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Bioactive Phenolics and Polyphenols 2024

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 April 2025) | Viewed by 6012

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Special Issue Information

Dear Colleagues, 

The scientific interest in plant phenolics as chemopreventive and therapeutic agents against chronic and degenerative diseases has been increasing since the late 1990s, when the French paradox was associated with the high intake of polyphenols present in red wine. Since then, research advances include their biosynthesis, biological activities, purification, and chemical characterization in different plant species. Furthermore, research on the stability of phenolics in food processing techniques and storage is an area of major interest.

Contributions to this Special Issue may cover all aspects of phenolics and polyphenols including their chemical characterization on different plant species and methods for their extraction, purification, and quantification; elucidation of their mechanism of action; development of innovative methods for evaluating their bioactivity in vitro and in vivo; evaluation of their stability to thermal and non-thermal food processing techniques; elicitation of the plant phenolic biosynthesis pathway; and the effects of postharvest handling on the phenolic profiles of plant foods. Papers on developing food products and dietary supplements enriched with plant phenolics will be also be considered.

Prof. Dr. Davide Barreca
Guest Editor

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Keywords

  • phenolic metabolism
  • biological activities
  • stability to food processing
  • elicitation
  • methods of analysis
  • dietary supplements
  • nutraceutical ingredients
  • non-thermal processing
  • extraction and purification

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Published Papers (4 papers)

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Research

15 pages, 2977 KiB  
Article
Jeju Citrus (Citrus unshiu) Leaf Extract and Hesperidin Inhibit Small Intestinal α-Glucosidase Activities In Vitro and Postprandial Hyperglycemia in Animal Model
by Gi-Jung Kim, Yelim Jang, Kyoung-Tae Kwon, Jae-Won Kim, Seong-IL Kang, Hee-Chul Ko, Jung-Yun Lee, Emmanouil Apostolidis and Young-In Kwon
Int. J. Mol. Sci. 2024, 25(24), 13721; https://doi.org/10.3390/ijms252413721 - 23 Dec 2024
Cited by 1 | Viewed by 761
Abstract
Citrus fruits are widely distributed in East Asia, and tea made from citrus peels has demonstrated health benefits, such as a reduction in fever, inflammation, and high blood pressure. However, citrus leaves have not been evaluated extensively for their possible health benefits. In [...] Read more.
Citrus fruits are widely distributed in East Asia, and tea made from citrus peels has demonstrated health benefits, such as a reduction in fever, inflammation, and high blood pressure. However, citrus leaves have not been evaluated extensively for their possible health benefits. In this study, the α-glucosidase-inhibitory activity of Jeju citrus hot-water (CW) and ethyl alcohol (CE) extracts, along with hesperidin (HP) (a bioactive compound in citrus leaf extracts), was investigated, and furthermore, their effect on postprandial blood glucose reduction in an animal model was determined. The hesperidin contents of CW and CE were 15.80 ± 0.18 and 39.17 ± 0.07 mg/g-extract, respectively. Hesperidin inhibited α-glucosidase (IC50, 4.39), sucrase (0.50), and CE (2.62) and demonstrated higher α-glucosidase inhibitory activity when compared to CW (4.99 mg/mL). When using an SD rat model, during sucrose and starch loading tests with CE (p < 0.01) and HP (p < 0.01), a significant postprandial blood glucose reduction effect was observed when compared to the control. The maximum blood glucose levels (Cmax) of the CE administration group decreased by about 15% (from 229.3 ± 14.5 to 194.0 ± 7.4, p < 0.01) and 11% (from 225.1 ± 13.8 to 201.1 ± 7.2 hr·mg/dL, p < 0.05) in the sucrose and starch loading tests, respectively. Our findings suggest that citrus leaf extracts standardized to hesperidin may reduce postprandial blood glucose levels through the observed inhibitory effect against sucrase, which results in delayed carbohydrate absorption. Our findings provide a biochemical rationale for further evaluating the benefits of citrus leaves. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2024)
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20 pages, 2554 KiB  
Article
In Vitro Biological Activities of Paederia grandidieri Leaf Extracts
by Faratiana Jenny Rasoariseheno, Nicoletta Fidanza, Elena Coccia, Dyana Jackson Ratovomanarivo, Daniela Sateriale, Lucia Abbatiello, Caterina Pagliarulo, Rosanna Filosa, Jeanne Angelphine Rasoamananjara and Marina Paolucci
Int. J. Mol. Sci. 2024, 25(23), 12960; https://doi.org/10.3390/ijms252312960 - 2 Dec 2024
Viewed by 891
Abstract
In many developing countries, human health problems are solved using local plants. Knowledge of their chemical composition and biological activities can contribute to the creation of natural-based products usefully employed in human health. In this work, we analysed Paederia grandidieri leaves extracted with [...] Read more.
In many developing countries, human health problems are solved using local plants. Knowledge of their chemical composition and biological activities can contribute to the creation of natural-based products usefully employed in human health. In this work, we analysed Paederia grandidieri leaves extracted with diverse eco-compatible procedures and subjected to chemical, microbiological, and cellular compatibility assays. Fresh leaves of P. grandidieri were harvested in southern Madagascar, where most of the population relies on P. grandidieri for daily dental care. Leaves were dried and powdered. Distilled water and ethanol at 25 °C and 60 °C from 6 to 24 h were used for extraction. Polyphenol composition, antioxidant activity, and antibacterial, prebiotic, and cytotoxic properties of the extracts were analysed. The aqueous extracts contained higher levels of flavan-3-ols and flavanones, while the hydro-alcoholic extracts were richer in flavonols and flavones. The aqueous extracts showed the highest total phenolic and total flavonoid contents, and antioxidant activity. The hydro-alcoholic extracts showed antibacterial effects against Listeria monocytogenes and Pseudomonas aeruginosa, two key foodborne and environmental pathogens, while the aqueous extracts showed prebiotic effects against Streptococcus salivarius. The cytotoxic effects of P. grandidieri leaf extracts were evaluated using the MTT assay on mouse fibroblasts (L929 cell line). The most cytotoxic extract was the aqueous extract at 25 °C. Given that P. grandidieri is routinely employed by the southern Madagascar population with healthy and strong teeth with fewer cases of tooth decay with respect to other regions, and in light of the significant chemical and microbiological properties, we maintain that P. grandidieri can be a suitable candidate for the production of pro-health products for the oral cavity. More in-depth studies will ensure a broader picture of the impact of extracts, especially for possible oral use. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2024)
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21 pages, 7256 KiB  
Article
6′-O-Caffeoylarbutin from Quezui Tea: A Highly Effective and Safe Tyrosinase Inhibitor
by Dong Xie, Wengan Fu, Tiantian Yuan, Kangjia Han, Yuxiu Lv, Qi Wang, Qian Jiang, Yingjun Zhang, Guolei Zhu, Junming Xu, Ping Zhao and Xiaoqin Yang
Int. J. Mol. Sci. 2024, 25(2), 972; https://doi.org/10.3390/ijms25020972 - 12 Jan 2024
Cited by 6 | Viewed by 1590
Abstract
Tyrosinase is vital in fruit and vegetable browning and melanin synthesis, crucial for food preservation and pharmaceuticals. We investigated 6′-O-caffeoylarbutin’s inhibition, safety, and preservation on tyrosinase. Using HPLC, we analyzed its effect on mushroom tyrosinase and confirmed reversible competitive inhibition. UV_vis [...] Read more.
Tyrosinase is vital in fruit and vegetable browning and melanin synthesis, crucial for food preservation and pharmaceuticals. We investigated 6′-O-caffeoylarbutin’s inhibition, safety, and preservation on tyrosinase. Using HPLC, we analyzed its effect on mushroom tyrosinase and confirmed reversible competitive inhibition. UV_vis and fluorescence spectroscopy revealed a stable complex formation with specific binding, causing enzyme conformational changes. Molecular docking and simulations highlighted strong binding, enabled by hydrogen bonds and hydrophobic interactions. Cellular tests showed growth reduction of A375 cells with mild HaCaT cell toxicity, indicating favorable safety. Animal experiments demonstrated slight toxicity within safe doses. Preservation trials on apple juice showcased 6′-O-caffeoylarbutin’s potential in reducing browning. In essence, this study reveals intricate mechanisms and applications of 6′-O-caffeoylarbutin as an effective tyrosinase inhibitor, emphasizing its importance in food preservation and pharmaceuticals. Our research enhances understanding in this field, laying a solid foundation for future exploration. Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2024)
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17 pages, 2718 KiB  
Article
Individual Differences in Growth and in Accumulation of Secondary Metabolites in Rhodiola rosea Cultivated in Western Siberia
by Anna A. Erst, Olga V. Kotsupiy, Andrey S. Erst and Alexander A. Kuznetsov
Int. J. Mol. Sci. 2023, 24(14), 11244; https://doi.org/10.3390/ijms241411244 - 8 Jul 2023
Cited by 3 | Viewed by 1720
Abstract
In this study, growth parameters of underground parts and concentrations of phenylpropanoids, phenylethanoids, flavonoids, hydroxybenzoic acids, and catechins in aqueous–ethanol extracts of 6-year-old cultivated plants of Rhodiola rosea (propagated in vitro) of Altai Mountain origin were analyzed, and differences in chemical composition among [...] Read more.
In this study, growth parameters of underground parts and concentrations of phenylpropanoids, phenylethanoids, flavonoids, hydroxybenzoic acids, and catechins in aqueous–ethanol extracts of 6-year-old cultivated plants of Rhodiola rosea (propagated in vitro) of Altai Mountain origin were analyzed, and differences in chemical composition among plant specimens and between plant parts (rhizome and root) were evaluated. High-performance liquid chromatography detected 13 phenolic compounds. Roots contained 1.28 times higher phenylethanoids levels (1273.72 mg/100 g) than rhizomes did. Overall, the concentration of phenylethanoids in underground organs was not high and ranged from 21.36 to 103.00 mg/100 g. High variation among R. rosea individual plants was noted both in growth characteristics and in levels of secondary metabolites under our cultivation conditions. It was found that concentrations of phenylpropanoids, phenylethanoids, and catechins significantly depend on the plant part analyzed (p ≤ 0.05). Specimen No. 4 is characterized by the highest concentration of rosavins (1230.99 mg/plant) and the lowest concentration of cinnamyl alcohol (62.87 mg/plant). Despite the wide range of values, all 10 tested specimens (underground part) met the minimum requirements of the United States Pharmacopeia (2015) for rosavins (0.3%) and of the Russia State Pharmacopoeia (2015) for the average level of rosavins (roots): (1%). Full article
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2024)
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