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Issue 20, 2017
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Photo-induced cytotoxicity and anti-metastatic activity of ruthenium(II)–polypyridyl complexes functionalized with tyrosine or tryptophan

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Abstract

The synergistic effect of oxygen, light, and photosensitizer (PS) has found applications in medicine for the treatment of cancer through photodynamic therapy (PDT). Induction of apoptosis to cancerous cells will prevent tumor metastasis that spreads cancer cells to the neighboring organs/tissues. Herein, we report the two apoptotic Ru(II)–polypyridyl complexes that are functionalized with pendant amino acid moieties tyrosine (1) and tryptophan (2), respectively. These two water soluble complexes were found to interact strongly (K1a = (1.18 ± 0.28) × 105 M−1 and K2a = (1.57 ± 0.77) × 105 M−1) with CT-DNA. Isothermal titration calorimetry (ITC) studies revealed that these complexes bind to CT-DNA through an entropically driven process. Both the complexes showed photo-induced cytotoxicity and exhibit apoptotic activity under photo-irradiation conditions. The comet assay indicated that these complexes can damage cellular DNA, which is attributed to the significant build-up of 1O2 level even on irradiation with low intensity light (10 J cm−2, λRange 450–480 nm). This photoinduced DNA damage and apoptosis in A549 cells was induced by reactive oxygen species (ROS) and occurred through up-regulation of apoptotic marker caspase-3. Control experiments under dark conditions revealed an insignificant cytotoxicity towards these cells for two photosensitive molecules.

Graphical abstract: Photo-induced cytotoxicity and anti-metastatic activity of ruthenium(ii)–polypyridyl complexes functionalized with tyrosine or tryptophan

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Publication details

The article was received on 23 Feb 2017, accepted on 18 Apr 2017 and first published on 19 Apr 2017


Article type: Paper
DOI: 10.1039/C7DT00670E
Citation: Dalton Trans., 2017,46, 6634-6644
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    Photo-induced cytotoxicity and anti-metastatic activity of ruthenium(II)–polypyridyl complexes functionalized with tyrosine or tryptophan

    V. Ramu, S. Aute, N. Taye, R. Guha, M. G. Walker, D. Mogare, A. Parulekar, J. A. Thomas, S. Chattopadhyay and A. Das, Dalton Trans., 2017, 46, 6634
    DOI: 10.1039/C7DT00670E

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