A novel fluorescent indicator displacement assay for sensing the anticancer drug gefitinib

作者：Xi, Yun-Yun; Tang, Qing; Huang, Ying^*; Tao, Zhu; Xue, Sai-Feng; Zhou, Qingdi; Wei, Gang^*

来源：Supramolecular Chemistry, 2017, 29(3): 229-235.

DOI：10.1080/10610278.2016.1202413

• Cucurbit[8]uril
• cell imaging
• fluorescent indicator displacement assay
• gefitinib

Fluorescent indicator displacement assays have become popular for converting synthetic receptors into optical sensors. We have now shown that a 1: 2 host-guest complex between cucurbit[8]uril (Q[8]) and proflavine (PF) can be used as a fluorescent indicator for sensing the anticancer drug gefitinib. The 2PF@Q[8] complex can be used to detect gefitinib with high selectivity using fluorescence spectrometry with a detection limit of 6.63 x 10(-8) mol(-L). The proposed sensing mechanism was investigated using H-1 nuclear magnetic resonance spectroscopy (H-1 NMR), isothermal titration calorimetry and electrospray ionisation mass spectrometry. The 2PF@Q[8] complex was shown to be suitable for imaging gefitinib in prostate cancer (PC3) cells, which may help to elucidate relevant biological processes at the molecular level. We have developed a novel F-IDA to detect the anticancer drug GEF with high selectivity. The new indicator has excellent selectivity and a low detection limit for GEF. We have also demonstrated that the F-IDA can be used for the practical determination of drugs in living cells.

• 出版日期2017
• 单位贵州大学; CSIRO