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Aaptamine attenuates the proliferation and progression of non-small cell lung carcinoma
Kaikai Gong1, Shuang Miao1, Lijuan Yang1
1Cancer Research Institute, Binzhou Medical University Hospital, Binzhou, PR China.
Context:
Aaptamine is a potent ocean-derived non-traditional drug candidate against human cancers. However, the underlying molecular mechanisms governing aaptamine-mediated repression of lung cancer cells remain largely undefined.
Objective:
To examine the inhibitory effect of aaptamine on proliferation and progression of non-small cell lung carcinoma (NSCLC) and dissect the potential mechanisms involved in its anticancer functions.
Materials And Methods:
In vitro assays of cell proliferation, cell cycle analysis, clonal formation, apoptosis and migration were performed to examine the inhibitory effects of aaptamine (8, 16 and 32 μg/mL) on NSCLC cells. The expression levels of proteins were analysed using western blotting analysis when cells were treated with a single drug or a combination treatment for 48 h.
Results:
Aaptamine significantly inhibited A549 and H1299 cells proliferation with IC50 values of 13.91 and 10.47 μg/mL. At the concentrations of 16 and 32 μg/mL, aaptamine significantly reduced capacities in clonogenicity, enhanced cellular apoptosis and decreased the motile and invasive cellular phenotype. In addition, aaptamine arrested cell cycle at G1 phase via selectively abating cell cycle regulation drivers (CDK2/4 and Cyclin D1/E). Western blotting results showed that aaptamine attenuated the protein expression of MMP-7, MMP-9 and upregulated the expression of cleaved-PARP and cleaved-caspase 3. Moreover, aaptamine inhibited PI3K/AKT/GSK3β signalling cascades through specifically degrading the phosphorylated AKT and GSK3β.
Discussion And Conclusions:
Aaptamine retarded the proliferation and invasion of NSCLC cells by selectively targeting the pathway PI3K/AKT/GSK3β suggesting it as a potential chemotherapeutic agent for repressing tumorigenesis and progression of NSCLC in humans.
Insights
Aaptamine, a marine compound, effectively inhibits non-small cell lung cancer (NSCLC) progression by halting cell cycle and inducing apoptosis. It targets the PI3K/AKT/GSK3β pathway, showing potential as a lung cancer therapeutic.
Area of Science:
- Marine natural products chemistry
- Cancer biology
- Molecular pharmacology
Background:
- Aaptamine is an ocean-derived compound with anticancer potential.
- Its precise mechanisms against lung cancer remain unclear.
Purpose of the Study:
- To investigate aaptamine's effects on non-small cell lung carcinoma (NSCLC) proliferation and progression.
- To elucidate the molecular pathways involved in aaptamine's anticancer activity.
Main Methods:
- In vitro assays assessed NSCLC cell proliferation, cell cycle, clonogenicity, apoptosis, and migration.
- Protein expression was analyzed via Western blotting after aaptamine treatment.
Main Results:
- Aaptamine inhibited NSCLC cell proliferation (IC50: 13.91 and 10.47 μg/mL) and reduced clonogenicity, migration, and invasion.
- It induced apoptosis, arrested the cell cycle at G1 phase, and modulated key proteins (MMP-7, MMP-9, cleaved-PARP, cleaved-caspase 3).
- Aaptamine suppressed the PI3K/AKT/GSK3β signaling pathway by degrading phosphorylated AKT and GSK3β.
Conclusions:
- Aaptamine effectively inhibits NSCLC cell proliferation and invasion.
- Its mechanism involves targeting the PI3K/AKT/GSK3β pathway.
- Aaptamine shows promise as a chemotherapeutic agent for NSCLC.
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