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15 pages, 3170 KiB  
Article
Preparation and Characterization of Small-Size and Strong Antioxidant Nanocarriers to Enhance the Stability and Bioactivity of Curcumin
by Shanshan Tie, Yujin Yang, Jiawei Ding, Yanyan Li, Mengmeng Xue, Jianrui Sun, Fang Li, Qiuxia Fan, Ying Wu and Shaobin Gu
Foods 2024, 13(23), 3958; https://doi.org/10.3390/foods13233958 (registering DOI) - 8 Dec 2024
Abstract
The purpose of this study was to design nanocarriers with small-size and antioxidant properties for the effective encapsulation of curcumin. Here, procyanidins, vanillin, and amino acids were used to successfully prepare nanocarriers of a controllable size in the range of 328~953 nm and [...] Read more.
The purpose of this study was to design nanocarriers with small-size and antioxidant properties for the effective encapsulation of curcumin. Here, procyanidins, vanillin, and amino acids were used to successfully prepare nanocarriers of a controllable size in the range of 328~953 nm and to endow antioxidant ability based on a one-step self-assembly method. The reaction involved a Mannich reaction on the phenolic hydroxyl groups of procyanidins, aldehyde groups of vanillin, and amino groups of amino acids. Subsequently, curcumin nanoparticles were prepared by loading curcumin with this nanocarrier, and the encapsulation efficiency of curcumin was 85.97%. Compared with free curcumin, the antioxidant capacity and photothermal stability of the embedded curcumin were significantly improved, and it could be slowly released into simulated digestive fluid. Moreover, using the corticosterone-induced PC12 cell injury model, the cell viability increased by 23.77% after the intervention of curcumin nanoparticles, and the cellular antioxidant capacity was also significantly improved. The nanoparticles prepared in this work can effectively improve the solubility, stability, and bioactivity of curcumin, which provides a reference for the embedding and delivery of other hydrophobic bioactive compounds. Full article
(This article belongs to the Section Food Nutrition)
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<p>Preparation and particle size characterization of nanocarriers. (<b>a</b>) A schematic diagram of the preparation of NCs−1~NCs−8 using PCs, vanillin, and amino acids as raw materials. (<b>b</b>) Particle size, polydispersity index (PDI), and (<b>c</b>) particle size distribution of amino acid-dependent nanocarriers NCs−1~NCs−3. (<b>d</b>) Particle size, PDI, and (<b>e</b>) particle size distribution of PC-dependent nanocarriers NCs−1 and NCs−4~NCs−5. (<b>f</b>) Particle size, PDI, and (<b>g</b>) particle size distribution of vanillin-dependent nanocarriers NCs−1 and NCs−6~NCs−8. Note: the lower letters a, b, and c indicate that there are statistically significant differences between the samples.</p>
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<p>Formation and spectral characterization. (<b>a</b>) Schematic illustration of the reaction pathway of NCs. FTIR spectra of (<b>b</b>) vanillin (Van), Lys, (<b>c</b>) PCs, and NCs. (<b>d</b>) UV-Vis spectra and (<b>e</b>) crystal structure of PCs and NCs.</p>
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<p>Preparation and characterization of Cur NPs. (<b>a</b>) A schematic diagram of preparation, SEM image, and (<b>b</b>) embedding efficiency (EE) of Cur NPs. (<b>c</b>) FTIR spectra, (<b>d</b>) UV−vis spectra and (<b>e</b>) crystal structure of Cur NPs.</p>
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<p>Antioxidant capacity experiment. (<b>a</b>) DPPH and (<b>b</b>) ABTS radical scavenging activities for Cur, NCs, and Cur NPs. Note: the lower letters a, b, and c indicate that there are statistically significant differences between the samples.</p>
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<p>(<b>a</b>) UV irradiation and (<b>b</b>) thermal stability analyses for Cur and Cur NPs. Note: the lower letters a, b, and indicate that there are statistically significant differences between the samples.</p>
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<p>(<b>a</b>) Schematic diagram of simulated digestion and (<b>b</b>) release profile of Cur NPs.</p>
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<p>Cell viability analysis. (<b>a</b>) The effect of different concentrations of CORT on the viability of PC12 cells. Effect of (<b>b</b>) NCs, (<b>c</b>) Cur, and (<b>d</b>) Cur NPs on the cell viability of 400 μM CORT-induced PC12 cells. Note: the lower letters a−e indicate that there are statistically significant differences between the samples.</p>
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<p>Effect of Cur, NCs, and Cur NPs on the levels of (<b>a</b>) T-SOD, (<b>b</b>) CAT, and (<b>c</b>) MDA in PC12 cells induced by CORT. Note: the lower letters a, b, c, and d indicate that there are statistically significant differences between the samples.</p>
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<p>(<b>a</b>) Optical images of Cur NPs and NCs. (<b>b</b>) Optical images and hemolysis rate (HR) of negative control, positive control, Cur NPs, and NCs after treatment of red blood cells.</p>
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15 pages, 1329 KiB  
Article
Antimicrobial Mixture Based on Micronized Kaolinite and Ziziphora Essential Oil as a Promising Formulation for the Management of Infected Wounds
by Aigerim A. Karaubayeva, Tolkyn Bekezhanova, Karlygash Zhaparkulova, Katarzyna Susniak, Jan Sobczynski, Paulina Kazimierczak, Agata Przekora, Krystyna Skalicka-Wozniak, Łukasz Kulinowski, Anna Glowniak-Lipa, Zuryiadda B. Sakipova and Izabela Korona-Głowniak
Int. J. Mol. Sci. 2024, 25(23), 13192; https://doi.org/10.3390/ijms252313192 (registering DOI) - 8 Dec 2024
Abstract
Kaolinite stands out as a promising natural geomaterial for developing new therapeutic systems aimed at addressing global health challenges, such as multidrug-resistant infections. In this study, we report on the formulation and biological activity of a therapeutic mixture composed of white micronized kaolinite [...] Read more.
Kaolinite stands out as a promising natural geomaterial for developing new therapeutic systems aimed at addressing global health challenges, such as multidrug-resistant infections. In this study, we report on the formulation and biological activity of a therapeutic mixture composed of white micronized kaolinite (KAO) and Ziziphora essential oil (ZEO), intended for topical application on infected wounds. GC–MS analysis revealed that the primary component of ZEO is pulegone, constituting 72.98% of the oil. ZEO demonstrated good bioactivity against bacterial and fungal strains (MIC 1.25–5 mg/mL). Additionally, ZEO at a concentration of 0.0156% (0.156 mg/mL) was found to significantly stimulate collagen synthesis. The antimicrobial activity of the tested KAO–ZEO mixture formulation (30% KAO/0.25% ZEO in an excipient base) showed the highest effectiveness against Candida spp. (MIC 0.08–25 mg/mL) and Gram-positive bacteria (MIC 0.16–25 mg/mL), with lower activity against Gram-negative bacteria (MIC 25–50 mg/mL). Moreover, the KAO–ZEO mixture was nontoxic (cell viability near 100%) to human skin fibroblasts according to the ISO 10993-5 standard and promoted collagen synthesis by skin cells. This is the first documented formulation combining KAO and ZEO, demonstrating significant antimicrobial properties along with the ability to stimulate collagen production in fibroblasts. These properties highlight KAO–ZEO as a promising novel treatment, which may synergize with current care standards and improve wound healing outcomes. Full article
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<p>The GC–MS chromatogram of Ziziphora EO (ZEO).</p>
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<p>The picture of gel formulation containing micronized kaolinite clay and Ziziphora essential oil.</p>
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<p>Evaluation of the biological properties of ZEO and KAO–ZEO on normal human skin fibroblasts (BJ): (<b>a</b>) Screening cytotoxicity test on different concentrations of ZEO ranging from 0.0039% to 0.2500% and cytotoxicity assessment of KAO–ZEO extract prepared by soaking 100 mg of the sample in 1 mL of the culture medium for 24 h at 37 °C; (<b>b</b>) Evaluation of cell proliferation after exposure to the highest non-toxic concentration of ZEO (0.0156%) and KAO–ZEO extract (prepared at the ratio 100 mg/mL); (<b>c</b>) Collagen synthesis assessment after exposure to the highest non-toxic concentration of ZEO (0.0156%) and KAO–ZEO extract (prepared at the ratio 100 mg/mL); (control—cells maintained in the culture medium without the ZEO and KAO–ZEO; * statistically significant results considered at <span class="html-italic">p</span> &lt; 0.05 compared to the control cells according to One-way ANOVA with post hoc Dunnett’s test).</p>
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14 pages, 5665 KiB  
Article
Sustainable Lipase Immobilization: Chokeberry and Apple Waste as Carriers
by Karina Jasińska, Maksym Nowosad, Aleksander Perzyna, Andrzej Bielacki, Stanisław Dziwiński, Bartłomiej Zieniuk and Agata Fabiszewska
Biomolecules 2024, 14(12), 1564; https://doi.org/10.3390/biom14121564 (registering DOI) - 8 Dec 2024
Abstract
In the modern world, the principles of the bioeconomy are becoming increasingly important. Recycling and reusability play a crucial role in sustainable development. Green chemistry is based on enzymes, but immobilized biocatalysts are still often designed with synthetic polymers. Insoluble carriers for immobilized [...] Read more.
In the modern world, the principles of the bioeconomy are becoming increasingly important. Recycling and reusability play a crucial role in sustainable development. Green chemistry is based on enzymes, but immobilized biocatalysts are still often designed with synthetic polymers. Insoluble carriers for immobilized biocatalysts, particularly those derived from agro-industrial waste such as mesoporous lignocellulosic materials, offer a promising alternative. By using waste materials as support for enzymes, we can reduce the environmental impact of waste disposal and contribute to the development of efficient bioprocessing technologies. The current study aimed to assess the possibility of using apple and chokeberry pomace as carriers for the immobilization of Palatase 20000L (lipase from Rhizomucor miehei). The analysis of lignocellulosic materials revealed that chokeberry pomace has a higher neutral detergent fiber (NDF) and lignin contents than apple pomace. Moreover, Scanning Electron Microscopy (SEM) observations indicated similar compact structures in both pomaces. The lipase activity assays demonstrated that immobilization of lipase from R. miehei onto apple and chokeberry pomace improves their properties, especially the synthetic activity. The findings highlight the potential of utilizing fruit pomaces not only as a source of bioactive compounds but also in enhancing enzyme stability for industrial applications. Full article
(This article belongs to the Special Issue Recent Advances in the Enzymatic Synthesis of Bioactive Compounds)
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<p>Scanning electron microphotographs (×200 and ×600) of (<b>A</b>,<b>B</b>)—native chokeberry pomace and (<b>C</b>,<b>D</b>)—native apple pomace.</p>
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<p>The hydrolytic activities of immobilized lipase onto chokeberry pomace—ChoP (native, after hexane and ethanol treatment) and apple pomace—AP (native, after hexane and ethanol treatment, measured initially (dark magenta bars) and after 6 months of storage (violet bars). Means with the same letter a or b for initial activity and A for activity after 6 months of storage did not differ significantly (α = 0.05). Means with * within one immobilized lipase preparation differ significantly (α = 0.05).</p>
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<p>The synthetic activities of immobilized lipase onto chokeberry pomace—ChoP (native, after hexane and ethanol treatment) and apple pomace—AP (native, after hexane and ethanol treatment, measured initially (dark magenta bars) and after 6 months of storage (violet bars). Means with the same letter (a–e) or (A–D) did not differ significantly. Means with * within one immobilized lipase preparation differ significantly (α = 0.05).</p>
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<p>The specific hydrolytic activities of Palatase 20000L in the free form (PAL) and immobilized onto different carrier forms. Means with the same letter (a–c) did not differ significantly (α = 0.05). Abbreviations: ChoP—chokeberry pomace, AP—apple pomace.</p>
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<p>The specific synthetic activities of Palatase 20000L in the free form (PAL) and immobilized onto different carrier forms. Means with the same letter (a–f) did not differ significantly (α = 0.05). Abbreviations: ChoP—chokeberry pomace, AP—apple pomace.</p>
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<p>Comparison of hydrolytic activity of biocatalysts for the following substrates: <span class="html-italic">p</span>-nitrophenyl butyrate (C4:0), <span class="html-italic">p</span>-nitrophenyl laurate (C12:0), <span class="html-italic">p</span>-nitrophenyl palmitate (C16:0), and <span class="html-italic">p</span>-nitrophenyl oleate (C18:1). The means compared within one enzyme preparation, marked with different lowercase letters, are statistically different (α = 0.05). Abbreviations: ChoP—chokeberry pomace, AP—apple pomace.</p>
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<p>The effect of pH (ranging from 5 to 8) on the hydrolytic activity of the produced biocatalyst. The averages compared within a single enzyme preparation across the examined pH range, indicated by distinct lowercase letters, are significantly different (α = 0.05). Abbreviations: ChoP—chokeberry pomace, AP—apple pomace.</p>
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<p>Recovery analysis of lipase immobilized onto chokeberry pomace. The highest hydrolytic activities of all biocatalysts were defined as 100%. Abbreviation: ChoP—chokeberry pomace.</p>
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<p>Recovery analysis of lipase immobilized onto apple pomace. The highest hydrolytic activities of all biocatalysts were defined as 100%. Abbreviation: AP—apple pomace.</p>
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11 pages, 544 KiB  
Article
Protective Effects of a Brassica nigra Sprout Hydroalcoholic Extract on Lipid Homeostasis, Hepatotoxicity, and Nephrotoxicity in Cyclophosphamide-Induced Toxicity in Rats
by Hassan Barakat, Thamer Aljutaily, Raghad I. Alkhurayji, Huda Aljumayi, Khalid S. Alhejji and Sami O. Almutairi
Metabolites 2024, 14(12), 690; https://doi.org/10.3390/metabo14120690 (registering DOI) - 8 Dec 2024
Abstract
Background: Brassica nigra possesses a significant concentration of bioactive compounds and has been demonstrated to have a variety of pharmacological properties, although its sprout has not been extensively studied. Thus, the protective effects of Brassica nigra sprout hydroalcoholic extract (BNSE) on lipid [...] Read more.
Background: Brassica nigra possesses a significant concentration of bioactive compounds and has been demonstrated to have a variety of pharmacological properties, although its sprout has not been extensively studied. Thus, the protective effects of Brassica nigra sprout hydroalcoholic extract (BNSE) on lipid homeostasis, hepatotoxicity, and nephrotoxicity in cyclophosphamide (CYP)-induced toxicity in rats were examined in this study. Methods: Four experimental rat groups (n = 8 for each group) were examined as follows: NR, normal rats that received normal saline by oral gavage daily; CYP, injected with a single dose of CYP at 250 mg kg−1 intraperitoneally (i.p.) and did not receive any treatment, receiving only normal saline by oral gavage daily; CYP + BNSE250, injected with a single dose of CYP at 250 mg kg−1 i.p. and treated with BNSE at 250 mg kg−1 by oral gavage daily for three weeks; and CYP + BNSE500, injected with a single dose of CYP at 250 mg kg−1 i.p. and treated with BNSE at 500 mg kg−1 by oral gavage daily for three weeks. Results: The results indicated a significant increase (p < 0.05) in triglyceride (TG), cholesterol (CHO), low-density lipoprotein cholesterol (LDL-c), and very low-density lipoprotein cholesterol (VLDL-c) levels in CYP-induced toxicity rats. The administration of BNSE at 250 and 500 mg kg−1 significantly (p < 0.05) attenuated TG, CHO, LDL-c, and VLDL-c at values comparable with the NR group. The most efficient treatment for improving the lipid profile and atherogenicity complication was BNSE at 500 mg kg−1, performing even better than 250 mg kg−1. Administrating BNSE at 250 or 500 mg kg−1 improved the liver’s function in a dose-dependent manner. Comparing the lower dose of 250 mg kg−1 of BNSE with 500 mg kg−1 showed that administrating 250 mg kg−1 attenuated alanine transaminase (ALT) by 28.92%, against 33.36% when 500 mg kg−1 was given. A similar trend was observed in aspartate aminotransferase (AST), where 19.44% was recorded for BNSE at 250 mg kg−1 and 34.93% for BNSE at 500 mg kg−1. Higher efficiency was noticed for BNSE at 250 and 500 mg kg−1 regarding alkaline phosphatase (ALP). An improvement of 38.73% for BNSE at 500 mg kg−1 was shown. The best treatment was BNSE at 500 mg kg−1, as it markedly improved liver function, such as total bilirubin (T.B.), in a dose-dependent manner. The administration of BNSE attenuated the total protein (T.P.), albumin, and globulin levels to be close to or higher than the typical values in NR rats. Conclusions: BNSE might be used for its promising hypolipidemic, hepatoprotective, and nephroprotective potential and to prevent diseases related to oxidative stress. Further research on its application in humans is highly recommended. Full article
(This article belongs to the Special Issue Plants and Plant-Based Foods for Metabolic Disease Prevention)
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<p>Effects of <span class="html-italic">B. nigra</span> sprout extract at different doses on AI in rats with CYP-induced immunosuppression (mean ± SE), <span class="html-italic">n</span> = 8. <sup>a,b,</sup> and <sup>c</sup>: bars not sharing similar letters differed significantly (<span class="html-italic">p</span> &gt; 0.05), for experimental groups, see Materials and Methods.</p>
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20 pages, 4655 KiB  
Article
Formulation of Ready-to-Use Broccoli Extracts Rich in Polyphenols and Glucosinolates Using Natural Deep Eutectic Solvents
by Ivona Karaula, Emma Vasung, Anja Damjanović, Manuela Panić, Mia Radović, Kristina Radošević, Martina Bagović Kolić, Marina Cvjetko Bubalo and Ivana Radojčić Redovniković
Molecules 2024, 29(23), 5794; https://doi.org/10.3390/molecules29235794 (registering DOI) - 7 Dec 2024
Abstract
Broccoli is rich in biologically active compounds, especially polyphenols and glucosinolates, known for their health benefits. Traditional extraction methods have limitations, leading to a shift towards using natural deep eutectic solvents (NADESs) to create high-quality extracts with enhanced biological activity. This study focuses [...] Read more.
Broccoli is rich in biologically active compounds, especially polyphenols and glucosinolates, known for their health benefits. Traditional extraction methods have limitations, leading to a shift towards using natural deep eutectic solvents (NADESs) to create high-quality extracts with enhanced biological activity. This study focuses on preparing broccoli extracts in NADES, enriched with polyphenols and glucosinolates, without additional purification steps. Using the COSMOtherm software, the solubility of polyphenols and glucosinolates in NADESs was predicted, and five biocompatible betaine-based NADESs were prepared with glucose (B:Glc1:1 and B:Glc5:2), sucrose (B:Suc), glycerol (B:Gly), and malic acid (B:MA) as hydrogen bond donors. The resulting extracts were assessed for total polyphenol and glucosinolate content, along with antioxidant capacity, using the ORAC assay. The results demonstrated that NADES extracts contained higher polyphenol content and exhibited enhanced antioxidant effects compared to the reference ethanol extract, with B:Glc1:1 extract showing the highest performance among all the extracts tested. On the other hand, the extract based on B:MA exhibited nearly six times higher total glucosinolate content compared to the ethanol extract. Additionally, polyphenols and glucosinolates were generally more stable in NADES extracts than in the reference solvent. Finally, the B:Glc1:1 extract, identified as optimal in terms of polyphenol and glucosinolate content and stability, exhibited mild stimulation of HaCaT cells growth and facilitated the wound-healing process. Through green chemistry parameter calculations, we demonstrated that the extraction of broccoli bioactives using B:Glc1:1 can be considered sustainable, underscoring the potential of NADESs for producing ready-to-use plant extracts. Full article
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<p>Structures of quercetin, ferulic acid, and glucoraphanin used as input parameters for COSMOtherm calculations.</p>
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<p>(<b>A</b>) Total polyphenolic content in the prepared broccoli extracts. (<b>B</b>) ORAC values of the prepared extracts. Results are expressed as the means (<span class="html-italic">n</span> = 3) ± S.D.</p>
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<p>Glucosinolate profile of NADESs and ethanol (70%, <span class="html-italic">v</span>/<span class="html-italic">v</span>) extracts of broccoli. Results are presented as mean ± S.D. (<span class="html-italic">n</span> = 3).</p>
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<p>Residual concentration of total polyphenols in broccoli extracts: polyphenol content in extracts stored at 4 °C (<b>A</b>) and 25 °C (<b>B</b>), expressed as the ratio of polyphenols concentration in the extract after incubation and the initial polyphenol concentration in the extract. Results are presented as mean ± S.D. (<span class="html-italic">n</span> = 3).</p>
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<p>Residual concentration of glucosinolates in broccoli extracts: aliphatic glucosinolates in extracts stored at 25 °C (<b>A</b>) and 4 °C (<b>B</b>), and indole glucosinolates in extracts stored at 25 °C (<b>C</b>) and 4 °C (<b>D</b>), expressed as the ratio of glucosinolate concentration in the extract after incubation to the initial glucosinolate concentration in the extract. Results are presented as mean ± S.D. (<span class="html-italic">n</span> = 3).</p>
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<p>Radar plot evaluating the extracts in terms of target properties. The radar chart is bounded by the specific lower and upper limits for each target property. Ratings, ranging from 0 to 100, reflect the performance of extracts relative to the best candidate for each target property.</p>
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<p>(<b>A</b>) Effect of B:Glc<sub>1:1</sub> and corresponding extract on HaCat cell viability determined by the MTS assay in volume ratio 0.5–5% (<span class="html-italic">v</span>/<span class="html-italic">v</span>). (<b>B</b>) Migration assessment of HaCaT cells: the percentage of wound closure, determined from changes in gap width from the initial scratch over 24 and 48 h. (<b>C</b>) Microscopic images from in vitro scratch wound-healing assays showing cell migration into the cell-free gap (outlined) over time, comparing untreated cells as control with cells treated with B:Glc<sub>1:1</sub> broccoli extract and B:Glc<sub>1:1</sub> alone.</p>
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13 pages, 1317 KiB  
Article
Bioactivation, Mutagenicity, DNA Damage, and Oxidative Stress Induced by 3,4-Dimethylaniline
by Mariam R. Habil, Raúl A. Salazar-González, Mark A. Doll and David W. Hein
Biomolecules 2024, 14(12), 1562; https://doi.org/10.3390/biom14121562 (registering DOI) - 7 Dec 2024
Abstract
3,4-Dimethylaniline (3,4-DMA) is present in cigarette smoke and widely used as an intermediate in dyes, drugs, and pesticides. Nucleotide excision repair-deficient Chinese hamster ovary (CHO) cells stably transfected with human CYP1A2 and N-acetyltransferase 1 (NAT1) alleles: NAT1*4 (reference allele) or NAT1*14B (the most [...] Read more.
3,4-Dimethylaniline (3,4-DMA) is present in cigarette smoke and widely used as an intermediate in dyes, drugs, and pesticides. Nucleotide excision repair-deficient Chinese hamster ovary (CHO) cells stably transfected with human CYP1A2 and N-acetyltransferase 1 (NAT1) alleles: NAT1*4 (reference allele) or NAT1*14B (the most common variant allele) were utilized to assess 3,4-DMA N-acetylation and hypoxanthine phosphoribosyl transferase (HPRT) mutations, double-strand DNA breaks and reactive oxygen species (ROS). CHO cells expressing NAT1*4 exhibited significantly (p < 0.001) higher 3,4-DMA N-acetylation rates than CHO cells expressing NAT1*14B both in vitro and in situ. In CHO cells expressing CYP1A2 and NAT1, 3,4-DMA caused concentration-dependent increases in reactive oxygen species (ROS), double-stranded DNA damage, and HPRT mutations. CHO cells expressing NAT1*4 and NAT1*14B exhibited concentration-dependent increases in ROS following treatment with 3,4-DMA (linear trend p < 0.001 and p < 0.0001 for NAT1*4 and NAT1*14B, respectively) that were lower than in CHO cells expressing CYP1A2 alone. DNA damage and oxidative stress induced by 3,4-DMA did not differ significantly (p >0.05) between CHO cells expressing NAT1*4 and NAT1*14B. CHO cells expressing NAT1*14B showed higher HPRT mutants (p < 0.05) than CHO cells expressing NAT1*4. These findings confirm 3,4-DMA genotoxicity consistent with potential carcinogenicity. Full article
(This article belongs to the Special Issue DNA Damage, Mutagenesis, and Repair Mechanisms)
14 pages, 4938 KiB  
Article
Attenuating Oxidative Damage with Macelignan in Glutamate-Induced HT22 Hippocampal Cells
by Mei Tong He, Kiwon Jung, Chan-Woong Park, Young-Won Chin and Ki Sung Kang
Appl. Sci. 2024, 14(23), 11408; https://doi.org/10.3390/app142311408 (registering DOI) - 7 Dec 2024
Abstract
Macelignan, from Myristica fragrans (nutmeg), is a bioactive compound with various pharmacological properties, including anti-inflammatory and neuroprotective activities. The purpose of this work was to investigate the antioxidant and anti-apoptotic effects of macelignan in glutamate-treated HT22 mouse hippocampal neurons. Macelignan was extracted and [...] Read more.
Macelignan, from Myristica fragrans (nutmeg), is a bioactive compound with various pharmacological properties, including anti-inflammatory and neuroprotective activities. The purpose of this work was to investigate the antioxidant and anti-apoptotic effects of macelignan in glutamate-treated HT22 mouse hippocampal neurons. Macelignan was extracted and identified in a methanol extract of M. fragrans seeds. The DPPH was used to assess the antioxidative activity of macelignan. Glutamate (5 mM) was used to induce neurotoxicity in the HT22 cells. Neuroprotective effects were measured using relevant biochemical and imaging assays, including cell viability, ROS production, nuclear staining, apoptotic cell death, and protein expression. Macelignan markedly and concentration-dependently enhanced DPPH radical scavenging activity. In the HT22 cell model, glutamate induced cell damage by decreasing cell viability, promoting ROS generation, and increasing apoptotic cell death according to cell morphological changes. However, macelignan treatment restored cell viability, inhibited ROS generation concentration-dependently, and reduced apoptosis. Moreover, glutamate significantly up-regulated the phosphorylation of MAPK-pathway-related proteins, which was reversed by macelignan treatment. In conclusion, macelignan shows notable neuroprotective effects on oxidative stress and apoptotic cell death in glutamate-induced cells, and this study provides useful information on its potential therapeutic implications in neurological disorders. Full article
18 pages, 4884 KiB  
Article
Evaluation of the Leaves and Seeds of Cucurbitaceae Plants as a New Source of Bioactive Compounds for Colorectal Cancer Prevention and Treatment
by Mercedes Peña, Ana Guzmán, Cristina Mesas, Jesús M. Porres, Rosario Martínez, Francisco Bermúdez, Consolación Melguizo, Laura Cabeza and Jose Prados
Nutrients 2024, 16(23), 4233; https://doi.org/10.3390/nu16234233 (registering DOI) - 7 Dec 2024
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Abstract
Background/Objectives: The Cucurbitaceae family represents an important source of bioactive compounds with antioxidant, antimicrobial, anti-inflammatory and antitumor activities. This study aims to investigate the potential application of Cucurbitaceae leaves and seed extracts to prevent and treat colorectal cancer (CRC). Methods: Four extracts (ethanol [...] Read more.
Background/Objectives: The Cucurbitaceae family represents an important source of bioactive compounds with antioxidant, antimicrobial, anti-inflammatory and antitumor activities. This study aims to investigate the potential application of Cucurbitaceae leaves and seed extracts to prevent and treat colorectal cancer (CRC). Methods: Four extracts (ethanol extracts and protein extracts and hydrolysates) from the leaves and seeds of cucurbits were tested in T-84, HCT-15 and HT-29 CRC cells. The antitumor, antiangiogenic, antioxidant and chemopreventive potentials and bioactive composition of the active extracts were characterized. Results: Cold ethanolic extracts from the leaves and seeds of two interspecific Cucurbita genera (CLU01002 and COK01001) exhibited potent antiproliferative, specific and non-hepatotoxic activity against CRC cell lines, with a slight synergistic effect in combination with oxaliplatin. This antitumor activity was related to G2/M cell cycle arrest, the extrinsic apoptosis pathway, cytokinesis inhibition and autophagy. The extracts also inhibited tumor clonogenicity and angiogenesis, and modulated cancer stem cell (CSC) gene expression, as well as expressing antioxidant and chemopreventive cellular capabilities. Finally, phenolic and cucurbitane-type triterpenoid compounds (pengxianencins and cucurbitacins) were tentatively identified in the active extracts by UPLC-MS analysis and bioguided fractionation. Conclusions: Extracts from leaves the and seeds of two interspecific Cucurbita genera (CLU01002 and COK01001) may contribute to the improvement of prevention and treatment strategies for CRC patients. Full article
(This article belongs to the Section Phytochemicals and Human Health)
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<p>Antitumor potential of cEtOH from the leaves (L) and seeds (S) of CLU and COK plants alone or in combination with chemotherapeutic drugs. (<b>a</b>) Relative proliferation (RP, %) of cell lines treated with cEtOH for 72 h was determined by SRB assay. Data are the mean ± SD of three replicates from two different extractions. (<b>b</b>) HSA synergy scores of T-84 cells co-treated with cEtOH and 5-FU or OXA were plotted on heatmaps with red for synergy (&gt;10), white for additive effect (from −10 to 10) and green for antagonism (&lt;−10), using SynergyFinder Plus.</p>
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<p>Cell cycle and apoptosis analysis of T-84 cells treated with cEtOH extracts from CLU and COK plants. (<b>a</b>) Cell population distribution of T-84 cells exposed to cEtOH from the leaves (L) and seeds (S) of CLU and COK for cell cycle analysis (48 and 72 h) and (<b>b</b>) for the study of apoptosis (48 h) using flow cytometry. Results are expressed as mean ± SD of three replicates. (<b>c</b>) Representative Western blot images of T-84 cells treated with cEtOH from L and S of CLU and COK for 24 h (caspase-8 and -9 and γ-H2AX) and 72 h (PARP1). WB images of PARP1 were obtained by splicing different lanes. (<b>d</b>) Relative protein expression was calculated as the mean ± SD of three measurements from three Western blot experiments. Statistical significance compared to control cells: <span class="html-italic">p</span> value &lt; 0.05 (*); &lt;0.01 (**); &lt;0.001 (***).</p>
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<p>Cellular microtubule organization and autophagy process in T-84 cells treated with cEtOH extracts from CLU and COK plants. (<b>a</b>) Representative fluorescent microscopy images of α-tubulin (upper-green, amplified from 20× magnification) and acidic vesicles (lower-red, indicated by arrows, original 40× magnification) in cells treated with cEtOH from the leaves (L) and seeds (S) of CLU and COK for 24 h. Cell nuclei (blue) were stained with Hoechst 33342. (<b>b</b>) Lysotracker/Hoechst staining ratio relative to control cells was quantified using ImageJ software as the mean ± SD of three images from four replicates. (<b>c</b>) Determination of LC3B protein expression in T-84 cells treated with cEtOH from L and S of CLU and COK (24 h) by Western blot. The LC3B-II/LC3B-I ratio was calculated as the mean ± SD of three Western blot replicates. Statistical significance compared to control cells: <span class="html-italic">p</span> value &lt; 0.001 (***).</p>
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<p>Study of clonogenicity and cell migration of T-84 cells treated with cEtOH extracts from CLU and COK plants. (<b>a</b>) Representative images of T-84 cells colonies (12 days) stained with SRB and graph representation of the percentage of colony formation. Cells were pretreated (72 h) with cEtOH (IC<sub>25</sub> and IC<sub>75</sub>) from the leaves (L) and seeds (S) of CLU and COK. (<b>b</b>) Representative light microscopy images of wound healing assay in T-84 cells treated with cEtOH from L and S of CLU and COK (4× magnification), and graphical representation of the percentage of cell migration. Data were represented as the mean ± SD of triplicate cultures. Statistical significance compared to control cells: <span class="html-italic">p</span> value &lt; 0.05 (*); &lt;0.001 (***).</p>
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<p>Study of the antiangiogenic potential of cEtOH extracts from CLU and COK plants. (<b>a</b>) Stereomicroscope images of the CAM (treatment, external and intermediate areas respect to the ring) treated with saline solution (40 μL/egg; negative control), aflibercept (4 mg/mL; positive control) and cEtOH from the leaves (L) and seeds (S) of CLU and COK (250 μg/mL) for 72 h (3× magnification). (<b>b</b>) Vascular density and vascular length density areas presented as the mean ± SD (n = 4). (<b>c</b>) Western blot of T-84 cells’ VEGFA expression after treatment (24 h) with cEtOH from L and S of CLU and COK. WB images of VEGFA were obtained by splicing different lanes. The VEGFA/β-actin ratio was presented as the mean ± SD of three measures from three Western blot experiments. Statistical significance compared to negative control: <span class="html-italic">p</span> value &lt; 0.05 (*); &lt;0.01 (**); &lt;0.001 (***).</p>
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<p>In vitro antioxidant and chemopreventive activity of cEtOH extracts from CLU and COK plants. (<b>a</b>) Percentage of relative viability of cells pretreated with cEtOH extracts (non-toxic doses) and exposed to hydrogen peroxide (H<sub>2</sub>O<sub>2</sub>). Relative viability (RV, %) was calculated by MTT assay and results are expressed as the mean ± SD of 8 replicates. The statistically significant differences were calculated compared to treated cells treated with H<sub>2</sub>O<sub>2</sub>: <span class="html-italic">p</span> value &lt; 0.01 (**); &lt;0.001 (***). (<b>b</b>) Glutathione S-Transferase (GST) and NAD(P)H quinone oxidoreductase (QR) activity in cytosolic fractions obtained from HT-29 cells treated with cEtOH. Sulforaphane (SFN) was used as positive control. Statistical significance compared to control cells: <span class="html-italic">p</span> value &lt; 0.05 (*); &lt;0.001 (***).</p>
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<p>UPLC-MS chromatographic profiles of cEtOH obtained from leaves and seeds of CLU and COK plants. The highest peaks were highlighted and tentatively identified in mass spectrometry databases such as the Dictionary of Natural Products and the Chemspider database.</p>
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28 pages, 1315 KiB  
Article
In Vitro Evaluation, Chemical Profiling, and In Silico ADMET Prediction of the Pharmacological Activities of Artemisia absinthium Root Extract
by Asma N. Alsaleh, Ibrahim M. Aziz, Reem M. Aljowaie, Rawan M. Alshalan, Noorah A. Alkubaisi and Mourad A. M. Aboul-Soud
Pharmaceuticals 2024, 17(12), 1646; https://doi.org/10.3390/ph17121646 (registering DOI) - 7 Dec 2024
Viewed by 37
Abstract
Artemisia absinthium L., is a plant with established pharmacological properties, but the A. absinthium root extract (AARE) remains unexplored. The aim of this study was to examine the chemical composition of AARE and assess its biological activity, which included antidiabetic, antibacterial, anticancer, and [...] Read more.
Artemisia absinthium L., is a plant with established pharmacological properties, but the A. absinthium root extract (AARE) remains unexplored. The aim of this study was to examine the chemical composition of AARE and assess its biological activity, which included antidiabetic, antibacterial, anticancer, and antioxidant properties. GC-MS was used to analyze the chemical components. The antioxidant activity of the total phenolic and flavonoid content was evaluated. Antibacterial activity and cytotoxic effects were identified. Enzyme inhibition experiments were performed to determine its antidiabetic potential. Molecular docking was utilized to evaluate the potential antioxidant, antibacterial, and anticancer activities of the compounds from AARE using Maestro 11.5 from the Schrödinger suite. AARE exhibited moderate antioxidant activity in DPPH (IC50: 172.41 ± 3.15 μg/mL) and ABTS (IC50: 378.94 ± 2.18 μg/mL) assays. Cytotoxicity tests on MCF-7 and HepG2 cancer cells demonstrated significant anticancer effects, with IC50 values of 150.12 ± 0.74 μg/mL and 137.11 ± 1.33 μg/mL, respectively. Apoptotic studies indicated an upregulation of pro-apoptotic genes (caspase-3, 8, 9, Bax) and a downregulation of anti-apoptotic markers (Bcl-2 and Bcl-Xl). AARE also inhibited α-amylase and α-glucosidase, suggesting potential antidiabetic effects, with IC50 values of 224.12 ± 1.17 μg/mL and 243.35 ± 1.51 μg/mL. Antibacterial assays revealed strong activity against Gram-positive bacteria. Molecular docking and pharmacokinetic analysis identified promising inhibitory effects of key AARE compounds on NADPH oxidase, E. coli Gyrase B, and Topoisomerase IIα, with favorable drug-like properties. These findings suggest AARE’s potential in treating cancer, diabetes, and bacterial infections, warranting further in vivo and clinical studies. Full article
21 pages, 6961 KiB  
Article
Composition of Human-Associated Gut Microbiota Determines 3-DF and 3-HF Anti-Colitic Activity in IL-10 -/- Mice
by Jose Haro-Reyes, Jayaprakash Kanijam Raghupathi and Lavanya Reddivari
Nutrients 2024, 16(23), 4232; https://doi.org/10.3390/nu16234232 (registering DOI) - 7 Dec 2024
Viewed by 78
Abstract
Background: Gut bacterial dysbiosis along with intestinal mucosal disruption plays a critical role in inflammatory disorders like ulcerative colitis. Flavonoids and other food bioactives have been studied in mice models as alternative treatments with minimal side effects. However, most of the research has [...] Read more.
Background: Gut bacterial dysbiosis along with intestinal mucosal disruption plays a critical role in inflammatory disorders like ulcerative colitis. Flavonoids and other food bioactives have been studied in mice models as alternative treatments with minimal side effects. However, most of the research has been carried out with mice-native microbiota, which limits the comprehension of the interaction between flavonoids and human-associated bacteria. Hence, the objective of our study was to determine the effect of healthy human-associated microbiota on the anti-colitic activity of diets rich in anthocyanins (3-HF) and phlobaphenes (3-DF). Methods: In this regard, the interleukin (IL)-10 -/- mice model was utilized. Mice were divided into three groups for inoculation with human gut bacteria from three different healthy donors and assigned to four diets. A purified diet (Diet P) and three diets containing 25% near-isogenic lines (NILs) of corn were evaluated. Diets were substituted with NILs expressing only 3-DFs (diet B), only 3-HFs (diet C), and both 3-DF and 3-HF (diet D). Results: In an overall analysis, flavonoid-rich diets did not affect inflammatory markers, microbiota diversity, or gut metabolites, but diets containing anthocyanins improved barrier function parameters. However, when data was segmented by the recipient’s microbiota from different human donors, the diet effects became significant. Furthermore, 3-HFs showed more beneficial effects than 3-DFs across the recipient’s microbiota. Conclusions: Our study suggests that the anti-colitic activity of 3-DF and 3-HF and their gut metabolites depends on the donor’s microbial composition. Full article
(This article belongs to the Special Issue Anthocyanins and Human Health—2nd Edition)
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<p>Experimental design. Fecal microbial transplantation (FMT), near-isogenic lines (NILs), ulcerative colitis (UC). Human fecal donors: H-1, H-2, and H-3.</p>
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<p>Overall diet effects on anatomic and symptomatic parameters. Liver (<b>A</b>), spleen (<b>B</b>), kidneys (<b>C</b>), colon (<b>D</b>), cecum (<b>E</b>), and colon length (<b>F</b>) are expressed as ratios of body weight, together with the percentage of weight loss (<b>G</b>) and disease activity index (<b>H</b>). Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D). Replicates (<span class="html-italic">n</span> = 9–12) are shown for every diet. Statistical differences are represented by (*) <span class="html-italic">p</span> ≤ 0.05, and (#) <span class="html-italic">p</span> ≤ 0.10.</p>
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<p>Diet effects on anatomic and symptomatic parameters by microbiota of donor’s recipients. Liver (<b>A</b>), spleen (<b>B</b>), kidneys (<b>C</b>), colon (<b>D</b>), cecum (<b>E</b>), and colon length (<b>F</b>) are expressed as ratios of body weight, together with the percentage of weight loss <b>G</b>) and disease activity index (<b>H</b>). Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D). Human fecal donors: H-1, H-2, and H-3. Replicates (<span class="html-italic">n</span> = 3–5) are shown for every diet per donor. Statistical differences are represented by (*) <span class="html-italic">p</span> ≤ 0.05, and (#) <span class="html-italic">p</span> ≤ 0.10.</p>
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<p>Overall diet effects on PRRs and inflammatory markers. mRNA expression of TLR-4 (<b>A</b>), TLR-5 (<b>B</b>), NF-κB (<b>C</b>), TNF-α (<b>D</b>), IL-1β (<b>E</b>), and IL-6 (<b>F</b>). Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D). Replicates (<span class="html-italic">n</span> = 9–12) are shown for every diet.</p>
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<p>Diet effects on PPRs and inflammatory markers by microbiota of donor’s recipients. mRNA expression of TLR-4 (<b>A</b>), TLR-5 (<b>B</b>), NF-κB (<b>C</b>), TNF-α (<b>D</b>), IL-1β (<b>E</b>), and IL-6 (<b>F</b>). Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D). Human fecal donors: H-1, H-2, and H-3. Replicates (<span class="html-italic">n</span> = 3–5) are shown for every diet per donor. Statistical differences are represented by (*) <span class="html-italic">p</span> ≤ 0.05, and (#) <span class="html-italic">p</span> ≤ 0.10.</p>
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<p>The effect of diet on gut permeability, mucus protection, and tight junction proteins. FITC concentration in serum (<b>A</b>), mRNA expression of Muc2 (<b>B</b>), occludin (<b>C</b>), and TJP-1 (<b>D</b>). Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D). Replicates (<span class="html-italic">n</span> = 9–12) are shown for every diet. Statistical differences are represented by (*) <span class="html-italic">p</span> ≤ 0.05, and (#) <span class="html-italic">p</span> ≤ 0.10.</p>
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<p>On the effect of diet on gut permeability, mucus protection, and tight junction proteins by the microbiota of each donor’s recipients. FITC serum concentration (<b>A</b>), mRNA expression of Muc2 (<b>B</b>), occludin (<b>C</b>), and TJP-1 (<b>D</b>). Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D). Human fecal donors: H-1, H-2, and H-3. Replicates (<span class="html-italic">n</span> = 3–5) are shown for every diet per donor. Statistical differences are represented by (*) <span class="html-italic">p</span> ≤ 0.05, and (#) <span class="html-italic">p</span> ≤ 0.10.</p>
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<p>Overall diet effects on α-diversity indexes. Shannon index (<b>A</b>), Pielou evenness (<b>B</b>), Faith phylogenetic diversity (<b>C</b>), and observed features (<b>D</b>). Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D). Replicates (<span class="html-italic">n</span> = 9–12) are shown for every diet.</p>
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<p>Principal coordinate analysis of β-diversity. Jaccard index (<b>A</b>) and Bray–Curtis dissimilarity (<b>B</b>), unweighted UniFrac (<b>C</b>), and weighted UniFrac (<b>D</b>) distances. Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D). Human fecal donors: H-1, H-2, and H-3. Replicates (<span class="html-italic">n</span> = 9–12) are shown for every diet.</p>
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<p>Overall taxonomic diversity plot showing the relative abundance of gut microbiota at the family level per dietary treatment. Taxa higher than 1% relative abundance is plotted. Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D).</p>
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<p>Taxonomic diversity plot showing diet effects in the relative abundance of gut microbiota Families by donor of microbiota. Taxa higher than 1% relative abundance is plotted. H-1, H-2, and H-3 refer to the human fecal donors. Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D).</p>
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<p>Overall diet effect on gut metabolites: short-chain fatty acids and primary bile acids. SCFAs: acetate (<b>A</b>), propionate (<b>B</b>), butyrate (<b>C</b>), and bile acids: glycocholic acid, GCA (<b>D</b>), taurochenodeoxycholic acid, TCDCA (<b>E</b>), tauroursodeoxycholic acid, TUDCA (<b>F</b>), cholic acid, CA (<b>G</b>), chenodeoxycholic acid, CDCA (<b>H</b>), α-murocholic acid, α-MCA (<b>I</b>) and β-murocholic acid, β-MCA (<b>J</b>). Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D). Replicates (<span class="html-italic">n</span> = 9–12) are shown for every diet. Statistical differences are represented by (*) <span class="html-italic">p</span> ≤ 0.05.</p>
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<p>Dietary effect on gut metabolites: short-chain fatty acids and primary bile acids by microbiota of donor’s recipients. SCFAs: acetate (<b>A</b>), propionate (<b>B</b>), butyrate (<b>C</b>), and bile acids: glycocholic acid, GCA (<b>D</b>), taurochenodeoxycholic acid, TCDCA (<b>E</b>), tauroursodeoxycholic, TUDCA (<b>F</b>), cholic acid, CA (<b>G</b>), chenodeoxycholic acid, CDCA (<b>H</b>), α-murocholic acid, α-MCA (<b>I</b>) and β-murocholic acid, β-MCA (<b>J</b>). Diets: purified (P), and 25% inclusion of maize NIL with 3-DFs (B), 3-HFs (C), or both 3-DF + 3HF (D). Human fecal donors: H-1, H-2, and H-3. Replicates (<span class="html-italic">n</span> = 3–5) are shown for every diet per donor. Statistical differences are represented by (*) <span class="html-italic">p</span> ≤ 0.05, and (#) <span class="html-italic">p</span> ≤ 0.10.</p>
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<p>Correlation heatmap between biomarkers and gut metabolites. Darker colors represent higher positive correlations, while lighter represent highly negative correlations. Only significant <span class="html-italic">p</span> &lt; 0.05 correlations are shown. Pattern recognition receptors: toll-like receptor-4, TLR-4, toll-like receptor-5, TLR-5. Inflammatory markers: interleukin-1β, IL-1β, interleukin 6, IL-6, tumor necrotic factor- α, TNF-α. Tight junction proteins: occludin and tight junction protein 1, TJP-1. Mucin 2: Muc2. Disease activity index: DAI. Bile acids: glycocholic acid, GCA, taurochenodeoxycholic acid, TCDCA, tauroursodeoxycholic, TUDCA, cholic acid, CA, chenodeoxycholic acid, CDCA, α-murocholic acid, α-MCA, and β-murocholic acid, β-MCA.</p>
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22 pages, 3147 KiB  
Article
Deciphering the Phytochemical Potential of Hemp Hairy Roots: A Promising Source of Cannabisins and Triterpenes as Bioactive Compounds
by Naomi Kaminsky, Jane Hubert, Cédric Guerin, Malak Mazlani, Alexis Kotland, Victor Pozzobon, Blandine Marant, Héloïse Mailhac and Stéphane Poigny
Molecules 2024, 29(23), 5792; https://doi.org/10.3390/molecules29235792 (registering DOI) - 7 Dec 2024
Viewed by 87
Abstract
Cannabis sativa L., specifically hemp, is a traditional herbaceous plant with industrial and medicinal uses. While much research has focused on cannabinoids and terpenes, the potential of hemp roots is less explored due to bioproduction challenges. Still, this material is rich in bioactive [...] Read more.
Cannabis sativa L., specifically hemp, is a traditional herbaceous plant with industrial and medicinal uses. While much research has focused on cannabinoids and terpenes, the potential of hemp roots is less explored due to bioproduction challenges. Still, this material is rich in bioactive compounds and demonstrates promising anti-inflammatory, antimicrobial, and antioxidant properties. Biotechnological methods, such as hairy root cultures, enable the efficient production of specialized metabolites while avoiding the issues of outdoors cultures. Despite these benefits, the chemical diversity understanding of hemp hairy roots remains limited. In this study, we conducted an extensive NMR and LC/MS chemical profiling of hemp hairy roots to determine their chemical composition, revealing the presence of cannabisins for the first time. We then investigated the accumulation of cannabisins and triterpenes in both hemp hairy roots and hemp aeroponic roots. Our findings reveal that hairy roots produce 12 times more cannabisins and 6 times more triterpenes than aeroponic roots, respectively, in addition to yielding 3 times more biomass in bioreactors. Preliminary bioassays also suggest antioxidant and antifungal properties. This research underscores the potential of hemp hairy roots as a valuable source of specialized metabolites and calls for further exploration into their bioactive compounds and applications. Full article
(This article belongs to the Special Issue Recent Advances in Cannabis and Hemp Research)
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<p>HHR and HAR development from 0 to 42 days of culture and harvested biomass. In vitro HHRs were grown in Erlenmeyer for 21 days, transferred to a 1 L-bioreactor (<span class="html-italic">n</span> = 3), and further cultivated until the harvest at 42 days. HARs were grown from 10-day plantlets (<span class="html-italic">n</span> = 3) and transferred to a semi-controlled indoor aeroponic system until the harvest on day 42.</p>
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<p>Chemical structures of the prevailing molecules unambiguously identified by NMR in HHR-UP and HHR-LOW.</p>
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<p>LC/MS BPI chromatogram (ESI+ and ESI−) of the extracts HHR-UP and HHR-LOW.</p>
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<p>Chemical structures of cannabisins.</p>
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<p>Chromatograms of friedelin and epifriedelanol quantification in HHR DMSO extract by GC-FID and their chemical structures.</p>
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<p>Quantification of triterpenes and cannabisins in HHRs and HARs. (<b>a</b>) Quantification of triterpenes from DMSO extracts of HHRs and HARs using GC-FID. Significantly higher amounts of triterpenes have been quantified in HHRs compared to HARs. Data are shown in mg/g. (<b>b</b>) Quantification of cannabisins from methanolic extracts of HHRs and HARs using UHPLC-QToF. Significantly higher amounts of cannabisins have been quantified in HHRs compared to HARs. Data are shown in µg/g. The values are displayed as the mean ± standard deviation of the biological triplicate (<span class="html-italic">n</span> = 3) and the technical triplicate (<span class="html-italic">n</span> = 3). Significant differences are indicated by asterisks: ***, <span class="html-italic">p</span> &lt; 0.001; ****, <span class="html-italic">p</span> &lt; 0.00001.</p>
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<p>Antifungal and antioxidant activities of HHR and HAR non-polar extracts: (<b>a</b>) Inhibition of <span class="html-italic">Saccharomyces cerevisiae</span> growth over time by 200 µg of HHR and HAR non-polar extracts prepared at 100 mg/mL in DMSO with DMSO as a negative control. (<b>b</b>) Radical Scavenging Activity shows as gallic acid equivalent, showing assessment of HHR and HAR non-polar extract antioxidant activities at 10 µg in reaction to ABTS solution. The values are displayed as the mean ± standard deviation of the technical replicate (<span class="html-italic">n</span> = 3).</p>
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<p>Establishment of hemp hairy root clones. (<b>a</b>) Selected hemp hairy root clone in solid culture media. (<b>b</b>) PCR analysis of HHR transformed with <span class="html-italic">R. rhizogenes</span> to verify the presence of <span class="html-italic">rol</span> B (T-DNA marker) and <span class="html-italic">Vir</span> G genes (<span class="html-italic">R. rhizogenes</span> marker). The DNA of <span class="html-italic">R. rhizogenes</span> was used as positive control (+) and water as negative control (−).</p>
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26 pages, 1451 KiB  
Review
Thraustochytrids: Evolution, Ultrastructure, Biotechnology, and Modeling
by Aleksei G. Menzorov, Daniil A. Iukhtanov, Ludmila G. Naumenko, Aleksandr V. Bobrovskikh, Ulyana S. Zubairova, Ksenia N. Morozova and Alexey V. Doroshkov
Int. J. Mol. Sci. 2024, 25(23), 13172; https://doi.org/10.3390/ijms252313172 (registering DOI) - 7 Dec 2024
Viewed by 112
Abstract
The thraustochytrids are a group of marine protists known for their significant ecological roles as decomposers and parasites as well as for their potential biotechnological applications, yet their evolutionary and structural diversity remains poorly understood. Our review critically examines the phylogeny of this [...] Read more.
The thraustochytrids are a group of marine protists known for their significant ecological roles as decomposers and parasites as well as for their potential biotechnological applications, yet their evolutionary and structural diversity remains poorly understood. Our review critically examines the phylogeny of this taxa, utilizing available up-to-date knowledge and their taxonomic classifications. Additionally, advanced imaging techniques, including electron microscopy, are employed to explore the ultrastructural characteristics of these organisms, revealing key features that contribute to their adaptive capabilities in varying marine environments. The integration of this knowledge with available omics data highlights the huge biotechnological potential of thraustochytrids, particularly in producing ω-3 fatty acids and other bioactive compounds. Our review underscores the importance of a systems biology approach in understanding thraustochytrids biology and highlights the urgent need for novel, accurate omics research to unlock their full biotechnological potential. Overall, this review aims to foster a deeper appreciation of thraustochytrids by synthesizing information on their evolution, ultrastructure, and practical applications, thereby providing a foundation for future studies in microbiology and biotechnology. Full article
(This article belongs to the Section Molecular Genetics and Genomics)
30 pages, 3535 KiB  
Review
Exploring Antimicrobial Compounds from Agri-Food Wastes for Sustainable Applications
by Mattia Di Maro, Luca Gargiulo, Giovanna Gomez d’Ayala and Donatella Duraccio
Int. J. Mol. Sci. 2024, 25(23), 13171; https://doi.org/10.3390/ijms252313171 (registering DOI) - 7 Dec 2024
Viewed by 133
Abstract
Transforming agri-food wastes into valuable products is crucial due to their significant environmental impact, when discarded, including energy consumption, water use, and carbon emissions. This review aims to explore the current research on the recovery of bioactive molecules with antimicrobial properties from agri-food [...] Read more.
Transforming agri-food wastes into valuable products is crucial due to their significant environmental impact, when discarded, including energy consumption, water use, and carbon emissions. This review aims to explore the current research on the recovery of bioactive molecules with antimicrobial properties from agri-food waste and by-products, and discusses future opportunities for promoting a circular economy in its production and processing. Mainly, antibacterial molecules extracted from agri-food wastes are phenolic compounds, essential oils, and saponins. Their extraction and antimicrobial activity against a wide spectrum of bacteria is analyzed in depth. Also, their possible mechanisms of activity are described and classified based on their effect on bacteria, such as the (i) alteration of the cell membrane, (ii) inhibition of energy metabolism and DNA synthesis, and iii) disruption of quorum sensing and biofilm formation. These bioactive molecules have a wide range of possible applications ranging from cosmetics to food packaging. However, despite their potential, the amount of wastes transformed into valuable compounds is very low, due to the high costs relating to their extraction, technical challenges in managing supply chain complexity, limited infrastructure, policy and regulatory barriers, and public perception. For these reasons, further research is needed to develop cost-effective, scalable technologies for biomass valorization. Full article
(This article belongs to the Special Issue Bioactive Materials with Antimicrobial Properties: 2nd Edition)
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<p>The application green principles to valorize agricultural waste within a circular economy framework. Reproduced from [<a href="#B11-ijms-25-13171" class="html-bibr">11</a>].</p>
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<p>Some examples of antimicrobial tests carried out using biomolecules obtained from agri-food waste valorization. (<b>1</b>) Antimicrobial activity of four grape seed extracts (<b>A</b>–<b>D</b>) against <span class="html-italic">S. aureus</span> (zone 1, 0.50 mg/mL extract; zone 2, 0.25 mg/mL; zone 3, 0.10 mg/mL; zone 4, 0.05 mg/mL; zone 5, negative control) (reproduced from [<a href="#B60-ijms-25-13171" class="html-bibr">60</a>]). (<b>2</b>) Inhibition halos obtained for <span class="html-italic">C. perfringens</span>, <span class="html-italic">C. botulinum</span> and <span class="html-italic">C. difficile</span> in the screening test using two different extracts of saffron petals (SPE A and SPE B) (reproduced from [<a href="#B70-ijms-25-13171" class="html-bibr">70</a>]) and (<b>3</b>) (<b>a</b>) MIC of ‘Maria Bruvele’ extract against <span class="html-italic">C. albicans</span> by the two-fold serial broth microdilution method; (<b>b</b>) MBC of the same extract against <span class="html-italic">P. aeruginosa</span> and <span class="html-italic">C. albicans</span> (reproduced from [<a href="#B65-ijms-25-13171" class="html-bibr">65</a>]).</p>
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<p>Schematic diagram of antimicrobial mechanisms exerted by biomolecules extracted from waste biomass.</p>
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<p><span class="html-italic">B. cereus</span> morphology observed by TEM. (<b>A</b>) <span class="html-italic">B. cereus</span> treated with 1/2 MIC. (<b>B</b>) <span class="html-italic">B. cereus</span> treated with MIC. (<b>C</b>) <span class="html-italic">B. cereus</span> treated with MBC. (<b>D</b>) positive control (<span class="html-italic">Cefixime</span>). (<b>E</b>) negative control (untreated <span class="html-italic">B. cereus</span>). Reprinted with permission from Ref. [<a href="#B126-ijms-25-13171" class="html-bibr">126</a>]. Copyright 2020 by Elsevier. For more clarity, a scale bar has been added under each image.</p>
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<p>Circular bioeconomy model in food packaging: integrating renewable resources in biorefineries to produce recyclable, eco-friendly materials. Reproduced from [<a href="#B127-ijms-25-13171" class="html-bibr">127</a>].</p>
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25 pages, 16929 KiB  
Article
Potential Antimicrobial and Cytotoxic Activity of Caralluma indica Seed Extract
by Shunmuga Vadivu Ramalingam, Senthil Bakthavatchalam, Karnan Ramachandran, Vasthi Gnanarani Soloman, Afrin Khan Ajmal, Mohammad Khalid Al-Sadoon and Ramachandran Vinayagam
Antibiotics 2024, 13(12), 1193; https://doi.org/10.3390/antibiotics13121193 (registering DOI) - 7 Dec 2024
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Abstract
Background: Plant-derived phytochemicals are crucial in fighting bacterial infections and in cancer therapy. Objective: This study investigates the phytochemical composition of the ethanolic extract obtained from Caralluma indica (C. indica) seeds and assesses its antimicrobial, anticancer, and antioxidant activities. Results: GC-MS [...] Read more.
Background: Plant-derived phytochemicals are crucial in fighting bacterial infections and in cancer therapy. Objective: This study investigates the phytochemical composition of the ethanolic extract obtained from Caralluma indica (C. indica) seeds and assesses its antimicrobial, anticancer, and antioxidant activities. Results: GC-MS analysis found 30 phytochemicals in C. indica seeds, including 5 bioactive compounds that have been shown to have antioxidant, antimicrobial, and cytotoxicity properties, through in silico evaluation. Phytochemical screening of C. indica identified and measured the phenolic compounds, providing insight into its bioactive potential and therapeutic properties. C. indica exhibited robust antioxidant capacity (DPPH, ABTS, nitric oxide, and H2O2 radical scavenging) alongside potent antimicrobial activity against oral pathogen and cytotoxicity activity on a human oral squamous carcinoma cell line (OECM-1) (EC50 of 169.35 µg/mL) and yeast cell Saccharomyces cerevisiae (215.82 µg/mL), with a selective index of 1.27. The subminimum % MBC/MFC of C. indica significantly reduced biofilm formation against oral pathogens (p < 0.05). Molecular docking studies showed a strong correlation (r = 0.862) between antifungal and anticancer targets, suggesting that the antimicrobial agents in C. indica contribute to cancer prevention mechanisms. Conclusions: These findings propose C. indica seeds as promising candidates for combating oral pathogens, inhibiting biofilm formation, and reducing the risk of oral cancer progression. Full article
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<p>GC-MS chromatogram of the <span class="html-italic">C. indica</span> seed ethanolic extract.</p>
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<p>In vitro antioxidant activity of the <span class="html-italic">C. indica</span> seed ethanolic extract. (<b>a</b>) DPPH, (<b>b</b>) ABTS, (<b>c</b>) NO, and (<b>d</b>) H<sub>2</sub>O<sub>2</sub> radical scavenging; AA—ascorbic acid and CISEE—<span class="html-italic">C. indica</span> seed ethanolic extract.</p>
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<p>Antimicrobial activity of the <span class="html-italic">C. indica</span> seed ethanolic extract against oral-infection-causing pathogens. (<b>a</b>) <span class="html-italic">S. aureus</span> biofilm formation inhibitory activity of 25, 50, and 75% MBC concentrations (n = 3). (<b>b</b>) <span class="html-italic">C. albicans</span> biofilm formation inhibitory activity of 25, 50, and 75% MFC concentrations (n = 3). (<b>c</b>–<b>e</b>) Antimicrobial activity of <span class="html-italic">C. indica</span> seed ethanolic extract (50, 75, and 100 µg/mL) against oral pathogens (n = 3). (*) Statistically significant with the compared control (<span class="html-italic">p</span> &lt; 0.05); within each concentration, the different letters <sup>a,b,c</sup> indicate significance (<span class="html-italic">p</span> &lt; 0.05), and the same letters indicate non-significance (<span class="html-italic">p</span> &gt; 0.05), using a one-way ANOVA followed by Duncan’s multiple range test (DMRT); the significance level is <span class="html-italic">p</span> &lt; 0.05.</p>
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<p>In vitro cytotoxicity activity of the <span class="html-italic">C. indica</span> seed ethanolic extract. * significant difference from the control at <span class="html-italic">p</span> &lt; 0.05 using a one-way ANOVA followed by DMRT. (<b>a</b>) OECM-1 cell line. (<b>b</b>) Yeast <span class="html-italic">Saccharomyces cerevisiae</span> cell model.</p>
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<p>Morphology of normal and <span class="html-italic">C. indica</span> seed ethanolic extract-treated cells on OECM-1. (<b>a</b>) Control, (<b>b</b>–<b>f</b>) various concentrations of the CISEE extract, and (<b>g</b>) the standard as cisplatin.</p>
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<p>Morphological examination of the cytotoxicity (antiproliferative) activity of the <span class="html-italic">C. indica</span> seed ethanolic extract against yeast cells (the blue color arrow indicates a live cell (without staining) and the red color arrow indicates cell death (with blue color staining)). (<b>a</b>) Control and (<b>b</b>–<b>f</b>) various concentrations of the <span class="html-italic">C. indica</span> seed ethanolic extract.</p>
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<p>Molecular docking of the <span class="html-italic">C. indica</span> seed ethanolic extract phytochemicals against the antibacterial target of sortase A (PDB: 1T2W).</p>
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<p>Molecular docking of the <span class="html-italic">C. indica</span> seed ethanolic extract phytochemicals against the antibacterial target of sortase A (PDB: 1T2W).</p>
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<p>Molecular docking of <span class="html-italic">C. indica</span> seeds phytochemicals against the antifungal target of N-myristoyl transferase (PDB ID: 1NMT).</p>
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<p>Molecular docking of <span class="html-italic">C. indica</span> seed phytochemicals against the anticancer molecular target of DNMT1 (PDB ID: 4WXX).</p>
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<p>Molecular docking of <span class="html-italic">C. indica</span> seed phytochemicals against the anticancer molecular target of DNMT1 (PDB ID: 4WXX).</p>
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<p>Hierarchical tree clustering analysis between the targets (n = 5; <span class="html-italic">C. indica</span> seed bioactive compound binding affinity (kcal/mol) against targets on antimicrobial and anti-oral cancer).</p>
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<p>Graphical representation of the <span class="html-italic">C. indica</span> seed and the bioactive compound binding affinity score, which was similarly involved across all molecular targets for anti-oral microbial and anti-oral cancer.</p>
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<p>Molecular target homology modeling using phylogenetic tree analysis. (<b>a</b>) Antibacterial molecular target homology modeling. (<b>b</b>) Antifungal molecular target homology modeling. Red box indicates the targeted protein of micro orgaisms.</p>
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<p>Collection of <span class="html-italic">C. indica</span> seeds.</p>
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24 pages, 3827 KiB  
Article
Berries, Leaves, and Flowers of Six Hawthorn Species (Crataegus L.) as a Source of Compounds with Nutraceutical Potential
by Natalia Żurek, Michał Świeca and Ireneusz Tomasz Kapusta
Molecules 2024, 29(23), 5786; https://doi.org/10.3390/molecules29235786 (registering DOI) - 7 Dec 2024
Viewed by 134
Abstract
Designing new forms of food, food additives, and nutraceuticals is necessary due to the growing needs of consumers, as well as the inflammation of civilization diseases, the prevention and treatment of which can be significantly supported by dietary intervention. For this reason, this [...] Read more.
Designing new forms of food, food additives, and nutraceuticals is necessary due to the growing needs of consumers, as well as the inflammation of civilization diseases, the prevention and treatment of which can be significantly supported by dietary intervention. For this reason, this study aimed to obtain highly bioactive preparations in the form of powders from the fruits, leaves, and flowers of six species of hawthorn (Crataegus L.) using solid phase extraction (SPE). Ultra-performance liquid chromatography analysis (UPLC-PDA-MS/MS) showed a high concentration of phenolic compounds (in the range from 31.50 to 66.06 mg/g), including the highest concentration in hawthorn fruit preparations. Fruit preparations also showed the highest antioxidant activity (through scavenging of O2˙ and OH˙ radicals), antidiabetic activity (inhibition of α-amylase and α-glucosidase), and anticancer activity, mainly against colon cancer cells (Caco-2). At the same time, hawthorn flower preparations showed the highest biocompatibility against normal colon cells (CCD841CoN) and anti-inflammatory activity (trypsin inhibition). Correlation and principal component analysis (PCA) showed that the health-promoting potential was most influenced by the content of falavan-3-ols. The above findings provide a basis for the industrial use of the developed preparations, which is in line with the current trend in food technology related to the search for new sources of bioactive compounds and the design of highly bioactive food. Full article
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<p>pH value (<b>A</b>), equilibrium moisture content (<b>B</b>), and water solubility index (<b>C</b>) of hawthorn berries, leaves, and flower preparations. Results are expressed as mean (n = 3) ± SD. The values in the columns marked with different letters (lowercase letters, between species and morphological parts; uppercase letters, between means for morphological parts) indicate statistically significant differences (<span class="html-italic">p</span> &lt; 0.05). Explanations: C, <span class="html-italic">Crataegus</span>; 1–6, hawthorn species (see <a href="#sec2dot2-molecules-29-05786" class="html-sec">Section 2.2</a>. Plant material); B, berries; L, leaves; F, flowers.</p>
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<p>Total content of polyphenols (<b>A</b>), flavonoids (<b>B</b>), and proanthocyanidins (<b>C</b>) in hawthorn berries, leaves, and flower preparations. Results are expressed as mean (n = 3) ± SD. The values in the columns marked with different letters (lowercase letters, between species and morphological parts; uppercase letters, between means for morphological parts) indicate statistically significant differences (<span class="html-italic">p</span> &lt; 0.05). Explanations: C, <span class="html-italic">Crataegus</span>; 1–6, hawthorn species (see <a href="#sec2dot2-molecules-29-05786" class="html-sec">Section 2.2</a>. Plant material); B, berries; L, leaves; F, flowers.</p>
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<p>PCA analysis between studied hawthorn species, morphological parts, and analyzed parameters. Explanations: B, Berries; L, Leaves; F, Flowers; 1–6, hawthorn species (see <a href="#sec2dot2-molecules-29-05786" class="html-sec">Section 2.2</a>. Plant material).</p>
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<p>Pearson correlation illustrating the relationships between the studied variables for preparations obtained from hawthorn berries.</p>
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<p>Pearson correlation illustrating the relationships between the studied variables for preparations obtained from hawthorn leaves.</p>
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<p>Pearson correlation illustrating the relationships between the studied variables for preparations obtained from hawthorn flowers.</p>
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