期刊
ACS APPLIED MATERIALS & INTERFACES
卷 7, 期 18, 页码 9784-9791出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsami.5b01665
关键词
perylene bisimide; DNA intercalator; cell imaging; nucleic accumulation; anticancer activity; planar aromatic nanoscaffold
资金
- National Natural Science Foundation of China [21174012, 51103008, 51221002]
- 973 Program [2013CB127603]
- Project for Extramural Scientists of State Key Laboratory of Agro-biotechnology [2015SKLAB6-22]
- Beijing Natural Science Foundation [2142026]
The molecular properties concerning size, shape, and electric charges of the planar aromatic DNA intercalators are still poorly understood. Herein, a series of water-soluble perylene bisimide (PBI) derivatives containing a rigid and planar aromatic nanoscaffold with different size, shape, and electric charges were synthesized. Using histochemistry and cell viability assays on animal tissues and cancer cells, we revealed the molecular properties required for successful DNA intercalators to localize in cell nuclei and inhibit cancer cells. Small molecular size and the strong polarity of hydrophilic substituents are prerequisites for PBI-based DNA intercalators. A large number of charges facilitate the nucleic accumulation of these DNA intercalators, while fewer charges and planar aromatic nanoscaffold more efficiently inhibit cancer cell growth.
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