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Innovative Approaches to Enhancing Bioavailability and Bioaccessibility of Bioactive Compounds from Plant and Food Extracts

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

Deadline for manuscript submissions: closed (20 March 2026) | Viewed by 4537

Special Issue Editor

Dr. Ana-Maria Vlase

E-Mail Website
Guest Editor
Department of Pharmaceutical Botany, Faculty of Pharmacy, Iuliu Hațieganu University of Medicine and Pharmacy, 32, Gheorghe Marinescu Street, 400337 Cluj-Napoca, Romania
Interests: pharmacy; natural products research; bioactive compounds; antioxidant activity; deep eutectic solvents; modern extraction techniques; optimization of extraction of bioactive compounds
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In recent years, there has been a growing interest in plant extracts, nutraceuticals, and functional foods due to their potential health benefits and role in preventing and managing chronic diseases. Understanding the mechanisms by which these natural compounds exert their beneficial effects is critical to uncover their full potential. As research continues to explore the complex interactions between bioactive compounds and biological systems, innovative approaches are needed to enhance their bioavailability and bioaccessibility, thereby maximizing their efficacy.

As the Guest Editor of this special issue, I invite contributions which aim to present innovative studies that enhance the health benefits of bioactive compounds by employing novel approaches and investigating molecular mechanisms.

This Special Issue could explore a range of important topics, including but not limited to:

  • Investigate how nanotechnology, liposomes, or other delivery systems can improve the bioavailability of bioactive compounds.
  • Examine how combinations of plant and food extracts can enhance the bioaccessibility and bioavailability of bioactive compounds. Studies investigating molecular synergy between different compounds, including their interactions and their combined effects on biological pathways are welcome.
  • Discuss the latest molecular models for assessing bioavailability and bioaccessibility, including in vitro assays and preclinical models that incorporate biomolecular experiments. Submissions that include clinical or model-based research with a strong emphasis on molecular biology and molecular mechanisms are welcome.
  • Explore how the food matrix and different processing methods influence the stability, bioavailability, and bioaccessibility of bioactive compounds.
  • Understand how bioactive compounds are absorbed, transported, and metabolized in the body and how these processes affect their bioavailability and efficacy. This Special Issue will provide insights into the molecular pathways and mechanisms through which these compounds exert their effects, contributing to a deeper understanding of their potential therapeutic benefits.
  • The use of molecular techniques such as proteomics, genomics, and metabolomics to identify biomarkers and pathways that are influenced by bioactive compounds, thus allowing the development of more targeted and effective formulations. Understanding these molecular interactions will significantly contribute to translating laboratory results into practical applications that can improve human health through diet and nutrition.

Researchers and scholars are welcomed to submit their original research articles, comprehensive reviews, and short communications that align with the themes of this special issue intended to provide a unique platform for advancing the collective understanding of bioactive compounds and their vital role in promoting health.

Dr. Ana-Maria Vlase
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 250 words) can be sent to the Editorial Office for assessment.

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

  • bioactive compounds
  • nutraceuticals
  • functional foods
  • in vitro and in vivo models
  • bioavailability
  • bioaccessibility
  • nanotechnology
  • delivery systems
  • molecular mechanisms
  • proteomics
  • genomics
  • metabolomics

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Published Papers (4 papers)

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Research

12 pages, 8415 KB  
Article
Flavonoids as Inhibitors of VEGFR2 Signaling: Structural Insights for the Development of Safer Anti-Angiogenic Therapies
by Andrew Yim, Jianming Lu and Wei Wen
Int. J. Mol. Sci. 2026, 27(8), 3605; https://doi.org/10.3390/ijms27083605 - 18 Apr 2026
Viewed by 282
Abstract
Vascular endothelial growth factor (VEGF) is a key regulator of angiogenesis and an established therapeutic target in diseases such as cancer and ocular disorders. However, long-term use of most current anti-VEGF agents is often limited by their associated side effects, including hypertension, bleeding, [...] Read more.
Vascular endothelial growth factor (VEGF) is a key regulator of angiogenesis and an established therapeutic target in diseases such as cancer and ocular disorders. However, long-term use of most current anti-VEGF agents is often limited by their associated side effects, including hypertension, bleeding, and gastrointestinal complications. These limitations have stimulated interest in naturally occurring VEGF inhibitors derived from dietary sources, which may offer safer alternatives due to their favorable safety profiles. In this study, we investigated shared structural features of potent VEGFR2 inhibitors, focusing on naturally derived polyphenols. Polyphenols representing multiple structural subclasses were evaluated for their ability to inhibit VEGFR2 kinase activity using an in vitro kinase assay, to suppress VEGF-induced phosphorylation of VEGFR2 and downstream MAPK signaling in endothelial cells by Western blot, and to reduce VEGF-stimulated endothelial cell proliferation. Across all assays, flavonoids with strong VEGFR2 inhibitory activity displayed consistent structural characteristics, including the number and specific positioning of hydroxyl groups on the A- and B-rings, as well as specific structural elements of the C-ring. Our findings provide a strong foundation for further structure–activity relationship (SAR) studies and facilitate identification of key molecular determinants required for VEGFR2 inhibition. Elucidation of these structural patterns may contribute to the development of more effective and safer angiogenesis inhibitors with reduced adverse effects. Full article
(This article belongs to the Special Issue Innovative Approaches to Enhancing Bioavailability and Bioaccessibility of Bioactive Compounds from Plant and Food Extracts)
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14 pages, 3983 KB  
Article
Therapeutic Potential of Baicalein in Endometrial Cancer: Suppression of mTOR Signaling and Synergy with Metformin
by Alison L. Dumitriu, Wei Wen, Jin Yan, Quanhua Xing, Finn E. Ro, Ernest S. Han and John H. Yim
Int. J. Mol. Sci. 2025, 26(22), 11061; https://doi.org/10.3390/ijms262211061 - 15 Nov 2025
Cited by 2 | Viewed by 962
Abstract
Baicalein, a natural flavonoid derived from traditional medicinal herbs, has demonstrated anticancer activity in various malignancies, but its role in endometrial cancer remains largely unexplored. In this study, we investigated the therapeutic potential of baicalein, alone and in combination with metformin, in human [...] Read more.
Baicalein, a natural flavonoid derived from traditional medicinal herbs, has demonstrated anticancer activity in various malignancies, but its role in endometrial cancer remains largely unexplored. In this study, we investigated the therapeutic potential of baicalein, alone and in combination with metformin, in human endometrial cancer cells. Given that the mTOR signaling pathway is frequently dysregulated in endometrial cancer due to PTEN loss, we examined how baicalein affects this pathway. Our results demonstrated that baicalein significantly inhibited cell proliferation in a dose-dependent manner, which was associated with increased DDIT4 expression, activation of AMPK, and decreased phosphorylation of mTOR downstream targets S6K1 and S6. In vivo, baicalein treatment led to a reduction in tumor volume in HEC-1A xenograft female nude mice without affecting body weight. While metformin also reduced cell viability, baicalein achieved comparable effects at lower concentrations. The combination of baicalein and metformin produced a synergistic anti-tumor effect and more effectively inhibited the AMPK/PI3K/mTOR signaling pathway than either agent alone. These findings suggest that baicalein may represent a promising, non-toxic therapeutic option for endometrial cancer, particularly when used in combination with metformin. Further investigation is warranted to assess the clinical relevance of this strategy. Full article
(This article belongs to the Special Issue Innovative Approaches to Enhancing Bioavailability and Bioaccessibility of Bioactive Compounds from Plant and Food Extracts)
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16 pages, 2871 KB  
Article
Proteomic Profiling of Cardiomyocytes Revealed Potential Radioprotective Effects of Different Resveratrol Pretreatment Regimens
by Michalina Gramatyka, Marta Gawin, Agata Kurczyk, Adam Gądek, Monika Pietrowska and Piotr Widłak
Int. J. Mol. Sci. 2025, 26(20), 10223; https://doi.org/10.3390/ijms262010223 - 21 Oct 2025
Viewed by 711
Abstract
Resveratrol may protect against radiation by modulating cellular metabolism and enhancing the cellular response to stress. Here, we explored its effects on human cardiomyocytes exposed to ionizing radiation. Resveratrol (5 µM) was administered for 1, 7, and 30 days before a single 2 [...] Read more.
Resveratrol may protect against radiation by modulating cellular metabolism and enhancing the cellular response to stress. Here, we explored its effects on human cardiomyocytes exposed to ionizing radiation. Resveratrol (5 µM) was administered for 1, 7, and 30 days before a single 2 Gy dose of irradiation, and then radiation toxicity and changes in the proteome were evaluated. Extended resveratrol treatment (7 or 30 days) induced more profound proteomic changes than one-day treatment and partially counteracted toxic effects of radiation, leading to increased cell survival, reduced cell death, and fewer cells arrested in the G1 phase. Though resveratrol administration itself had a greater impact on the proteome than radiation alone, we identified three subsets of proteins differently affected by radiation depending on the resveratrol context. The first subset (84 differentially expressed proteins; DEPs) represented proteins influenced by radiation in all resveratrol pretreatment regimens. The second subset (228 DEPs), linked to DNA repair, cell cycle checkpoints, and apoptosis, was affected by radiation only in the absence of resveratrol preconditioning, indicating the compound’s protective effect. The third subset (252 DEPs) involved in metabolism regulation appeared only after extended resveratrol preconditioning. In conclusion, the results demonstrate that hypothetical time-dependent cardioprotective effects of resveratrol are linked to significant proteomic reprogramming of cardiomyocytes caused by long-term pretreatment. Full article
(This article belongs to the Special Issue Innovative Approaches to Enhancing Bioavailability and Bioaccessibility of Bioactive Compounds from Plant and Food Extracts)
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13 pages, 3677 KB  
Article
Preparation of a Micronutrient-Enriched Apricot Kernel Oil and Assessment of In Vitro Chemopreventive Properties
by Melania Elettra Vaccari, Valeria Cavalloro, Martina Bedeschi, Patrizia Serra, Giorgia Simonetti, Emanuele Casali, Alessio Porta, Alice Fossati, Emanuela Martino, Simona Collina and Anna Tesei
Int. J. Mol. Sci. 2025, 26(18), 9237; https://doi.org/10.3390/ijms26189237 - 22 Sep 2025
Cited by 1 | Viewed by 1675
Abstract
Apricot kernels (Prunus armeniaca L.) represent a valuable by-product of stone fruit cultivation, offering diverse applications in food, cosmetic, and pharmaceutical industries. While apricot kernel oil is recognized for its rich composition of unsaturated fatty acids, phenolics, and tocopherols, its therapeutic potential, [...] Read more.
Apricot kernels (Prunus armeniaca L.) represent a valuable by-product of stone fruit cultivation, offering diverse applications in food, cosmetic, and pharmaceutical industries. While apricot kernel oil is recognized for its rich composition of unsaturated fatty acids, phenolics, and tocopherols, its therapeutic potential, particularly in cancer prevention, remains unexplored. This study investigated a purified fraction (FOPF) obtained from Farclo variety kernel oil, cultivated in the Emilia-Romagna region of Italy and selected for its naturally low amygdalin content. In vitro studies demonstrated FOPF’s significant antiproliferative effects against colorectal cancer (LoVo, HT29) and hepatocarcinoma (Hep3B) cell lines, with GI50 values ranging from 0.06 to 0.09 mg/mL. The fraction induced cell cycle arrest and significantly inhibited cancer cell migration, effects mediated through PPAR-γ expression modulation. These findings establish FOPF’s potential as a natural chemopreventive agent and provide a foundation for its development as a nutraceutical ingredient targeting colorectal and hepatic cancers. Full article
(This article belongs to the Special Issue Innovative Approaches to Enhancing Bioavailability and Bioaccessibility of Bioactive Compounds from Plant and Food Extracts)
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