title: Conjugation of Kahalalide F with gold nanoparticles to enhance in vitro antitumoral activity.
abstract: Two Cys-containing analogues of the anticancer drug Kahalalide F are synthesized and conjugated to 20 and 40 nm gold nanoparticles (GNPs). The resulting complexes are characterized by different analytical techniques to confirm the attachment of peptide to the GNPs. The self-assembly capacity of a peptide dramatically influences the final ratio number of molecules per nanoparticle, saturating the nanoparticle surface and prompting multilayered capping on the surface. In such way, the nanoparticle could act as a concentrator for the delivery of drugs, thereby increasing bioactivity. The GNP sizes and the conjugation have influence on the biological activities. Kahalalide F analogues conjugated with GNPs are located subcellularly at lysosome-like bodies, which may be related to the action mechanism of Kahalalide F. The results suggest that the selective delivery and activity of Kahalalide F analogues can be improved by conjugating the peptides to GNPs.
authors.affiliation: Institute for Research in Biomedicine, CIBER-BBN, Networking Centre on Bioengineering, Biomaterials and Nanomedicine, Institute for Bioengineering of Catalonia, Spain.
authors.forename: Leticia
authors.initials: L
authors.lastname: Hosta
authors.forename: Mateu
authors.initials: M
authors.lastname: Pla-Roca
authors.forename: Jordi
authors.initials: J
authors.lastname: Arbiol
authors.forename: Carmen
authors.initials: C
authors.lastname: López-Iglesias
authors.forename: Josep
authors.initials: J
authors.lastname: Samitier
authors.forename: Luis J
authors.initials: LJ
authors.lastname: Cruz
authors.forename: Marcelo J
authors.initials: MJ
authors.lastname: Kogan
authors.forename: Fernando
authors.initials: F
authors.lastname: Albericio
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry*; D002478:Cells, Cultured; D047630:Depsipeptides / Q000008:administration & dosage* / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D006046:Gold; D006801:Humans; D008247:Lysosomes / Q000378:metabolism; D053768:Metal Nanoparticles / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D047630:Depsipeptides; D004337:Drug Carriers; D006046:Gold; C097897:kahalalide F