Studies on the haemolytic action of amphiphilic substances in vitro: Inhibition by O-(β-hydroxyethyl)-rutosides

Abstract

the water soluble rutin derivative O-(β-hydroxyethyl)rutosides (HR) † was found to inhibit the haemolytic action of a variety of amphiphilic substances on human red blood cells, without causing haemolysis by itself. the effect of HR on haemolysis caused by aescin, digitonin, cetyltrimethyl-ammonium bromide, sodium dodecyl sulfate, polidocanol, sodium deoxycholate, chiorpromazine, promethazine, and thiazinamium was investigated in vitro. The antihaemolytic potency of HR was detennined for each haemolysin and expressed as the AH 50, which is the concentration necessary to reduce 50 per cent haemolysis to 25 per cent. the biphasic behavior of the unsperific haemolysins in hypotonic buffer solution was studied in the presence and absence of 2 × 10 −2 M HR. Both the stabilizing and the destabilizing part of the curve were shifted to higher concentrations, with the exception of sodium deoxycholate, where only the destabilizing part was affected. Two possible mechanisms are discussed: (1) the unspecific, hydrophobic interaction of HR with the single haemolysins resulting in complex formation, and (2) the protection of the membrane by competition of the inhibitor with the haemolysin for the binding site.