Cell nucleus localization and high anticancer activity of quinoline-benzopyran rhodium() metal complexes as therapeutic and fluorescence imaging agents

Four novel rhodium( iii ) complexes, [Rh III (QB1)Cl 3 (DMSO)] ( RhN1 ), [Rh III (QB2)Cl 3 (CH 3 OH)]·CH 3 OH ( RhN2 ), [Rh III (QB3)Cl 3 (CH 3 OH)]·CH 3 OH ( RhS ), and [Rh III (QB4)Cl 3 (DMSO)] ( RhQ ), bearing quinoline-benzopyran ligands (QB1-QB4) were synthesized and used to develop highly anti...

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Published in:Dalton transactions : an international journal of inorganic chemistry 2022-08, Vol.51 (34), p.12866-12875
Main Authors: Wang, Zhen-Feng, Nai, Xiao-Ling, Xu, Yue, Pan, Feng-Hua, Tang, Fu-Shun, Qin, Qi-Pin, Yang, Lin, Zhang, Shu-Hua
Format: Article
Language:English
Subjects:
Anticancer properties
Apoptosis
Biocompatibility
Cancer
Chemical compounds
Coordination compounds
Fluorescence
Fluoroscopic imaging
Ligands
Nuclei (cytology)
Pharmacology
Quinoline
Rhodium
Toxicity
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Summary:Four novel rhodium( iii ) complexes, [Rh III (QB1)Cl 3 (DMSO)] ( RhN1 ), [Rh III (QB2)Cl 3 (CH 3 OH)]·CH 3 OH ( RhN2 ), [Rh III (QB3)Cl 3 (CH 3 OH)]·CH 3 OH ( RhS ), and [Rh III (QB4)Cl 3 (DMSO)] ( RhQ ), bearing quinoline-benzopyran ligands (QB1-QB4) were synthesized and used to develop highly anticancer therapeutic and fluorescence imaging agents. Compared with the QB1-QB4 ligands (IC 50 > 89.2 ± 1.7 μM for A549/DDP), RhN1 , RhN2 , RhS and RhQ exhibit selective cytotoxicity against lung carcinoma cisplatin-resistant A549/DDP (A549CDDP) cancer cells, with IC 50 values in the range of 0.08-2.7 μM. The fluorescent imaging agent RhQ with the more extended planar QB4 ligand exhibited high anticancer activity in A549CDDP cells and was found in the cell nucleus fraction, whereas RhS had no fluorescence properties. RhQ and RhS may trigger cell apoptosis by causing DNA damage and initiating the mitochondrial dysfunction pathway. Furthermore, RhQ has a higher antitumor efficacy ( ca. 55.3%) than RhS (46.4%) and cisplatin (CDDP, 33.1%), and RhQ demonstrated significantly lower toxicity in vivo than CDDP, making it a promising Rh( iii )-based anticancer therapeutic and fluorescence imaging agent. RhQ can be used to target DNA as a highly anticancer therapeutic and fluorescence imaging agent. Importantly, RhQ exhibited significantly more potency than RhS and cisplatin.
ISSN:1477-9226
1477-9234
DOI:10.1039/d2dt01929a