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Dual Functional Half‐Sandwich Ru(II) Complexes: Lysosome‐Targeting Probes and Anticancer Agents
Author(s) -
Liu Zhe,
Li JuanJuan,
Kong Deliang,
Tian Meng,
Zhao Yao,
Xu Zhishan,
Gao Wenyuan,
Zhou Yumin
Publication year - 2019
Publication title -
european journal of inorganic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.667
H-Index - 136
eISSN - 1099-0682
pISSN - 1434-1948
DOI - 10.1002/ejic.201801339
Subject(s) - chemistry , ruthenium , a549 cell , apoptosis , programmed cell death , reactive oxygen species , lysosome , biophysics , cancer cell , cell , cell growth , cell culture , biochemistry , cancer , medicine , genetics , biology , enzyme , catalysis
It is known that the proposed biologically active form of ruthenium is its oxidation state II other than oxidation state III, and ruthenium complexes offer the potential of a novel mechanism of action, reduced toxicity. Herein, three half‐sandwich Ru II complexes [(η 6 ‐ p ‐cym)Ru(N ^ N)Cl]PF 6 were designed and synthesized. Lysosomes are involved in various aspects of cancer cell immortalization and cell death. Thus, lysosomes are attractive pharmacological targets for selective killing of cancer cells. We demonstrated that Ru2 can accumulate in lysosomes. In addition, A549 cell viability remained at 87.81 % after exposure to Ru2 for 24 h at the working concentration. Meanwhile, Ru2 exhibited relatively high photostability and suitability for long‐term tracking. At increased concentration after 24 h of exposure to the complex toward A549 cell line, Ru2 induced a high apoptotic rate, cell cycle arrest, mitochondrial membrane potential loss, and reactive oxygen species overload. Ru2 integrated the anticancer properties and imaging capabilities and is expected to be developed as a dual functional theranostic agent.