ArticleChemistry (Weinheim an der Bergstrasse, Germany)2016
Chemical Swarming: Depending on Concentration, an Amphiphilic Ruthenium Polypyridyl Complex Induces Cell Death via Two Different Mechanisms.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 36 citations in OpenAlex.
- Estrogen-Functionalized Ru(II) Polypyridyl Complexes Self-Assemble into Aggregates and Exhibit Selective Phototoxicity against Breast Cancer Cells.Inorganic chemistry · 2025Article
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- Factors that influence singlet oxygen formation vs. ligand substitution for light-activated ruthenium anticancer compounds.Current opinion in chemical biology · 2022Review
- Investigating Alkylated Prodigiosenes and Their Cu(II)-Dependent Biological Activity: Interactions with DNA, Antimicrobial and Photoinduced Anticancer Activity.ChemMedChem · 2022Article
- Ruthenium-based PACT agents based on bisquinoline chelates: synthesis, photochemistry, and cytotoxicity.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2021Article
- Organoplatinum(II) Complexes Self-Assemble and Recognize AT-Rich Duplex DNA Sequences.Inorganic chemistry · 2021Article
- Photo-Uncaging of a Microtubule-Targeted Rigidin Analogue in Hypoxic Cancer Cells and in a Xenograft Mouse Model.Journal of the American Chemical Society · 2019Article
- Synthesis and Avidin Binding of Ruthenium Complexes Functionalized with a Light-Cleavable Free Biotin Moiety.European journal of inorganic chemistry · 2018Article
- New Ru(ii) complex for dual photochemotherapy: release of cathepsin K inhibitor andDalton transactions (Cambridge, England : 2003) · 2018Article
- Spectroscopic Studies on Photoinduced Reactions of the Anticancer Prodrug, trans,trans,trans-[Pt(NChemistry (Weinheim an der Bergstrasse, Germany) · 2018Article
- Effects of the Bidentate Ligand on the Photophysical Properties, Cellular Uptake, and (Photo)cytotoxicity of Glycoconjugates Based on the [Ru(tpy)(NN)(L)]Chemistry (Weinheim an der Bergstrasse, Germany) · 2018Article
- The development of anticancer ruthenium(ii) complexes: from single molecule compounds to nanomaterials.Chemical Society reviews · 2017Review
- Apoptosis-independent organoruthenium anticancer complexes that overcome multidrug resistance: self-assembly and phenotypic screening strategies.Chemical science · 2017Article
- Chemical Swarming: Depending on Concentration, an Amphiphilic Ruthenium Polypyridyl Complex Induces Cell Death via Two Different Mechanisms.Chemistry (Weinheim an der Bergstrasse, Germany) · 2016Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The crystal structure and in vitro cytotoxicity of the amphiphilic ruthenium complex [3](PF6 )2 are reported. Complex [3](PF6 )2 contains a Ru-S bond that is stable in the dark in cell-growing medium, but is photosensitive. Upon blue-light irradiation, complex [3](PF6 )2 releases the cholesterol-thioether ligand 2 and an aqua ruthenium complex [1](PF6 )2 . Although ligand 2 and complex [1](PF6 )2 are by themselves not cytotoxic, complex [3](PF6 )2 was unexpectedly found to be as cytotoxic as cisplatin in the dark, that is, with micromolar effective concentrations (EC50 ), against six human cancer cell lines (A375, A431, A549, MCF-7, MDA-MB-231, and U87MG). Blue-light irradiation (λ=450 nm, 6.3 J cm(-2) ) had little influence on the cytotoxicity of [3](PF6 )2 after 6 h of incubation time, but it increased the cytotoxicity of the complex by a factor 2 after longer (24 h) incubation. Exploring the unexpected biological activity of [3](PF6 )2 in the dark elucidated an as-yet unknown bifaceted mode of action that depended on concentration, and thus, on the aggregation state of the compound. At low concentration, it acts as a monomer, inserts into the membrane, and can deliver [1](2+) inside the cell upon blue-light activation. At higher concentrations (>3-5 μm), complex [3](PF6 )2 forms supramolecular aggregates that induce non-apoptotic cell death by permeabilizing cell membranes and extracting lipids and membrane proteins.
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