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Updated: Jun 16, 2025

Preparation of Naringenin Solution for In Vivo Application
Published on: August 10, 2021
Exploring the Cytotoxic and Anticancer Potential of Naringin on Oral Cancer Cell Line
Beniel Vincer1, Jospin Sindya1, Jeevitha Rajanathadurai1
1Cancer Genomics Laboratory, Saveetha Medical College and Hospitals, Saveetha Institute of Medical and Technical Sciences, Saveetha University, Chennai, IND.
Abstract:
Introduction Oral cancer is the most persistent, aggressive primary malignant sarcoma that is globally prevalent. Though chemotherapy is the only treatment option, it has not progressed for years to overcome its detrimental side effects. Introducing novel therapeutic techniques to improve effectiveness is the need of the hour. Aim This study aimed to investigate the pro-apoptotic effects of naringin in oral cancer cell lines. Methodology The cell viability of oral cancer cells treated with naringin was measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method. Naringin was given to oral cancer cells (KB-1) in concentrations ranging from 20 to 200 µM/mL for 24 hours. A phase-contrast microscope is used to examine cell morphology changes. Ethidium bromide (EtBr) staining was employed to study nuclear morphological alterations in oral cancer cells. The apoptotic nuclei were viewed under a fluorescent microscope. To determine pro-apoptotic levels, quantitative real-time polymerase chain reaction (PCR) gene expression analysis was performed to evaluate the expression of transforming growth factor-beta (TGF-β), suppressor of mothers against decapentaplegic 2 (SMAD2), tumor necrosis factor alpha (TNFα), and nuclear factor kappa B (NFκB). A scratch wound healing experiment was used to evaluate naringin's anti-migratory properties. Results Our study found that naringin treatment significantly reduced cell viability in oral cancer cells compared to the control group (p < 0.05). In oral cancer cells, we found an inhibitory concentration (IC50) of 125.3 μM/mL. Following treatment, fewer cells were present, and those that were present shrunk and displayed cytoplasmic membrane blebbing. The EtBr staining reveals chromatin condensation and nuclear breakage in treated cells. The study found that naringin downregulates the expression of B-cell leukemia/lymphoma 2 (Bcl-2), TGF-β, SMAD2, TNFα, and NFκB and upregulates the expression of Bcl-2-associated agonist of cell death (BAD), Bcl-2-associated protein X (BAX), and caspase-3. Furthermore, when compared to control cells, naringin significantly reduced cell migration. Naringin treatment significantly promotes apoptosis and inhibits migration by altering the SMAD2 signaling pathway. Conclusion Overall, this study highlights the promising role of naringin as a pro-apoptotic and cytotoxic phytochemical regulating the gene expression of Bcl-2, TGF-β, SMAD2, TNFα, NFκB, BAD, BAX, and caspase-3, thereby treating oral cancer.
Insights
Naringin, a natural compound, effectively induces apoptosis and inhibits migration in oral cancer cells by modulating key gene expressions. This study highlights naringin
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Oral cancer is a prevalent and aggressive malignancy with limited treatment advancements.
- Current chemotherapy options for oral cancer have significant detrimental side effects.
- Novel therapeutic strategies are urgently needed to improve oral cancer treatment efficacy.
Purpose of the Study:
- To investigate the pro-apoptotic and anti-migratory effects of naringin in oral cancer cell lines.
- To evaluate the impact of naringin on the gene expression of key apoptotic and signaling pathway regulators.
- To assess naringin's potential as a therapeutic agent for oral cancer.
Main Methods:
- Cell viability was assessed using the MTT assay.
- Morphological changes were observed via phase-contrast microscopy and Ethidium bromide (EtBr) staining.
- Quantitative real-time PCR (qPCR) was used to analyze gene expression (Bcl-2, TGF-β, SMAD2, TNFα, NFκB, BAD, BAX, caspase-3).
- Scratch wound healing assays were performed to evaluate anti-migratory properties.
Main Results:
- Naringin significantly reduced oral cancer cell viability with an IC50 of 125.3 μM/mL.
- Morphological analysis showed decreased cell numbers, shrinkage, cytoplasmic blebbing, chromatin condensation, and nuclear fragmentation.
- Naringin downregulated Bcl-2, TGF-β, SMAD2, TNFα, and NFκB, while upregulating BAD, BAX, and caspase-3 expression.
- Naringin significantly inhibited cell migration and altered the SMAD2 signaling pathway.
Conclusions:
- Naringin exhibits significant pro-apoptotic and cytotoxic effects on oral cancer cells.
- Naringin modulates the expression of key genes involved in apoptosis and cell signaling, including Bcl-2, TGF-β, SMAD2, TNFα, NFκB, BAD, BAX, and caspase-3.
- Naringin demonstrates potential as a promising phytochemical agent for oral cancer treatment due to its ability to inhibit cancer cell proliferation and migration.
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