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In Vitro Anti-Glioblastoma Activity of a Novel Pt(IV)-Ganoderic Acid A Conjugate
Ludovica Gaiaschi1, Fabrizio De Luca1, Stefano Artin Serapian2
1Laboratory of Cell Biology and Neurobiology, Department of Biology and Biotechnology "L. Spallanzani", University of Pavia, 27100 Pavia, Italy.
Abstract:
Glioblastoma is the most aggressive primary malignant tumor of the central nervous system in adults, with a poor prognosis and high resistance to conventional therapies. Platinum drugs like cisplatin are effective but limited by systemic toxicity, poor blood-brain barrier penetration, and resistance. Natural compounds are increasingly studied for their anticancer potential and ability to enhance existing therapies. Based on this rationale, we designed Pt(IV)Ac-GA, a novel platinum(IV) complex obtained by conjugating cisplatin with ganoderic acid A, a triterpenoid from Ganoderma lucidum known for anticancer and immunomodulatory effects. The compound was synthesized, structurally characterized, and showed high stability and favorable pharmacokinetics. In vitro, Pt(IV)Ac-GA strongly reduced the viability of U251 and T98G glioblastoma cells while sparing normal astrocytes. It triggered apoptosis, cell cycle arrest, impaired migration, and increased sensitivity to ferroptosis and mitochondrial dysfunction. These results highlight Pt(IV)Ac-GA as a promising candidate to overcome current limitations in glioblastoma treatment.
Insights
A new platinum(IV) complex, Pt(IV)Ac-GA, effectively targets glioblastoma cells by inducing apoptosis and cell death. This novel compound shows promise in overcoming treatment resistance and toxicity associated with traditional platinum drugs.
Area of Science:
- Oncology
- Neuro-oncology
- Pharmacology
Background:
- Glioblastoma is an aggressive brain tumor with poor outcomes.
- Conventional platinum drugs face challenges like toxicity and poor blood-brain barrier penetration.
- Natural compounds offer potential for enhanced anticancer therapies.
Purpose of the Study:
- To design and synthesize a novel platinum(IV) complex, Pt(IV)Ac-GA, by conjugating cisplatin with ganoderic acid A.
- To evaluate the efficacy and mechanisms of Pt(IV)Ac-GA against glioblastoma cells in vitro.
- To assess its potential to overcome glioblastoma treatment resistance.
Main Methods:
- Synthesis and structural characterization of the Pt(IV)Ac-GA complex.
- In vitro evaluation of cytotoxicity against glioblastoma cell lines (U251, T98G) and normal astrocytes.
- Assessment of apoptosis, cell cycle arrest, migration, ferroptosis, and mitochondrial dysfunction induction.
Main Results:
- Pt(IV)Ac-GA demonstrated significant reduction in glioblastoma cell viability while sparing normal cells.
- The compound induced apoptosis, cell cycle arrest, and impaired cell migration.
- Pt(IV)Ac-GA enhanced sensitivity to ferroptosis and mitochondrial dysfunction.
Conclusions:
- Pt(IV)Ac-GA is a stable and well-characterized platinum(IV) complex with favorable pharmacokinetics.
- This novel compound exhibits potent anti-glioblastoma activity in vitro.
- Pt(IV)Ac-GA represents a promising therapeutic candidate for glioblastoma treatment.
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