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Natural Compounds as Potential Anticancer, Anti-inflammatory and Antioxidant Agents in...
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Natural Compounds as Potential Anticancer, Anti-inflammatory and Antioxidant Agents in Medicine

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: 31 December 2025 | Viewed by 16533

Special Issue Editor

Dr. Justyna Stefanowicz-Hajduk

E-Mail Website
Guest Editor
Department of Biology and Pharmaceutical Botany, Medical University of Gdansk, 80-416 Gdansk, Poland
Interests: cell culture; cytotoxicity assays; plant extracts and secondary metabolites; phytochemistry; anticancer; antioxidant; antimicrobial activity of natural plant extracts
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

For many years, natural products have been the main source of ingredients which are important for the prevention and treatment of many diseases. In particular, plant extracts and their secondary metabolites should be mentioned. Many of them are still used successfully today. However, it is important to research known raw materials as well as constantly search for new ones that could be used, among others, as anticancer, anti-inflammatory and antioxidant agents. Chronic inflammation and oxidative stress may promote the development of many cancers, which is why studies on the therapeutic potential of natural compounds are extremely valuable.

This Special Issue aims to collect scientific papers concerning studies in vitro and in vivo on the anticancer, anti-inflammatory and antioxidant activities of natural compounds or products. Topics of interest include the evaluation of their mechanisms of biological and pharmacological action, the chemistry of active natural compounds, etc.

Dr. Justyna Stefanowicz-Hajduk
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. Pharmaceuticals is an international peer-reviewed open access monthly 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 2900 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

  • phytochemistry of plant extracts
  • plant secondary metabolites
  • clinical applications
  • in vitro, in vivo, ex vivo studies
  • cell and tissue cultures

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Published Papers (6 papers)

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Research

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20 pages, 1717 KB  
Article
Coleus aromaticus Benth.—A Plant with Strong Anticancer and Antioxidant Potential In Vitro
by Justyna Stefanowicz-Hajduk, Anna Hering, Rafał Hałasa, Szymon Masiak, Karolina Turczyn, J. Renata Ochocka and Monika Asztemborska
Pharmaceuticals 2025, 18(11), 1756; https://doi.org/10.3390/ph18111756 - 18 Nov 2025
Viewed by 756
Abstract
Background/Objectives: Gastrointestinal cancers, including gastric and colon cancers, constitute a serious threat to global health due to their high incidence and limited treatment outcomes. Thus, natural products are becoming increasingly popular as potential chemopreventive agents. Coleus aromaticus Benth. is mainly used as [...] Read more.
Background/Objectives: Gastrointestinal cancers, including gastric and colon cancers, constitute a serious threat to global health due to their high incidence and limited treatment outcomes. Thus, natural products are becoming increasingly popular as potential chemopreventive agents. Coleus aromaticus Benth. is mainly used as a tasty addition to dishes and juices due to its aromatic and nutritional properties. The plant has many biological and pharmacological effects that require deeper evaluation. In this study, anticancer, antioxidant, and antimicrobial activities of ethanol, ethanol/water extracts, and juice from C. aromaticus leaves were evaluated. Methods: (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) MTT assay, DPPH (2,2-diphenyl-1-picrylhydrazyl), ABTS (2,2-azinobis-(3-ethylbenzothiazoline-6-sulfonate)), molybdenum reducing power assay, and broth microdilution technique were used, respectively. Additionally, total phenolic (TPC) and total flavonoid content (TFC) with basic phytochemical composition of volatile compounds by GC-MS and GC-FID were assessed. Results: The results indicate that the strongest anticancer activity was provided by the ethanol extract with IC50 values of 4.94 ± 0.48 and 24.99 ± 1.80 µg/mL on human gastric AGS cells and human colorectal HCT 116 cells, respectively. The antioxidant potential was also the highest for the ethanol extract with IC50 values of 13.34 ± 0.11 (ABTS), 22.90 ± 1.30 (DPPH), and 290.17 ± 4.23 µg/mL (molybdenum reducing power). Antimicrobial experiments revealed that ethanol and ethanol/water extracts were the most potent on Clostridium perfringens (MIC value was <0.02 mg/mL). Phytochemical analysis showed a significant content of phenolic and flavonoid compounds in the ethanol extract (75.87 ± 0.96 mg gallic acid equivalent/g dry extract and 176.01 ± 3.58 mg quercetin equivalent/g dry extract, respectively). Furthermore, all the extracts contained carvacrol (49.09, 28.15, and 25.68% of volatile fraction in ethanol, ethanol/water extracts and juice, respectively). Camphor and oleamide were also detected in large quantity. Conclusions: C. aromaticus can be considered as a potential agent in the prevention and treatment of gastrointestinal cancers, especially the ethanol extract from the plant leaves due to its strong anticancer and antioxidant properties. Full article
(This article belongs to the Special Issue Natural Compounds as Potential Anticancer, Anti-inflammatory and Antioxidant Agents in Medicine)
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13 pages, 2086 KB  
Article
Bioactivity-Guided Fractionation and Mechanistic Insights into Aristolochia ringens Root Extract-Induced G1 Phase Arrest and Mitochondria-Mediated Apoptosis in Human Colon Adenocarcinoma Cells
by Saheed O. Anifowose, Abdalrhaman M. Salih, Musa K. Oladejo, Ahmad Rady, Mobarak S. Al Mosallam, Hasan A. Aljohi, Mansour I. Almansour, Saad Hussin Alkahtani, Ibrahim O. Alanazi and Badr A. Al-Dahmash
Pharmaceuticals 2025, 18(9), 1250; https://doi.org/10.3390/ph18091250 - 23 Aug 2025
Viewed by 1026
Abstract
Background/Objectives: Aristolochia ringens, a medicinal plant widely used in traditional medicine, has shown potential therapeutic applications. This study aimed to investigate the anticancer mechanism of action of its crude extract against human colorectal adenocarcinoma cells (Caco-2 and HT-29). Methods: Cell [...] Read more.
Background/Objectives: Aristolochia ringens, a medicinal plant widely used in traditional medicine, has shown potential therapeutic applications. This study aimed to investigate the anticancer mechanism of action of its crude extract against human colorectal adenocarcinoma cells (Caco-2 and HT-29). Methods: Cell viability was assessed using the MTT assay to determine IC50 values. Immunofluorescence microscopy was used to examine nuclear morphology and microtubule integrity. Flow cytometry with PI staining was used for cell cycle analysis and Annexin V-FITC/PI staining for apoptosis detection. Mitochondrial membrane potential was evaluated using JC-1 dye. Bioactivity-guided fractionation was performed via HPLC, and GC–MS was used to profile active constituents. Results: The extract exhibited dose-dependent cytotoxicity with IC50 values below 30 µg/mL in colon adenocarcinoma cell lines. Treated Caco-2 cells showed nuclear shrinkage and disrupted microtubules. PI-based flow cytometry revealed G1 phase arrest, and Annexin V-FITC/PI staining indicated enhanced late apoptosis. JC-1 staining demonstrated mitochondrial depolarization. HPLC fractionation identified fractions 2 and 3 as active, and preliminary GC–MS analysis tentatively annotated the presence of alkaloids, sesquiterpenes/diterpenes, and steroidal compounds. Conclusions: A. ringens exerts anticancer effects through a mitochondria-mediated apoptotic pathway, involving G1 checkpoint arrest and cytoskeletal disruption. These findings provide the first integrated cellular and mechanistic evidence of its anticancer potential in colorectal cancer, supporting its promise as a source of novel therapeutic lead compounds. Full article
(This article belongs to the Special Issue Natural Compounds as Potential Anticancer, Anti-inflammatory and Antioxidant Agents in Medicine)
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14 pages, 6584 KB  
Article
The Role of Curcumin in Preventing Naturally Occurring Leiomyoma in the Galline Model
by Kazim Sahin, Cemal Orhan, Mehmet Tuzcu, Nurhan Sahin, Ibrahim H. Ozercan, Nashwa Kabil, Omer Kucuk and Bulent Ozpolat
Pharmaceuticals 2024, 17(12), 1732; https://doi.org/10.3390/ph17121732 - 21 Dec 2024
Cited by 1 | Viewed by 3084
Abstract
Background: Leiomyoma (LM) is the most commonly identified tumor in the genital tract, occurring in 70–80% of women. The only treatment option is surgery, which significantly influences healthcare costs and negatively influences women’s survival and reproductive capacity. Therefore, identifying safe and effective chemopreventive [...] Read more.
Background: Leiomyoma (LM) is the most commonly identified tumor in the genital tract, occurring in 70–80% of women. The only treatment option is surgery, which significantly influences healthcare costs and negatively influences women’s survival and reproductive capacity. Therefore, identifying safe and effective chemopreventive and treatment modalities is needed. Methods: We investigated the effects of 12 months of daily curcumin (0, 25.8, and 53 mg/kg) diet on the incidence and growth of spontaneously developing LM tumors in a galline (hen) model. Results: LM tumors were detected in 58.9% (53/90) of the control hens as spontaneous occurrences, while they were observed in 37.7% (34/90) and 24.5% (22/90) of hens treated with daily doses of 25.8 mg or 53.0 mg, respectively, over 12 months. This reduced LM development by 35% and 58.5%, respectively (p = 0.004). We also observed a dose-dependent inhibition of LM-tumor growth and NF-κB, mTOR, p70S6K1, and 4E-BP1 signaling while inducing Nrf2/HO1 pathway induction LM tumors collected from hens fed with curcumin (p < 0.05). Curcumin intake notably reduced levels of TGF-β1, α-SMA, and collagen type 1, with dose-dependent effects (p < 0.001). Conclusions: The findings suggest that daily curcumin consumption significantly reduces the incidence of naturally occurring LMs and suppresses tumor growth. This indicates that regular curcumin intake may be an effective preventive measure against LMs. Full article
(This article belongs to the Special Issue Natural Compounds as Potential Anticancer, Anti-inflammatory and Antioxidant Agents in Medicine)
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18 pages, 13037 KB  
Article
Bufadienolides from Chansu Injection Synergistically Enhances the Antitumor Effect of Erlotinib by Inhibiting the KRAS Pathway in Pancreatic Cancer
by Yanli Guo, Yu Jin, Jie Gao, Ding Wang, Yanming Wang, Liya Shan, Mengyu Yang, Xinzhi Li and Ketao Ma
Pharmaceuticals 2024, 17(12), 1696; https://doi.org/10.3390/ph17121696 - 16 Dec 2024
Cited by 2 | Viewed by 1780
Abstract
Background and Objectives: The Chansu injection (CSI), a sterile aqueous solution derived from Chansu, is applied in clinical settings to support antitumor and anti-radiation treatments. CSI’s principal active components, bufadienolides (≥90%), demonstrate potential effects on pancreatic cancer (PDAC), but their underlying mechanisms remain [...] Read more.
Background and Objectives: The Chansu injection (CSI), a sterile aqueous solution derived from Chansu, is applied in clinical settings to support antitumor and anti-radiation treatments. CSI’s principal active components, bufadienolides (≥90%), demonstrate potential effects on pancreatic cancer (PDAC), but their underlying mechanisms remain unclear. This study aimed to elucidate the antitumor effects and pathways associated with CSI in PDAC. Methods: Network pharmacology and bioinformatics analyses explored CSI’s mechanisms against PDAC. MTT, colony-formation, and migration assays evaluated CSI’s impact on proliferation and migration in PANC-1 and MIA PACA-2 cells, both as a single agent and in combination with erlotinib (EGFR inhibitor). Cell cycle analysis employed flow cytometry. Animal experiments were performed on tumor-bearing mice, with targets and pathways assessed via molecular docking and western blotting. Results: CSI treatment suppressed PDAC cell proliferation and migration by inducing G2/M phase arrest. Network pharmacology, bioinformatics, and molecular docking indicated that CSI’s anti-PDAC effects may involve EGFR pathway modulation, with CSI lowering p-EGFR/KRAS/p-ERK1/2 pathway expressions in PDAC cells. Additionally, sustained KRAS activation in mediating erlotinib resistance in PDAC and CSI potentiated erlotinib’s antitumor effects through enhanced KRAS and p-ERK1/2 inhibition. CSI also enhanced erlotinib’s efficacy in tumor-bearing mice without causing detectable toxicity in renal, cardiac, or hepatic tissues at therapeutic doses. Conclusions: CSI as an adjuvant used in antitumor and anti-radiation therapies enhanced erlotinib’s antitumor effects through modulation of the KRAS pathway. CSI and erlotinib’s synergistic interaction represents a promising approach for addressing erlotinib resistance in PDAC treatment. Full article
(This article belongs to the Special Issue Natural Compounds as Potential Anticancer, Anti-inflammatory and Antioxidant Agents in Medicine)
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44 pages, 6622 KB  
Article
Chia Seed (Salvia hispanica) Attenuates Chemically Induced Lung Carcinomas in Rats through Suppression of Proliferation and Angiogenesis
by Naglaa A. Ali, Ghada H. Elsayed, Safaa H. Mohamed, Asmaa S. Abd Elkarim, Mohamed S. Aly, Abdelbaset M. Elgamal, Wael M. Elsayed and Samah A. El-Newary
Pharmaceuticals 2024, 17(9), 1129; https://doi.org/10.3390/ph17091129 - 27 Aug 2024
Cited by 9 | Viewed by 4275
Abstract
In 2022, 2.5 million cases of lung cancer were diagnosed, resulting in 1.8 million deaths. These statistics have motivated us to introduce a new natural product which is feasible in lung cancer therapies. This comprehensive study was performed to study the effects of [...] Read more.
In 2022, 2.5 million cases of lung cancer were diagnosed, resulting in 1.8 million deaths. These statistics have motivated us to introduce a new natural product which is feasible in lung cancer therapies. This comprehensive study was performed to study the effects of chia seed extracts (70% ethanol and petroleum ether) on lung cancer in vitro and in vivo models. The invitro cytotoxicity activity of the chia extracts was studied in lung cancer cell lines (A549 cells). After 48 h, chia alcohol and ether extracts showed more inhibitory influence (IC50, 16.08, and 14.8 µg/mL, respectively) on A549 cells compared to Dox (IC50, 13.6 µg/mL). In vivo, administration of chia alcohol and ether extracts (500 mg/kg/day, orally for 20 weeks) recovered 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK)-induced lung cancer, as a significant reduction in the lung cancer biomarkers, including the relative weight of the lung (20.0 and 13.33%), ICAM(31.73 and 15.66%), and c-MYC (80 and 96%) and MMP9(60 and 69%) expression genes, and improvement in these changes were observed by histopathological examinations of the lung tissues compared to the lung control. Chia seeds fought lung cancer via suppression of proliferation, angiogenesis, inflammation, and activation apoptosis. These activities may be attributed to the chemical composition of chia, which is identified by LC-Mass, such as caffeic acid, vanillic acid, kaempferol-3-O-glucuronide, and taxifolin. Finally, we can conclude that chia seeds have an anti-lung cancer effect with a good safety margin. Full article
(This article belongs to the Special Issue Natural Compounds as Potential Anticancer, Anti-inflammatory and Antioxidant Agents in Medicine)
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Review

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26 pages, 2072 KB  
Review
Distribution, Phytochemical Insights, and Cytotoxic Potential of the Sesbania Genus: A Comprehensive Review of Sesbania grandiflora, Sesbania sesban, and Sesbania cannabina
by Fatma Alzahraa Mokhtar, Mariam Ahmed, Aishah Saeed Al Dhanhani, Serag Eldin I. Elbehairi, Mohammad Y. Alfaifi, Ali A. Shati and Amal M. Fakhry
Pharmaceuticals 2025, 18(1), 64; https://doi.org/10.3390/ph18010064 - 9 Jan 2025
Cited by 5 | Viewed by 4702
Abstract
This review evaluates the cytotoxic potential of the Sesbania genus, with a focus on Sesbania sesban, Sesbania grandiflora, and Sesbania cannabina. These species, known for their diverse phytochemical compositions, exhibit notable cytotoxic effects that suggest their utility in natural cancer [...] Read more.
This review evaluates the cytotoxic potential of the Sesbania genus, with a focus on Sesbania sesban, Sesbania grandiflora, and Sesbania cannabina. These species, known for their diverse phytochemical compositions, exhibit notable cytotoxic effects that suggest their utility in natural cancer treatments. Compounds such as quercetin, kaempferol, and sesbagrandiforian A and B have been highlighted for their strong antioxidant and antiproliferative effects, further emphasizing their therapeutic potential. The genus Sesbania exhibits a wide range of in vitro and in vivo bioactivities. Extensive research on S. grandiflora has uncovered mechanisms such as the activation of caspase cascades and the induction of apoptosis, attributed to its rich content of flavonoids and alkaloids. Notably, sesbanimides derived from S. grandiflora seeds have demonstrated potent cytotoxic effects by disrupting mitochondrial function. While S. sesban and S. cannabina have been less extensively studied, early findings highlight their potential through the inhibition of key cancer pathways and the identification of bioactive compounds such as galactomannan derivatives and 2-arylbenzofurans. Notably, the galactomannan derivatives from S. sesban exhibit significant immune-modulating properties. Additionally, nanoparticles synthesized from Sesbania species, including Cadmium oxide and PEGylated silver nanoparticles, have demonstrated promising cytotoxic activity by disrupting mitosis and enhancing immune responses. While further research is warranted, the Sesbania genus offers a promising basis for the development of innovative anticancer therapies. Full article
(This article belongs to the Special Issue Natural Compounds as Potential Anticancer, Anti-inflammatory and Antioxidant Agents in Medicine)
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