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Bioactive Compounds: Applications and Benefits for Human Health
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Bioactive Compounds: Applications and Benefits for Human Health

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: 31 July 2025 | Viewed by 4314

Special Issue Editors

Dr. Sara Baldelli

E-Mail Website
Guest Editor
1. Department for the Promotion of Human Science and Quality of Life, San Raffaele Open University, Via di Val Cannuta, 247, 00166 Rome, Italy
2. IRCCS San Raffaele Roma, Via di Val Cannuta, 247, 00166 Rome, Italy
Interests: bioactive compounds; polyphenols; terpenoids; alkaloids; glucosinolates; antioxidant; anti-inflammatory
Special Issues, Collections and Topics in MDPI journals
Dr. Gilda Aiello

E-Mail Website
Guest Editor
Department for the Promotion of Human Science and Quality of Life, San Raffaele Open University, Via di Val Cannuta, 247, 00166 Rome, Italy
Interests: plant proteins; discovery and identification of bioactive peptides; functional food; food analysis by mass spectrometry; peptide stability
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Mauro Lombardo

E-Mail Website
Guest Editor
Department of Human Sciences and Promotion of the Quality of Life, San Raffaele Roma Open University, 00166 Rome, Italy
Interests: obesity; sports nutrition; bariatric surgery; body composition; Mediterranean diet; clinical nutrition
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Bioactive compounds are natural constituents found in many foods such as vegetables, fruits, olive oil, wine, tea, spices, cereals, beer and chocolate, but they can also be derived from animals and microbial sources, or be chemically synthesized. Among the most commonly analyzed bioactive compounds are polyphenols, terpenoids, alkaloids and glucosinolates, which, having antioxidant and anti-inflammatory properties, are able to modulate some important physiological functions, molecular pathways and biological activities. Thus, bioactive compounds can exert beneficial effects on human health. In fact, many scientific studies to date have explored the consequences of the consumption of bioactive compounds with respect to some pathologies, such as cardiovascular diseases, bacterial and viral infections, modulation of the microbiota, neurodegenerative diseases, cancer and even sarcopenia.

This Special Issue focuses on the analysis of the molecular effects of bioactive compounds in different physiological or pathological conditions (cardiovascular diseases, bacterial and viral infections, neurodegenerative diseases, cancer and sarcopenia). Furthermore, it will include studies regarding the identification, purification and extraction of bioactive compounds and their use in pre-clinical and clinical research.

Dr. Sara Baldelli
Dr. Gilda Aiello
Dr. Mauro Lombardo
Guest Editors

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. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). 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

  • bioactive compounds
  • polyphenols
  • terpenoids
  • alkaloids
  • glucosinolates
  • antioxidant
  • anti-inflammatory
  • cardiovascular diseases
  • bacterial and viral infections
  • microbiota
  • neurodegenerative diseases
  • cancer
  • sarcopenia
  • identification
  • purification
  • extraction
  • pre-clinical
  • clinical

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Published Papers (4 papers)

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Research

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20 pages, 4162 KiB  
Article
Anti-Angiogenic Potential of Marine Streptomyces-Derived Lucknolide A on VEGF/VEGFR2 Signaling in Human Endothelial Cells
by Byeoung-Kyu Choi, Min-Hee Jo, Hee Jae Shin and Sun Joo Park
Molecules 2025, 30(5), 987; https://doi.org/10.3390/molecules30050987 - 20 Feb 2025
Viewed by 591
Abstract
Angiogenesis, primarily driven by the vascular endothelial growth factor (VEGF) and its receptor, the VEGFR, plays a key role in various pathological processes such as cancer progression. Here, we investigated the anti-angiogenic effects of Lucknolide A (LA), a marine Streptomyces-derived compound, and [...] Read more.
Angiogenesis, primarily driven by the vascular endothelial growth factor (VEGF) and its receptor, the VEGFR, plays a key role in various pathological processes such as cancer progression. Here, we investigated the anti-angiogenic effects of Lucknolide A (LA), a marine Streptomyces-derived compound, and evaluated its potential as a VEGFR2 inhibitor. LA selectively inhibited the proliferation of human endothelial cells EA.hy926 and HUVEC while exhibiting minimal effects on normal fibroblasts and various tumor cells. LA induced S-phase cell cycle arrest and apoptosis in EA.hy926 cells, increasing apoptotic markers p53, Bax, and p21 and decreasing the anti-apoptotic protein Bcl-2, with these effects being further enhanced under VEGF stimulation. Additionally, LA suppressed VEGFR2 phosphorylation and its downstream signaling pathways, including Akt/mTOR/p70S6K, MEK/ERK, Src, FAK, and p38 MAPK, which are crucial for endothelial survival and angiogenesis. Molecular docking studies revealed that LA binds to both inactive (DFG-out, PDB: 4ASD) and active (DFG-in, PDB: 3B8R) VEGFR2 conformations, with a significantly stronger affinity for the active state (−107.96 kcal/mol) than the inactive state (−33.56 kcal/mol), suggesting its potential as a VEGFR2 kinase inhibitor. Functionally, LA significantly inhibited VEGF-induced endothelial migration, tube formation, and microvessel sprouting in both in vitro and ex vivo rat aortic ring assays. Additionally, LA reduced tumor-associated tube formation induced by human breast tumor cells (MDA-MB-231), indicating its potential to suppress VEGF-dependent tumor angiogenesis. These findings suggest that LA is a promising selective anti-angiogenic agent with potential therapeutic applications in angiogenesis-related diseases such as cancer. Full article
(This article belongs to the Special Issue Bioactive Compounds: Applications and Benefits for Human Health)
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21 pages, 3263 KiB  
Article
Effects of Echinacea purpurea and Alkylamides on Respiratory Virus Replication and IL-8 Expression In Vitro
by Keely Puchalski, Johanne A. Gerstel, Abiola Jimoh, Yalda Shokoohinia and Jeffrey Langland
Molecules 2025, 30(2), 386; https://doi.org/10.3390/molecules30020386 - 17 Jan 2025
Viewed by 988
Abstract
Echinacea purpurea is a perennial medicinal herb with important immunomodulatory and anti-inflammatory properties, especially purported for the alleviation of cold and flu symptoms. Different classes of secondary metabolites of the plant, such as alkylamides, caffeic acid derivatives, polysaccharides, flavonoids, and glycoproteins, are believed [...] Read more.
Echinacea purpurea is a perennial medicinal herb with important immunomodulatory and anti-inflammatory properties, especially purported for the alleviation of cold and flu symptoms. Different classes of secondary metabolites of the plant, such as alkylamides, caffeic acid derivatives, polysaccharides, flavonoids, and glycoproteins, are believed to be biologically and pharmacologically active. Although previous research suggests that the alkylamides present in Echinacea may be responsible for reducing the symptoms associated with the common cold or flu through their immunomodulatory activity, the roles of specific alkylamides and their targets (i.e., immune and/or antiviral) have not been well-elucidated or established. This study tested the antiviral and cytokine regulatory activity of various specific alkylamides that are present predominantly in Echinacea root extracts and found that one specific alkylamide, Dodeca-2E,4E-Dienoic acid isobutylamide, had potent antiviral activity against rhinovirus (the causative agent of most common colds) and influenza virus, as well as potent inhibition of IL-8 cytokine production. IL-8 is responsible for many of the symptoms associated with the common cold and is upregulated in other common respiratory infections. The broad activity and low cytotoxicity of this specific alkylamide support its potential use for treating rhinovirus and influenza virus infections. Full article
(This article belongs to the Special Issue Bioactive Compounds: Applications and Benefits for Human Health)
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20 pages, 4459 KiB  
Article
S-(+)-Carvone, a Monoterpene with Potential Anti-Neurodegenerative Activity—In Vitro, In Vivo and Ex Vivo Studies
by Karolina A. Wojtunik-Kulesza, Monika Rudkowska, Katarzyna Klimek, Jarosław Mołdoch, Monika Agacka-Mołdoch, Barbara Budzyńska and Anna Oniszczuk
Molecules 2024, 29(18), 4365; https://doi.org/10.3390/molecules29184365 - 13 Sep 2024
Cited by 1 | Viewed by 1751
Abstract
Carvone, a natural monoterpene, has been identified in various plants, giving them a characteristic scent. Enantiomers (R-(–) and S-(+)) reveal specific biological activities that are successfully used in traditional medicine for their antifungal, antibacterial, antiparasitic, and anti-influenza properties. The presented [...] Read more.
Carvone, a natural monoterpene, has been identified in various plants, giving them a characteristic scent. Enantiomers (R-(–) and S-(+)) reveal specific biological activities that are successfully used in traditional medicine for their antifungal, antibacterial, antiparasitic, and anti-influenza properties. The presented paper is based on S-(+)-carvone, characterized by a specific caraway scent, which revealed rich biological activities both in vitro and in vivo. Thus, the aim of the study was to evaluate the potential anti-neurodegenerative activity of S-(+)-carvone, including in vitro experiments (butyrylcholinesterase inhibitory, neuro- and hepatotoxicity as well as neuro- and hepatoprotective activity), in vivo (memory acquisition, locomotor activity), and ex vivo (determination of S-(+)-carvone’s level in tissues collected from mice). Results revealed the multidirectional character of S-(+)-carvone. It has been shown that S-(+)-carvone is capable of butyrylcholinesterase inhibition (40% for 0.025 mg applied onto the plate), and neuroprotection and hepatoprotection at selective concentrations against reactive oxygen species generation and lipid peroxidation along with non-hepatotoxicity character. Additionally, multiple-dose administration of the monoterpene at a dose of 100 mg/kg had a positive influence on memory acquisition. Gas chromatography–mass spectrometry analysis of the plasma and the brain showed that S-(+)-carvone can cross the blood–brain barrier and accumulate in the hippocampus (0.217 µg/mg of tissue), a crucial part of the brain associated with cognition and mental functions. Full article
(This article belongs to the Special Issue Bioactive Compounds: Applications and Benefits for Human Health)
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Review

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14 pages, 847 KiB  
Review
Preventive and Therapeutic Effects of Baicalein, Galangin, and Isorhamnetin in Chronic Liver Diseases: A Narrative Review
by Giuseppe Guido Maria Scarlata, Ivo Lopez, Maria Luisa Gambardella, Maja Milanović, Nataša Milić and Ludovico Abenavoli
Molecules 2025, 30(6), 1253; https://doi.org/10.3390/molecules30061253 - 11 Mar 2025
Viewed by 526
Abstract
Chronic liver diseases (CLDs), including fatty liver disease, fibrosis, and cirrhosis, pose significant global health challenges due to the limitedness of therapeutic options. Flavonoids, a class of polyphenolic compounds mainly contained in natural sources and in the foods of the Mediterranean diet, have [...] Read more.
Chronic liver diseases (CLDs), including fatty liver disease, fibrosis, and cirrhosis, pose significant global health challenges due to the limitedness of therapeutic options. Flavonoids, a class of polyphenolic compounds mainly contained in natural sources and in the foods of the Mediterranean diet, have emerged as potential candidates for liver protection due to their anti-inflammatory, antioxidant, and anti-fibrotic properties. Baicalein, derived from Scutellaria baicalensis, exhibits hepatoprotective effects by attenuating oxidative stress, inhibiting fibrogenesis, and modulating lipid metabolism. Galangin, a flavonoid derived from Alpinia officinarum, has demonstrated anti-inflammatory and anti-fibrotic properties, while isorhamnetin, a methylated flavonoid found in various fruits and herbs, has been shown to possess hepatoprotective qualities, as it reduces oxidative stress and mitigates inflammation in CLDs. This narrative review highlights the preventive and therapeutic potential of these three flavonoids, emphasizing their role as promising agents for managing CLDs and guiding future research. Full article
(This article belongs to the Special Issue Bioactive Compounds: Applications and Benefits for Human Health)
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