title: Rapid entry of bitter and sweet tastants into liposomes and taste cells: implications for signal transduction.
abstract: Some amphipathic bitter tastants and non-sugar sweeteners are direct activators of G proteins and stimulate transduction pathways in cells not related to taste. We demonstrate that the amphipathic bitter tastants quinine and cyclo(Leu-Trp) and the non-sugar sweetener saccharin translocate rapidly through multilamellar liposomes. Furthermore, when rat circumvallate (CV) taste buds were incubated with the above tastants for 30 s, their intracellular concentrations increased by 3.5- to 7-fold relative to their extracellular concentrations. The time course of this dramatic accumulation was also monitored in situ in rat single CV taste buds under a confocal laser-scanning microscope. Tastants were clearly localized to the taste cell cytosol. It is proposed that, due to their rapid permeation into taste cells, these amphipathic tastants may be available for activation of signal transduction components (e. g., G proteins) directly within the time course of taste sensation. Such activation may occur in addition to the action of these tastants on putative G protein-coupled receptors. This phenomenon may be related to the slow taste onset and lingering aftertaste typically produced by many bitter tastants and non-sugar sweeteners.
authors.affiliation: Institute of Biochemistry, Food Science, and Nutrition, Rehovot 76-100, Israel.
authors.forename: I
authors.initials: I
authors.lastname: Peri
authors.forename: H
authors.initials: H
authors.lastname: Mamrud-Brains
authors.forename: S
authors.initials: S
authors.lastname: Rodin
authors.forename: V
authors.initials: V
authors.lastname: Krizhanovsky
authors.forename: Y
authors.initials: Y
authors.lastname: Shai
authors.forename: S
authors.initials: S
authors.lastname: Nir
authors.forename: M
authors.initials: M
authors.lastname: Naim
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000493:pharmacokinetics; D001692:Biological Transport / Q000502:physiology; D002628:Chemoreceptor Cells / Q000502:physiology*; D004058:Diffusion; D004847:Epithelial Cells / Q000378:metabolism; D005456:Fluorescent Dyes; D019204:GTP-Binding Proteins / Q000378:metabolism; D008081:Liposomes / Q000378:metabolism*; D008297:Male; D008565:Membrane Proteins / Q000378:metabolism; D010879:Piperazines / Q000493:pharmacokinetics; D011803:Quinine / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D011956:Receptors, Cell Surface; D012439:Saccharin / Q000493:pharmacokinetics; D015398:Signal Transduction / Q000502:physiology*; D013649:Taste / Q000502:physiology*
chemical_list: D000962:Antimalarials; D005456:Fluorescent Dyes; D008081:Liposomes; D008565:Membrane Proteins; D010879:Piperazines; D011956:Receptors, Cell Surface; C032323:cyclo(L-leucyl-L-tryptophyl); D011803:Quinine; D019204:GTP-Binding Proteins; D012439:Saccharin