| Title |
Anticancer activities of self-assembled molecular bowls containing a phenanthrene-based donor and Ru(II) acceptors
|
|---|---|
| Published in |
International Journal of Nanomedicine, August 2015
|
| DOI | 10.2147/ijn.s88287 |
| Pubmed ID | |
| Authors |
Seong Soo An, Ki-Whan Chi, Inhye Kim, Young Ho Song, Nem Singh, Yong Joon Jeong, Jung Eun Kwon, Hyunuk Kim, Young Cho, Chan Kang |
| Abstract |
Nano-sized multinuclear ruthenium complexes have rapidly emerged as promising therapeutic candidates with unique anticancer activities. Here, we describe the coordination-driven self-assembly and anticancer activities of a set of three organometallic tetranuclear Ru(II) molecular bowls. [2+2] Coordination-driven self-assembly of 3, 6-bis(pyridin-3- ylethynyl) phenanthrene (bpep) (1) and one of the three dinuclear arene ruthenium clips, [(η6-p-iPrC6H4Me)2Ru2-(OO\OO)][OTf]2 (OO\OO =2, 5-dioxido-1, 4-benzoquinonato, OTf = triflate) (2), 5, 8-dioxido-1, 4-naphthoquinonato (3), or 6, 11-dioxido-5, 12-naphthacenediona (4), resulted in three molecular bowls 5-7 of general formula [{(η6-p-iPrC6H4Me)2Ru2-(OO\OO)}2(bpep)2][OTf]4. All molecular bowls were obtained as triflate salts in very good yields (>90%) and were fully characterized using multinuclear nuclear magnetic resonance (NMR), electrospray ionization-mass spectrometry (ESI-MS), and elemental analysis. The structure of the representative molecular bowl 5 was confirmed by single-crystal X-ray diffraction analysis. The anticancer activities of molecular bowls 5-7 were determined by 3-[4, 5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide, autophagy, and Western blot analysis. Bowl 6 showed the strongest cytotoxicity in AGS human gastric carcinoma cells and was more cytotoxic than doxorubicin. In addition, autophagic activity and the ratio of apoptotic cell death increased in AGS cells by treatment with bowl 6. Bowl 6 also induced autophagosome formation via upregulation of p62 and promotion of the conversion of LC3-I to LC3-II. Moreover, bowl 6 promoted apoptotic cell death through downregulation of Akt/mTOR activation, followed by increased caspase-3 activity. These results suggest that bowl 6 induces gastric cancer cell death via modulation of autophagy and apoptosis. Bowl 6 is a potent anticancer agent and a potential treatment for human gastric cancer that merits further study. |
X Demographics
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Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 23 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 23 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 7 | 30% |
| Student > Master | 4 | 17% |
| Researcher | 3 | 13% |
| Other | 2 | 9% |
| Student > Bachelor | 1 | 4% |
| Other | 4 | 17% |
| Unknown | 2 | 9% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 8 | 35% |
| Biochemistry, Genetics and Molecular Biology | 5 | 22% |
| Pharmacology, Toxicology and Pharmaceutical Science | 3 | 13% |
| Agricultural and Biological Sciences | 1 | 4% |
| Chemical Engineering | 1 | 4% |
| Other | 2 | 9% |
| Unknown | 3 | 13% |
Attention Score in Context
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#22,760,732
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Outputs from International Journal of Nanomedicine
#3,598
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Outputs of similar age from International Journal of Nanomedicine
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