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Updated: Jul 28, 2026
Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay
Published on: November 10, 2013
Development of novel ruthenium(II)-arene complexes displaying potent anticancer effects in glioblastoma cells
Priyaranjan Kumar1, Indranil Mondal, Ritu Kulshreshtha
1Department of Chemistry, Indian Institute of Technology Kanpur, Kanpur 208016, Uttar Pradesh, India. akpatra@iitk.ac.in.
Abstract:
Glioblastomas (GBs) are highly aggressive and malignant brain tumors, which are highly resistant to conventional multimodal treatments, leading to their abysmal prognosis. Herein, we designed two organometallic half-sandwich Ru(ii)-η6-p-cymene complexes containing Schiff bases derived from 3-aminoquinoline and 2-hydroxy-benzaldehyde (L1) and 2-hydroxy-naphthaldehyde (L2), namely [Ru(η6-p-cymene)(L1)Cl] (1) and [Ru(η6-p-cymene)(L2)Cl] (2), respectively, and studied their activity on GB cells. Both complexes were structurally characterized using single-crystal X-ray diffraction, which exhibited their half-sandwich three-legged piano-stool geometry. Furthermore, we studied their physicochemical behavior, solution speciation, aquation kinetics, and photo-substitution reactions using various spectroscopic methods. The complexes exhibited a moderate binding affinity with calf-thymus (CT)-DNA (Kb ∼ 105 M-1). The complexes effectively interacted with human serum albumin (HSA) (K ∼ 105 M-1) with preferential tryptophan binding, as determined via synchronous fluorescence studies. The in vitro studies showed their significant antiproliferative activity against an aggressive human GB cell line, LN-229 (IC50 = 22.8 μM), with moderate selectivity relative to normal mouse fibroblast L929 cells. Notably, [Ru(η6-p-cymene)(L1)Cl] (1) exhibited a higher selectivity index (S.I.) than [Ru(η6-p-cymene)(L2)Cl] (2) and cisplatin. We evaluated the clonogenic potential of the GB cells using a colony formation assay in the presence of complex 1. Excitingly, it showed ∼75% inhibition of the clonogenic potential of GB cells at the IC50 concentration. Complex 1 also effectively lowered the migratory potential of the GB cells, as assessed by the wound healing assay. The studied compound led to the apoptosis of GB cells, as evidenced by nuclear condensation, blebbing, and enhanced caspase 3/7 activity, and thus has anticipated utility in the treatment of GBs using photochemotherapy.
Insights
New ruthenium complexes show promise for treating aggressive glioblastomas (GBs). Complex 1 effectively inhibited GB cell proliferation, migration, and colony formation, inducing apoptosis for potential photochemotherapy applications.
Area of Science:
- Organometallic Chemistry
- Cancer Biology
- Medicinal Chemistry
Background:
- Glioblastomas (GBs) are aggressive brain tumors with poor treatment outcomes.
- Conventional therapies show limited efficacy against GBs, necessitating novel therapeutic strategies.
- Organometallic complexes offer unique mechanisms for cancer treatment.
Purpose of the Study:
- To synthesize and characterize novel half-sandwich ruthenium(ii)-p-cymene complexes with Schiff base ligands.
- To evaluate the antiproliferative and mechanistic effects of these complexes on glioblastoma cells.
- To explore their potential utility in photochemotherapy for glioblastoma treatment.
Main Methods:
- Synthesis and structural characterization of ruthenium complexes using single-crystal X-ray diffraction.
- Physicochemical studies, including DNA/HSA binding affinity and solution speciation.
- In vitro evaluation of antiproliferative activity, clonogenic potential, migration inhibition, and apoptosis induction in glioblastoma cell lines.
Main Results:
- Two novel ruthenium complexes, [Ru(η6-p-cymene)(L1)Cl] (1) and [Ru(η6-p-cymene)(L2)Cl] (2), were synthesized and characterized.
- Complex 1 demonstrated significant antiproliferative activity against human glioblastoma cells (LN-229) with notable selectivity over normal cells.
- Complex 1 effectively inhibited colony formation, reduced cell migration, and induced apoptosis, showing potential for photochemotherapy.
Conclusions:
- The synthesized ruthenium complexes exhibit promising anticancer activity against glioblastoma.
- Complex 1 displays superior selectivity and efficacy compared to complex 2 and cisplatin.
- These findings suggest the potential of complex 1 as a therapeutic agent for glioblastoma, possibly in combination with photochemotherapy.
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