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Targeting Lymphoma With Benzoxazole Derivatives: Effects on Viability and Protein Expression in Cell Lines
Esma Bilajac1, Una Glamočlija2, Lejla Mahmutović1
1Department of Genetics and Bioengineering, Faculty of Engineering and Natural Sciences, International University of Sarajevo, Sarajevo, Bosnia and Herzegovina.
Abstract:
Benzoxazoles possess a wide range of therapeutic activities, including antimicrobial, antitumor, anti-inflammatory, and other. Using in silico and in vitro approaches, we determined the potential antitumor activity of benzoxazoles synthesized from thymoquinone in diffuse large B-cell lymphoma (DLBCL) cells. Molecular docking analysis showed strong binding affinities of benzoxazoles toward Akt and nuclear factor kappa B (NF-κB) protein targets that promote cancer cell proliferation and survival and whose expression is linked to tumorigenesis of activated B-cell (ABC) and germinal center B-cell (GCB) DLBCL subtypes. WST-8 assay showed the highest inhibitory activity of benzoxazole derivative bearing thiophene substituent in both DLBCL models. Western blot analysis indicated the inhibitory activity of selected compounds in HBL-1 cells, with decreased p-NF-κB and p-Akt protein expression, whereas treatment of DHL-4 cells stimulated the expression of p-Akt and p-NF-κB protein levels. These data suggest distinct, cell line-dependent activities of the substances that potentially act through diverse oncogenic signaling pathways in DLBCL cells and activation of compensatory cell mechanisms that could be an important step for combinatorial treatment approaches.
Insights
Benzoxazoles synthesized from thymoquinone show potential antitumor activity in diffuse large B-cell lymphoma (DLBCL) cells. These compounds inhibit key cancer targets, but their effects vary by cell type, suggesting tailored treatment strategies.
Area of Science:
- Medicinal Chemistry
- Oncology
- Pharmacology
Background:
- Benzoxazoles are known for diverse therapeutic properties, including antitumor effects.
- Diffuse large B-cell lymphoma (DLBCL) is an aggressive non-Hodgkin lymphoma with distinct subtypes.
- Targeting oncogenic pathways like Akt and NF-κB is crucial for DLBCL treatment.
Purpose of the Study:
- To evaluate the antitumor potential of novel benzoxazoles derived from thymoquinone against DLBCL.
- To investigate the molecular mechanisms underlying the activity of these compounds in DLBCL cells.
- To explore the differential effects of benzoxazoles in activated B-cell (ABC) and germinal center B-cell (GCB) DLBCL subtypes.
Main Methods:
- In silico molecular docking to predict binding affinities to Akt and NF-κB.
- In vitro WST-8 assays to assess cell viability and inhibitory activity.
- Western blot analysis to evaluate protein expression levels (p-Akt, p-NF-κB).
Main Results:
- Molecular docking revealed strong binding of benzoxazoles to Akt and NF-κB targets.
- A benzoxazole derivative with a thiophene substituent exhibited significant inhibitory activity in both DLBCL models.
- Compound effects were cell line-dependent: HBL-1 cells showed decreased p-Akt/p-NF-κB, while DHL-4 cells showed increased levels.
Conclusions:
- Benzoxazoles synthesized from thymoquinone demonstrate promising antitumor activity in DLBCL.
- The compounds potentially target oncogenic signaling pathways, but exhibit distinct, cell-specific effects.
- Observed differential responses suggest complex interactions and potential for combinatorial therapy in DLBCL.
