Chimeric analogs of human β-defensin 1 and θ-defensin disrupt pre-established bacterial biofilms. Issue 15 (1st August 2017)

• Record Type: Journal Article
• Authors: Mathew, Basil; Olli, Sudar; Guru, Ankeeta; Nagaraj, Ramakrishanan
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 15(2017)
• Page Start: 3264
• Page End: 3266
• Publication Date: 2017-08-01
• Subjects: Antibiofilm activity -- Defensin analogs -- Enantiomeric peptides; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.06.031
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Antibiofilm activity of several human defensin analogs that have the ability to kill planktonic bacteria, against pre-established biofilms of Escherichia coli MG1655 and Staphylococcus aureus NCTC 8530 were examined. Linear and linear fatty acylated analogs did not show any activity while disulfide constrained analogs disrupted pre-established S. aureus biofilms. Chimeric analogs of human β-defensin 1 and θ-defensin, hBTD-1 and [d ]hBTD-1 were highly active against S. aureus biofilms. Among the analogs tested, only thed -enantiomer [d ]hBTD-1 showed activity against E. coli biofilm. Our study provides insights into the structural requirements for the eradication of pre-established biofilms in defensin analogs.