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Mechanistic Evaluation of Thymoquinone Derivative-Induced Apoptosis in Human Glioblastoma Cells
Manmeet Kour1,2, Jagjeet Kour3, Bisma Yousuf1
1Pharmacology Division, CSIR- Indian Institute of Integrative Medicine, Jammu, Jammu and Kashmir, India.
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.
Insights
A novel thymoquinone (TQ) derivative, SS-03, shows potent anticancer effects against glioblastoma. This compound selectively kills cancer cells by inducing apoptosis and halting cell cycle progression.
Area of Science:
- Natural Product Derivatives
- Cancer Therapeutics
- Molecular Oncology
Background:
- Glioblastoma is an aggressive brain tumor with limited therapeutic options.
- Thymoquinone (TQ), a natural compound, has anticancer potential but requires modification for enhanced efficacy.
Purpose of the Study:
- To synthesize and evaluate novel TQ derivatives for enhanced anticancer activity, particularly against glioblastoma.
- To identify and characterize the most effective TQ derivative for glioblastoma treatment.
Main Methods:
- Synthesis of TQ derivatives (SS-01 to SS-05) and parent compound (SS-06).
- Cytotoxicity screening using Sulforhodamine B (SRB) assay across multiple cancer cell lines and a normal fibroblast line.
- In-depth evaluation of the lead derivative (SS-03) in U251 glioblastoma cells via colony formation assay, Western blotting for apoptosis markers, and cell cycle analysis.
Main Results:
- SS-03 demonstrated the highest cytotoxicity, especially against U251 glioblastoma cells.
- SS-03 treatment significantly increased the Bax/Bcl-2 ratio, induced apoptosis, and arrested the cell cycle in S-phase.
- SS-03 exhibited selective toxicity towards cancer cells, sparing normal fibroblasts, and suppressed colony formation dose-dependently.
Conclusions:
- SS-03 is a potent TQ derivative with significant anticancer activity against glioblastoma.
- The mechanism of action involves apoptosis induction and cell cycle arrest in glioblastoma cells.
- SS-03 shows promise as a targeted therapeutic agent for glioblastoma.
