Natural Bioactives: Exploring Their Therapeutic Potential—2nd Edition

A special issue of Life (ISSN 2075-1729). This special issue belongs to the section "Pharmaceutical Science".

Deadline for manuscript submissions: 20 August 2025 | Viewed by 2978

Special Issue Editor


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Guest Editor
Department of Pharmacognosy, Jagiellonian University Collegium Medicum, Medyczna 9, 30-688 Cracow, Poland
Interests: rapanone; embelin; polyphenols; phytochemical analysis; CNS biological activity in vivo; anti-tyrosinase activity; Ardisia crenata; quantification of plant metabolites
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Dear Colleagues,

The exploration of therapeutic agents represents an ongoing process. Nature, a trove of biodiversity, continually offers us biologically active compounds. Time-tested natural bioactives, such as artemisinin, which is isolated from the plant Artemisia annua and has been used for decades as a key treatment for malaria, or the Madagascar-periwinkle-derived anticancer agents vincristine and vinblastine, demonstrate nature’s therapeutic potential. Today, at least 70,000 medicinal plants are known to be used worldwide, highlighting vast potential that is still to be fully explored.

Over recent decades, research has focused on exploring therapeutics for non-communicable diseases, which represent a growing and overwhelming medical problem. It has been shown in many studies that agents with antioxidant, anti-inflammatory, and cytotoxic properties (as well as their more specific activities) can be useful in the prophylaxis and/or treatment of central nervous system disorders, cancer, and cardiovascular and metabolic diseases. Many phytochemicals, such as phenolic compounds (flavonoids, tannins, quinones, or curcuminoids), terpenoids, steroids, or alkaloids, have been found to show complex and beneficial modes of biological action. Consequently, they have continuously represented an important subject of interest for researchers. Furthermore, the last several years have shown that infectious diseases can also be an unexpected global threat, and this time, nature-derived substances are being extensively explored, as herbs and microbes are known sources of antibiotic agents.

For this Special Issue, our aim is to bring together the latest discoveries and fresh insights, taking a closer look at diverse phytochemicals and compounds from plants, marine organisms, fungi, and microbes. Both original research articles and comprehensive reviews are welcome.

To read the publications in the previous edition, please visit the following webpage: https://www.mdpi.com/journal/life/special_issues/Natural_Bioactives

Dr. Dagmara Wróbel-Biedrawa
Guest Editor

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Keywords

  • bioactive compounds
  • medicinal plants
  • bioactive metabolites with antioxidant properties
  • anti-inflammatory properties
  • antitumor properties
  • cytotoxic properties
  • antipsychotic properties
  • anxiolytic properties
  • neuroprotective properties
  • hypotensive properties
  • vasorelaxant properties
  • antimicrobial properties (antiviral, antibacterial, antifungal, and antiparasitic properties)

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Related Special Issue

Published Papers (4 papers)

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Research

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27 pages, 2356 KiB  
Article
Exploring the Anticancer Activity of Artocarpus heterophyllus Leaves: Selective Effects on Triple-Negative Breast Cancer and HPV16-Positive Tumorigenic Cells
by Ariana Cabrera-Licona, Gustavo A. Hernández-Fuentes, Oscar F. Beas-Guzmán, Alejandra E. Hernández-Rangel, Janet Diaz-Martinez, Osval A. Montesinos-López, José Guzmán-Esquivel, Víctor H. Cervantes-Kardasch, Mario Ramírez-Flores, Alejandrina Rodriguez-Hernandez, Erika R. González-Espinosa, Ana B. Castellanos-Gutiérrez, Francisco Orozco-Ramos, Valery Melnikov and Iván Delgado-Enciso
Life 2025, 15(7), 1090; https://doi.org/10.3390/life15071090 - 11 Jul 2025
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Abstract
Artocarpus heterophyllus (jackfruit) is widely distributed in subtropical and tropical regions, and some phytochemicals isolated from this species have demonstrated anti-proliferative effects. However, its impact on triple-negative breast cancer (TNBC) and HPV-related cervical cancer models remains unclear. This study evaluated the phytochemical profile [...] Read more.
Artocarpus heterophyllus (jackfruit) is widely distributed in subtropical and tropical regions, and some phytochemicals isolated from this species have demonstrated anti-proliferative effects. However, its impact on triple-negative breast cancer (TNBC) and HPV-related cervical cancer models remains unclear. This study evaluated the phytochemical profile and anticancer activity of an ethanolic extract from A. heterophyllus leaves (AHEE) in the TNBC cell line MDA-MB-231 and in the HPV-16+ murine cancer cell line TC-1. Phytochemical screening and spectroscopic analyses (UV-Vis, IR, 1H, and 13C NMR) revealed the presence of tannins, alkaloids, steroids, coumarins, and flavone-type flavonoids, with a total phenolic content of 3.34 µg GAE/mg and flavonoid content of 0.44 mg QE/g extract. In 2D cultures, AHEE reduced cell viability by 49% in TC-1 and 24% in MDA-MB-231 at 300 µg/mL, inhibited colony formation and migration in TC-1, and impaired survival but not migration in MDA-MB-231. In 3D cultures, 250 µg/mL inhibited proliferation, migration, and anchorage-independent growth in both cell lines. Furthermore, the combination of AHEE with one-fifth of the IC50 of doxorubicin or cisplatin produces an effect comparable to that observed with the full IC50 of these drugs. These findings suggest that AHEE possesses anticancer activity with cell-type-specific effects and highlight its potential as an adjuvant therapy. Further studies are warranted to elucidate its mechanisms of action. Full article
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19 pages, 2692 KiB  
Article
Low-Dose Quercetin Dephosphorylates AKT and Suppresses Proteins Related to Migration in Human Metastatic Uveal Melanoma Cells
by Petra Fodor, József Király, Zsuzsanna Szabó, Katalin Goda, Barbara Zsebik and Gábor Halmos
Life 2025, 15(6), 979; https://doi.org/10.3390/life15060979 - 18 Jun 2025
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Abstract
Background: Uveal melanoma (UM) is the most common intraocular cancer of the eye, with high metastatic potential in adults. In 50% of patients, UM spreads to other tissues, causing a fatal outcome. Flavonoids are bioactive phenolic compounds found in fruits and plants, thus [...] Read more.
Background: Uveal melanoma (UM) is the most common intraocular cancer of the eye, with high metastatic potential in adults. In 50% of patients, UM spreads to other tissues, causing a fatal outcome. Flavonoids are bioactive phenolic compounds found in fruits and plants, thus commonly present in the natural diet. Quercetin is the most remarkable agent among flavonols proved to have an anticancer effect. Thus, we aimed to investigate the effect of quercetin on a metastatic UM cell line MM28. Methods: MM28 cells were treated with increasing concentrations of quercetin (0.1–10 µM). The changes of proliferation and migration markers were studied both in gene and protein expression level by qPCR, Western blotting, and Proteome Profiler Human XL Oncology Array. Results: Quercetin had only a slight anti-proliferative effect on MM28 cells. However, 1 µM of quercetin significantly elevated the mRNA expression of the Maspin gene and downregulated MMP2 gene expression. In addition, the protein expression levels of pAKT, NF-κB, and MMP8 were significantly decreased by the treatment. Conclusions: Our findings indicate that low-dose (1 µM) quercetin treatment is able to suppress the expression of certain migration markers, and therefore, it might be a useful adjuvant compound to reduce metastasis formation of UM. Full article
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Review

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17 pages, 900 KiB  
Review
Watercress (Nasturtium officinale) as a Functional Food for Non-Communicable Diseases Prevention and Management: A Narrative Review
by Chikondi Maluwa, Blecious Zinan’dala, Hataichanok Chuljerm, Wason Parklak and Kanokwan Kulprachakarn
Life 2025, 15(7), 1104; https://doi.org/10.3390/life15071104 - 15 Jul 2025
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Abstract
Non-communicable diseases (NCDs) such as cardiovascular disease, diabetes, cancer, and chronic respiratory conditions are the leading causes of death globally, largely driven by modifiable lifestyle factors. With growing interest in dietary strategies for NCDs prevention and management, functional foods like watercress (Nasturtium [...] Read more.
Non-communicable diseases (NCDs) such as cardiovascular disease, diabetes, cancer, and chronic respiratory conditions are the leading causes of death globally, largely driven by modifiable lifestyle factors. With growing interest in dietary strategies for NCDs prevention and management, functional foods like watercress (Nasturtium officinale) have attracted attention for their rich phytochemical content and potential health benefits. This narrative review synthesizes 88 sources published between 2019 and March 2025, exploring the effects of watercress bioactive compounds on major NCDs. Watercress is abundant in glucosinolates, isothiocyanates (especially phenethyl isothiocyanate), flavonoids, vitamins, and minerals. These compounds contribute to antioxidant, anti-inflammatory, and metabolic regulatory effects. Preclinical and clinical studies show that watercress supplementation may improve lipid profiles, reduce oxidative stress, and modulate inflammation in cardiovascular and respiratory conditions. It also appears to enhance insulin function and reduce blood glucose levels. In cancer models, watercress extracts exhibit antiproliferative, pro-apoptotic, and chemoprotective properties, with selective toxicity towards cancer cells and protective effects on normal cells. These findings highlight the therapeutic potential of watercress as a dietary adjunct in NCDs prevention and management, supporting the need for further clinical research. Full article
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31 pages, 1909 KiB  
Review
Centella asiatica: Advances in Extraction Technologies, Phytochemistry, and Therapeutic Applications
by Zaw Myo Hein, Prarthana Kalerammana Gopalakrishna, Anil Kumar Kanuri, Warren Thomas, Farida Hussan, Venkatesh R. Naik, Nisha Shantakumari, Muhammad Danial Che Ramli, Mohamad Aris Mohd Moklas, Che Mohd Nasril Che Mohd Nassir and Thirupathirao Vishnumukkala
Life 2025, 15(7), 1081; https://doi.org/10.3390/life15071081 - 9 Jul 2025
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Abstract
Centella asiatica (C. asiatica) has attracted significant scientific interest due to its extensive medicinal properties and long-established use in traditional medicine. This review synthesizes recent advances in the technological exploitation of C. asiatica, covering the extraction of bioactive constituents to [...] Read more.
Centella asiatica (C. asiatica) has attracted significant scientific interest due to its extensive medicinal properties and long-established use in traditional medicine. This review synthesizes recent advances in the technological exploitation of C. asiatica, covering the extraction of bioactive constituents to product development. Modern extraction techniques such as supercritical fluid extraction (SFE) and microwave-assisted extraction (MAE) have substantially improved the yield, selectivity, and preservation of key phytochemicals, particularly triterpenoids, saponins, and flavonoids. These compounds are now routinely characterized using advanced analytical platforms, ensuring product quality, consistency, and standardization. Moreover, the use of innovative formulation technologies and advanced delivery systems has facilitated the development of C. asiatica-based products tailored for various therapeutic areas, including pharmaceuticals, nutraceuticals, and cosmeceuticals targeting neuroprotection, wound healing, skin aging, and stress modulation. Alongside these developments, stringent quality control protocols, toxicological evaluations, and adherence to evolving regulatory standards enhance the safety and efficacy of C. asiatica-derived interventions. This review highlights the integration of traditional knowledge with modern science across the domains of extraction, analysis, formulation, and regulation. It serves as a comprehensive resource for researchers, formulators, and regulatory stakeholders aiming to develop high-quality, evidence-based C. asiatica products with improved bioavailability and therapeutic value. Full article
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