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Open AccessArticle

Microwave-Assisted Synthesis of Arene Ru(II) Complexes Induce Tumor Cell Apoptosis Through Selectively Binding and Stabilizing bcl-2 G-Quadruplex DNA

1
School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China
2
The First Affiliated Hospital of Guangdong Pharmaceutical University, Guangzhou 510080, China
3
The Third Affiliated Hospital of Sun Yat-Sen University, Guangzhou 440100, China
4
School of Nursing, Guangdong Pharmaceutical University, Guangzhou 510310, China
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Dinesh Agrawal
Materials 2016, 9(5), 386; https://doi.org/10.3390/ma9050386
Received: 1 March 2016 / Revised: 6 May 2016 / Accepted: 10 May 2016 / Published: 17 May 2016
(This article belongs to the Special Issue Microwave Materials Processing)
A series of arene Ru(II) complexes coordinated with phenanthroimidazole derivatives, [(η6-C6H6)Ru(l)Cl]Cl(1b L = p-ClPIP = 2-(4-Chlorophenyl)imidazole[4,5f] 1,10-phenanthroline; 2b L = m-ClPIP = 2-(3-Chlorophenyl)imidazole[4,5f] 1,10-phenanthroline; 3b L = p-NPIP = 2-(4-Nitrophenyl)imidazole[4,5f] 1,10-phenanthroline; 4b L = m-NPIP = 2-(3-Nitrophenyl) imidazole [4,5f] 1,10-phenanthroline) were synthesized in yields of 89.9%–92.7% under conditions of microwave irradiation heating for 30 min to liberate four arene Ru(II) complexes (1b, 2b, 3b, 4b). The anti-tumor activity of 1b against various tumor cells was evaluated by MTT assay. The results indicated that this complex blocked the growth of human lung adenocarcinoma A549 cells with an IC50 of 16.59 μM. Flow cytometric analysis showed that apoptosis of A549 cells was observed following treatment with 1b. Furthermore, the in vitro DNA-binding behaviors that were confirmed by spectroscopy indicated that 1b could selectively bind and stabilize bcl-2 G-quadruplex DNA to induce apoptosis of A549 cells. Therefore, the synthesized 1b has impressive bcl-2 G-quadruplex DNA-binding and stabilizing activities with potential applications in cancer chemotherapy. View Full-Text
Keywords: arene Ru(II) complexes; microwave-assisted synthesis; apoptosis inducer; selective stabilizing; bcl-2 G-quadruplex DNA arene Ru(II) complexes; microwave-assisted synthesis; apoptosis inducer; selective stabilizing; bcl-2 G-quadruplex DNA
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MDPI and ACS Style

Chen, Y.; Wu, Q.; Wang, X.; Xie, Q.; Tang, Y.; Lan, Y.; Zhang, S.; Mei, W. Microwave-Assisted Synthesis of Arene Ru(II) Complexes Induce Tumor Cell Apoptosis Through Selectively Binding and Stabilizing bcl-2 G-Quadruplex DNA. Materials 2016, 9, 386.

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