Conjugation of Kahalalide F with Gold Nanoparticles to Enhance in Vitro Antitumoral Activity

Leticia Hosta Rigau, Mateu Pla-Roca, Jordi Arbiol, Carmen Lopez-Iglesias, Josep Samitier, Luis J. Cruz, Marcelo J. Kogan, Fernando Albericio

Research output: Contribution to journalJournal articleResearchpeer-review


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.
Original languageEnglish
JournalBioconjugate Chemistry
Issue number1
Pages (from-to)138-146
Number of pages9
Publication statusPublished - 2009
Externally publishedYes


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