Abstract

The interaction between cucurbit[8]uril (Q[8]) and chloramphenicol (CPE) was investigated using single-crystal X-ray diffraction, spectroscopy, isothermal titration calorimetry (ITC) and UV-Vis, NMR and IR spectroscopy. The effects of Q[8] on the stability, in vitro release performance and antibacterial activity of CPE were also studied. The results showed that CPE and Q[8] formed a 1:1 inclusion complex (CPE@Q[8]) with an inclusion constant of 5.4736 × 105 L/mol. The intervention of Q[8] did not affect the stability of CPE, but obviously reduced the release rate of CPE in artificial gastric and intestinal juice; Q[8] has a slow-release effect on CPE. The antibacterial results showed that the minimum inhibitory concentration (MIC) of CPE and CPE@Q[8] toward Escherichia coli (E. coli) was 1.5 × 10–3 and 1.0 × 10–3 mol/L, respectively, and toward Staphylococcus aureus (SA), the MIC was 2.0 × 10–3 mol/L for both CPE and CPE@Q[8]. Therefore, Q[8] enhanced the inhibitory activity of CPE against E. coli.

Keywords:  Chloramphenicol, cucurbit[8]uril, host-guest interaction, stability, in vitro cumulative release, antibacterial activity.

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Zhang, L.; Zheng, J.; Luo, G.; Li, X.; Zhang, Y.; Tao, Z.; Zhang, Q. Beilstein Arch. 2021, 202162. doi:10.3762/bxiv.2021.62.v1

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