通过荷电反转两亲性杯[5]芳烃靶向细胞膜实现选择性杀伤癌细胞。
Targeting the Cell Membrane by Charge-Reversal Amphiphilic Pillar[5]arene for the Selective Killing of Cancer Cells.
机构信息
Key Lab of Organic Optoelectronics & Molecular Engineering, Department of Chemistry , Tsinghua University , Beijing 100084 , China.
Department of Chemistry , Fudan University , Shanghai 200438 , China.
出版信息
ACS Appl Mater Interfaces. 2019 Oct 23;11(42):38497-38502. doi: 10.1021/acsami.9b13492. Epub 2019 Oct 8.
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.
报告了一种带有 10 个电荷反转头基的荷电反转两亲性柱[5]芳烃 P5NH-DCA。它靶向癌细胞的细胞膜，并通过破坏细胞膜选择性地摧毁癌细胞。在酸性肿瘤微环境中，由于酸不稳定酰胺基团的水解，P5NH-DCA 的头基电荷从负变为正。带多个正电荷的水解产物可以与细胞膜结合，然后有效地破坏癌细胞的膜。然而，在健康细胞的中性微环境中，带负电荷的 P5NH-DCA 保持稳定，细胞毒性大大降低。通过破坏细胞膜杀死癌细胞的策略可能代表癌症化疗的新途径。
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