Complexation of an Antimicrobial Peptide by Large-Sized Macrocycles for Decreasing Hemolysis and Improving Stability.
Angew Chem Int Ed Engl
; 60(20): 11288-11293, 2021 05 10.
Article
in En
| MEDLINE
| ID: mdl-33709627
Traditional macrocyclic hosts have finite cavity sizes, generally 5-10â
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 â
M-1 for PXG/WQP3 and (2.46±0.44)×105 â
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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Antimicrobial Cationic Peptides
/
Macrocyclic Compounds
/
Calixarenes
Language:
En
Journal:
Angew Chem Int Ed Engl
Year:
2021
Document type:
Article
Country of publication:
Germany