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Sci. Pharm.
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Anticancer Potential of Natural Products
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Anticancer Potential of Natural Products

A Special Issue of Scientia Pharmaceutica (ISSN 2218-0532).

Deadline for manuscript submissions: 31 December 2026 | Viewed by 3571

Editor

Dr. Yulin Ren

E-Mail Website
Guest Editor
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
Interests: natural product anticancer drug design and discovery; isolation of the bioactive components from natural resources supported by chromatography techniques; determination of the complete structures of the isolates by analysis of their spectroscopic and the single-crystal X-ray diffraction data; synthetic modification of the lead compounds determined through organic reactions; evaluation of bioactivities of the isolates, using specific bioassays; characterization of mechanisms of action of the bioactive compounds through various bioassays; identification of the molecular targets for the lead compounds through a series of bioassays supported with molecular modeling

Special Issue Information

Dear Colleagues,

Cancer becomes one of the most serious diseases, and major of the current cancer chemotherapy is insufficient for complete treatment of cancer, due to the adverse effects and the development of multidrug resistance. Natural products mediate their bioactivities through different cellular mechanisms, of which several compounds have been developed successfully as anticancer agents. In addition, many of these products have been reported for their immunoregulatory property, which is supportive of cancer immunotherapy, one of the most promising therapies for the treatment of cancer. Thus, further investigations on natural products could provide critical information for the development of effective anticancer agents. This Special Issue aims to investigate a journey of the development of natural products as effective anticancer agents. We thus welcome Original Research, Review, Mini Review, and Perspective articles on this theme, including but not limited to:

  • Identification of natural products showing potential anticancer activity.
  • Structural insights and medicinal chemistry for synthetic modifications on natural products.
  • Oncology biology for testing potential anticancer activity of natural products.
  • Molecular biology and modeling for identification of the molecular targets of natural products.
  • Tumor immunity about natural products.

Dr. Yulin Ren
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-anonymized peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Scientia Pharmaceutica is an international peer-reviewed open access quarterly 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 1000 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

  • anticancer agents
  • anticancer drug design and discovery
  • molecular modeling
  • molecular targets
  • natural products
  • synthetic modification
  • tumor immunity

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Published Papers (5 papers)

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Research

Jump to: Review

17 pages, 1111 KB  
Article
Structural Characterization and Cytotoxic Effects of Bioactive Compounds Isolated from Caulerpa sertularioides Against Human Cancer Cell Lines
by Edgar Sandoval-Petris, Rosalio Ramos-Payan, Hisila del Carmen Santacruz-Ortega, Maribel Plascencia-Jatomea, María Guadalupe Burboa-Zazueta, Idalia Osuna-Ruíz, Elsa Maribel Aguilar-Medina and Carmen María López-Saiz
Sci. Pharm. 2026, 94(3), 79; https://doi.org/10.3390/scipharm94030079 - 9 Sep 2026
Abstract
Compounds isolated from the macroalga Caulerpa sertularioides have been reported to exhibit cytotoxic activity. The objective of this study was to assess the antioxidant effects of compounds isolated from C. sertularioides as well as their antiproliferative effect against cancerous cell lines and to [...] Read more.
Compounds isolated from the macroalga Caulerpa sertularioides have been reported to exhibit cytotoxic activity. The objective of this study was to assess the antioxidant effects of compounds isolated from C. sertularioides as well as their antiproliferative effect against cancerous cell lines and to elucidate their chemical structure. The antiproliferative activity of C. sertularioides extracts was evaluated using the MTT standard assay in cancerous and non-cancerous cell lines. Morphological changes were observed via fluorescence microscopy, and the chemical structure of bioactive compounds was determined by nuclear magnetic resonance. Antioxidant activity was assessed using ABTS and DPPH methods. Among all extracts, the acetone extract exhibited the highest antioxidant activity (IC50 of 27.3 ± 6.1 μg/mL) in the ABTS assay, which classifies it as a very potent antioxidant. Among the tested extracts, the hexane extract showed the strongest antiproliferative activity in breast (MDA-MB-231) and cervical cancer (HeLa) cell lines. The most active fraction (F15), obtained by open-column chromatography of hexane extract, exhibited the highest bioactivity against the MDA-MB-231 cell line (IC50 of 55 ± 3.1 µg/mL); these cells exhibited morphological changes consistent with apoptosis. NMR analysis revealed signals tentatively assigned to 1-monolinolein, glycerol, bis(2-ethylhexyl) phthalate and bis(2-ethylhexyl) terephthalate. These findings support the potential of C. sertularioides as a source of bioactive compounds with antioxidant and antiproliferative properties. Full article
(This article belongs to the Special Issue Anticancer Potential of Natural Products)
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33 pages, 7725 KB  
Article
Phytochemical Study and Cytotoxic Properties of Hydroalcoholic Extracts of Epilobium parviflorum Schreb.: In Silico and In Vitro Insights
by Christian Goldiș, Roxana Racoviceanu, Mihaela Jorgovan, Roxana Negrea-Ghiulai, Codruța Șoica, Alexandra Prodea, Oana Bătrîna, Gabriela Antal and Alexandra Mioc
Sci. Pharm. 2026, 94(3), 71; https://doi.org/10.3390/scipharm94030071 - 23 Aug 2026
Viewed by 259
Abstract
Epilobium parviflorum Schreb. is a medicinal plant used traditionally against inflammatory disorders whose cytotoxic potential is still incompletely revealed. The current study investigates the phytochemical composition and in vitro cytotoxic activity of four hydroalcoholic extracts prepared from the aerial parts of E. parviflorum [...] Read more.
Epilobium parviflorum Schreb. is a medicinal plant used traditionally against inflammatory disorders whose cytotoxic potential is still incompletely revealed. The current study investigates the phytochemical composition and in vitro cytotoxic activity of four hydroalcoholic extracts prepared from the aerial parts of E. parviflorum by using maceration and Soxhlet extraction. The extracts were characterized in terms of total phenolic, flavonoid and tannins composition and LC-MS was used to identify its individual polyphenols. Their biological effects were assessed against four cancer cell lines (A375 melanoma, HT-29 colorectal adenocarcinoma, PANC-1 pancreatic carcinoma and SK-OV-3 ovarian adenocarcinoma cells), while using HaCaT keratinocytes as healthy cells in order to assess selectivity. Cell viability, cytoskeletal and nuclear morphology, mitochondrial respiration and network pharmacology were further investigated. A complex phenolic profile was revealed, with hyperoside being identified as the main component in all extracts while the extraction parameters strongly influenced the recovery of various phenolic compounds. All extracts reduced cancer cell viability in a dose-dependent manner after 24 h exposure, with the most pronounced effects observed at 720 and 1000 μg/mL, while HaCaT cells were left relatively unaffected. The morphological assessment indicated nuclear condensation, fragmentation and cytoskeletal disruption following the application of extracts. Moreover, high-resolution respirometry showed reduced oxidative phosphorylation and electron transfer system capacity thus indicating that early mitochondrial dysfunction may contribute to the cytotoxic effects. Network pharmacology revealed that ERBB2, CTNNB1, HSP90AA1 and HDAC6 might act as molecular targets in melanoma. Thus, these findings support the hypothesis that E. parviflorum hydroalcoholic extracts, particularly the 40% ethanol Soxhlet extract, may serve as important sources of bioactive phytocompounds with antiproliferative and apoptotic properties. Full article
(This article belongs to the Special Issue Anticancer Potential of Natural Products)
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Review

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24 pages, 144769 KB  
Review
The Role of Phenolic Compounds in NF-κB, Nrf2, and STAT3 Transcription Factors Regulation: Therapeutic Potential and Limitations in Cancer Treatment
by Eirini Roungeri, Evangelia K. Konstantinou, Kallirroi Dimiza, Maria Dimitriou, Anastasios Darras and Athanasios A. Panagiotopoulos
Sci. Pharm. 2026, 94(3), 77; https://doi.org/10.3390/scipharm94030077 - 4 Sep 2026
Viewed by 371
Abstract
Cancer is still one of the major causes of death globally. While there are many cancer therapies, they often come with significant adverse effects and limitations. A lot of studies have shown that using natural products can improve the efficacy of conventional therapies [...] Read more.
Cancer is still one of the major causes of death globally. While there are many cancer therapies, they often come with significant adverse effects and limitations. A lot of studies have shown that using natural products can improve the efficacy of conventional therapies and decrease their toxicity. Natural products and their derivatives encompassing unmodified molecules, semi-synthetic analogs, and synthetic structures featuring natural pharmacophores, represent a major foundation for approved anticancer agents. Phenolic compounds are a large family of naturally occurring compounds found in plants and have attracted a lot of attention for their potential anticancer properties. Preclinical studies have shown that phenolic compounds have anticancer activity through different mechanisms, mainly by modulating inflammation, which plays a critical role in cancer development. Inflammatory processes in cancer involve complex molecular mechanisms regulated by both oncogenic and tumor-suppressing transcription factors. This review focuses on how phenolic compounds regulate transcription factors, such as nuclear factor kappa-light-chain-enhancer of activated B-cells (NF-κB), nuclear factor erythroid 2-related factor 2 (Nrf2), and signal transducer and activator of transcription 3 (STAT3), which are critical in cancer-related gene expression, ultimately leading to the inhibition of cancer cell proliferation, invasion, and metastasis. Furthermore, phenolic compounds have been shown to synergize with conventional anticancer drugs, enhancing their efficacy and reducing side effects. This review investigates the role of phenolic compounds in regulating transcription factors in cancer animal models, highlighting both the therapeutic potential and limitations of these compounds in cancer prevention and treatment. Full article
(This article belongs to the Special Issue Anticancer Potential of Natural Products)
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43 pages, 5749 KB  
Review
Cytokines, the Tumor Microenvironment, and Selected Plant-Derived Natural Products
by Yulin Ren and A. Douglas Kinghorn
Sci. Pharm. 2026, 94(3), 69; https://doi.org/10.3390/scipharm94030069 - 19 Aug 2026
Viewed by 558
Abstract
Cytokines are produced by immune and other cells and work as cellular messengers to regulate an immune response and other biological processes. As the main components of the tumor microenvironment (TME), cytokines are involved in the major events of cancer development, including cancer [...] Read more.
Cytokines are produced by immune and other cells and work as cellular messengers to regulate an immune response and other biological processes. As the main components of the tumor microenvironment (TME), cytokines are involved in the major events of cancer development, including cancer and cancer stem cell proliferation, angiogenesis, invasion, and metastasis. They also modulate immune functions and inhibit tumor progression and resistance to conventional therapies and thus have been regarded as promising targets for cancer treatment. Recently, tumor reversibility has attracted wide interest, for which the TME plays a critical role. Many plant-derived products exhibit potential tumor-inhibitory and cytokine-modulatory activities, including andrographolide, artemisinin, berberine, camptothecin, capsaicin, curcumin, digoxin, morphine, paclitaxel, and vinblastine, indicating their possible use in cancer reversal. Thus, in the present review, correlations among cytokines, the TME, tumor immunity, and tumor reversibility have been discussed, and the potential effects of selected plant-derived natural products on these issues have been addressed. Full article
(This article belongs to the Special Issue Anticancer Potential of Natural Products)
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20 pages, 1716 KB  
Review
Flavonoids in Cancer Therapy: Nanocarrier Strategies to Overcome Bioavailability Limitations
by Maykon Jhuly Martins de Paiva, Walmirton Bezerra D’Alessandro, Iangla Araújo de Melo Damasceno, Juliane Farinelli Panontin, Taides Tavares dos Santos, Sávia Denise Silva Carlotto Herrera, Mateus Silva Santos and Márcio Trevisan
Sci. Pharm. 2026, 94(2), 51; https://doi.org/10.3390/scipharm94020051 - 19 Jun 2026
Cited by 1 | Viewed by 1465
Abstract
Flavonoids are a structurally diverse class of plant-derived polyphenolic compounds widely recognized for their pleiotropic biological activities, including antioxidant, anti-inflammatory, and anticancer effects. In oncology, these compounds have demonstrated the ability to modulate key signaling pathways involved in cell proliferation, apoptosis, angiogenesis, and [...] Read more.
Flavonoids are a structurally diverse class of plant-derived polyphenolic compounds widely recognized for their pleiotropic biological activities, including antioxidant, anti-inflammatory, and anticancer effects. In oncology, these compounds have demonstrated the ability to modulate key signaling pathways involved in cell proliferation, apoptosis, angiogenesis, and metastasis, highlighting their potential as multitarget therapeutic agents. However, their clinical translation remains significantly limited by unfavorable pharmacokinetic properties, such as poor aqueous solubility, extensive first-pass metabolism, rapid systemic clearance, and consequently low oral bioavailability. In this context, nanotechnology has emerged as a promising strategy to overcome these limitations. This review provides a comprehensive and critical analysis of current nanocarrier-based delivery systems for flavonoids, including polymeric nanoparticles, lipid-based nanocarriers (liposomes, solid lipid nanoparticles, and nanoemulsions), micelles, and cyclodextrin complexes, emphasizing their role in improving drug stability, enhancing cellular uptake, and enabling targeted delivery to tumor tissues through both passive mechanisms, such as the enhanced permeability and retention effect, and active targeting approaches. In addition, recent in vitro and in vivo studies demonstrating the superior antitumor efficacy of nanoencapsulated flavonoids compared to free compounds are discussed. Finally, the major translational challenges, safety considerations, and future perspectives for the clinical application of flavonoid-based nanomedicines in cancer therapy are highlighted. Full article
(This article belongs to the Special Issue Anticancer Potential of Natural Products)
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