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11 pages, 1808 KiB

Open AccessArticle

Insight into the Inhibitory Mechanisms of Hesperidin on α-Glucosidase through Kinetics, Fluorescence Quenching, and Molecular Docking Studies

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Kumaravel Kaliaperumal

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Foods 2023, 12(22), 4142; https://doi.org/10.3390/foods12224142 - 16 Nov 2023

Viewed by 562

Abstract

The α-glucosidase inhibitor is of interest to researchers due to its association with type-II diabetes treatment by suppressing postprandial hyperglycemia. Hesperidin is a major flavonoid in orange fruit with diverse biological properties. This paper evaluates the effects of hesperidin on α-glucosidase through inhibitory [...] Read more.

The α-glucosidase inhibitor is of interest to researchers due to its association with type-II diabetes treatment by suppressing postprandial hyperglycemia. Hesperidin is a major flavonoid in orange fruit with diverse biological properties. This paper evaluates the effects of hesperidin on α-glucosidase through inhibitory kinetics, fluorescence quenching, and molecular docking methods for the first time. The inhibition kinetic analysis shows that hesperidin reversibly inhibited the α-glucosidase activity with an IC₅₀ value of 18.52 μM and the inhibition was performed in an uncompetitive type. The fluorescence quenching studies indicate that the intrinsic fluorescence of α-glucosidase was quenched via a static quenching process and only one binding site was present between the hesperidin and α-glucosidase. The interaction between them was spontaneous and mainly driven by hydrogen bonds, as well as hydrophobic forces. Furthermore, the molecular docking results suggest that hesperidin might bond to the entrance or outlet part of the active site of α-glucosidase through a network of five hydrogen bonds formed between hesperidin and the four amino acid residues (Trp709, Arg422, Asn424, and Arg467) of α-glucosidase and the hydrophobic effects. These results provide new insight into the inhibitory mechanisms of hesperidin on α-glucosidase, supporting the potential application of a hesperidin-rich orange product as a hypoglycemic functional food. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds from Food on Human Health)

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15 pages, 2326 KiB

Open AccessArticle

Bioavailable Phenolic Compounds from Olive Pomace Present Anti-Neuroinflammatory Potential on Microglia Cells

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Luana Schmidt

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Bruna Krieger Vargas

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Camila Sant’Anna Monteiro

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Lauren Pappis

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Renius de Oliveira Mello

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Alencar Kolinski Machado

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Tatiana Emanuelli

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Marco Antônio Zachia Ayub

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José Cláudio Fonseca Moreira

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Paula Rossini Augusti

Foods 2023, 12(22), 4048; https://doi.org/10.3390/foods12224048 - 07 Nov 2023

Viewed by 568

Abstract

The neuroinflammatory process is considered one of the main characteristics of central nervous system diseases, where a pro-inflammatory response results in oxidative stress through the generation of reactive oxygen and nitrogen species (ROS and RNS). Olive (Olea europaea L.) pomace is a [...] Read more.

The neuroinflammatory process is considered one of the main characteristics of central nervous system diseases, where a pro-inflammatory response results in oxidative stress through the generation of reactive oxygen and nitrogen species (ROS and RNS). Olive (Olea europaea L.) pomace is a by-product of olive oil production that is rich in phenolic compounds (PCs), known for their antioxidant and anti-inflammatory properties. This work looked at the antioxidant and anti-neuroinflammatory effects of the bioavailable PC from olive pomace in cell-free models and microglia cells. The bioavailable PC of olive pomace was obtained through the process of in vitro gastrointestinal digestion of fractionated olive pomace (OPF, particles size < 2 mm) and micronized olive pomace (OPM, particles size < 20 µm). The profile of the PC that is present in the bioavailable fraction as well as its in vitro antioxidant capacity were determined. The anti-neuroinflammatory capacity of the bioavailable PC from olive pomace (0.03–3 mg L⁻¹) was evaluated in BV-2 cells activated by lipopolysaccharide (LPS) for 24 h. The total bioavailable PC concentration and antioxidant activity against peroxyl radical were higher in the OPM than those observed in the OPF sample. The activation of BV-2 cells by LPS resulted in increased levels of ROS and nitric oxide (NO). The bioavailable PCs from both OPF and OPM, at their lowest concentrations, were able to reduce the ROS generation in activated BV-2 cells. In contrast, the highest PC concentration of OPF and OPM was able to reduce the NO levels in activated microglial cells. Our results demonstrate that bioavailable PCs from olive pomace can act as anti-neuroinflammatory agents in vitro, independent of particle size. Moreover, studies approaching ways to increase the bioavailability of PCs from olive pomace, as well as any possible toxic effects, are needed before a final statement on its nutritional use is made. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds from Food on Human Health)

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13 pages, 564 KiB

Open AccessArticle

Valorization of Pumpkin Byproducts: Antioxidant Activity and Carotenoid Characterization of Extracts from Peel and Filaments

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Beniamino Terzo Cenci-Goga

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Lina Cossignani

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Francesca Blasi

Foods 2023, 12(21), 4035; https://doi.org/10.3390/foods12214035 - 05 Nov 2023

Viewed by 550

Abstract

Pumpkin (Cucurbita sp.) represents an unquestionable source of valuable nutrients and bioactive compounds having a broad spectrum of health-promoting effects. The goal of this work was to characterize the byproducts (peels and filaments) of different pumpkin varieties belonging to C. moschata (Butternut, [...] Read more.

Pumpkin (Cucurbita sp.) represents an unquestionable source of valuable nutrients and bioactive compounds having a broad spectrum of health-promoting effects. The goal of this work was to characterize the byproducts (peels and filaments) of different pumpkin varieties belonging to C. moschata (Butternut, Lunga di Napoli, Moscata di Provenza, and Violina rugosa) and C. maxima (Delica, Delica vanity, Hokkaido, and Mantovana) species in terms of total carotenoid content, antioxidant activity, and carotenoid profiling. The research revealed that peels and filaments were a good source of β-carotene and other non-esterified carotenoids, as well as esterified carotenoids. Considering the growing market demand for safe and healthy food products, pumpkin byproducts, having also an interesting antioxidant bioactivity, could be useful in the development of novel functional products. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds from Food on Human Health)

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13 pages, 1977 KiB

Open AccessArticle

Yeast-Hydrolysate-Derived 1-Methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic Acid Inhibits Fat Accumulation during Adipocyte Differentiation

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Foods 2023, 12(18), 3466; https://doi.org/10.3390/foods12183466 - 18 Sep 2023

Cited by 1 | Viewed by 786

Abstract

This study aimed to investigate the impact of yeast hydrolysate (YH) on lipogenesis, elucidate its mechanistic action, and identify the active compounds responsible for its anti-adipogenic effects. YH (2 mg/mL) significantly reduced Oil Red O-stained lipids. YH (2 mg/mL) also downregulated C/EBPβ and [...] Read more.

This study aimed to investigate the impact of yeast hydrolysate (YH) on lipogenesis, elucidate its mechanistic action, and identify the active compounds responsible for its anti-adipogenic effects. YH (2 mg/mL) significantly reduced Oil Red O-stained lipids. YH (2 mg/mL) also downregulated C/EBPβ and upregulated KLF2, both of which are early adipogenic factors. Moreover, YH (2 mg/mL) decreased C/EBPα, PPARγ, FABP4, FAS, ACC, and HMGCR mRNA expression. Additionally, YH significantly downregulated SEBP1c and SREBP2 and their target genes, which govern fatty acid and cholesterol metabolism; however, 2 mg/mL YH had a greater suppressive effect on SREBP1c than on SREBP2. YH (2 mg/mL) also significantly reduced the mRNA level of G6PD and malic enzyme, which are enzymes that synthesize NADPH for lipid synthesis, compared with the control. Furthermore, 1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid (MTCA) was identified as the active compound with anti-adipogenic effects using solvent fractionation and chromatographic analysis of YH, and 1.1 μg/mL MTCA significantly downregulated SREBP1c/SREBP2 mRNAs by 47.8% and 69.2%, respectively, along with the target genes FAS, ACC, and HMGCR by 79.0%, 77.0%, and 40.9%, respectively. Collectively, YH effectively suppressed adipogenic lipid storage by downregulating SREBP- and NADPH-synthesizing genes. These findings suggest that YH containing MTCA has the potential to act as an anti-obesity agent. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds from Food on Human Health)

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17 pages, 5833 KiB

Open AccessArticle

Integrated Transcriptomics and Metabolomics Reveal the Mechanism of Alliin in Improving Hyperlipidemia

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Foods 2023, 12(18), 3407; https://doi.org/10.3390/foods12183407 - 13 Sep 2023

Viewed by 670

Abstract

This research aims to assess the anti-hyperlipidemia effects of alliin in vivo and its potential mechanisms through transcriptomics and metabolomics analysis. A hyperlipidemia mode was established in C57BL/6 mice fed a high-fat diet, and the related physiological parameters of the animals were recorded. [...] Read more.

This research aims to assess the anti-hyperlipidemia effects of alliin in vivo and its potential mechanisms through transcriptomics and metabolomics analysis. A hyperlipidemia mode was established in C57BL/6 mice fed a high-fat diet, and the related physiological parameters of the animals were recorded. Serum TC and MDA in livers significantly decreased by 12.34% and 29.59%, respectively, and SOD and CAT in livers significantly increased by 40.64% and 39.05%, respectively, after high doses of alliin interventions. In total, 148 significantly different genes, particularly Cel, Sqle, Myc, and Ugt1a2, were revealed for their potential roles in HFD-induced alliin, mainly through steroid biosynthesis, triglyceride metabolism, drug metabolism–cytochrome P450, and the PI3K–Akt signaling pathway, according to transcriptomics analysis. Metabolomics results revealed 18 significantly different metabolites between the alliin group and HFD group, which were classified as carboxylic acids, such as N-undecanoylglycine, adipic acid, D-pantothenic acid, cyprodenate, and pivagabine. We found pantothenic acid played a vital role and was effective through pantothenic acid and CoA biosynthesis metabolism. The “steroid biosynthesis pathway” was identified as the most significant metabolic pathway by integrated transcriptomics and metabolomics analysis. This work offered a theoretical framework for the mechanism of alliin lipid lowering in the future. The development and utilization of alliin will be a viable strategy to improve the health status of people with hyperlipidemia, suggesting prospective market opportunities. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds from Food on Human Health)

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16 pages, 509 KiB

Open AccessArticle

Low-Temperature Vacuum Drying on Broccoli: Enhanced Anti-Inflammatory and Anti-Proliferative Properties Regarding Other Drying Methods

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Gabriela Valenzuela-Barra

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Angara Zambrano

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Maria Gabriela Goñi

Foods 2023, 12(17), 3311; https://doi.org/10.3390/foods12173311 - 02 Sep 2023

Viewed by 1071

Abstract

Low-temperature vacuum drying (LTVD) has shown great potential for drying vegetables. It could avoid excessive degradations of active compounds with potential therapeutic agents. In this study, the effect on several relevant bioactive compounds, anti-inflammatory activity, and anti-proliferative activity of broccoli (Brassica oleracea [...] Read more.

Low-temperature vacuum drying (LTVD) has shown great potential for drying vegetables. It could avoid excessive degradations of active compounds with potential therapeutic agents. In this study, the effect on several relevant bioactive compounds, anti-inflammatory activity, and anti-proliferative activity of broccoli (Brassica oleracea var. italica) were evaluated. Effects of other drying methods, including vacuum drying (VD), convective drying (CD), infrared drying (IRD), and freeze drying (FD), were also comparatively evaluated. The results of all dried samples showed high polyunsaturated fatty acid contents (of up to 71.3%) and essential amino acid contents (of up to 8.63%). The LTVD method stands out above the other drying methods, since it obtained the highest content of total phenols, chlorogenic acid, and ferulic acid. Both the LTVD and CD samples demonstrated high anti-inflammatory and anti-proliferative activities. These CD and LTVD samples were also the most active against the breast carcinoma MDA-MB-23 cell line. Due to the good retention of bioactive compounds via LTVD, the obtained dried broccoli here can be used in a near time as an ingredient for the development of novel natural products with anti-inflammatory and anti-proliferative effects. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds from Food on Human Health)

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20 pages, 6840 KiB

Open AccessArticle

Ginsenoside Rh4 Improves Hepatic Lipid Metabolism and Inflammation in a Model of NAFLD by Targeting the Gut Liver Axis and Modulating the FXR Signaling Pathway

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Foods 2023, 12(13), 2492; https://doi.org/10.3390/foods12132492 - 26 Jun 2023

Cited by 1 | Viewed by 1093

Abstract

Non-alcoholic fatty liver disease (NAFLD) is a series of disorders of liver metabolism caused by the accumulation of lipids in the liver, which is considered the main cause of hepatocellular carcinoma. Our previous study demonstrated the promising efficacy of ginsenoside Rh4 in improving [...] Read more.

Non-alcoholic fatty liver disease (NAFLD) is a series of disorders of liver metabolism caused by the accumulation of lipids in the liver, which is considered the main cause of hepatocellular carcinoma. Our previous study demonstrated the promising efficacy of ginsenoside Rh4 in improving the intestinal tract and its related metabolites. Meanwhile, many studies in the literature have investigated the gut microbiota and its metabolites, such as bile acids (BAs) and short-chain fatty acids (SCFAs), which play a key role in the pathogenesis of NAFLD. Therefore, this study focused on whether Rh4 could achieve therapeutic effects on NAFLD through the gut–liver axis. The results showed that Rh4 exhibited sound therapeutic effects on the NAFLD model induced by the Western diet and CCl₄ in mice. In the liver, the degrees of hepatic steatosis, lobular inflammation levels, and bile acid in the liver tissue were improved after Rh4 treatment. At the same time, Rh4 treatment significantly increased the levels of intestinal SCFAs and BAs, and these changes were accompanied by the complementary diversity and composition of intestinal flora. In addition, correlation analysis showed that Rh4 affected the expression of proteins involved in the farnesoid X receptor (FXR) signaling pathway in the liver and intestine, which modulates hepatic lipid metabolism, inflammation, and proteins related to bile acid regulation. In conclusion, our study provides a valuable insight into how Rh4 targets the gut–liver axis for the development of NAFLD, which indicates that Rh4 may be a promising candidate for the clinical therapy of NAFLD. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds from Food on Human Health)

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Review

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31 pages, 2171 KiB

Open AccessReview

Beyond the Bottle: Exploring Health-Promoting Compounds in Wine and Wine-Related Products—Extraction, Detection, Quantification, Aroma Properties, and Terroir Effects

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Foods 2023, 12(23), 4277; https://doi.org/10.3390/foods12234277 - 27 Nov 2023

Viewed by 551

Abstract

Health-promoting compounds in wine and wine-related products are important due to their potential benefits to human health. Through an extensive literature review, this study explores the presence of these compounds in wine and wine-related products, examining their relationship with terroir and their impact [...] Read more.

Health-promoting compounds in wine and wine-related products are important due to their potential benefits to human health. Through an extensive literature review, this study explores the presence of these compounds in wine and wine-related products, examining their relationship with terroir and their impact on the aromatic and flavor properties that are perceived orally: sunlight exposure, rainfall patterns, and soil composition impact grapevines’ synthesis and accumulation of health-promoting compounds. Enzymes, pH, and the oral microbiome are crucial in sensory evaluation and perception of health promotion. Moreover, their analysis of health-promoting compounds in wine and wine-related products relies on considerations such as the specific target compound, selectivity, sensitivity, and the complexity of the matrix. Full article

(This article belongs to the Special Issue Advances in Bioactive Compounds from Food on Human Health)

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