In recent decades, studies on the functional features of Se nanoparticles (SeNP) have gained great popularity due to their high biocompatibility, stability, and pronounced selectivity. A large number of works prove the anticarcinogenic effect of SeNP. In this work, the molecular mechanisms regulating the cytotoxic effects of SeNP, obtained by laser ablation, were studied by the example of four human cancer cell lines: A-172 (glioblastoma), Caco-2, (colorectal adenocarcinoma), DU-145 (prostate carcinoma), MCF-7 (breast adenocarcinoma). It was found that SeNP had different concentration-dependent effects on cancer cells of the four studied human lines. SeNP at concentrations of less than 1 μg/mL had no cytotoxic effect on the studied cancer cells, with the exception of the A-172 cell line, for which 0.5 μg/mL SeNP was the minimum concentration affecting its metabolic activity. It was shown that SeNP concentration-dependently caused cancer cell apoptosis, but not necrosis. In addition, it was found that SeNP enhanced the expression of pro-apoptotic genes in almost all cancer cell lines, with the exception of Caco-2 and activated various pathways of adaptive and pro-apoptotic signaling pathways of UPR. Different effects of SeNP on the expression of ER-resident selenoproteins and selenium-containing glutathione peroxidases and thioredoxin reductases, depending on the cell line, were established. In addition, SeNP triggered Ca²⁺ signals in all investigated cancer cell lines. Different sensitivity of cancer cell lines to SeNP can determine the induction of the process of apoptosis in them through regulation of the Ca²⁺ signaling system, mechanisms of ER stress, and activation of various expression patterns of genes encoding pro-apoptotic proteins. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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Review

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52 pages, 2669 KiB

Open AccessReview

Effects of Functional Phenolics Dietary Supplementation on Athletes’ Performance and Recovery: A Review

by Ana C. Gonçalves, Dário Gaspar, José David Flores-Félix, Amílcar Falcão, Gilberto Alves and Luís R. Silva

Int. J. Mol. Sci. 2022, 23(9), 4652; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23094652 - 22 Apr 2022

Cited by 13 | Viewed by 4659

Abstract

In recent years, many efforts have been made to identify micronutrients or nutritional strategies capable of preventing, or at least, attenuating, exercise-induced muscle damage and oxidative stress, and improving athlete performance. The reason is that most exercises induce various changes in mitochondria and cellular cytosol that lead to the generation of reactive species and free radicals whose accumulation can be harmful to human health. Among them, supplementation with phenolic compounds seems to be a promising approach since their chemical structure, composed of catechol, pyrogallol, and methoxy groups, gives them remarkable health-promoting properties, such as the ability to suppress inflammatory processes, counteract oxidative damage, boost the immune system, and thus, reduce muscle soreness and accelerate recovery. Phenolic compounds have also already been shown to be effective in improving temporal performance and reducing psychological stress and fatigue. Therefore, the aim of this review is to summarize and discuss the current knowledge on the effects of dietary phenolics on physical performance and recovery in athletes and sports practitioners. Overall, the reports show that phenolics exert important benefits on exercise-induced muscle damage as well as play a biological/physiological role in improving physical performance. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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16 pages, 892 KiB

Open AccessReview

The Health Benefits of Emodin, a Natural Anthraquinone Derived from Rhubarb—A Summary Update

by Monika Stompor-Gorący

Int. J. Mol. Sci. 2021, 22(17), 9522; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms22179522 - 01 Sep 2021

Cited by 49 | Viewed by 5692

Abstract

Emodin (6-methyl-1,3,8-trihydroxyanthraquinone) is a naturally occurring anthraquinone derivative found in roots and leaves of various plants, fungi and lichens. For a long time it has been used in traditional Chinese medicine as an active ingredient in herbs. Among other sources, it is isolated from the rhubarb Rheum palmatum or tuber fleece-flower Polygonam multiflorum. Emodin has a wide range of biological activities, including diuretic, antibacterial, antiulcer, anti-inflammatory, anticancer and antinociceptive. According to the most recent studies, emodin acts as an antimalarial and antiallergic agent, and can also reverse resistance to chemotherapy. In the present work the potential therapeutic role of emodin in treatment of inflammatory diseases, cancers and microbial infections is analysed. Full article

(This article belongs to the Special Issue Bioactive Compounds: From Diet to Therapeutic Use)

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