Mechanistic Evaluation of Thymoquinone Derivative-Induced Apoptosis in Human Glioblastoma Cells
Background: Glioblastoma is a highly aggressive brain tumor with limited treatment options, necessitating the development of targeted and effective therapeutics. Thymoquinone (TQ), a natural compound with known anticancer potential, has been modified to enhance its efficacy. Materials and Methods: A...
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| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Wolters Kluwer Medknow Publications
2025-06-01
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| Series: | Journal of Pharmacy and Bioallied Sciences |
| Subjects: | |
| Online Access: | https://journals.lww.com/10.4103/jpbs.jpbs_1967_24 |
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| Summary: | Background:
Glioblastoma is a highly aggressive brain tumor with limited treatment options, necessitating the development of targeted and effective therapeutics. Thymoquinone (TQ), a natural compound with known anticancer potential, has been modified to enhance its efficacy.
Materials and Methods:
A series of TQ derivatives (SS-01 to SS-05) and the parent compound (SS-06) were synthesized and screened for cytotoxic activity using the Sulforhodamine B (SRB) assay against various cancer cell lines—glioblastoma (SNB-19, U251), breast carcinoma (MCF-7, MD-MBA-231), pancreatic carcinoma (MIAPaCa, PANC-1), lung carcinoma (A549), prostate carcinoma (PC3)—and a normal fibroblast cell line (FR2). The most promising derivative, SS-03, was further evaluated in U251 glioblastoma cells using colony formation assay, Western blotting for apoptotic markers, and flow cytometry for cell cycle analysis.
Results:
Among all derivatives, SS-03 exhibited the highest cytotoxicity, particularly against U251 glioblastoma cells. SS-03 treatment significantly increased the Bax/Bcl-2 ratio, induced apoptosis, arrested the cell cycle in S-phase, and suppressed colony formation in a dose-dependent manner. Importantly, SS-03 showed selective toxicity towards cancer cells while sparing normal fibroblasts.
Conclusion:
SS-03, a novel TQ derivative, demonstrates potent anticancer activity against glioblastoma cells through apoptosis induction and cell cycle arrest. |
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| ISSN: | 0976-4879 0975-7406 |