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Natural Polyphenols and Human Health
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Natural Polyphenols and Human Health

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 6178

Special Issue Editor

Dr. HyeMee Kim

E-Mail Website
Guest Editor
Department of Food Science and Nutrition, Pusan National University, Busan 46241, Republic of Korea
Interests: bioactive compounds; polyphenols; metabolites; bioavailability; gut microbiota; inflammation; inflammatory bowel disease; obesity; chronic disease
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Polyphenols are secondary metabolites of plants, that have antioxidant and anti-inflammatory capacities and potential health benefits. Recent studies have reported the prebiotic properties of polyphenols and the two-way interaction between polymeric polyphenols and gut microbiota and their effects on chronic disease. Polyphenols consumption influences the composition of gut microbiota by increasing beneficial bacteria and reducing pathogenic bacteria. In addition, gut microbiota can biotransform polymeric polyphenols into their metabolites and increase their biological properties. Although there are many studies ongoing about the effects of polyphenol–gut microbiota interactions, figuring out how to synergize the properties of polyphenols by altering the gut microbiota composition would be helpful to understand their effects on human health and disease prevention.

Therefore, this Special Issue, “Natural Polyphenols and Human Health,” welcomes the submission of articles (original research papers and reviews) that focus on the metabolism, effects, and underlying mechanisms of polyphenols in health and disease prevention, especially studies about simultaneous intake of probiotics and polyphenols.

Dr. HyeMee Kim
Guest Editor

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. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Bioactive compounds
  • Polyphenols
  • Metabolites
  • Gut microbiota
  • Inflammation
  • Health benefits
  • Chronic disease

Published Papers (3 papers)

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Research

20 pages, 4578 KiB  
Article
Exploring the Inhibition of Quercetin on Acetylcholinesterase by Multispectroscopic and In Silico Approaches and Evaluation of Its Neuroprotective Effects on PC12 Cells
by Yijing Liao, Xi Mai, Xiaqing Wu, Xing Hu, Xiaoqiao Luo and Guowen Zhang
Molecules 2022, 27(22), 7971; https://doi.org/10.3390/molecules27227971 - 17 Nov 2022
Cited by 11 | Viewed by 1946
Abstract
This study investigated the inhibitory mechanism of quercetin in acetylcholinesterase (AChE) and its neuroprotective effects on β-amyloid25–35-induced oxidative stress injury in PC12 cells. Quercetin inhibited AChE in a reversible mixed manner with an IC50 of 4.59 ± 0.27 µM. The [...] Read more.
This study investigated the inhibitory mechanism of quercetin in acetylcholinesterase (AChE) and its neuroprotective effects on β-amyloid25–35-induced oxidative stress injury in PC12 cells. Quercetin inhibited AChE in a reversible mixed manner with an IC50 of 4.59 ± 0.27 µM. The binding constant of quercetin with AChE at 25 °C was (5.52 ± 0.05) × 104 L mol−1. Hydrogen bonding and van der Waals forces were the main interactions in forming the stable quercetin–AChE complex. Computational docking revealed that quercetin was dominant at the peripheral aromatic site in AChE and induced enzymatic allosterism; meanwhile, it extended deep into the active center of AChE and destabilized the hydrogen bond network, which caused the constriction of the gorge entrance and prevented the substrate from entering the enzyme, thus resulting in the inhibition of AChE. Molecular dynamics (MD) simulation emphasized the stability of the quercetin–AChE complex and corroborated the previous findings. Interestingly, a combination of galantamine hydrobromide and quercetin exhibited the synergistic inhibition effect by binding to different active sites of AChE. In a β-amyloid25–35-induced oxidative stress injury model in PC12 cells, quercetin exerted neuroprotective effects by increasing the glutathione level and reducing the malondialdehyde content and reactive oxygen species levels. These findings may provide novel insights into the development and application of quercetin in the dietary treatment of Alzheimer’s disease. Full article
(This article belongs to the Special Issue Natural Polyphenols and Human Health)
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12 pages, 2508 KiB  
Article
Honeysuckle Berry (Lonicera caerulea L.) Inhibits Lipase Activity and Modulates the Gut Microbiota in High-Fat Diet-Fed Mice
by Jong-Yeon Kim, You-Suk Lee, Eun-Jung Park and Hae-Jeung Lee
Molecules 2022, 27(15), 4731; https://doi.org/10.3390/molecules27154731 - 24 Jul 2022
Cited by 6 | Viewed by 1959
Abstract
Honeysuckle berry (HB, Lonicera caerulea L.) is an oriental herbal medicine reported to have beneficial effects on metabolic disorders, such as obesity and non-alcoholic fatty liver disease. The fruit part of HB is rich in anthocyanin, a type of polyphenol. Most studies credit [...] Read more.
Honeysuckle berry (HB, Lonicera caerulea L.) is an oriental herbal medicine reported to have beneficial effects on metabolic disorders, such as obesity and non-alcoholic fatty liver disease. The fruit part of HB is rich in anthocyanin, a type of polyphenol. Most studies credit the antioxidant and anti-inflammatory properties of HB as the mechanisms of its effectiveness. This study investigated the inhibitory effects of HB on lipase using an in vitro assay and the modulatory effect of HB on gut microbiota in high-fat diet (HFD)-fed mice. HB inhibited pancreatic lipase activity with IC50 values of approximately 0.47 mg/mL. The fecal triglyceride (TG) levels were higher from the HFD of the HB-fed mice than they were for the control mice. Moreover, the fecal microbiota from the HFD of the HB-fed mice had relatively lower Firmicutes and higher Bacteroidetes than that from the HFD-only mice. These results suggest that HB modulates gut microbiota composition, which may contribute to body fat reduction. Hence, HB could present a useful agent for treating metabolic diseases through lower TG uptake and the regulation of gut microflora. Full article
(This article belongs to the Special Issue Natural Polyphenols and Human Health)
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12 pages, 1880 KiB  
Article
Structural Investigation of the Interaction Mechanism between Chlorogenic Acid and AMPA Receptor via In Silico Approaches
by Wei Zhu, Fengming Wu, Jindie Hu, Wenjing Wang, Jifeng Zhang and Guoqing Guo
Molecules 2022, 27(11), 3394; https://doi.org/10.3390/molecules27113394 - 25 May 2022
Cited by 2 | Viewed by 1483
Abstract
Chlorogenic acid (CGA), an important metabolite in natural plant medicines such as honeysuckle and eucommia, has been shown to have potent antinociceptive effects. Nevertheless, the mechanism by which CGA relieves chronic pain remains unclear. α-amino-3-hydroxy-5-methyl-4-isooxazolpropionic acid receptor (AMPAR) is a major ionotropic glutamate [...] Read more.
Chlorogenic acid (CGA), an important metabolite in natural plant medicines such as honeysuckle and eucommia, has been shown to have potent antinociceptive effects. Nevertheless, the mechanism by which CGA relieves chronic pain remains unclear. α-amino-3-hydroxy-5-methyl-4-isooxazolpropionic acid receptor (AMPAR) is a major ionotropic glutamate receptor that mediates rapid excitatory synaptic transmission and its glutamate ionotropic receptor AMPA type subunit 1 (GluA1) plays a key role in nociceptive transmission. In this study, we used Western blot, surface plasmon resonance (SPR) assay, and the molecular simulation technologies to investigate the mechanism of interaction between CGA and AMPAR to relieve chronic pain. Our results indicate that the protein expression level of GluA1 showed a dependent decrease as the concentration of CGA increased (0, 50, 100, and 200 μM). The SPR assay demonstrates that CGA can directly bind to GluA1 (KD = 496 μM). Furthermore, CGA forms a stable binding interaction with GluA1, which is validated by molecular dynamics (MD) simulation. The binding free energy between CGA and GluA1 is −39.803 ± 14.772 kJ/mol, where van der Waals interaction and electrostatic interaction are the major contributors to the GluA1–CGA binding, and the key residues are identified (Val-32, Glu-33, Ala-36, Glu-37, Leu-48), which play a crucial role in the binding interaction. This study first reveals the structural basis of the stable interaction between CGA and GluA1 to form a binding complex for the relief of chronic pain. The research provides the structural basis to understand the treatment of chronic pain and is valuable to the design of novel drug molecules in the future. Full article
(This article belongs to the Special Issue Natural Polyphenols and Human Health)
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