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17 pages, 1631 KiB

Open AccessArticle

Potential of Polar Lipids Isolated from the Marine Sponge Haliclona (Halichoclona) vansoesti against Melanoma

by Nadia Ruocco, Genoveffa Nuzzo, Serena Federico, Roberta Esposito, Carmela Gallo, Marcello Ziaco, Emiliano Manzo, Angelo Fontana, Marco Bertolino, Giacomo Zagami, Valerio Zupo, Clementina Sansone and Maria Costantini

Int. J. Mol. Sci. 2024, 25(13), 7418; https://doi.org/10.3390/ijms25137418 - 6 Jul 2024

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Abstract

Marine sponges represent a good source of natural metabolites for biotechnological applications in the pharmacological, cosmeceutical, and nutraceutical fields. In the present work, we analyzed the biotechnological potential of the alien species Haliclona (Halichoclona) vansoesti de Weerdt, de Kluijver & Gomez, [...] Read more.

Marine sponges represent a good source of natural metabolites for biotechnological applications in the pharmacological, cosmeceutical, and nutraceutical fields. In the present work, we analyzed the biotechnological potential of the alien species Haliclona (Halichoclona) vansoesti de Weerdt, de Kluijver & Gomez, 1999, previously collected in the Mediterranean Sea (Faro Lake, Sicily). The bioactivity and chemical content of this species has never been investigated, and information in the literature on its Caribbean counterpart is scarce. We show that an enriched extract of H. vansoesti induced cell death in human melanoma cells with an IC₅₀ value of 36.36 µg mL⁻¹, by (i) triggering a pro-inflammatory response, (ii) activating extrinsic apoptosis mediated by tumor necrosis factor receptors triggering the mitochondrial apoptosis via the involvement of Bcl-2 proteins and caspase 9, and (iii) inducing a significant reduction in several proteins promoting human angiogenesis. Through orthogonal SPE fractionations, we identified two active sphingoid-based lipid classes, also characterized by nuclear magnetic resonance and mass spectrometry, as the main components of two active fractions. Overall, our findings provide the first evaluation of the anti-cancer potential of polar lipids isolated from the marine sponge H. (Halichoclona) vansoesti, which may lead to new lead compounds with biotechnological applications in the pharmaceutical field. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Disease)

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41 pages, 4123 KiB

Open AccessArticle

Bioactive Compounds and Potential Health Benefits through Cosmetic Applications of Cherry Stem Extract

by Abigail García-Villegas, Álvaro Fernández-Ochoa, María Elena Alañón, Alejandro Rojas-García, David Arráez-Román, María de la Luz Cádiz-Gurrea and Antonio Segura-Carretero

Int. J. Mol. Sci. 2024, 25(7), 3723; https://doi.org/10.3390/ijms25073723 - 27 Mar 2024

Cited by 3 | Viewed by 1445

Abstract

Cherry stems, prized in traditional medicine for their potent antioxidant and anti-inflammatory properties, derive their efficacy from abundant polyphenols and anthocyanins. This makes them an ideal option for addressing skin aging and diseases. This study aimed to assess the antioxidant and anti-inflammatory effects [...] Read more.

Cherry stems, prized in traditional medicine for their potent antioxidant and anti-inflammatory properties, derive their efficacy from abundant polyphenols and anthocyanins. This makes them an ideal option for addressing skin aging and diseases. This study aimed to assess the antioxidant and anti-inflammatory effects of cherry stem extract for potential skincare use. To this end, the extract was first comprehensively characterized by HPLC-ESI-qTOF-MS. The extract’s total phenolic content (TPC), antioxidant capacity, radical scavenging efficiency, and its ability to inhibit enzymes related to skin aging were determined. A total of 146 compounds were annotated in the cherry stem extract. The extract effectively fought against NO^· and HOCl radicals with IC₅₀ values of 2.32 and 5.4 mg/L. Additionally, it inhibited HYALase, collagenase, and XOD enzymes with IC₅₀ values of 7.39, 111.92, and 10 mg/L, respectively. Based on the promising results that were obtained, the extract was subsequently gently integrated into a cosmetic gel at different concentrations and subjected to further stability evaluations. The accelerated stability was assessed through temperature ramping, heating-cooling cycles, and centrifugation, while the long-term stability was evaluated by storing the formulations under light and dark conditions for three months. The gel formulation enriched with cherry stem extract exhibited good stability and compatibility for topical application. Cherry stem extract may be a valuable ingredient for creating beneficial skincare cosmeceuticals. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Disease)

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18 pages, 11130 KiB

Open AccessArticle

Jozimine A₂, a Dimeric Naphthylisoquinoline (NIQ) Alkaloid, Shows In Vitro Cytotoxic Effects against Leukemia Cells through NF-κB Inhibition

by Roxana Damiescu, Rümeysa Yücer, Sabine M. Klauck, Gerhard Bringmann, Thomas Efferth and Mona Dawood

Int. J. Mol. Sci. 2024, 25(6), 3087; https://doi.org/10.3390/ijms25063087 - 7 Mar 2024

Viewed by 1458

Abstract

Naphthylisoquinoline (NIQ) alkaloids are rising as a promising class of secondary metabolites with pharmaceutical potential. NF-κB has already been recognized as a significant modulator of cancer proliferation and drug resistance. We have previously reported the mechanisms behind the cytotoxic effect of dioncophylline A, [...] Read more.

Naphthylisoquinoline (NIQ) alkaloids are rising as a promising class of secondary metabolites with pharmaceutical potential. NF-κB has already been recognized as a significant modulator of cancer proliferation and drug resistance. We have previously reported the mechanisms behind the cytotoxic effect of dioncophylline A, an NIQ monomer, in leukemia cells. In the current study, we have investigated the cytotoxic effect of jozimine A₂, an NIQ dimer, on leukemia cells in comparison to a second, structurally unsymmetric dimer, michellamine B. To this end, molecular docking was applied to predict the binding affinity of the dimers towards NF-κB, which was then validated through microscale thermophoresis. Next, cytotoxicity assays were performed on CCRF-CEM cells and multidrug-resistant CEM/ADR5000 cells following treatment. Transcriptome analysis uncovered the molecular networks affected by jozimine A₂ and identified the cell cycle as one of the major affected processes. Cell death modes were evaluated through flow cytometry, while angiogenesis was measured with the endothelial cell tube formation assay on human umbilical vein endothelial cells (HUVECs). The results indicated that jozimine A₂ bound to NF-κB, inhibited its activity and prevented its translocation to the nucleus. In addition, jozimine A₂ induced cell death through apoptosis and prevented angiogenesis. Our study describes the cytotoxic effect of jozimine A₂ on leukemia cells and explains the interactions with the NF-κB signaling pathway and the anticancer activity. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Disease)

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13 pages, 6024 KiB

Open AccessArticle

Mass Spectrometry Study about In Vitro and In Vivo Reaction between Metformin and Glucose: A Preliminary Investigation on Alternative Biological Behavior

by Gianluca Bartolucci, Marco Pallecchi, Laura Braconi, Silvia Dei, Elisabetta Teodori, Annunziata Lapolla, Giovanni Sartore and Pietro Traldi

Int. J. Mol. Sci. 2024, 25(1), 180; https://doi.org/10.3390/ijms25010180 - 22 Dec 2023

Cited by 1 | Viewed by 1214

Abstract

Metformin is the most prescribed glucose-lowering drug worldwide; globally, over 100 million patients are prescribed this drug annually. Some different action mechanisms have been proposed for this drug, but, surprisingly, no metabolite of metformin has ever been described. It was considered interesting to [...] Read more.

Metformin is the most prescribed glucose-lowering drug worldwide; globally, over 100 million patients are prescribed this drug annually. Some different action mechanisms have been proposed for this drug, but, surprisingly, no metabolite of metformin has ever been described. It was considered interesting to investigate the possible reaction of metformin with glucose following the Maillard reaction pattern. The reaction was first performed in in vitro conditions, showing the formation of two adducts that originated by the condensation of the two molecular species with the losses of one or two water molecules. Their structures were investigated by liquid chromatography coupled with mass spectrometry (HPLC-MS), tandem mass spectrometry (MS/MS) and accurate mass measurements (HRMS). The species originated via the reaction of glucose and metformin and were called metformose and dehydrometformose, and some structural hypotheses were conducted. It is worth to emphasize that they were detected in urine samples from a diabetic patient treated with metformin and consequently they must be considered metabolites of the drug, which has never been identified before now. The glucose-related substructure of these compounds could reflect an improved transfer across cell membranes and, consequently, new hypotheses could be made about the biological targets of metformin. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Disease)

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Review

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27 pages, 2830 KiB

Open AccessReview

Marine Polyphenols in Cardiovascular Health: Unraveling Structure–Activity Relationships, Mechanisms, and Therapeutic Implications

by D. P. Nagahawatta, N. M. Liyanage, Thilina U. Jayawardena and You-Jin Jeon

Int. J. Mol. Sci. 2024, 25(15), 8419; https://doi.org/10.3390/ijms25158419 - 1 Aug 2024

Cited by 1 | Viewed by 1097

Abstract

Cardiovascular diseases (CVDs) are responsible for significant mortality rates globally that have been raised due to the limitation of the available treatments and prevalence of CVDs. The innovative research and identification of potential preventives for CVDs are essential to alleviate global deaths and [...] Read more.

Cardiovascular diseases (CVDs) are responsible for significant mortality rates globally that have been raised due to the limitation of the available treatments and prevalence of CVDs. The innovative research and identification of potential preventives for CVDs are essential to alleviate global deaths and complications. The marine environment is a rich source of bioactive substances and provides a unique chemical arsenal against numerous ailments due to its unrivaled biodiversity. Marine polyphenolic compounds (MPCs) are unique because of their structural variety and biologically significant activity. Further, MPCs are well-reported for their valuable biological activities, such as anti-inflammatory, cardioprotective, and antioxidant, demonstrating encouraging results in preventing and treating CVDs. Therefore, investigation of the structure–activity relationship (SAR) between MPCs and CVDs provides insights that reveal how the structural components of these compounds affect their effectiveness. Further, comprehending this correlation is essential for advancing medications and nutraceuticals sourced from marine sources, which could transform the strategy for treating and preventing cardiovascular diseases. Therefore, this study provides a comprehensive analysis of existing research by emphasizing the role of MPCs in CVD treatments and evaluating the SAR between MPCs and CVDs with challenges and future directions. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Disease)

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15 pages, 504 KiB

Open AccessReview

Dietary Phenolic Compounds—Wellbeing and Perspective Applications

by Dasha Mihaylova, Maria Dimitrova-Dimova and Aneta Popova

Int. J. Mol. Sci. 2024, 25(9), 4769; https://doi.org/10.3390/ijms25094769 - 27 Apr 2024

Cited by 6 | Viewed by 2296

Abstract

Contemporary living is continuously leading to poor everyday choices resulting in the manifestation of various diseases. The benefits of plant-based nutrition are undeniable and research on the topic is rising. Modern man is now aware of the possibilities that plant nutrition can provide [...] Read more.

Contemporary living is continuously leading to poor everyday choices resulting in the manifestation of various diseases. The benefits of plant-based nutrition are undeniable and research on the topic is rising. Modern man is now aware of the possibilities that plant nutrition can provide and is seeking ways to benefit from it. Dietary phenolic compounds are among the easily accessible beneficial substances that can exhibit antioxidant, anti-inflammatory, antitumor, antibacterial, antiviral, antifungal, antiparasitic, analgesic, anti-diabetic, anti-atherogenic, antiproliferative, as well as cardio-and neuroprotective activities. Several industries are exploring ways to incorporate biologically active substances in their produce. This review is concentrated on presenting current information about the dietary phenolic compounds and their contribution to maintaining good health. Additionally, this content will demonstrate the importance and prosperity of natural compounds for various fields, i.e., food industry, cosmetology, and biotechnology, among others. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Disease)

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11 pages, 479 KiB

Open AccessReview

Exploring the Impact of Alternative Sources of Dietary Nitrate Supplementation on Exercise Performance

by Maciej Jędrejko, Karol Jędrejko, Víctor M. Gómez-Renaud, Katarzyna Kała and Bożena Muszyńska

Int. J. Mol. Sci. 2024, 25(7), 3650; https://doi.org/10.3390/ijms25073650 - 25 Mar 2024

Viewed by 1756

Abstract

An increase in the level of nitric oxide (NO) plays a key role in regulating the human cardiovascular system (lowering blood pressure, improving blood flow), glycemic control in type 2 diabetes, and may help enhance exercise capacity in healthy individuals (including athletes). This [...] Read more.

An increase in the level of nitric oxide (NO) plays a key role in regulating the human cardiovascular system (lowering blood pressure, improving blood flow), glycemic control in type 2 diabetes, and may help enhance exercise capacity in healthy individuals (including athletes). This molecule is formed by endogenous enzymatic synthesis and the intake of inorganic nitrate (NO₃⁻) from dietary sources. Although one of the most well-known natural sources of NO₃⁻ in the daily diet is beetroot (Beta vulgaris), this review also explores other plant sources of NO₃⁻ with comparable concentrations that could serve as ergogenic aids, supporting exercise performance or recovery in healthy individuals. The results of the analysis demonstrate that red spinach (Amaranthus spp.) and green spinach (Spinacia oleracea) are alternative natural sources rich in dietary NO₃⁻. The outcomes of the collected studies showed that consumption of selected alternative sources of inorganic NO₃⁻ could support physical condition. Red spinach and green spinach have been shown to improve exercise performance or accelerate recovery after physical exertion in healthy subjects (including athletes). Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Disease)

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20 pages, 1692 KiB

Open AccessReview

The Anti-Diabetic Potential of Baicalin: Evidence from Rodent Studies

by Tomasz Szkudelski and Katarzyna Szkudelska

Int. J. Mol. Sci. 2024, 25(1), 431; https://doi.org/10.3390/ijms25010431 - 28 Dec 2023

Cited by 5 | Viewed by 1809

Abstract

Baicalin is a biologically active flavonoid compound that benefits the organism in various pathological conditions. Rodent studies have shown that this compound effectively alleviates diabetes-related disturbances in models of type 1 and type 2 diabetes. Baicalin supplementation limited hyperglycemia and improved insulin sensitivity. [...] Read more.

Baicalin is a biologically active flavonoid compound that benefits the organism in various pathological conditions. Rodent studies have shown that this compound effectively alleviates diabetes-related disturbances in models of type 1 and type 2 diabetes. Baicalin supplementation limited hyperglycemia and improved insulin sensitivity. The anti-diabetic effects of baicalin covered the main insulin-sensitive tissues, i.e., the skeletal muscle, the adipose tissue, and the liver. In the muscle tissue, baicalin limited lipid accumulation and improved glucose transport. Baicalin therapy was associated with diminished adipose tissue content and increased mitochondrial biogenesis. Hepatic lipid accumulation and glucose output were also decreased as a result of baicalin supplementation. The molecular mechanism of the anti-diabetic action of this compound is pleiotropic and is associated with changes in the expression/action of pivotal enzymes and signaling molecules. Baicalin positively affected, among others, the tissue insulin receptor, glucose transporter, AMP-activated protein kinase, protein kinase B, carnitine palmitoyltransferase, acetyl-CoA carboxylase, and fatty acid synthase. Moreover, this compound ameliorated diabetes-related oxidative and inflammatory stress and reduced epigenetic modifications. Importantly, baicalin supplementation at the effective doses did not induce any side effects. Results of rodent studies imply that baicalin may be tested as an anti-diabetic agent in humans. Full article

(This article belongs to the Special Issue The Role of Bioactive Compounds in Human Health and Disease)

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