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Natural-Derived Bioactive Compounds in Disease Treatment

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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 (20 January 2026) | Viewed by 43939

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Prof. Dr. Adelina Vlad

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Physiology Department, Faculty of Medicine, “Carol Davila” University of Medicine and Pharmacy, 050474 Bucharest, Romania
Interests: atherosclerosis; coronary artery disease; scavenger receptors; anesthetic preconditioning; endothelial progenitor cells; non coding RNA; nutraceuticals; phytocompounds
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Prof. Dr. Marilena Gilca

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Biochemistry Department, Faculty of Medicine, “Carol Davila” University of Medicine and Pharmacy, 050474 Bucharest, Romania
Interests: oxidative stress; antioxidants; medicinal plants; ethnopharmacology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

This Special Issue aims to explore the rich tradition of utilizing natural remedies in disease treatment, with a particular focus on the dynamic realm of natural bioactive compounds. Recent research highlights the efficacy of phytocompounds and other natural elements in regulating various biological processes, encompassing inflammation, immune response, apoptosis, angiogenesis, cell proliferation, cholesterol trafficking, and neuronal plasticity by modulating the activity of various targets (enzymes, receptors, transporters, ion channels). The combination of synthetic drugs with plant-based agents, vitamins, or other natural bioactive compounds emerges as an efficient strategy for preventing and treating multifactorial diseases while mitigating side effects.

This Special Issue covers diverse topics, including the identification and characterization of new bioactive compounds, and investigating therapeutic applications for preventing, managing, or treating diseases, with an emphasis on cellular and molecular aspects of their mechanism of action. Specific areas of interest include pharmacokinetics, drug–phytochemical interactions, synergistic effects of natural compounds, regulatory activity of phytochemicals on phase I and II detoxifying enzymes, technology’s role in valorizing traditional medical knowledge, and the development of databases on the actions of medicinal plants and natural compounds.

A key focus lies in exploring the role of natural bioactive compounds in developing nutraceuticals and functional foods, bridging ancient medical wisdom with contemporary scientific advancements. The Special Issue welcomes contributions that present findings from clinical studies evaluating the efficacy and safety of these compounds in human populations. We invite researchers to contribute their original work and scientific reviews, fostering new insights and innovations in the realm of natural bioactive compounds and their impact on human health and diseases.

Dr. Adelina Vlad
Prof. Dr. Marilena Gilca
Guest Editors

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Keywords

medicinal plants
phytochemicals
vitamins
nutraceuticals
anti-oxidants
gene expression
protein expression
cellular signaling
nanoformulations

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Related Special Issue

Natural-Derived Bioactive Compounds in Disease Treatment, 2nd Edition in International Journal of Molecular Sciences

Published Papers (11 papers)

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Research

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18 pages, 2732 KB

Open AccessArticle

Melipona quadrifasciata Geopropolis Extract as a Modulator of Inflammation and Pro-Regenerative Responses in Human Macrophages

by Luiza Naemi Koga Zapotoski, Maria Carolina de Oliveira Ribeiro, Marcelo José Pena Ferreira, Denise V. Tambourgi and Paula Cristiane Pohl

Int. J. Mol. Sci. 2026, 27(7), 3229; https://doi.org/10.3390/ijms27073229 - 2 Apr 2026

Viewed by 677

Abstract

Geopropolis, a complex natural product composed of propolis, wax, plant resins, and soil produced by Meliponine (stingless) bees, has traditionally been used for its therapeutic properties. Its chemically diverse composition and broad biological activities have recently attracted growing scientific interest. In this study, we characterized the physicochemical and immunomodulatory properties of a hydroalcoholic extract of geopropolis (HEG) from Melipona quadrifasciata (Mandaçaia). Physicochemical characteristics were determined by measuring moisture, ash, and wax content, and its bioactive constituents were identified by GC–MS. THP-1-derived macrophages were exposed to increasing HEG concentrations to assess cytotoxicity, and two sublethal doses were selected for immunomodulatory assays with or without LPS stimulation. Cytokine and chemokine secretion were quantified by CBA, and the expression of key immunoregulatory and angiogenic genes was evaluated by RT-qPCR. Chemical profiling revealed a high wax content and a predominance of di- and triterpenoids, largely derived from coniferous sources. In mccrophages stimulated with LPS, HEG at 31.25 and 62.50 µg/mL significantly reduced the secretion of pro-inflammatory mediators (IL-6, CCL2, CCL5, CXCL9, and CXCL10) while preserving cell viability. In unstimulated macrophages, HEG upregulated the expression of genes VEGFA and TGFB1 as well as the protein CXCL8, all of them associated with angiogenesis and tissue repair. These findings demonstrate that M. quadrifasciata geopropolis extract modulates macrophage activity, promoting a shift toward a reparative phenotype that integrates inflammatory resolution with pro-healing effects. These results underscore its pharmacological potential as a terpenoid-rich natural product with complementary anti-inflammatory and regenerative activities. Full article

(This article belongs to the Special Issue Natural-Derived Bioactive Compounds in Disease Treatment)

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15 pages, 1564 KB

Open AccessArticle

Pawpaw (Asimina triloba) Seed Extract Suppresses High-Fat Diet-Induced Obesity in Mice

by Shiori Takano, Sakura Kaneko, Ryo Midorikawa, Honoka Nara, Yurie Sato, Minori Uchiyama, Haruka Iobe, Yuki Saito-Matsuzawa, Hideyuki Sone and Shin Kamiyama

Int. J. Mol. Sci. 2025, 26(16), 7719; https://doi.org/10.3390/ijms26167719 - 9 Aug 2025

Viewed by 2480

Abstract

Asimina triloba (pawpaw), a member of the Annonaceae family, contains various bioactive phytochemicals, including alkaloids, polyphenols, and acetogenins. In this study, the effects of pawpaw seed extract (PSE) on obesity and plasma lipid concentrations were investigated in mice with high-fat diet (HFD)-induced obesity. Male C57BL/6J mice were fed a normal diet (ND) or an HFD for two weeks. The mice in the latter group were then divided into three groups: HFD, L-PSE, and H-PSE. Following a two-week adaptive period, the L-PSE and H-PSE groups were fed an experimental diet containing 250 mg and 500 mg PSE/kg of HFD, respectively, for two weeks. Mice in the HFD group exhibited significantly higher body weights than that of mice in the ND group. A significant decrease in body weight was observed in the H-PSE group compared with that in the HFD group. The perirenal, testicular, and total visceral fat masses of the mice in the H-PSE group were consistently lower than those of the mice in the HFD group. Administration of high-dose PSE decreased the expression of Fasn (encoding fatty acid synthase) and Dgat2 (encoding diglyceride acyltransferase 2) in testicular fat tissues. However, PSE administration did not decrease blood glucose and plasma cholesterol levels compared with that in the HFD group. These findings suggest that the administration of PSE suppresses HFD-induced obesity in mice, while its hypoglycemic or cholesterol-lowering actions are less pronounced. Full article

(This article belongs to the Special Issue Natural-Derived Bioactive Compounds in Disease Treatment)

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21 pages, 3063 KB

Open AccessArticle

Total Antioxidant Capacity of Arachis hypogaea Seed Kernels and Coats: An Analytical and Sensory Investigation

by Julie Marshall, Lissa Gilliam, Melanie McGilton, Ana Patty, Lily Sowell, Ashley Cherry, Brian Fisher, Matt Scholten, Chris Liebold, Darlene Cowart and Samara Sterling

Int. J. Mol. Sci. 2025, 26(13), 5990; https://doi.org/10.3390/ijms26135990 - 22 Jun 2025

Viewed by 2283

Abstract

Antioxidants are critical components of the body’s defense system, providing protection against cell-damaging free radicals responsible for oxidative damage of biomolecules. Humans benefit from the consumption of plants with high antioxidant content, which have been shown to positively impact health. In plant physiology, antioxidants provide protection from biotic and abiotic stress, particularly during the development of seeds and germination. Peanut seeds and seed coats have been shown to contain several beneficial antioxidants and are a good source of phytonutrients. Seed coat color can vary greatly and impact the antioxidant capacity of the edible portion of the peanut. Additionally, the seed coat can provide bitter notes in products, affecting their palatability and potentially negating the beneficial properties of the antioxidants present. A total of 42 accessions from the Germplasm Resource Information Network (GRIN) with a variety of seed coat colors were obtained and analyzed for total antioxidant capacity to provide a baseline assessment of the distribution of antioxidants in kernel versus seed coats. The results demonstrated that seed coat color somewhat impacts antioxidant capacity, and 56–88% of the total antioxidant capacity resides in the seed kernel. Three control samples, not part of the germplasm collection, were roasted and prepared for analysis by the descriptive sensory panel. Seed coats were added back to the roasted paste in increasing proportion for analysis by the panel, and perceptions regarding bitterness and overall organoleptic properties were noted. Based on the results of this study, several accessions were selected and then planted for increase and potential crossbreeding with appropriate commercial cultivars. This information could be used to selectively add antioxidant capacity to peanut breeding programs to provide additional health benefits to consumers without compromising the sensory perception and desirability and peanut products in nutrition. Full article

(This article belongs to the Special Issue Natural-Derived Bioactive Compounds in Disease Treatment)

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13 pages, 5931 KB

Open AccessArticle

In Silico Predicting the Presence of the S100B Motif in Edible Plants and Detecting Its Immunoreactive Materials: Perspectives for Functional Foods, Dietary Supplements and Phytotherapies

by Vincenzo Romano Spica, Veronica Volpini, Federica Valeriani, Giovanni Carotenuto, Manuel Arcieri, Serena Platania, Tiziana Castrignanò, Maria Elisabetta Clementi and Fabrizio Michetti

Int. J. Mol. Sci. 2024, 25(18), 9813; https://doi.org/10.3390/ijms25189813 - 11 Sep 2024

Cited by 2 | Viewed by 2240

Abstract

The protein S100B is a part of the S100 protein family, which consists of at least 25 calcium-binding proteins. S100B is highly conserved across different species, supporting important biological functions. The protein was shown to play a role in gut microbiota eubiosis and is secreted in human breast milk, suggesting a physiological trophic function in newborn development. This study explores the possible presence of the S100B motif in plant genomes, and of S100B-like immunoreactive material in different plant extracts, opening up potential botanical uses for dietary supplementation. To explore the presence of the S100B motif in plants, a bioinformatic workflow was used. In addition, the immunoreactivity of S100B from vegetable and fruit samples was tested using an ELISA assay. The S100B motif was expected in silico in the genome of different edible plants belonging to the Viridiplantae clade, such as Durio zibethinus or Malus domestica and other medicinal species. S100B-like immunoreactive material was also detected in samples from fruits or leaves. The finding of S100B-like molecules in plants sheds new light on their role in phylogenesis and in the food chain. This study lays the foundation to elucidate the possible beneficial effects of plants or derivatives containing the S100B-like principle and their potential use in nutraceuticals. Full article

(This article belongs to the Special Issue Natural-Derived Bioactive Compounds in Disease Treatment)

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33 pages, 9785 KB

Open AccessArticle

Combination of Tramiprosate, Curcumin, and SP600125 Reduces the Neuropathological Phenotype in Familial Alzheimer Disease PSEN1 I416T Cholinergic-like Neurons

by Nicolas Gomez-Sequeda, Marlene Jimenez-Del-Rio and Carlos Velez-Pardo

Int. J. Mol. Sci. 2024, 25(9), 4925; https://doi.org/10.3390/ijms25094925 - 30 Apr 2024

Cited by 6 | Viewed by 2755

Abstract

Familial Alzheimer’s disease (FAD) is a complex and multifactorial neurodegenerative disorder for which no curative therapies are yet available. Indeed, no single medication or intervention has proven fully effective thus far. Therefore, the combination of multitarget agents has been appealing as a potential therapeutic approach against FAD. Here, we investigated the potential of combining tramiprosate (TM), curcumin (CU), and the JNK inhibitor SP600125 (SP) as a treatment for FAD. The study analyzed the individual and combined effects of these two natural agents and this pharmacological inhibitor on the accumulation of intracellular amyloid beta iAβ; hyperphosphorylated protein TAU at Ser²⁰²/Thr²⁰⁵; mitochondrial membrane potential (ΔΨ_m); generation of reactive oxygen species (ROS); oxidized protein DJ-1; proapoptosis proteins p-c-JUN at Ser⁶³/Ser⁷³, TP53, and cleaved caspase 3 (CC3); and deficiency in acetylcholine (ACh)-induced transient Ca²⁺ influx response in cholinergic-like neurons (ChLNs) bearing the mutation I416T in presenilin 1 (PSEN1 I416T). We found that single doses of TM (50 μM), CU (10 μM), or SP (1 μM) were efficient at reducing some, but not all, pathological markers in PSEN 1 I416T ChLNs, whereas a combination of TM, CU, and SP at a high (50, 10, 1 μM) concentration was efficient in diminishing the iAβ, p-TAU Ser²⁰²/Thr²⁰⁵, DJ-1Cys¹⁰⁶-SO₃, and CC3 markers by −50%, −75%, −86%, and −100%, respectively, in PSEN1 I417T ChLNs. Although combinations at middle (10, 2, 0.2) and low (5, 1, 0.1) concentrations significantly diminished p-TAU Ser²⁰²/Thr²⁰⁵, DJ-1Cys¹⁰⁶-SO₃, and CC3 by −69% and −38%, −100% and −62%, −100% and −62%, respectively, these combinations did not alter the iAβ compared to untreated mutant ChLNs. Moreover, a combination of reagents at H concentration was able to restore the dysfunctional ACh-induced Ca²⁺ influx response in PSEN 1 I416T. Our data suggest that the use of multitarget agents in combination with anti-amyloid (TM, CU), antioxidant (e.g., CU), and antiapoptotic (TM, CU, SP) actions might be beneficial for reducing iAβ-induced ChLN damage in FAD. Full article

(This article belongs to the Special Issue Natural-Derived Bioactive Compounds in Disease Treatment)

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Review

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15 pages, 960 KB

Open AccessReview

Impact of the Combination of Epigallocatechin Gallate and Ellagic Acid Supplemented with Ketone Bodies on Energetic Restoration of Mitochondrial Dysfunction and Metabolic Inefficiencies in Patients with Multiple Sclerosis: A Review

by Jose Enrique de la Rubia Ortí, Alba Roig-Soriano, Sandra Carrera-Juliá, Alejandra Castelló-Guillen, Marisa Machado, Rocío García-Villalba, Jorge Alarcón-Jiménez, Nieves de Bernardo and María Benlloch

Int. J. Mol. Sci. 2026, 27(5), 2168; https://doi.org/10.3390/ijms27052168 - 25 Feb 2026

Viewed by 799

Abstract

Multiple sclerosis (MS) is characterized by progressive mitochondrial dysfunction affecting complexes I, III, and IV of the electron transport chain, contributing to axonal energy failure and neurodegeneration. This review examines the potential of combining β-hydroxybutyrate (βHB), epigallocatechin-3-gallate (EGCG), and ellagic acid (EA) as a multi-target therapeutic strategy to restore mitochondrial function in patients with MS. Experimental and clinical studies demonstrate that each compound exerts complementary mechanisms. Ketone bodies provide an alternative energy substrate and restore complex I activity via sirtuin-dependent pathways. EGCG acts predominantly at the peripheral level by reducing systemic inflammation and oxidative stress. EA-derived urolithins effectively cross the blood–brain barrier to directly enhance mitochondrial biogenesis and respiratory chain function in the central nervous system. Clinical trials have reported improvements in fatigue, cognition, mood, and muscle function following supplementation with these compounds. The convergence of their actions on energy restoration, reactive oxygen species reduction, and epigenetic modulation of protective pathways suggests their synergistic potential. Optimized delivery strategies, including exogenous ketone salts, liposomal EGCG, and microencapsulated EA, may overcome bioavailability limitations and interindividual variability in the gut microbiota metabolism. Full article

(This article belongs to the Special Issue Natural-Derived Bioactive Compounds in Disease Treatment)

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26 pages, 4230 KB

Open AccessReview

Immunomodulatory Effects of Flavonoids in Colitis-Associated Colorectal Cancer

by Sonia H. Navia, Libia Vega, Tonathiu Rodríguez and Miriam Rodríguez-Sosa

Int. J. Mol. Sci. 2026, 27(4), 1883; https://doi.org/10.3390/ijms27041883 - 15 Feb 2026

Cited by 1 | Viewed by 1069

Abstract

Flavonoids present in plants and fruits have been used in traditional medicine to reduce inflammation under various inflammatory conditions, including colitis. The pharmacological mechanisms that regulate intestinal inflammation are associated with the colonic microbiota, protection against oxidative stress, preservation of epithelial barrier function, and immune homeostasis. This review describes the main flavonoids present in the diet and examines their role in mitigating colon inflammation, as well as their impact when chronic inflammation progresses to colitis-associated colorectal cancer (CAC), in which flavonoids may promote immune evasion and tumor growth. Understanding the effects of flavonoids on colon physiology offers an opportunity to use these compounds rationally in the treatment of colitis and prevention of the development of colorectal cancer (CRC). Full article

(This article belongs to the Special Issue Natural-Derived Bioactive Compounds in Disease Treatment)

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33 pages, 1055 KB

Open AccessReview

Nrf2-Activating Natural Compounds in Neurodegenerative Diseases: Targeting Oxidative Stress and Protein Aggregation

by Lucia Chico, Erika Schirinzi, Linda Balestrini, Maico Polzella and Gabriele Siciliano

Int. J. Mol. Sci. 2026, 27(3), 1592; https://doi.org/10.3390/ijms27031592 - 5 Feb 2026

Cited by 1 | Viewed by 2441

Abstract

Neurodegenerative diseases (NDs) are among the leading causes of disability and mortality worldwide and are characterized by multifactorial pathogenesis involving interconnected mechanisms, such as oxidative stress, protein misfolding and aggregation, neuroinflammation, and mitochondrial dysfunction. Dysregulation of transcription factors, governing cellular defense responses, particularly nuclear factor erythroid 2–related factor 2 (Nrf2), a key regulator of antioxidant and proteostatic pathways, plays a critical role in neurodegenerative processes. Currently, available pharmacological treatments for NDs are largely symptomatic, as no disease-modifying therapies exist. Natural bioactive compounds have emerged as promising multi-target agents, demonstrating antioxidant, anti-aggregative, and anti-apoptotic properties, frequently mediated through activation of the Nrf2 signaling pathways. These compounds may represent valuable supportive strategies alongside conventional drug treatments, potentially contributing to the modulation of multiple pathogenic mechanisms. This review summarizes key oxidative stress- and protein aggregation-driven mechanisms underlying Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis, and Huntington’s disease. It further examines the neuroprotective potential of plant-, fungi-, and marine-derived natural compounds, with particular emphasis on Nrf2 activation. Beyond redox regulation, the broader role of Nrf2 in maintaining proteostasis is discussed. Overall, the review highlights Nrf2-inducing nutraceuticals as promising complementary, multi-target approaches for neuroprotection in NDs. Full article

(This article belongs to the Special Issue Natural-Derived Bioactive Compounds in Disease Treatment)

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22 pages, 533 KB

Open AccessReview

Modulation of Glutathione-S-Transferase by Phytochemicals: To Activate or Inhibit—That Is the Question

by Irina Anna-Maria Stoian, Adelina Vlad, Marilena Gilca and Dorin Dragos

Int. J. Mol. Sci. 2025, 26(15), 7202; https://doi.org/10.3390/ijms26157202 - 25 Jul 2025

Cited by 12 | Viewed by 4625

Abstract

Glutathione S-transferases (GSTs) are phase II detoxification enzymes that display several enzymatic activities, including transferase, peroxidase, reductase, and isomerase functions, as well as non-enzymatic roles (e.g., serving as binding proteins). Their complex functionality lies in the biotransformation of xenobiotics (e.g., pesticides, drugs) and certain endogenous compounds, primarily metabolites produced by phase I detoxification enzymes. Several plant-derived compounds have been shown to modulate the activity and expression levels of these enzymes. Phytochemical activators of GSTs are potentially beneficial for detoxification in cases of exposure to various toxic compounds, whereas inhibitors of GSTs could have positive effects as adjuvant treatments for cancers that express high levels of GSTs associated with drug resistance. Full article

(This article belongs to the Special Issue Natural-Derived Bioactive Compounds in Disease Treatment)

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49 pages, 2527 KB

Open AccessReview

Cellular and Molecular Mechanisms Modulated by Genistein in Cancer

by Valeria Naponelli, Annamaria Piscazzi and Domenica Mangieri

Int. J. Mol. Sci. 2025, 26(3), 1114; https://doi.org/10.3390/ijms26031114 - 27 Jan 2025

Cited by 35 | Viewed by 8004

Abstract

Genistein (4′,5,7-trihydroxyisoflavone) is a phytoestrogen belonging to a subclass of natural flavonoids that exhibits a wide range of pharmacological functions, including antioxidant and anti-inflammatory properties. These characteristics make genistein a valuable phytochemical compound for the prevention and/or treatment of cancer. Genistein effectively inhibits tumor growth and dissemination by modulating key cellular mechanisms. This includes the suppression of angiogenesis, the inhibition of epithelial–mesenchymal transition, and the regulation of cancer stem cell proliferation. These effects are mediated through pivotal signaling pathways such as JAK/STAT, PI3K/Akt/mTOR, MAPK/ERK, NF-κB, and Wnt/β-catenin. Moreover, genistein interferes with the function of specific cyclin/CDK complexes and modulates the activation of Bcl-2/Bax and caspases, playing a critical role in halting tumor cell division and promoting apoptosis. The aim of this review is to discuss in detail the key cellular and molecular mechanisms underlying the pleiotropic anticancer effects of this flavonoid. Full article

(This article belongs to the Special Issue Natural-Derived Bioactive Compounds in Disease Treatment)

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33 pages, 10873 KB

Open AccessReview

Effects of Cannabinoids on Intestinal Motility, Barrier Permeability, and Therapeutic Potential in Gastrointestinal Diseases

by Kijan Crowley, Łukasz Kiraga, Edyta Miszczuk, Sergiusz Skiba, Joanna Banach, Urszula Latek, Marta Mendel and Magdalena Chłopecka

Int. J. Mol. Sci. 2024, 25(12), 6682; https://doi.org/10.3390/ijms25126682 - 18 Jun 2024

Cited by 20 | Viewed by 14984

Abstract

Cannabinoids and their receptors play a significant role in the regulation of gastrointestinal (GIT) peristalsis and intestinal barrier permeability. This review critically evaluates current knowledge about the mechanisms of action and biological effects of endocannabinoids and phytocannabinoids on GIT functions and the potential therapeutic applications of these compounds. The results of ex vivo and in vivo preclinical data indicate that cannabinoids can both inhibit and stimulate gut peristalsis, depending on various factors. Endocannabinoids affect peristalsis in a cannabinoid (CB) receptor-specific manner; however, there is also an important interaction between them and the transient receptor potential cation channel subfamily V member 1 (TRPV1) system. Phytocannabinoids such as Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD) impact gut motility mainly through the CB1 receptor. They were also found to improve intestinal barrier integrity, mainly through CB1 receptor stimulation but also via protein kinase A (PKA), mitogen-associated protein kinase (MAPK), and adenylyl cyclase signaling pathways, as well as by influencing the expression of tight junction (TJ) proteins. The anti-inflammatory effects of cannabinoids in GIT disorders are postulated to occur by the lowering of inflammatory factors such as myeloperoxidase (MPO) activity and regulation of cytokine levels. In conclusion, there is a prospect of utilizing cannabinoids as components of therapy for GIT disorders. Full article

(This article belongs to the Special Issue Natural-Derived Bioactive Compounds in Disease Treatment)

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