title: Photosensitizer binding to lipid bilayers as a precondition for the photoinactivation of membrane channels.
abstract: The photodynamic activity of sulfonated aluminum phthalocyanines (AlPcS(n), 1 </= n </= 4) was found to correlate with their affinity for membrane lipids. Adsorbing to the surface of large unilamellar vesicles (LUVs), aluminum phthalocyanine disulfonate induced the highest changes in their electrophoretic mobility. AlPcS(2) was also most efficient in mediating photoinactivation of gramicidin channels, as revealed by measurements of the electric current across planar lipid bilayers. The increase in the degree of sulfonation of phthalocyanine progressively reduced its affinity for the lipid bilayer as well as its potency of sensitizing gramicidin channel photoinactivation. The portion of photoinactivated gramicidin channels, alpha, increased with rising photosensitizer concentration up to some optimum. The concentration at which alpha was at half-maximum amounted to 80 nM, 30 nM, 200 nM, and 2 microM for AlPcS(1), AlPcS(2), AlPcS(3), and AlPcS(4), respectively. At high concentrations alpha was found to decrease, which was attributed to quenching of reactive oxygen species and self-quenching of the photosensitizer triplet state by its ground state. Fluoride anions were observed to inhibit both AlPcS(n) (2 </= n </= 4) binding to LUVs and sensitized photoinactivation of gramicidin channels. It is concluded that photosensitizer binding to membrane lipids is a prerequisite for the photodynamic inactivation of gramicidin channels.
authors.affiliation: A. N. Belozersky Institute of Physico-Chemical Biology, Moscow State University, Moscow 119899, Russia.
authors.forename: T I
authors.initials: TI
authors.lastname: Rokitskaya
authors.forename: M
authors.initials: M
authors.lastname: Block
authors.forename: Y N
authors.initials: YN
authors.lastname: Antonenko
authors.forename: E A
authors.initials: EA
authors.lastname: Kotova
authors.forename: P
authors.initials: P
authors.lastname: Pohl
mesh_terms: D001665:Binding Sites; D055592:Biophysical Phenomena; D001703:Biophysics; D006096:Gramicidin / Q000737:chemistry; D066298:In Vitro Techniques; D007211:Indoles; D007473:Ion Channels / Q000737:chemistry / Q000187:drug effects / Q000528:radiation effects; D008051:Lipid Bilayers / Q000737:chemistry*; D009942:Organometallic Compounds; D018462:Photobiology; D017319:Photosensitizing Agents / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D007211:Indoles; D007473:Ion Channels; D008051:Lipid Bilayers; D009942:Organometallic Compounds; D017319:Photosensitizing Agents; D006096:Gramicidin; C060570:aluminum phthalocyanine