title: Characterisation of the membrane affinity of an isoniazide peptide conjugate by tensiometry, atomic force microscopy and sum-frequency vibrational spectroscopy, using a phospholipid Langmuir monolayer model.
abstract: Tensiometry, sum-frequency vibrational spectroscopy, and atomic force microscopy were employed to assess the cell penetration ability of a peptide conjugate of the antituberculotic agent isoniazide. Isoniazide was conjugated to peptide (91)SEFAYGSFVRTVSLPV(106), a functional T-cell epitope of the immunodominant 16 kDa protein of Mycobacterium tuberculosis. As a simple but versatile model of the cell membrane a phospholipid Langmuir monolayer at the liquid/air interface was used. Changes induced in the structure of the phospholipid monolayer by injection of the peptide conjugate into the subphase were followed by tensiometry and sum-frequency vibrational spectroscopy. The drug penetrated lipid films were transferred to a solid support by the Langmuir-Blodgett technique, and their structures were characterized by atomic force microscopy. Peptide conjugation was found to strongly enhance the cell penetration ability of isoniazide.
authors.affiliation: Laboratory of Interfaces and Nanostructures, Institute of Chemistry, Eötvös Loránd University, P.O. Box 32, Budapest 112, H-1518, Hungary.
authors.forename: Katalin
authors.initials: K
authors.lastname: Hill
authors.forename: Csanád Botond
authors.initials: CB
authors.lastname: Pénzes
authors.forename: Donát
authors.initials: D
authors.lastname: Schnöller
authors.forename: Kata
authors.initials: K
authors.lastname: Horváti
authors.forename: Szilvia
authors.initials: S
authors.lastname: Bosze
authors.forename: Ferenc
authors.initials: F
authors.lastname: Hudecz
authors.forename: Tamás
authors.initials: T
authors.lastname: Keszthelyi
authors.forename: Eva
authors.initials: E
authors.lastname: Kiss
mesh_terms: D000595:Amino Acid Sequence; D000995:Antitubercular Agents / Q000737:chemistry* / Q000493:pharmacokinetics; D001426:Bacterial Proteins / Q000737:chemistry*; D002463:Cell Membrane Permeability; D018984:Epitopes, T-Lymphocyte / Q000737:chemistry; D006801:Humans; D007538:Isoniazid / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D008567:Membranes, Artificial; D018625:Microscopy, Atomic Force; D008969:Molecular Sequence Data; D009169:Mycobacterium tuberculosis / Q000737:chemistry*; D010455:Peptides / Q000737:chemistry* / Q000493:pharmacokinetics; D010743:Phospholipids / Q000378:metabolism*; D013057:Spectrum Analysis; D014376:Tuberculosis / Q000188:drug therapy
chemical_list: D000995:Antitubercular Agents; D001426:Bacterial Proteins; D018984:Epitopes, T-Lymphocyte; D008567:Membranes, Artificial; D010455:Peptides; D010743:Phospholipids; D007538:Isoniazid