Haemolytic properties of some water-soluble para-sulphonato-calix-[n]-arenes.
In this paper, we describe the haemolytic effect of parent para-sulphonato-calix-[n]-arenes and their derivatives bearing one pendant group at the lower rim of calix-arene towards human erythrocytes. A maximum of 30% of haemolysis has been observed for para-sulphonato-calix-[8]-arene for a concentration of 200 mM representing 300 g of calix-arene per liter of human blood, para-sulphonato-calix-[4]-arene and para-sulphonato-calix-[6]-arene show much lower haemolytic effects, 0.5 and 8%, respectively at 200 mM concentration. Coupling of a methoxy-carboxylate function at the phenolic group reduces haemolytic effects in all cases. The presence of an ethoxy-amine function increases the haemolytic behaviour for the calix-[4]-arene and calix-[6]-arene systems, but reduces the effect for the calix-[8]-arene derivatives.
IBCP, CNRS-UMR 5086, 7 Passage du Vercors, Lyon Cedex 07 F69367, France.
Eric
E
Da Silva
Patrick
P
Shahgaldian
Anthony W
AW
Coleman
D001190:Arylsulfonates / Q000737:chemistry / Q000633:toxicity*; D047250:Calixarenes; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000737:chemistry / Q000633:toxicity; D004912:Erythrocytes / Q000187:drug effects*; D006461:Hemolysis / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D046911:Macromolecular Substances; D011083:Polycyclic Compounds / Q000737:chemistry / Q000633:toxicity*; D012995:Solubility; D013329:Structure-Activity Relationship
D001190:Arylsulfonates; D004337:Drug Carriers; D046911:Macromolecular Substances; D011083:Polycyclic Compounds; D047250:Calixarenes