A novel substituted benzo[g]quinoxaline-based cyclometalated Ru(II) complex as a biocompatible membrane-targeted PDT colon cancer stem cell agent
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F24%3A73627596" target="_blank" >RIV/61989592:15310/24:73627596 - isvavai.cz</a>
Result on the web
<a href="https://pubs.acs.org/doi/epdf/10.1021/acs.jmedchem.4c02357" target="_blank" >https://pubs.acs.org/doi/epdf/10.1021/acs.jmedchem.4c02357</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/acs.jmedchem.4c02357" target="_blank" >10.1021/acs.jmedchem.4c02357</a>
Alternative languages
Result language
angličtina
Original language name
A novel substituted benzo[g]quinoxaline-based cyclometalated Ru(II) complex as a biocompatible membrane-targeted PDT colon cancer stem cell agent
Original language description
Herein, we describe and investigate biological activity of three octahedral ruthenium(II) complexes of the type [Ru(C∧N)(phen)2]+, RuL1-RuL3, containing a π-expansive cyclometalating substituted benzo[g]quinoxaline ligand (C∧N ligand) (phen = 1,10-phenanthroline). Compounds RuL1-RuL3 in cervical, melanoma, and colon human cancer cells exhibit high phototoxicity after irradiation with light (particularly blue), with the phototoxicity index reaching 100 for the complex RuL2 in most sensitive HCT116 cells. RuL2 accumulates in the cellular membranes. If irradiated, it induces lipid peroxidation, likely connected with photoinduced ROS generation. Oxidative damage to the fatty acids leads to the attenuation of the membranes, the activation of caspase 3, and the triggering of the apoptotic pathway, thus implementing membrane-localized photodynamic therapy. RuL2 is the first photoactive ruthenium-based complex capable of killing the hardly treatable colon cancer stem cells, a highly resilient subpopulation within a heterogeneous tumor mass, responsible for tumor recurrence and the metastatic progression of cancer.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10610 - Biophysics
Result continuities
Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2024
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
JOURNAL OF MEDICINAL CHEMISTRY
ISSN
0022-2623
e-ISSN
1520-4804
Volume of the periodical
67
Issue of the periodical within the volume
23
Country of publishing house
US - UNITED STATES
Number of pages
16
Pages from-to
21470-21485
UT code for WoS article
001368403800001
EID of the result in the Scopus database
2-s2.0-85211000293