Haemolytic properties of some water-soluble para-sulphonato-calix-[n]-arenes

被引：87

作者：

Da Silva, E ^{[1
]}

Shahgaldian, P ^{[1
]}

Coleman, AW ^{[1
]}

机构：

[1] CNRS, IBCP, UMR 5086, F-69367 Lyon 07, France

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2004年 / 273卷 / 1-2期

关键词：

water-soluble macrocycle; erythrocyte; haemolytic; para-sulphonato-calix-arene;

D O I：

10.1016/j.ijpharm.2003.12.008

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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. (C) 2004 Elsevier B.V. All rights reserved.

引用

页码：57 / 62

页数：6

共 33 条

[1] Complexation of native L-α-aminoacids by water soluble calix[4]arenes [J].