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The Role of Bioactive Compounds in Cancer, Inflammation and Other Diseases

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: closed (27 April 2024) | Viewed by 5054

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Special Issue Editor

Prof. Dr. Guan-Jhong Huang

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Guest Editor

Department of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, College of Chinese Medicine, China Medical University, No.91, Hsueh-Shih Road, Taichung 40402, Taiwan
Interests: metabolic disorders; cancer; inflammation; oxidative stress; natural compounds; molecular signaling
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

A bioactive compound is a compound that has an effect on a living organism, tissue or cell, usually demonstrated by basic research in vitro or in vivo in the laboratory. Bioactive compounds are commonly derived from plants, and can be synthetically produced. Examples of plant bioactive compounds are carotenoids, polyphenols, or phytosterols. Bioactive compounds from plants are vital for human health and disease, which are gaining wide attention for their anticancer activities and anti-inflammatory activity, etc., yet their significance remains underappreciated.

This Special Issue aims to provide a platform for molecular mechanistic research and potential medical applications on bioactive compound with a special focus on inhibition of inflammation, tumor growth and metastasis, enhancement of cancer therapeutic efficacy or amelioration of the associated adverse effects. Research and develop hyphenated technological platforms of metabolomics for deciphering the biosynthetic pathway(s) of specific bioactive phytocompounds in plants.

We warmly welcome your submissions of original papers and reviews based on results from molecular viewpoints.

This Special Issue is supervised by Prof. Dr. Guan-Jhong Huang and assisted by our Guest Editor’ assistant editor Dr. Xingkang Wu [email protected] (Modern Research Center for Traditional Chinese Medicine, the Key Laboratory of Chemical Biology and Molecular Engineering of Ministry of Education, Shanxi University).

Prof. Dr. Guan-Jhong Huang
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

cancer
inflammation
cardiovascular diseases
plants
bioactive compounds

Published Papers (6 papers)

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Research

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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

Viewed by 558

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 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 Cancer, Inflammation and Other Diseases)

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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 - 07 Mar 2024

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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, 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 Cancer, Inflammation and Other Diseases)

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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

Viewed by 636

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 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 Cancer, Inflammation and Other Diseases)

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Review

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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

Viewed by 489

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 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 Cancer, Inflammation and Other Diseases)

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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 680

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 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 Cancer, Inflammation and Other Diseases)

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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 2 | Viewed by 1058

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. 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 Cancer, Inflammation and Other Diseases)

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