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25 pages, 8550 KiB  
Article
Potential Mechanisms and Effects of Dai Bai Jie Ethanol Extract in Preventing Acute Alcoholic Liver Injury
by Niantong Xia, Hongwei Xue, Yihang Li, Jia Liu, Yang Lou, Shuyang Li, Yutian Wang, Juan Lu and Xi Chen
Curr. Issues Mol. Biol. 2025, 47(1), 3; https://doi.org/10.3390/cimb47010003 - 24 Dec 2024
Viewed by 369
Abstract
This study investigated the protective effect of Dai Bai Jie (DBJ) extract against acute alcoholic liver injury (AALI) and elucidated its potential mechanism. The total saponin level in the DBJ extracts was measured using vanillin–chloroform acid colorimetry. To observe the preventive and protective [...] Read more.
This study investigated the protective effect of Dai Bai Jie (DBJ) extract against acute alcoholic liver injury (AALI) and elucidated its potential mechanism. The total saponin level in the DBJ extracts was measured using vanillin–chloroform acid colorimetry. To observe the preventive and protective effects of DBJ on AML-12 cells in an ethanol environment, the effective components of DBJ were identified. An alcohol-induced AALI mouse model was used to evaluate the efficacy of DBJ against AALI. For this purpose, alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH) levels were assessed, liver function indices and oxidative and inflammatory markers were determined, and histopathological examinations were performed. Mechanistic investigations were conducted using RT-qPCR assays and immunohistochemical analysis to determine the protective effects of DBJ. The samples (DBJ-1, DBJ-2, and DBJ-3) were obtained by extracting DBJ with water, 50% ethanol, and 95% ethanol, yielding total saponin contents of 5.35%, 6.64%, and 11.83%, respectively. DBJ-3 was isolated and purified, and its components were identified by Ultra Performance Liquid Chromatography-Mass Spectrometry (UPLC-MS). DBJ-3 had the greatest effect on cell viability in an ethanol environment. Moreover, DBJ-3 reduced inflammatory infiltration, liver cell degeneration, and hemorrhage, while increasing ADH and ALDH levels in liver tissues. Additionally, DBJ-3 considerably decreased the serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), total cholesterol (TC), and triglyceride (TG) levels. DBJ-3 reduced malondialdehyde (MDA), reactive oxygen species (ROS), and inflammatory factors, such as tumor necrosis factor (TNF-α), interleukin-1β (IL-1β), and interleukin 6 (IL-6), while increasing superoxide dismutase (SOD) and glutathione S-transferase (GST) activities. Furthermore, DBJ-3 significantly increased alcohol dehydrogenase 1b (ADH1B) and aldehyde dehydrogenase 2 (ALDH2) expression at the gene and protein levels within alcohol metabolism pathways and reduced the nuclear factor kappa-B (NF-κB) gene and protein levels. These findings suggest that DBJ-3 can prevent AALI by enhancing alcohol metabolism via the regulation of ADH1B and ALDH2 and the modulation of the NF-κB pathway to improve antioxidant and anti-inflammatory effects. Full article
(This article belongs to the Special Issue Biochemical Composition and Activity of Medicinal Plants and Food)
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Figure 1

Figure 1
<p>Standard curve of ginsenoside Re.</p>
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<p>Total ion chromatogram of DBJ-3 in negative ion mode. The arrow in <a href="#cimb-47-00003-f002" class="html-fig">Figure 2</a> indicates the detected saponin.</p>
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<p>The effects of different DBJ extracts on AML-12 cell survival were evaluated after 24 h. (<b>A</b>) DBJ-1; (<b>B</b>) DBJ-2; (<b>C</b>) DBJ-3. All the data are presented as the means ± SDs (<span class="html-italic">n</span> = 6).</p>
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<p>After 24 h, the survival rate of the AML-12 cells was determined with different concentrations of ethanol. All the data are presented as the means ±SDs (<span class="html-italic">n</span> = 6); ** <span class="html-italic">p</span> &lt; 0.01 and *** <span class="html-italic">p</span> &lt; 0.001 vs. the normal control group.</p>
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<p>Alterations in the survival rate of AML-12 cells. All the data are presented as the means ± SDs (<span class="html-italic">n</span> = 6); <sup>###</sup> <span class="html-italic">p</span> &lt; 0.001 vs. the NC group; ** <span class="html-italic">p</span> &lt; 0.01 and *** <span class="html-italic">p</span> &lt; 0.001 vs. the M group.</p>
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<p>Changes in the serum biochemical indices. The NC group (normal control, distilled water), M group (model, 56% alcohol at 15 mL/kg), S group (silymarin, 60 mg/kg), DBJ-3-L group (100 mg/kg DBJ-3), DBJ-3-M group (300 mg/kg DBJ-3), DBJ-3-H group (600 mg/kg DBJ-3). (<b>A</b>) ALT; (<b>B</b>) AST; (<b>C</b>) TC; (<b>D</b>) TG. The symbol corresponding to each group represents the data for that group, and all the data are presented as the means ± SDs (n = 6); <sup>##</sup> <span class="html-italic">p</span> &lt; 0.01 vs. the NC group; * <span class="html-italic">p</span> &lt; 0.05 and ** <span class="html-italic">p</span> &lt; 0.01 vs. the M group.</p>
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<p>Changes in ADH and ALDH levels in mouse liver tissue. (<b>A</b>) ADH; (<b>B</b>) ALDH. All the data are presented as the means ± SDs (<span class="html-italic">n</span> = 6); <sup>##</sup> <span class="html-italic">p</span> &lt; 0.01 vs. the NC group; * <span class="html-italic">p</span> &lt; 0.05 and ** <span class="html-italic">p</span> &lt; 0.01 vs. the M group.</p>
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<p>Histopathological sections from each group. (<b>A</b>) NC group; (<b>B</b>) M group; (<b>C</b>) S group; (<b>D</b>) DBJ-3-L group; (<b>E</b>) DBJ-3-M group; (<b>F</b>) DBJ-3-H group. The left image scale bar was 500 μm, and the right image scale bar was 100 μm in each group. Yellow arrows indicate cellular swelling and cytoplasmic looseness with light staining, blue arrows indicate lipid vacuolation in hepatocytes, and red arrows indicate a small amount of vascular congestion. The black arrows represent slight hydropic degeneration of many hepatocytes in the liver tissue.</p>
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<p>Changes in ROS, MDA, SOD, and GST levels in mouse liver tissues. (<b>A</b>) ROS; (<b>B</b>) MDA; (<b>C</b>) SOD; (<b>D</b>) GST. All the data are presented as the means ±SDs (<span class="html-italic">n</span> = 6); <sup>##</sup> <span class="html-italic">p</span> &lt; 0.01 vs. the NC group; * <span class="html-italic">p</span> &lt; 0.05 and ** <span class="html-italic">p</span> &lt; 0.01 vs. the M group.</p>
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<p>Changes in TNF-α, IL-1β, and IL-6 levels in mouse liver tissues. (<b>A</b>) TNF-α; (<b>B</b>) IL-6; (<b>C</b>) IL-1β. All the data are presented as the means ± SDs (<span class="html-italic">n</span> = 6); <sup>##</sup> <span class="html-italic">p</span> &lt; 0.01 vs. the NC group; * <span class="html-italic">p</span> &lt; 0.05 and ** <span class="html-italic">p</span> &lt; 0.01 vs. the M group.</p>
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<p>Expression levels of the <span class="html-italic">Adh1b</span> and <span class="html-italic">Aldh2</span> mRNAs. (<b>A</b>) <span class="html-italic">Adh1b</span>; (<b>B</b>) <span class="html-italic">Aldh2</span>. All the data are presented as the means ± SDs (<span class="html-italic">n</span> = 6); <sup>##</sup> <span class="html-italic">p</span> &lt; 0.01 vs. the NC group; ** <span class="html-italic">p</span> &lt; 0.01 vs. the M group.</p>
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<p>Immunohistochemical staining analysis of ADH1B and ALDH2 in the different groups. (<b>A</b>) Images illustrating the immunoreactivity of ADH1B and ALDH2; (<b>B</b>) ADH1B; (<b>C</b>) ALDH2. All the data are presented as the means ±SDs (<span class="html-italic">n</span> = 6); <sup>##</sup> <span class="html-italic">p</span> &lt; 0.01 vs. the NC group; ** <span class="html-italic">p</span> &lt; 0.01 vs. the M group.</p>
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<p><span class="html-italic">Nf-κb</span> mRNA expression. All the data are presented as the means ± SDs (<span class="html-italic">n</span> = 6); <sup>##</sup> <span class="html-italic">p</span> &lt; 0.01 vs. the NC group; ** <span class="html-italic">p</span> &lt; 0.01 vs. the M group.</p>
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<p>IHC analysis of NF-κB in the different groups. (<b>A</b>) Images illustrating the IHC of NF-κB; (<b>B</b>) NF-κB P65 protein expression. All the data are presented as the means ± SDs (<span class="html-italic">n</span> = 6); <sup>##</sup> <span class="html-italic">p</span> &lt; 0.01 vs. the NC group; * <span class="html-italic">p</span> &lt; 0.05 vs. the M group.</p>
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15 pages, 1572 KiB  
Article
Qualitative Phytochemical Profiling and In Vitro Antioxidant Potential Evaluation of South African Momordica Balsamina Linn Fruit Pulp
by Buang Matseke, Sipho Mapfumari and Mmamosheledi Mothibe
Life 2025, 15(1), 4; https://doi.org/10.3390/life15010004 - 24 Dec 2024
Viewed by 305
Abstract
Momordica balsamina Linn is a well-known African traditional herb due to its tremendous medicinal and nutritional properties. It is used worldwide for the treatment of different ailments and diseases. In the present study, the phytochemical and antioxidant activity of South African M. balsamina [...] Read more.
Momordica balsamina Linn is a well-known African traditional herb due to its tremendous medicinal and nutritional properties. It is used worldwide for the treatment of different ailments and diseases. In the present study, the phytochemical and antioxidant activity of South African M. balsamina fruit pulp extracts was evaluated. The fruit pulp extracts were obtained by using the serial exhaustive extraction procedure using the solvents hexane, DCM, acetone, and methanol. The resulting extracts were subjected to different standard colorimetric tests for phytochemical analysis. The presence of compounds with antioxidant activity was determined using dot plot and TLC. The DPPH radical scavenging assay, hydrogen peroxide activity, and reducing power assay, coupled with linear regression, were employed to determine the quantity of antioxidants and their IC50. The results for qualitative phytochemical screening have shown that the fruit pulp contains alkaloids, cardiac glycosides, saponins, phenolic compounds, tannins, flavonoids, terpenoids, and steroids. All the extracts revealed the presence of antioxidant activity in both dot plot and TLC. Acetone extracts (0.279 mg/mL) showed the lowest IC50 compared to the standards gallic acid (0.4 mg/mL) and diosgenin (0.42 mg/mL). These findings confirmed that M. balsamina is very rich in phytochemical compounds and has strong antioxidant potential; therefore, it could be a potential source of drugs which in the future may serve the production of synthetically improved therapeutic agents. Full article
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<p>Dot plot of <span class="html-italic">M. balsamina</span> extracts before spraying with DPPH (<b>left</b>) and after spraying with DPPH (<b>right</b>).</p>
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<p>Chromatograms of <span class="html-italic">M. balsamina</span> (<b>A</b>) hexane, (<b>B</b>) DCM, (<b>C</b>) acetone and (<b>D</b>) methanol extracts developed with different solvent systems. The chromatograms are visualised from left to right under (1). visible light, (2). UV short wave (214 nm), (3). UV long wave (314 nm), and (4). DPPH spray for antioxidants.</p>
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<p>Percentage DPPH radical scavenging activity of <span class="html-italic">M. balsamina</span> extracts of different concentrations.</p>
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<p>Percentage hydrogen peroxide radical scavenging activity of <span class="html-italic">M. balsamina</span> extracts of different concentrations.</p>
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<p>Percentage reducing power of <span class="html-italic">M. balsamina</span> extracts of different concentrations.</p>
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16 pages, 1191 KiB  
Article
Gigaspora roseae and Coriolopsis rigida Fungi Improve Performance of Quillaja saponaria Plants Grown in Sandy Substrate with Added Sewage Sludge
by Guillermo Pereira, Diyanira Castillo-Novales, Cristian Salazar, Cristian Atala and Cesar Arriagada-Escamilla
J. Fungi 2025, 11(1), 2; https://doi.org/10.3390/jof11010002 - 24 Dec 2024
Viewed by 218
Abstract
The use of living organisms to treat human by-products, such as residual sludge, has gained interest in the last years. Fungi have been used for bioremediation and improving plant performance in contaminated soils. We investigated the impact of the mycorrhizal fungus (MF) Gigaspora [...] Read more.
The use of living organisms to treat human by-products, such as residual sludge, has gained interest in the last years. Fungi have been used for bioremediation and improving plant performance in contaminated soils. We investigated the impact of the mycorrhizal fungus (MF) Gigaspora roseae and the saprophytic fungus (SF) Coriolopsis rigida on the survival and growth of Quillaja saponaria seedlings cultivated in a sandy substrate supplemented with residual sludge. Q. saponaria is a sclerophyllous tree endemic to Chile, known for its high content of saponins. We inoculated plants with the MF, the SF, and a combination of both (MF + SF). Following inoculation, varying doses of liquid residual sludge equivalent to 0, 75, and 100% of the substrate’s field capacity were applied. After 11 months, we found a positive influence of the utilized microorganisms on the growth of Q. saponaria. Particularly, inoculation with the SF resulted in higher plant growth, mycorrhizal colonization percentage, and higher enzymatic activity, especially after the application of the sludge. This increase was more evident with higher doses of the applied sludge. These results highlight the potential of combined microorganism and residual sludge application as a sustainable strategy for enhancing plant growth and reducing waste. Full article
(This article belongs to the Special Issue Fungi Activity on Remediation of Polluted Environments, 2nd Edition)
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<p>Growth performance of <span class="html-italic">Q. saponaria</span> plants inoculated with mycorrhizal and saprophytic fungi in sandy substrate. Height growth (<b>A</b>) and DAC (<b>B</b>) of <span class="html-italic">Q. saponaria</span> plants inoculated with the MF <span class="html-italic">G. roseae</span> and the SF <span class="html-italic">C. rigida</span>, and with both (MF + SF) in sandy substrate. Different letters denote significant differences (Tukey test <span class="html-italic">p</span> &lt; 0.05).</p>
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<p>Aerial and radicle biomass of <span class="html-italic">Q. Saponaria</span> plants inoculated with the MF <span class="html-italic">G. roseae</span> and SF <span class="html-italic">C. rigida</span>, or their combination (MF + SF), under increasing doses of residual sludge. Different letters denote significant differences (Tukey test <span class="html-italic">p</span> &lt; 0.05).</p>
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<p>Mycorrhization % in <span class="html-italic">Q. saponaria</span> plants inoculated with the MF <span class="html-italic">G. roseae</span> or with a combination of MF + SF (<span class="html-italic">G. roseae</span> and <span class="html-italic">C. rigida</span>) after the addition of increasing concentrations of waste sludge. Different letters denote significant differences (Tukey test <span class="html-italic">p</span> &lt; 0.05).</p>
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19 pages, 2461 KiB  
Article
Optimization of Breeding Tools in Quinoa (Chenopodium quinoa) and Identification of Suitable Breeding Material for NW Europe
by Tim Vleugels, Chris Van Waes, Ellen De Keyser and Gerda Cnops
Plants 2025, 14(1), 3; https://doi.org/10.3390/plants14010003 - 24 Dec 2024
Viewed by 269
Abstract
Quinoa (Chenopodium quinoa) cultivation has become increasingly popular in NW Europe but little is known about the performance of contract-free varieties in this region. In this study, we phenotyped 25 quinoa varieties on a single-plant basis in a field trial in [...] Read more.
Quinoa (Chenopodium quinoa) cultivation has become increasingly popular in NW Europe but little is known about the performance of contract-free varieties in this region. In this study, we phenotyped 25 quinoa varieties on a single-plant basis in a field trial in Belgium. In addition, we optimized breeding tools such as NIRS (near-infrared reflectance spectroscopy) to estimate the seed crude protein content and a multiplex PCR set to identify true F1 progeny from pair crosses. We identified 14 varieties with sufficiently early maturity, 17 varieties with plant height below 150 cm, 21 large-seeded varieties, four varieties with a crude protein content exceeding 15%, and two low-saponin varieties. A variety of seed colors and plant morphological traits was observed. Seed yield was not correlated with maturity, plant height or saponin content, but was negatively correlated with seed crude protein content. NIRS could accurately predict seed crude protein content with a determination coefficient of 0.94. Our multiplex SSR set could correctly identify the paternity in 77% to 97% of progeny, depending on the pair cross. In conclusion, our study identified various contract-free varieties that may be suitable for cultivation in NW Europe. In addition, our study provides valuable phenotypic information and breeding tools that breeders can harness for breeding efforts in NW European quinoa. Full article
(This article belongs to the Special Issue Genomics-Assisted Improvement of Quinoa)
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Figure 1
<p>Daily average temperatures (black line, right axis) and daily precipitation (gray bars, left axis) for the trial site during the growing season of 2021, obtained from the Royal Meteorological Institute (KMI) in the form of interpolated data from nearby weather stations.</p>
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<p>Example of the phenotypic diversity observed in panicle traits among our panel of varieties and plants: narrow (<b>A</b>), intermediate (<b>B</b>,<b>C</b>) to broad (<b>D</b>) panicle width; dense (<b>A</b>), intermediate (<b>B</b>,<b>C</b>) to loose (<b>D</b>) panicle density; and purple (<b>A</b>), red (<b>B</b>), yellow (<b>C</b>) or green (<b>D</b>) panicle color.</p>
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<p>Measured crude protein content and NIRS-estimated crude protein content for 178 quinoa seed samples used in the calibration, with indication of the 163 samples that were used in the final calibration (circles) and the 18 outlier samples (triangles) that were omitted.</p>
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26 pages, 4557 KiB  
Article
Ethanolic Extract of Averrhoa carambola Leaf Has an Anticancer Activity on Triple-Negative Breast Cancer Cells: An In Vitro Study
by Oscar F. Beas-Guzmán, Ariana Cabrera-Licona, Gustavo A. Hernández-Fuentes, Silvia G. Ceballos-Magaña, José Guzmán-Esquivel, Luis De-León-Zaragoza, Mario Ramírez-Flores, Janet Diaz-Martinez, Idalia Garza-Veloz, Margarita L. Martínez-Fierro, Iram P. Rodríguez-Sanchez, Gabriel Ceja-Espíritu, Carmen Meza-Robles, Víctor H. Cervantes-Kardasch and Iván Delgado-Enciso
Pharmaceutics 2025, 17(1), 2; https://doi.org/10.3390/pharmaceutics17010002 - 24 Dec 2024
Viewed by 243
Abstract
Background/Objectives: Averrhoa carambola, or star fruit, is a shrub known for its medicinal properties, especially due to bioactive metabolites identified in its roots and fruit with anti-cancer activity. However, the biological effects of its leaves remain unexplored. This study aimed to [...] Read more.
Background/Objectives: Averrhoa carambola, or star fruit, is a shrub known for its medicinal properties, especially due to bioactive metabolites identified in its roots and fruit with anti-cancer activity. However, the biological effects of its leaves remain unexplored. This study aimed to assess the effects of ethanolic extract from A. carambola leaves on triple-negative breast cancer (TNBC), an aggressive subtype lacking specific therapy. Methods: Phytochemical analysis and HPLC profile and additional cell line evaluation employing MDA-MB-231 were carried out. Results: Phytochemical screening revealed that the ethanolic extract was rich in flavonoids, saponins, and steroids, demonstrating an antioxidant capacity of 45%. 1H NMR analysis indicated the presence of flavonoids, terpenes, and glycoside-like compounds. Cell viability assays showed a concentration-dependent decrease in viability, with an IC50 value of 20.89 μg/mL at 48 h. Clonogenic assays indicated significant inhibition of replicative immortality, with only 2.63% survival at 15 μg/mL. Migration, assessed through a wound healing assay, was reduced to 3.06% at 100 μg/mL, with only 16.23% of cells remaining attached. An additive effect was observed when combining lower concentrations of the extract with doxorubicin, indicating potential synergy. Conclusions: These results suggest that the ethanolic extract of A. carambola leaves contains metabolites with anti-cancer activity against TNBC cells, supporting further research into their bioactive compounds and therapeutic potential. Full article
(This article belongs to the Special Issue Pharmaceutical Applications of Plant Extracts, 2nd Edition)
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Figure 1
<p>Chromatograms obtained at 290 nm from HPLC analysis. (<b>A</b>) Chromatogram of standards: gallic acid (GA, Rt 2.385 min), cinnamic acid (CA, Rt 30.795 min), anthrone (ANT, Rt 20.000 min), quercetin (Q, Rt 17.955 min), and 4-methylumbelliferone (4-ML, Rt 10.908 min). (<b>B</b>) Chromatogram of the ethanolic extract of <span class="html-italic">A. carambola</span> (500 ppm). (<b>C</b>) Chromatogram of the hydrolysate of the leaves of <span class="html-italic">A. carambola</span> (500 ppm). S: signal.</p>
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<p>Viability experiments employing ethanolic extract of <span class="html-italic">A. carambola</span> on MDA-MB-231 cells. (<b>A</b>) No changes in viability were observed in cervical cancer cell line TC-1 exposed to A. carambola extract in increasing concentrations. (<b>B</b>) A concentration-dependent effect was observed on MDA-MB-231 cell line exposed to the extract. (<b>C</b>) The ethanolic extract of <span class="html-italic">A. carambola</span> leaves had an experimental IC<sub>50</sub> of 20.83 μg/mL in triple-negative breast cancer cell line. (<b>D</b>) Morphological changes and detached cells were observed from the concentration of 25 μg/mL of ethanolic extract. Magnification 10×. The <span class="html-italic">p</span>-values correspond to significant differences compared to the control, DMEM-F12 medium with 0.1% DMSO, * <span class="html-italic">p</span> &lt; 0.05.</p>
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<p>Ethanolic extract of <span class="html-italic">A. carambola</span> leaves decreases replicative immortality of MDA-MB-231 cells. (<b>A</b>) Photographs depict the number of colonies formed after the exposition of each treatment. It is observed that a concentration-dependent effect completely inhibits cell survival. (<b>B</b>) The graph shows the percentage of survival treatment. The <span class="html-italic">p</span>-values correspond to significant differences compared to the control, only DMEM medium, * <span class="html-italic">p</span> &lt; 0.05.</p>
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<p>Ethanolic extract of <span class="html-italic">A. carambola</span> leaves interferes with MDA-MB-231 cell migration. (<b>A</b>) Images captured at 48 h of the wound area made in MDA-MB-231 cell monolayers. Magnification 4×. (<b>B</b>) The graph shows the changes in the open area; a concentration-dependent inhibitory effect can be observed at 48 h that was superior to the doxorubicin effect. Comparison to 48 h control, * <span class="html-italic">p</span> &lt; 0.05.</p>
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<p>The ethanolic extract of <span class="html-italic">A. carambola</span> leaves affects the cell adhesion of MDA-MB-231 cells. (<b>A</b>) The micrographs show the adhesive capacity of cells recovered after exposure to <span class="html-italic">A. carambola</span> extract and reseeded for 24 h. The adhesive capacity decreases as the concentration of the extract increases. Magnification 10×. (<b>B</b>) The graphs show the percentage of cells adhered to the monolayer after being treated with the extract for 48, showing a concentration-dependent decrease in adhesion. (<b>C</b>) The graph shows the percentage of cell death after 48 h of treatment. (<b>D</b>) The graph shows the percentage of adhesion of detached cells after treatment that were recovered and reseeded. The <span class="html-italic">p</span>-values correspond to significant changes compared to the control, * <span class="html-italic">p</span> &lt; 0.05.</p>
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<p>The combination of a low dose of doxorubicin and intermediate doses of <span class="html-italic">A. carambola</span> extract reduces the cell viability of MDA-MB-231 cells. The graph shows the reduction in cell viability induced by the different combinations after 48 h of treatment. An additive effect was observed between the 1/5 IC<sub>50</sub> dose of doxorubicin (DOX) and the three tested concentrations of the extract. <sup>a</sup> 0.4 μM DOX + 15 μg/mL extract vs. 15 μg/mL of the extract, <sup>b</sup> 0.4 μM DOX + 25 μg/mL vs. 25 μg/mL, <sup>c</sup> 0.4 μM DOX + 50 μg/mL vs. 50 μg/mL, <sup>d</sup> 2 μM DOX + 15 μg/mL vs. 15 μg/mL, <sup>e</sup> 2 μM DOX + 25 μg/mL vs. 25 μg/mL, <sup>f</sup> 2 μM DOX + 50 μg/mL vs. 50 μg/Ml, <sup>a’</sup> 0.4 μM DOX + 15 μg/mL vs. 0.4 μM DOX, <sup>b’</sup> 0.4 μM DOX + 25 μg/mL vs. 0.4 μM DOX <sup>c’</sup> 0.4 μM DOX + 50 μg/mL vs. 0.4 μM DOX, <sup>d’</sup> 2 μM DOX + 15 μg/mL vs. 2 μM DOX, <sup>e’</sup> 2 μM DOX + 25 μg/mL vs. 2 μM DOX, <sup>f’</sup> 2 μM DOX + 50 μg/mL vs. 2 μM DOX, * <span class="html-italic">p</span> &lt; 0.05.</p>
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14 pages, 3895 KiB  
Article
In-Depth LC-ESI/HRMS-Guided Phytochemical Analysis and Antioxidant Activity Analysis of Eco-Sustainable Extracts of Cynara cardunculus (Carciofo di Paestum PGI) Leaves
by Antonietta Cerulli, Roberta Cuozzo, Maria Paola Melis, Gabriele Serreli, Monica Deiana, Milena Masullo and Sonia Piacente
Plants 2024, 13(24), 3591; https://doi.org/10.3390/plants13243591 - 23 Dec 2024
Viewed by 232
Abstract
The Italian Carciofo di Paestum (C. scolymus) PGI, an artichoke variety from the Campania region, was investigated for its potential to reuse by-products for food supplements. EtOH:H2O 50:50 and 75:25 extracts of its leaves were analyzed for phenolic and [...] Read more.
The Italian Carciofo di Paestum (C. scolymus) PGI, an artichoke variety from the Campania region, was investigated for its potential to reuse by-products for food supplements. EtOH:H2O 50:50 and 75:25 extracts of its leaves were analyzed for phenolic and flavonoid content and antioxidant activity (TEAC: 1.90 and 1.81 mM of Trolox; DPPH IC50: 106.31 µg/mL and 128.21 µg/mL; FRAP: 1.68 and 1.58 mM FeSO₄/g extract). To further investigate the antioxidant potential, the ability of the two extracts to scavenge reactive species was assessed in Caco-2 cell cultures, showing a dose-dependent antioxidant capacity. To highlight metabolites responsible for the activity, LC-ESI/HRMSMS analysis was achieved, revealing 28 compounds (sesquiterpenes, megastigmanes, quinic acid and hydroxycinnamic acid derivatives, flavonoids, lignans, triterpenoid saponins, and polar fatty acids), of which structures were determined using 1D- and 2D-NMR analysis. In addition, quantitative determination of caffeoyl, dicaffeoyl, and quinic acid derivatives (CQAs) was performed through LC-ESI/QTrap/MS/MS, highlighting that the most abundant compound was 5-caffeoylquinic acid (6), with values of 9.310 and 7.603 mg/g extract in EtOH:H2O (75:25) and EtOH:H2O (50:50), respectively. The analysis showed that extracts were rich in bioactive compounds, suggesting their potential for development into antioxidant-based food supplements that may protect cells from oxidative stress and support overall wellness. Full article
(This article belongs to the Special Issue Bio-Active Compounds in Horticultural Plants)
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<p>Total phenolic and flavonoid content, TEAC, DPPH, and FRAP assays of EtOH:H<sub>2</sub>O (50:50) (blue) and EtOH:H<sub>2</sub>O (75:25) (orange) extracts of “Carciofo di Paestum” PGI leaves.</p>
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<p>Percentage of viable Caco-2 cells calculated relative to the control (0 μM, 100% viability) following 24 h of incubation with different concentrations of EtOH:H<sub>2</sub>O (50:50) (<b>A</b>) and EtOH:H<sub>2</sub>O (75:25) (<b>B</b>) extracts (0.1–50 μM). Data are presented as the mean ± SD from independent experiments (n = 16).</p>
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<p>ROS levels, detected via H<sub>2</sub>-DCF-DA fluorescence and expressed as % of the control samples (CTR) in Caco-2 cells following 2 h of incubation with varying concentrations of the EtOH:H<sub>2</sub>O (50:50) (<b>A</b>) and EtOH:H<sub>2</sub>O (75:25) (<b>B</b>) (2.5–50 μM) in co-incubation with TBH 2.5 mM. °°° = <span class="html-italic">p</span> &lt; 0.001 TBH vs. CTR; * = <span class="html-italic">p</span> &lt; 0.05 extracts vs. TBH; ** = <span class="html-italic">p</span> &lt; 0.01 extracts vs. TBH; *** = <span class="html-italic">p</span> &lt; 0.001 extracts vs. TBH (n = 12).</p>
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<p>LC-ESI/HRMS profile of EtOH:H<sub>2</sub>O (50:50) (<b>A</b>) and EtOH:H<sub>2</sub>O (75:25) (<b>B</b>) extracts of “Carciofo di Paestum” PGI leaves.</p>
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<p>Specialized metabolites isolated from EtOH:H<sub>2</sub>O (50:50) extract of “Carciofo di Paestum” PGI leaves.</p>
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19 pages, 3607 KiB  
Article
Mass Spectrometric Based Metabolomics of the Saudi Cultivar of Fenugreek (Trigonella foenum-graecum L.): A Combined GC-MS, Antimicrobial and Computational Approach
by Nujud A. M. Almuzaini, Abdel Moneim E. Sulieman, Naimah A. Alanazi, Riadh Badraoui and Emad M. Abdallah
Pharmaceuticals 2024, 17(12), 1733; https://doi.org/10.3390/ph17121733 - 21 Dec 2024
Viewed by 675
Abstract
Background and Objective: In Saudi Arabia, numerous plant species with promising medicinal properties are cultivated, widely traded, and commonly utilized in traditional medicine, including fenugreek (Trigonella foenum-graecum). This study aimed to comprehensively assess the phytochemical composition and antimicrobial potential of the [...] Read more.
Background and Objective: In Saudi Arabia, numerous plant species with promising medicinal properties are cultivated, widely traded, and commonly utilized in traditional medicine, including fenugreek (Trigonella foenum-graecum). This study aimed to comprehensively assess the phytochemical composition and antimicrobial potential of the Saudi cultivar of fenugreek using an integrative approach combining in vitro and in silico methodologies. Methods: A comprehensive investigation was conducted on the ethanol extract of fenugreek seeds, assessing its antibacterial, antifungal, properties. Computational modeling was employed to predict pharmacokinetic behavior and potential toxicity of the identified bioactive compounds. Results: Qalitative phytochemical analysis showed presence of alkaloids, tannins, saponins, glycosides, flavonoids, and steroids, while terpenoids were notably absent. GC-MS analysis of Trigonella foenum-graecum (fenugreek) seeds identified 25 bioactive compounds, with Ethyl methane sulfonate (12.41%) being the predominant component. Other key compounds included n-Hexadecanoic acid, 4-Butyl-2(4-nitrophenyl)-1,3-thiazole, and α-Tocopherol. In silico modeling of fenugreek phytochemicals supported their antibacterial, antioxidant, and neuroprotective potential, with compounds 21 and 24 showing strong binding to key targets like Tyrosyl-tRNA Synthetase (TyrRS) of Staphylococcus aureus (S. aureus), Aspartic proteinase from Candida albicans (C. albicans) and human peroxiredoxin 5. Pharmacokinetic analysis indicated good oral bioavailability, minimal CYP inhibition, and blood-brain barrier penetration, suggesting potential for treating neurodegenerative diseases. These bioactive compounds, including diosgenin and trigonelline, support fenugreek’s therapeutic promise and warrant further in vitro, in vivo, and clinical studies. Conclusion: The Saudi fenugreek cultivar is rich in bioactive compounds with good antibacterial potential. These findings establish a robust foundation for continued pharmacological research on the Saudi cultivar of T. foenum-graecum, highlighting its potential as a rich source of bioactive compounds with significant medicinal value. Full article
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<p>Chromatogram of the ethanol extract of fenugreek seeds.</p>
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<p>Tridimensional illustrations of the 3 targeted receptors 1JIJ (<b>A</b>–<b>A″</b>), 2QZW (<b>B</b>–<b>B″</b>) and 1H2D (<b>C</b>–<b>C″</b>) with the three predicted best compounds identified in the fenugreek seeds. 1JIJ complexed with compounds no. <b>21</b> (<b>A</b>), <b>24</b> (<b>A′</b>), and <b>15</b> (<b>A″</b>). 2QZW complexed with compounds no. <b>21</b> (<b>B</b>), <b>24</b> (<b>B′</b>), and <b>15</b> (<b>B″</b>). 1HD2 complexed with compounds no. <b>24</b> (<b>C</b>), <b>21</b> (<b>C′</b>), and <b>23</b> (<b>C″</b>).</p>
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<p>Illustration of the 2D diagrams of interactions of the 3 targeted receptors 1JIJ (<b>A</b>–<b>A″</b>), 2QZW (<b>B</b>–<b>B″</b>) and 1H2D (<b>C</b>–<b>C″</b>) with the three predicted best compounds identified in the fenugreek seeds. 1JIJ complexed with compounds no. <b>21</b> (<b>A</b>), <b>24</b> (<b>A′</b>), and <b>15</b> (<b>A″</b>). 2QZW complexed with compounds no. <b>21</b> (<b>B</b>), <b>24</b> (<b>B′</b>), and <b>15</b> (<b>B″</b>). 1HD2 complexed with compounds no. <b>24</b> (<b>C</b>), <b>21</b> (<b>C′</b>), and <b>23</b> (<b>C″</b>).</p>
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<p>Chemical structure of the best compounds (<b>15</b>, <b>21</b>, <b>23</b> and <b>24</b>) from the docking analysis.</p>
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<p>Boiled-egg model of the identified phytochemicals. The yellow and white areas correspond to the BBB (for blood-brain-barrier) permeation and GI (for gastro-intestinal) absorption, respectively.</p>
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9 pages, 593 KiB  
Article
Plant Cell Culture-Derived Saponin Adjuvant Enhances Immune Response Against a Stabilized Human Metapneumovirus Pre-Fusion Vaccine Candidate
by Maarten Swart, Jessica Allen, Brendan Reed, Ana Izquierdo Gil, Johan Verspuij, Sonja Schmit-Tillemans, Anish Chakkumkal, Mark Findeis, Angela V. Hafner, Chandresh Harjivan, Rebecca Kurnat, Harmjan Kuipers, Roland Zahn and Boerries Brandenburg
Vaccines 2024, 12(12), 1435; https://doi.org/10.3390/vaccines12121435 - 20 Dec 2024
Viewed by 505
Abstract
Human metapneumovirus (HMPV) is a significant respiratory pathogen, particularly in vulnerable populations. Background: No vaccine for the prevention of HMPV is currently licensed, although several subunit vaccines are in development. Saponin-based adjuvant systems (AS), including QS-21, have transformed the field of subunit vaccines [...] Read more.
Human metapneumovirus (HMPV) is a significant respiratory pathogen, particularly in vulnerable populations. Background: No vaccine for the prevention of HMPV is currently licensed, although several subunit vaccines are in development. Saponin-based adjuvant systems (AS), including QS-21, have transformed the field of subunit vaccines by dramatically increasing their potency and efficacy, leading to the development of several licensed vaccines. However, naturally sourced tree bark-extracted QS-21 faces supply and manufacturing challenges, hindering vaccine development. Objective: This study reports on an alternative plant cell culture system for the consistent production of highly pure QS-21. Method: We evaluated the efficacy of cultured plant cell (cpc)-produced QS-21 in a novel HMPV vaccine, formulating a recombinant pre-fusion stabilized HMPV F protein (preF) with cpcQS-21 and a synthetic toll-like receptor 4 (TLR4) agonist adjuvant formulation. Results: In mice, TLR4 agonist containing adjuvant formulations with plant cell-produced QS-21 performed equally to licensed adjuvant AS01 containing tree-bark-extracted QS-21 and demonstrated a significant increase in immunogenicity against HMPV preF compared to the unadjuvanted control. Conclusion: Our findings pave the way for a reliable, scalable, and sustainable source of pure QS-21, enabling the development of highly effective HMPV and other vaccines with significant public health impact. Full article
(This article belongs to the Section Vaccine Adjuvants)
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<p>Anti-F antibody titers following immunization. AS01 formulated with cpcQS-21 or beQS-21 elicited similar humoral immune responses in a prime-boost model of HMPV vaccination. Anti-F serum IgG response from BALB/c mice immunized with two doses (day 0 and 28) of 5 µg recombinant HMPV A2 PreF combined with AS01<sub>B</sub>, AS01-SPQX, or AS100-SPQX. Anti-F antibody titers were measured by ELISA on day 27 (<b>A</b>) or 42 (<b>B</b>). Concentrations of TLR4 agonist (MPLA for AS01<sub>B</sub> or PHAD<sup>®</sup> for SPQX) and (be or cpc) QS-21 are indicated. Log10 relative potency (RP) titers are compared with a reference serum pool. Red horizontal bars indicate the median response per group, and the dotted line indicates the lower limit of detection (LLOD). Open symbols indicate that the response is at or below the LLOD. AS01B and AS01-SPQX were compared across doses by a t-test. AS100-SPQX was compared with 5:5 μg AS01B and 5:5 μg AS01-SPQX by a <span class="html-italic">t</span>-test. (ns, not significant; ** <span class="html-italic">p</span> ≤ 0.01).</p>
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<p>IFN-γ-secretion by splenocytes stimulated with an HMPV A2 F peptide pool. HMPV vaccine formulations containing cpcQS-21 or beQS-21 induced HMPV-specific T cell-mediated immunity. Fourteen days following the second immunization (boost), IFN-γ secretion was assessed upon ex vivo stimulation with an F-pool for 18 h. The frequency of IFN-γ-secreting cells is depicted as the number of spot-forming units (SFU) per million splenocytes. Horizontal red bars denote group geometric means, and horizontal dashed lines indicate the lower limit of detection (LLOD) based on the 95th percentile of the background response. Open symbols indicate the response is at or below the LLOD. AS01B and AS01-SPQX adjuvant formulations were compared across doses by a Cochran–Mantel–Haenszel test. AS100-SPQX was compared with 5:5 μg AS01B and 5:5 μg AS01-SPQX with a Mann-Whitney U-test. No significant differences were found. ns, not significant.</p>
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23 pages, 4328 KiB  
Article
Herbal Extracts Mixed with Essential Oils: A Network Approach for Gastric and Intestinal Motility Disorders
by Roberta Budriesi, Ivan Corazza, Simone Roncioni, Roberta Scanferlato, Dalila De Luca, Carla Marzetti, Roberto Gotti, Nicola Rizzardi, Christian Bergamini, Matteo Micucci, Davide Roncarati and Laura Beatrice Mattioli
Nutrients 2024, 16(24), 4357; https://doi.org/10.3390/nu16244357 - 17 Dec 2024
Viewed by 524
Abstract
Background: Three herbal extracts (Asparagus racemosus Willd., Tabebuia avellanedae Lorentz, and Glycyrrhiza glabra L.) were mixed with three essential oils (Foeniculum vulgare Mill., Mentha piperita L., and Pimpinella anisum L.) to formulate a product (HEMEO) whose active compounds include saponins and [...] Read more.
Background: Three herbal extracts (Asparagus racemosus Willd., Tabebuia avellanedae Lorentz, and Glycyrrhiza glabra L.) were mixed with three essential oils (Foeniculum vulgare Mill., Mentha piperita L., and Pimpinella anisum L.) to formulate a product (HEMEO) whose active compounds include saponins and steroids in Asparagus racemosus, known for their anti-inflammatory properties; glycyrrhizin and flavonoids in Glycyrrhiza glabra, which exhibit gastroprotective and antispasmodic effects; menthol in Mentha piperita, contributing with antispasmodic and antimicrobial properties; and anethole and polyphenols in Pimpinella anisum, which modulate intestinal motility and offer antimicrobial activity. Objective: HEMEO was formulated for applications in intestinal motility disorders. Methods: HEMEO was evaluated for spontaneous and induced motility effects in isolated guinea pig ileum, colon, and stomach. Ex vivo experiments were conducted using LabChart software v7.0, and the product’s antibacterial action against Helicobacter pylori and its antioxidant effects were assessed through disc diffusion and FRAP assays. The presence of the volatile compounds in the formulation was confirmed by GC-MS analysis; the TPC of HEMEO, determined using the Folin–Ciocalteu method, was 9.925 ± 0.42 mg GAE/g. Conclusions: HEMEO showed a phenolic content correlated with its antioxidant potential and in addition inhibited H. pylori growth and demonstrated notable antioxidant properties, suggesting its role as a supportive agent in digestive processes and in managing motility disorders. Full article
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<p>Overview of experimental design of HEMEO.</p>
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<p>Plants pictures and chemical structure of key compounds found in the plant extracts and essential oils.</p>
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<p>Example of experimental original recording of the concentration–response curve of HEMEO on spontaneous longitudinal (Long) stomach basal contractility. (<b>a</b>) Spontaneous contraction (SC) signals for each concentration; (<b>b</b>) mean contraction amplitude (MCA) and spontaneous contraction variability (SCV), represented as error bars in the MCA plot and contraction percentage variation for the control (BSMA) for each considered condition; all the comparisons resulted in being statistically significant (<span class="html-italic">p</span> &lt; 0.05); (<b>c</b>) power spectral density (PSD) and percentage variations. Despite statistically significant differences between muscular tones at different HEMEO concentrations, the MCA variations are not physiologically significant (less than 20%). MF and HF bands values increase over 50% only for concentrations of 5.0 mg/mL and 10 mg/mL, suggesting a slight increase in mixing and pain.</p>
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<p>Example of experimental original recording of the concentration–response curve of HEMEO on spontaneous longitudinal (Long) ileum basal contractility. (<b>a</b>) Spontaneous contraction (SC) signals for each concentration; (<b>b</b>) mean contraction amplitude (MCA) and spontaneous contraction variability (SCV), represented as error bars in the MCA plot and contraction percentage variation for the control (BSMA) for each considered condition; not statistically significant differences (<span class="html-italic">p</span> &gt; 0.05) between MCAs at different concentrations are reported in the graph with a curly bracket. All the comparisons not reported are to be considered significant (<span class="html-italic">p</span> &lt; 0.05); (<b>c</b>) power spectral density (PSD) and percentage variations. Longitudinal tones present a biphasic behavior: it increases for 0.1 mg/mL concentrations and then decreases until a maximum difference of −60%. LF and HF present the same tend.</p>
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<p>Example of experimental original recording of the concentration–response curve of HEMEO on spontaneous longitudinal (Long) colon basal contractility. (<b>a</b>) Spontaneous contraction (SC) signals for each concentration; (<b>b</b>) mean contraction amplitude (MCA) and spontaneous contraction variability (SCV), represented as error bars in the MCA plot and contraction percentage variation for the control (BSMA) for each considered condition; all the comparisons reported resulted statistically significant (<span class="html-italic">p</span> &lt; 0.05); (<b>c</b>) power spectral density (PSD) and percentage variations. Longitudinal tones present a biphasic behavior: it increases for 0.1 mg/mL concentrations and then decreases until a maximum difference of −80%. LF and HF bands present the same biphasic trend. MF has a maximum increase of 300% at 0.5 mg/mL, then decreases after 5.0 mg/mL.</p>
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<p>Effect of HEMEO on histamine-induced contraction in isolated guinea pig ileum (<b>a</b>) and in spontaneously beating right atrium (<b>b</b>). Cumulative concentration–response curves were obtained before and after exposure to HEMEO (1 mg/mL) for 30 min. Each point is the mean ± SEM (<span class="html-italic">n</span> = 5–6). Where error bars are not shown, these are covered by the point itself.</p>
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<p>(<b>a</b>) The antioxidant power of the HEMEO solution was measured using the FRAP assay. (<b>b</b>) Comparison of 1 mg/mL HEMEO antioxidant power with the reference compound ascorbate.</p>
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<p>Schematic diagram showing the detail of the experimental design.</p>
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15 pages, 3359 KiB  
Article
Optimization and Standardization of the Extraction Method of Balanites aegyptiaca Del. Seeds (Zygophyllaceae) Used in the Formulation of an Antiparasitic Phytomedicine
by Mohamed Bonewendé Belemlilga, Salfo Ouedraogo, Gilchrist Abdoul Laurent Boly, Do Harouna Dao, Jonas Tiami Coulibaly, Jean Claude Romaric Pingdwindé Ouedraogo, Souleymane Compaoré, Sidiki Traore, Moumouni Koala, Estelle Noëla Hoho Youl, Lazare Belemnaba, Félix Bondo Kini, Aristide Traore, Séni Kouanda and Sylvin Ouedraogo
Pharmaceuticals 2024, 17(12), 1698; https://doi.org/10.3390/ph17121698 - 17 Dec 2024
Viewed by 287
Abstract
Background/Objectives: Balanites aegyptiaca Del. (Zygophyllaceae) is widely used in traditional medicine, both human and veterinary, throughout Africa for its many properties, including antiparasitic properties. This experimental study aims to optimize the extraction conditions of the seeds of Balanites aegyptiaca Del. Methods: Aqueous [...] Read more.
Background/Objectives: Balanites aegyptiaca Del. (Zygophyllaceae) is widely used in traditional medicine, both human and veterinary, throughout Africa for its many properties, including antiparasitic properties. This experimental study aims to optimize the extraction conditions of the seeds of Balanites aegyptiaca Del. Methods: Aqueous maceration was carried out with mass-to-volume ratios of 40%, 30%, 20%, 10% and 5% and extraction times of 6, 12, 24, 36 and 48 h. Extraction yields, phytochemical screening, saponins assay, antioxidant activities ABTS+ free radical scavenging activities, Ferric-reducing antioxidant power (FRAP) assay and antiparasitic tests on Heligmosomoides bakeri were used to compare the different extracts. Results: The pharmaco-chemical study generally showed that aqueous maceration gave the best results, with a mass/volume ratio of 10% after 12 h of maceration. The yield obtained was 28.03% with a saponins content of 13.81 mg/g. The antioxidant activities were 4.25 ± 0.17 µg/mL by the ABTS method and 0.739 µg/mL by the FRAP method. The larvicidal activity also showed that the 10% 12 h extract produced 100% larval mortality from 25 µg/mL. Conclusions: These data provide a basis for guiding the extraction process parameters in producing this antiparasitic phytomedicine. Full article
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<p>Almond powder (<b>a</b>) and lyophilized extract (<b>b</b>) of <span class="html-italic">Balanites aegyptiaca</span> seeds.</p>
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<p>The residual moisture content of different lyophilizate. ** <span class="html-italic">p</span> &lt; 0.01, **** <span class="html-italic">p</span> &lt; 0.0001 is considered significant compared with the other % macerates (two-way ANOVA followed by the “Tukey” multiple comparison test; ns is considered not significant). <span class="html-italic">n</span> = 3.</p>
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<p>Extraction yield histogram of aqueous macerates mass/volume ratio as a function of time (hours). *** <span class="html-italic">p</span> &lt; 0.01, **** <span class="html-italic">p</span> &lt; 0.0001 is considered significant compared with the other % macerates (two-way ANOVA followed by the “Tukey” multiple comparison test; ns is considered not significant). <span class="html-italic">n</span> = 3.</p>
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<p>Analytical TLC profile of different extracts. (<b>a</b>) The presence of saponins revealed by sulfuric anisaldehyde after heating the plate observed in visible light. (<b>b</b>) Presence of flavonoids (at 254 nm) detected by NEU reagent.</p>
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<p>Larvicidal effect of <span class="html-italic">B. aegyptiaca</span> extracts and the standard on <span class="html-italic">H. bakeri</span>.</p>
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<p>Whole plant (<b>a</b>), fruits (<b>b</b>) and isolated saponins (<b>c</b>,<b>d</b>) of <span class="html-italic">Balanites aegyptiaca</span>.</p>
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22 pages, 5864 KiB  
Article
The Effect of Seasonal and Annual Variation on the Quality of Polygonatum Cyrtonema Hua Rhizomes
by Weiting Pu, Yefei Yu, Xiaoxiao Shi, Ye Shao, Bihuan Ye, Youwu Chen, Qiyan Song, Jianjun Shen and Haibo Li
Plants 2024, 13(24), 3459; https://doi.org/10.3390/plants13243459 - 10 Dec 2024
Viewed by 378
Abstract
This study aims to reveal the interannual and seasonal variations in functional components in Polygonatum cyrtonema Hua. rhizomes and evaluate whether the variations significantly affect the quality of rhizomes as a traditional Chinese herbal medicine. The interannual and seasonal variations in total flavonoid [...] Read more.
This study aims to reveal the interannual and seasonal variations in functional components in Polygonatum cyrtonema Hua. rhizomes and evaluate whether the variations significantly affect the quality of rhizomes as a traditional Chinese herbal medicine. The interannual and seasonal variations in total flavonoid content and total saponin content were analyzed. The global dynamic variation in secondary metabolites in the rhizomes during a five-year growth period and in two traditional harvesting seasons were investigated based on metabolomics method. Results clearly showed that the functional components in P. cyrtonema rhizomes exhibited a significant increase in accumulation during the one- to four-year growth period and a significant decrease in accumulation during the four- to five-year growth period. The most active accumulation occurred during the three- to four-year growth period. Drastic variations in functional components occurred from spring to autumn. The significant interannual variation and drastic seasonal variation were strongly associated with the enrichment in some pathways related to the biosynthesis of secondary metabolites and the metabolisms of amino acids. The interannual and seasonal variations in functional components significantly affected the quality of P. cyrtonema rhizomes. The four-year-old rhizomes had the most superior quality due to their higher content of functional components and much more newly formed components. The rhizomes harvested in spring or autumn had unequal quality because of their significant differences in composition and content of functional components. Specifically, the rhizomes from spring contained more flavonoids, alkaloids, and phenolic acids, while those from autumn comprised more steroids. In conclusion, this study reveals that the interannual and seasonal variations in functional components can significantly affect the quality of P. cyrtonema rhizomes as a traditional Chinese herbal medicine. This study provides foundational insights and theoretical guidance for determining an optimal cultivation period to obtain medicinal rhizomes with superior quality. It also offers a strategy for harvesting medicinal rhizomes in two different seasons to achieve unequal quality. Full article
(This article belongs to the Section Phytochemistry)
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<p>Total flavonoid content and total saponin content in <span class="html-italic">P. cyrtonema</span> rhizomes. (<b>A</b>), Total flavonoid content in five age sections; (<b>B</b>), total flavonoid content in entire rhizomes in spring and autumn; (<b>C</b>), total saponin content in five age sections; (<b>D</b>), total saponins content in entire rhizomes in spring and autumn. The letters PS and PA refer to the rhizomes harvested in spring and autumn, respectively. The abbreviated ns represents no significant difference. ****, ***, **, and * represent statistically significant at <span class="html-italic">p</span> &lt; 0.0001, <span class="html-italic">p</span> &lt; 0.001, <span class="html-italic">p</span> &lt; 0.01, and <span class="html-italic">p</span> &lt; 0.05, respectively.</p>
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<p>Basic information on secondary metabolites detected from <span class="html-italic">P. cyrtonema</span> rhizomes. (<b>A</b>), Clustered heatmap of secondary metabolites in samples of one-year-old age sections (AS1 group), two-year-old age sections (AS2 group), three-year-old age sections (AS3 group), four-year-old age sections (AS4 group), and five-year-old age sections (AS5 group); (<b>B</b>), clustered heatmap of secondary metabolites in samples of spring rhizome (PS group) and autumn rhizome (PA group). The shades of color indicate the quantity of metabolites, with redder shades representing more and greener shades representing fewer.</p>
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<p>Quantity of differential accumulated secondary metabolites (DASMs) in five pairwise comparisons.</p>
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<p>The differential accumulated homoisoflavonoids in <span class="html-italic">P. cyrtonema</span> rhizomes. (<b>A</b>), In five age sections of rhizomes during the entire five-year growing period; (<b>B</b>), in entire rhizomes during the growing period from spring to autumn. The letters AS1, AS2, AS3, AS4, and AS5 refer to one-, two-, three-, four-, and five-year-old age sections, respectively.</p>
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<p>Interannual and seasonal variation in secondary metabolites in <span class="html-italic">P. cyrtonema</span> rhizomes. (<b>A</b>), From the one- to five-year growing periods; (<b>B</b>), during the spring–autumn growing period.</p>
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<p>Class and quantity of main differential accumulated secondary metabolites (DASMs) in <span class="html-italic">P. cyrtonema</span> rhizomes. (<b>A</b>), From the one- to five-year growing periods; (<b>B</b>), during the spring–autumn growing period.</p>
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<p>The top 20 significantly enriched KEGG pathways identified from AS4 vs. AS3, AS5 vs. AS4, and PS vs. PA. The color of dots in plots refers to higher or lower <span class="html-italic">p</span>-values, with bluer shades representing higher and redder shades representing lower. The size of a dot represents more or fewer secondary metabolites, with larger dots representing more and smaller dots representing fewer.</p>
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<p>Five-year-old <span class="html-italic">P. cyrtonema</span> rhizomes used in this study. (<b>A</b>), <span class="html-italic">P. cyrtonema</span> plant; (<b>B</b>), the age sections of rhizome used for interannual variation analysis; (<b>C</b>), the entire rhizomes harvested in spring and autumn used for seasonal variation analysis. The letters AS1, AS2, AS3, AS4, and AS5 refer to the one-, two-, three-, four-, and five-year-old age sections, respectively; The letters PS and PA refer to the rhizomes harvested in spring and autumn, respectively.</p>
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13 pages, 2216 KiB  
Article
Mathematical Modeling of Inhibitory Microbial Lethality Synergistic: Secondary Phytocompounds from Purple Toronjil, Temperature, and Harvest Stress Effects on Escherichia coli
by AyslethSacar Celis-Segura, Juan Reséndiz-Muñoz, Edgar Jesús Delgado-Nuñez, Víctor Manuel Zamora-Gasa, José Luis Fernández-Muñoz, Blas Cruz-Lagunas, Flaviano Godinez-Jaimes, Miguel Angel Gruintal-Santos and Romeo Urbieta-Parrazales
Stresses 2024, 4(4), 870-882; https://doi.org/10.3390/stresses4040058 - 9 Dec 2024
Viewed by 592
Abstract
This research investigated the inhibition of *Escherichia coli* ATCC 25922 (E. coli) bacterial growth in situ, specifically on the stems and aerial parts of *Agastache mexicana* subsp. mexicana (Amm) or “purple toronjil” and on food-grade paper, [...] Read more.
This research investigated the inhibition of *Escherichia coli* ATCC 25922 (E. coli) bacterial growth in situ, specifically on the stems and aerial parts of *Agastache mexicana* subsp. mexicana (Amm) or “purple toronjil” and on food-grade paper, both contained within Kraft paper bags with a plastic window. The qualitative phytochemical profile of an aqueous extract of Amm revealed the presence of various compounds including alkaloids, coumarins, tannins, flavonoids, saponins, triterpenes, and sterols. The results indicate that these secondary metabolites exhibit a synergistic bactericidal effect, especially when combined with temperature and starvation stress. This was quantified using a decay equation referred to as the bacterial growth inhibition profile of E. coli (BGIPEc). Calculations, which included first derivatives, gradients based on substrate effects and temperature as well as the area under the curve of BGIPEc, demonstrated that higher temperatures led to the greater inhibition of colony forming units (CFUs), further enhanced by the presence of secondary metabolites. Additionally, a shorter half-life corresponded to a faster change rate and a lower area under the curve, indicating a reduced survival rate over time. At lower temperatures, E. coli exhibited a survival effect, which was corroborated by the preceding calculations. Full article
(This article belongs to the Section Animal and Human Stresses)
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<p>Inhibition curves of <span class="html-italic">E. coli</span> ATCC 25922: (<b>a</b>) <span class="html-italic">Amm</span> 35.5 °C, (<b>b</b>) control 35. 5 °C, (<b>c</b>) <span class="html-italic">Amm</span> 8.12 °C, and (<b>d</b>) control 8.12 °C.</p>
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<p>Inhibition of the <span class="html-italic">E. coli</span> ATCC 25922 four treatments: (<b>a</b>) comparative (<b>b</b>) inhibition change rate, (<b>c</b>) temperature effect, and (<b>d</b>) substrate effect.</p>
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<p>The area beneath the curve was calculated using integral Equation (13) over seven CFU measurement intervals.</p>
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<p>(<b>a</b>) Inoculated aerial parts of <span class="html-italic">Amm</span> with <span class="html-italic">E. coli</span> ATCC 25922 in a paper bag. (<b>b</b>) Food-grade paper being inoculated.</p>
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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 - 7 Dec 2024
Viewed by 603
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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19 pages, 4015 KiB  
Review
Asteroid Saponins: A Review of Their Bioactivity and Selective Cytotoxicity
by Stuart J. Smith, Tianfang Wang and Scott F. Cummins
Mar. Drugs 2024, 22(12), 552; https://doi.org/10.3390/md22120552 - 7 Dec 2024
Viewed by 714
Abstract
Saponins are a diverse class of secondary metabolites that are often reported to exhibit a variety of pharmacological applications. While research into the elucidation and application of plant and class Holothuroidea-derived saponins (i.e., sea cucumbers) is extensive, the class Asteroidea-derived saponins (i.e., seastars) [...] Read more.
Saponins are a diverse class of secondary metabolites that are often reported to exhibit a variety of pharmacological applications. While research into the elucidation and application of plant and class Holothuroidea-derived saponins (i.e., sea cucumbers) is extensive, the class Asteroidea-derived saponins (i.e., seastars) have been largely overlooked and primarily limited to elucidation. This review provides a comprehensive overview of the cytotoxic activities of asteroid-derived saponins against various cell cultures, for instance, mammalian erythrocytes, multiple microbial strains and cancer cell lines, including melanoma, breast, colon, and lung cancers. Highlighting the distinct structural variations in these saponins, this review examines their selective cytotoxicity and potency, with many demonstrating IC50 values in the low micromolar range. Specific compounds, such as asterosaponins and polyhydroxylated saponins, exhibit noteworthy effects, particularly against melanoma and lung carcinoma cells, while triterpenoid saponins were found to be highly cytotoxic to both erythrocytes and fungal cells. This review also addresses gaps in the research area, including the need for additional in vitro antimicrobial studies, in vivo studies, and further exploration of their mechanisms of action. By consolidating recent findings, we have shed light on the therapeutic potential of asteroid-derived steroidal saponins in developing novel antimicrobial and anticancer agents. Full article
(This article belongs to the Special Issue Biologically Active Compounds from Marine Invertebrates 2025)
11 pages, 1586 KiB  
Article
Three New Triterpene Glycosides from the Roots of Deutzia x Hybrida “Strawberry Fields” (Hydrangeaceae)
by Efstathia Karachaliou, David Pertuit, Antoine Bruguière, Marie-José Penouilh, Michel Picquet, Christine Belloir, Loïc Briand and Anne-Claire Mitaine-Offer
Molecules 2024, 29(23), 5781; https://doi.org/10.3390/molecules29235781 - 6 Dec 2024
Viewed by 542
Abstract
Three new triterpene glycosides were isolated from Deutzia x hybrida “Strawberry Fields” cultivar via aqueous–ethanolic extraction of the roots, including one derivative of sumaresinolic acid and two of echinocystic acid: 3-O-β-D-glucuronopyranosylsumaresinolic acid 28-O-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl ester, 3-O-β-D-glucuronopyranosylechinocystic acid 28- [...] Read more.
Three new triterpene glycosides were isolated from Deutzia x hybrida “Strawberry Fields” cultivar via aqueous–ethanolic extraction of the roots, including one derivative of sumaresinolic acid and two of echinocystic acid: 3-O-β-D-glucuronopyranosylsumaresinolic acid 28-O-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl ester, 3-O-β-D-glucuronopyranosylechinocystic acid 28-O-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl ester, and 3-O-α-L-arabinopyranosyl-(1→3)-β-D-glucuronopyranosylechinocystic acid 28-O-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl ester. As none of the isolated saponins were previously documented in the literature, their structural elucidation required extensive 1D and homo- and heteronuclear 2D NMR spectroscopy, as well as mass spectrometry analysis. All three glycosides were tested for their stimulatory activity of the sweet taste receptor TAS1R2/TAS1R3. It is the first chemical and biological investigation of Deutzia x hybrida “Strawberry Fields” as well as the first report of sumaresinolic acid glycosides in Deutzia genus. Full article
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<p>Structures of saponins <b>1</b>–<b>3</b>.</p>
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<p>Fragment ions (<span class="html-italic">m</span>/<span class="html-italic">z</span>) of pseudo-molecular ion peaks for <b>1</b>–<b>3</b> (HR-ESIMS positive-ion mode).</p>
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<p>Key HMBC and ROESY correlations for compound <b>1</b>.</p>
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<p>Diagram of TAS1R2/TAS1R3 activity response for sucralose (black curve) and compounds <b>1</b>–<b>3</b> (respectively green curve for <b>1</b>, blue for <b>2</b>, and red for <b>3</b>). The x-axis shows the concentration (µM). The y-axis shows the relative changes in fluorescence (ΔF/F0). The ΔF/F0 values are expressed as the mean ± sem (n = 6). EC50: half maximal effective concentration. Max: maximal amplitude of fluorescence signal.</p>
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