Journal
ACS APPLIED MATERIALS & INTERFACES
Volume 11, Issue 42, Pages 38497-38502Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsami.9b13492
Keywords
membrane disruption; charge reversal; pillararenes; amphiphiles; anticancer
Funding
- Ministry of Science and Technology of China [2018YFA0208900]
- National Postdoctoral Program for Innovative Talents [BX201600082]
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A charge-reversal amphiphilic pillar[5]arene, P5NH-DCA, bearing 10 charge-reversal headgroups is reported. It targets the cell membrane of cancer cells and selectively destroys the cancer cells by disrupting the membrane. In the acidic tumor microenvironment, the headgroup charge of P5NH-DCA reversed from negative to positive owing to hydrolysis of the acid-labile amide group. The hydrolyzed product bearing multiple positive charges can bind to the cell membrane and then disrupt the membrane of cancer cells with high efficiency. However, under the neutral microenvironment of healthy cells, the negatively charged P5NH-DCA remains stable and the cytotoxicity is considerably reduced. The strategy killing the cancer cells by membrane disruption may represent a new route of cancer chemotherapy.
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