Super-Cationic Peptide Dendrimers—Synthesis and Evaluation as Antimicrobial Agents
Estelle J. Ramchuran,
Isabel Pérez-Guillén,
Linda A. Bester,
René Khan,
Fernando Albericio,
Miguel Viñas,
Beatriz G. de la Torre
Affiliations
Estelle J. Ramchuran
Biomedical Resource Unit, School of Laboratory Medicine and Medical Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa
Isabel Pérez-Guillén
Lab Molecular Microbiology & Antimicrobials, Department of Pathology and Experimental Therapeutics, Medical School-IDIBELL, University of Barcelona, Hospitalet, 08907 Barcelona, Spain
Linda A. Bester
Biomedical Resource Unit, School of Laboratory Medicine and Medical Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban 4000, South Africa
René Khan
Discipline of Medical Biochemistry, School of Laboratory Medicine and Medical Science, University of KwaZulu-Natal, Durban 4001, South Africa
Fernando Albericio
Peptide Sciences Laboratory, School of Chemistry and Physics, University of KwaZulu-Natal, University Road, Westville, Durban 4001, South Africa
Miguel Viñas
Lab Molecular Microbiology & Antimicrobials, Department of Pathology and Experimental Therapeutics, Medical School-IDIBELL, University of Barcelona, Hospitalet, 08907 Barcelona, Spain
Beatriz G. de la Torre
KRISP, College of Health Sciences, University of KwaZulu-Natal, Westville, Durban 4001, South Africa
Microbial infections are a major public health concern. Antimicrobial peptides (AMPs) have been demonstrated to be a plausible alternative to the current arsenal of drugs that has become inefficient due to multidrug resistance. Herein we describe a new AMP family, namely the super-cationic peptide dendrimers (SCPDs). Although all members of the series exert some antibacterial activity, we propose that special attention should be given to (KLK)2KLLKLL-NH2 (G1KLK-L2KL2), which shows selectivity for Gram-negative bacteria and virtually no cytotoxicity in HepG2 and HEK293. These results reinforce the validity of the SCPD family as a valuable class of AMP and support G1KLK-L2KL2 as a strong lead candidate for the future development of an antibacterial agent against Gram-negative bacteria.