Synthesis, characterization, and antitumor activity of unusual pseudo five coordinate gold(III) complexes: Distinct cytotoxic mechanism or expensive ligand delivery systems?

Olsen, Pauline M; Ruiz, Charles J.; Lussier, Daniel J.; Le, Brian Khoa; Angel, Noah; Smith, Michelle M.; Hwang, Chihyun Brian; Khatib, Raneen; Jenkins, J. O.; Adams, Kaitlyn; Getcher, Jonathan; Tham, Fook S.; Chen, Zhou Georgia; Wilson, Emma H.; Eichler, Jack F.

doi:10.1016/j.jinorgbio.2014.08.014

Cited by 18 publications

(5 citation statements)

References 27 publications

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“…A silver(I) complex of phenanthroline was found to be more potent than cisplatin on HepG2 cells [49]. Gold(III) complexes with bidentate ligands based on the 1,10-phenanthroline and 2,2′-bipyridine scaffolds showed promising anticancer activity against a variety of tumor cell lines [50]. Interestingly, phenanthroline-based small molecules were used as a cellular imaging and cancer screening agent by Sergeeva and colleagues.…”

Section: Discussionmentioning

confidence: 99%

Gold(III) compounds-mediated inhibition of lung cancer cell proliferation

Bostancıoğlu

Kaya²,

Koparal³

et al. 2016

Anti-Cancer Drugs

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Research on chemotherapeutics for lung cancer is crucial for designing a new therapeutic strategy against malignant lung tumors. Although radiotherapy and chemotherapy, which are not selective for cancer cells and exert toxic effects on healthy cells, have a limited advantage, they are the primary treatment modalities for non-small lung cancer. In addition to cytotoxicity, resistance of chemotherapeutics results in failure of treatment. This is why it is of utmost importance to focus on the creation of new chemotherapeutics without toxicity for the successful treatment and improved survival of cancer patients. New gold(III) and Pt(II) compounds were synthesized with a heterocyclic ligand using 2-phenylimidazo[4,5-f][1,10]phenanthroline as a ligand and bis-1,4-di[([1,10] phenanthroline-5-il)amino]-2-buten as a bridge molecule. The characterization of the compounds was carried out using a variety of spectroscopic methods (H NMR, IR, MS, and elemental analysis). Their antiproliferative, antitumoral, and apoptotic activities were determined. IR spectra and NMR results confirmed the formation of dinuclear heterocyclic complexes for two metal complexes. Cytotoxicity studies on lung cancer cells (A549) and healthy cells (CHL) showed a marked increase in cytotoxicity with the use of gold(III) complexes, and especially [Au(L)B](PF6)2 showed higher cytotoxic and apoptotic features than cisplatin at lower concentrations in cancer cells. These findings have been supported by results from DAPI staining and colorimetric measurement of the caspase-3 enzyme in both cell lines. Compounds showed selective toxicity on the cancer cells. In the light of the high efficacy of our newly synthesized gold complexes, they might be good and promising anticancer agents compared with cisplatin.

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Section: Discussionmentioning

confidence: 99%

Gold(III) compounds-mediated inhibition of lung cancer cell proliferation

Bostancıoğlu

Kaya²,

Koparal³

et al. 2016

Anti-Cancer Drugs

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“…dsBPT was synthesized and purified according to a previously published protocol [15]. The purity of the final product was verified by thin layer chromatography (TLC), 1H NMR, and elemental analysis.…”

Section: Methodsmentioning

confidence: 99%

“…Several recent studies have addressed the antiproliferative potential of 1,10-phenanthroline (phen)-based ligands and their metal complexes in other types of cancer cells [8–11]. Previous studies have shown phen-based ligands also exhibit anti-proliferation properties when not coordinated to the gold metal center in vitro [12–15]. Therefore, the current study aimed to determine the anti-proliferative activity of 2,9-di- sec -butyl-1,10-phenanthroline (dsBPT).…”

Section: Introductionmentioning

confidence: 99%

Antitumor Activity of 2,9-Di-Sec-Butyl-1,10-Phenanthroline

et al. 2016

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The anti-tumor effect of a chelating phen-based ligand 2,9-di-sec-butyl-1,10-phenanthroline (dsBPT) and its combination with cisplatin were examined in both lung and head and neck cancer cell lines and xenograft animal models in this study. The effects of this agent on cell cycle and apoptosis were investigated. Protein markers relevant to these mechanisms were also assessed. We found that the inhibitory effect of dsBPT on lung and head and neck cancer cell growth (IC50 ranged between 0.1–0.2 μM) was 10 times greater than that on normal epithelial cells. dsBPT alone induced autophagy, G1 cell cycle arrest, and apoptosis. Our in vivo studies indicated that dsBPT inhibited tumor growth in a dose-dependent manner in a head and neck cancer xenograft mouse model. The combination of dsBPT with cisplatin synergistically inhibited cancer cell growth with a combination index of 0.3. Moreover, the combination significantly reduced tumor volume as compared with the untreated control (p = 0.0017) in a head and neck cancer xenograft model. No organ related toxicities were observed in treated animals. Our data suggest that dsBPT is a novel and potent antitumor drug that warrants further preclinical and clinical development either as a single agent or in combination with known chemotherapy drugs such as cisplatin.

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“…The mechanism by which Cu(II)phen complexes exert their toxicity is reported to be through strong DNA binding activity and by inducing oxidative stress through mitochondrial dysfunction initiating apoptosis [249,250]. A series of Au(III) bearing phen and derivative 2,2 -bipyridine (bipy) scaffolds have shown promising anticancer activity against the A549 cell line, which exhibited IC 50 values that were significantly lower than those of cisplatin control, possibly inducing cell death via a TrxR-mediated mechanism [256]. The coordination complexes [Au III (5-chloro-phen)Cl 2 ]PF 6 ) and [Au III (bipy)Cl 2 ]PF 6 displayed potent cytotoxicity in the A549 cell line, potentially through the inhibition of the water and glycerol channel aquaglyceroporin-3 (AQP3), which play crucial roles in cell apoptosis, proliferation, and migration and therefore have been proposed as new drug targets for cancer treatment [257].…”

Section: 10-phenanthroline and Its Metal Complexesmentioning

confidence: 99%

The Lung Microbiome in COPD and Lung Cancer: Exploring the Potential of Metal-Based Drugs

O’Shaughnessy,

Sheils,

Baird

2023

IJMS

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Chronic obstructive pulmonary disease (COPD) and lung cancer 17 are two of the most prevalent and debilitating respiratory diseases worldwide, both associated with high morbidity and mortality rates. As major global health concerns, they impose a substantial burden on patients, healthcare systems, and society at large. Despite their distinct aetiologies, lung cancer and COPD share common risk factors, clinical features, and pathological pathways, which have spurred increasing research interest in their co-occurrence. One area of particular interest is the role of the lung microbiome in the development and progression of these diseases, including the transition from COPD to lung cancer. Exploring novel therapeutic strategies, such as metal-based drugs, offers a potential avenue for targeting the microbiome in these diseases to improve patient outcomes. This review aims to provide an overview of the current understanding of the lung microbiome, with a particular emphasis on COPD and lung cancer, and to discuss the potential of metal-based drugs as a therapeutic strategy for these conditions, specifically concerning targeting the microbiome.

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Synthesis, characterization, and antitumor activity of unusual pseudo five coordinate gold(III) complexes: Distinct cytotoxic mechanism or expensive ligand delivery systems?

Cited by 18 publications

References 27 publications

Gold(III) compounds-mediated inhibition of lung cancer cell proliferation

Gold(III) compounds-mediated inhibition of lung cancer cell proliferation

Antitumor Activity of 2,9-Di-Sec-Butyl-1,10-Phenanthroline

The Lung Microbiome in COPD and Lung Cancer: Exploring the Potential of Metal-Based Drugs

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