Biodistribution, Stability, and Blood Distribution of the Cell Penetrating Peptide Maurocalcine in Mice

International Journal of Molecular Sciences

Pascale Perret²  Mitra Ahmadi²  Laurent Riou²  Sandrine Bacot²  Julien Pecher¹  Cathy Poillot²  Alexis Broisat²  Catherine Ghezzi²  Michel De Waard² 

[1] Smartox Biotechnologies, Bâtiment Nanobio, 570 rue de la Chimie, 38400 Saint Martin d’Hères, France;Grenoble Alpes University, 38041 Saint-Martin-d'Hères, France;

关键词: maurocalcine;    cell-penetrating peptide;    in vivo biodistribution;    drug delivery;    blood stability;   

DOI  :  10.3390/ijms161126054

来源: mdpi

【 摘 要 】

Maurocalcine (MCa) is the first natural cell penetrating peptide to be discovered in animal venom. In addition to the fact that it represents a potent vector for the cell penetration of structurally diverse therapeutic compounds, MCa also displays several distinguishing features that make it a potential peptide of choice for clinical and biotechnological applications. The aim of the present study was to gain new information about the properties of MCa in vivo in order to delineate the future potential applications of this vector. For this purpose, two analogues of this peptide with (Tyr-MCa) and without (Lin-Tyr-MCa) disulfide bridges were synthesized, radiolabeled with ¹²⁵I, and their in vitro stabilities were first evaluated in mouse blood. The results indicated that ¹²⁵I-Tyr-MCa was stable in vitro and that the disulfide bridges conferred a competitive advantage for the stability of peptide. Following in vivo injection in mice, ¹²⁵I-Tyr-MCa targeted peripheral organs with interesting quantitative differences and the main route of peptide elimination was renal.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.