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Complexation of an Antimicrobial Peptide by Large-Sized Macrocycles for Decreasing Hemolysis and Improving Stability.
Chen, Junyi; Meng, Qingbin; Zhang, Yadan; Dong, Ming; Zhao, Liang; Zhang, Yahan; Chen, Longming; Chai, Yao; Meng, Zhao; Wang, Chenhong; Jia, Xueshun; Li, Chunju.
Affiliation
  • Chen J; College of Environmental and Chemical Engineering, Shanghai University, Shanghai, 200444, P. R. China.
  • Meng Q; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Zhang Y; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Dong M; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Zhao L; Key Laboratory of Inorganic-Organic Hybrid Functional Material Chemistry, Ministry of Education, Tianjin Key Laboratory of Structure and Performance for Functional Molecules, College of Chemistry, Tianjin Normal University, Tianjin, 300387, China.
  • Zhang Y; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Chen L; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Chai Y; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Meng Z; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Wang C; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Jia X; State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, P. R. China.
  • Li C; College of Environmental and Chemical Engineering, Shanghai University, Shanghai, 200444, P. R. China.
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 5-10 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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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

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