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Antitumor Activity of Isalpinin from Paphiopedilum dianthum on Non-Small Cell Lung Cancer Cell Lines
Phisit Pouyfung1,2, Nonthalert Lertnitikul3,4, Hua Bai5
1Department of Occupational Health and Safety, School of Public Health, Walailak University, Nakhon Si Thammarat 80160, Thailand.
Abstract:
Lung cancer is a leading cause of cancer-related deaths globally, with current treatments having significant limitations, including drug resistance, metastasis, and tumor heterogeneity. This study investigated the anticancer potential of isalpinin, a flavonoid isolated from Paphiopedilum dianthum, against non-small cell lung cancer (NSCLC) cell lines A549, H23, and H460. Isalpinin significantly inhibited NSCLC cell viability in a dose- and time-dependent manner; H23 and H460 cells showed greater sensitivity (IC50 a ~ 44 μM at 48 h) compared to A549 cells (IC50 82 μM). Isalpinin suppressed proliferation, migration, and anchorage-independent growth, particularly in H23/H460 cells. Mechanistically, it induced apoptosis via increased ROS production and Bcl-2 downregulation, particularly in H23 and H460 cells. In a molecular docking analysis, isalpinin was found to directly bind to the ATP-binding pocket of AKT1, as confirmed by reduced Akt/GSK3β phosphorylation. These results suggest that isalpinin showed a potent multi-target natural compound against NSCLC that disrupts the key hallmarks of malignancy and pro-survival signaling. However, its subtype-specific efficacy warrants further in vivo studies and an investigation of combinatorial therapeutic approaches to elucidate its clinical potential.
Insights
Isalpinin, a natural flavonoid, effectively inhibited non-small cell lung cancer (NSCLC) cell growth and induced apoptosis. This compound targets key cancer pathways, showing promise as a novel NSCLC therapeutic agent.
Area of Science:
- Phytochemistry
- Cancer Biology
- Molecular Pharmacology
Background:
- Lung cancer remains a major global health challenge with limited treatment options.
- Drug resistance, metastasis, and tumor heterogeneity complicate current therapeutic strategies for non-small cell lung cancer (NSCLC).
Purpose of the Study:
- To evaluate the anticancer potential of isalpinin, a flavonoid from *Paphiopedilum dianthum*, against NSCLC cell lines.
- To elucidate the mechanisms underlying isalpinin's anti-NSCLC effects.
Main Methods:
- In vitro assays assessing cell viability, proliferation, migration, and anchorage-independent growth.
- Apoptosis induction analysis via reactive oxygen species (ROS) production and Bcl-2 expression.
- Molecular docking and Western blot analysis to investigate AKT1 signaling pathway inhibition.
Main Results:
- Isalpinin demonstrated dose- and time-dependent inhibition of NSCLC cell viability, with greater efficacy in H23 and H460 cells compared to A549.
- The compound suppressed proliferation, migration, and anchorage-independent growth, inducing apoptosis through increased ROS and Bcl-2 downregulation.
- Molecular docking revealed isalpinin's direct binding to the AKT1 ATP-binding pocket, confirmed by reduced Akt/GSK3β phosphorylation.
Conclusions:
- Isalpinin exhibits potent multi-target anticancer activity against NSCLC by disrupting key malignant hallmarks and pro-survival signaling.
- The compound's efficacy varies by NSCLC subtype, necessitating further in vivo research and exploration of combination therapies for clinical application.
