Abstract
AbstractTraditional macrocyclic hosts have finite cavity sizes, generally 5–10 Å, which are commonly adaptive to recognize small guests rather than biological macromolecules. Here two water‐soluble large‐sized quaterphen[n]arenes (WQPns, n=3, 4) were designed and synthesized. These two hosts present significantly distinct recognition abilities. Specifically, they could strongly complex an antimicrobial peptide, pexiganan (PXG) with the association constants (Ka) of (4.20±0.23)×104 M−1 for PXG/WQP3 and (2.46±0.44)×105 M−1 for PXG/WQP4. Complexation of PXG by WQP3 and WQP4 served to decrease the hemolysis of PXG in rabbit red blood cells in a statistically significant way. Furthermore, host–guest complexation was shown to substantially enhance metabolic stability of PXG in presence of proteinase K, rat plasma and liver or kidney homogenates.
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