Rationally designed Ru(ii)-metallacycle chemo-phototheranostic that emits beyond 1000 nm

Chonglu Li, Yuling Xu, Le Tu, Minhyeok Choi, Yifan Fan, Xiaoqiang Chen, Jonathan L. Sessler, Jong Seung Kim, Yao Sun

Research output: Contribution to journalArticlepeer-review

50 Citations (Scopus)


Ruthenium complexes are emerging as potential complements to platinum drugs. They also show promise as photo-diagnostic and therapeutic agents. However, most ruthenium species studied to date as potential drugs are characterized by short excitation/emission wavelengths. This limits their applicability for deep-tissue fluorescence imaging and light-based therapeutic treatments. Here, we report a Ru(ii) metallacycle (Ru1100) that emits at ≥1000 nm. This system possesses excellent deep-tissue penetration capability (∼7 mm) and displays good chemo-phototherapeutic performance. In vitro studies revealed that Ru1100 benefits from good cellular uptake and produces a strong anticancer response against several cancer cell lines, including a cisplatin-resistant A549 cell line (IC50 = 1.6 μM vs. 51.4 μM for cisplatin). On the basis of in vitro studies, it is concluded that Ru1100 exerts its anticancer action by regulating cell cycle progression and triggering cancer cell apoptosis. In vivo studies involving the use of a nanoparticle formulation served to confirm that Ru1100 allows for high-performance NIR-II fluorescence imaging-guided precise chemo-phototherapy in the case of A549 tumour mouse xenografts with no obvious side effects. This work thus provides a paradigm for the development of long-wavelength emissive supramolecular theranostic agents based on ruthenium.

Original languageEnglish
Pages (from-to)6541-6549
Number of pages9
JournalChemical Science
Issue number22
Publication statusPublished - 2022 May 18

Bibliographical note

Funding Information:
This work was supported by National Natural Science Foundation of China 22022404 and 22074050, supported by the State Key Laboratory of Materials-Oriented Chemical Engineering (KL20-05); supported by the Open Fund of Guangdong Provincial Key Laboratory of Luminescence from Molecular Aggregates, Guangzhou 510640, China (South China University of Technology, 2020-k11ma-06). This work was also supported by the National Research Foundation of Korea (NRF) (CRI Project No. 2018R1A3B1052702 and 2019M3E5D1A01068998, J. S. K.). J. L. S. acknowledges support from the Robert A. Welch Foundation (F-0018). All animal experiments were conducted in agreement with the guidelines of Institutional Animal Care and Use Committee (CCNU-IACUC-2011-058).

Publisher Copyright:
© 2022 The Royal Society of Chemistry

ASJC Scopus subject areas

  • General Chemistry


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