Space-filling effects in membrane disruption by cationic amphiphiles.
We studied the hemolytic activity towards bovine erythrocytes of novel synthetic steroid-polyamine conjugates consisting of a rigid hydrophobic steroid unit, and a flexible hydrophilic polyamine unit connected by a linker. The steroid structure, polyamine chain length, and the presence of a hydrophobic substituent on the steroid, all influenced the activity. Analysis of the time dependence of hemolysis suggested that these structurally related cationic amphiphiles have different mechanisms of membrane perturbation.
Fujiwara
T
T
Faculty of Pharmaceutical Sciences, Nagoya City University, Nagoya, Japan.
Hirashima
N
N
Hasegawa
S
S
Nakanishi
M
M
Ohwada
T
T
D000465:Algorithms; D000818:Animals; D002417:Cattle; D004337:Drug Carriers; D004910:Erythrocyte Membrane / Q000737:chemistry / Q000187:drug effects; D004912:Erythrocytes / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects*; D066298:In Vitro Techniques; D008081:Liposomes; D014677:Pharmaceutical Vehicles; D011073:Polyamines / Q000138:chemical synthesis* / Q000494:pharmacology; D013256:Steroids / Q000138:chemical synthesis* / Q000494:pharmacology; D014162:Transfection
D004337:Drug Carriers; D008081:Liposomes; D014677:Pharmaceutical Vehicles; D011073:Polyamines; D013256:Steroids