TY - JOUR
T1 - Effect of phloretin on the permeability of thin lipid membranes
AU - Andersen, Olaf Sparre
AU - Finkelstein, Alan
AU - Katz, Ira
AU - Cass, Albert
PY - 1976/6/1
Y1 - 1976/6/1
N2 - Phloretin dramatically increases cation conductances and decreases anion conductances of membranes treated with ion carriers (nonactin, valinomycin, carbonyl-cyanide-m-chiorophenylhydrazone [CCCP], and Hg(C6F5)2) or lipophilic ions (tetraphenylarsonium [TPhAs+] and tetraphenylborate [TPhB−]). For example, on phosphatidylethanolamine membranes, 10-4 M phloretin increases K+-nonactin and TPhAs+ conductances and decreases CCCP− and TPhB− conductances 103-fold; on lecithin: cholesterol membranes, it increases K+-nonactin conductance 1on-fold and decreases CCCP− conductance 103-fold. Similar effects are obtained with p- and m-nitrophenol at 10-2 M. These effects are produced by the un-ionized form of phioretin and the nitrophenols. We believe that phloretin, which possesses a large dipole moment, adsorbs and orients at the membrane surface to introduce a dipole potential of opposite polarity to the preexisting positive one, thus increasing the partition coefficient of cations into the membrane interior and decreasing the partition coefficient of anions. (Phloretin may also increase the fluidity of cholesterol-containing membranes; this is manifested by its two- to threefold increase in nonelectrolyte permeability and its asymmetrical effect on cation and anion conductances in cholesterol-containing membranes.) It is possible that phloretin’s inhibition of chloride, urea, and glucose transport in biological membranes results from the effects of these intense interfacial dipole fields on the translocator(s) of these molecules.
AB - Phloretin dramatically increases cation conductances and decreases anion conductances of membranes treated with ion carriers (nonactin, valinomycin, carbonyl-cyanide-m-chiorophenylhydrazone [CCCP], and Hg(C6F5)2) or lipophilic ions (tetraphenylarsonium [TPhAs+] and tetraphenylborate [TPhB−]). For example, on phosphatidylethanolamine membranes, 10-4 M phloretin increases K+-nonactin and TPhAs+ conductances and decreases CCCP− and TPhB− conductances 103-fold; on lecithin: cholesterol membranes, it increases K+-nonactin conductance 1on-fold and decreases CCCP− conductance 103-fold. Similar effects are obtained with p- and m-nitrophenol at 10-2 M. These effects are produced by the un-ionized form of phioretin and the nitrophenols. We believe that phloretin, which possesses a large dipole moment, adsorbs and orients at the membrane surface to introduce a dipole potential of opposite polarity to the preexisting positive one, thus increasing the partition coefficient of cations into the membrane interior and decreasing the partition coefficient of anions. (Phloretin may also increase the fluidity of cholesterol-containing membranes; this is manifested by its two- to threefold increase in nonelectrolyte permeability and its asymmetrical effect on cation and anion conductances in cholesterol-containing membranes.) It is possible that phloretin’s inhibition of chloride, urea, and glucose transport in biological membranes results from the effects of these intense interfacial dipole fields on the translocator(s) of these molecules.
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U2 - 10.1085/jgp.67.6.749
DO - 10.1085/jgp.67.6.749
M3 - Article
C2 - 946975
AN - SCOPUS:0017161652
SN - 0022-1295
VL - 67
SP - 749
EP - 771
JO - Journal of General Physiology
JF - Journal of General Physiology
IS - 6
ER -