SULFONIC-ACID POLYMERS AS A NEW CLASS OF HUMAN-IMMUNODEFICIENCY-VIRUS INHIBITORS

被引:63
作者
MOHAN, P
SCHOLS, D
BABA, M
DECLERCQ, E
机构
[1] FUKUSHIMA MED SCH, DEPT MICROBIOL, FUKUSHIMA 960, JAPAN
[2] KATHOLIEKE UNIV LEUVEN, REGA INST MED RES, LOUVAIN, BELGIUM
关键词
SULFONIC ACID POLYMER; HUMAN IMMUNODEFICIENCY VIRUS; GLYCOPROTEIN-GP120; CD4-RECEPTOR; SYNCYTIUM FORMATION;
D O I
10.1016/0166-3542(92)90034-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Four sulfonic acid polymers [poly(4-styrenesulfonic acid)(PSS), poly(anetholesulfonic acid)(PAS), poly(vinylsulfonic acid)(PVS), poly(2-acrylamido-2-methyl-1-propanesulfonic acid)(PAMPS)] have been found to inhibit the cytopathicity of HIV-1 and HIV-2 in MT-4 cells at concentrations that are not toxic to the host cells. The sulfonic acid polymers also inhibited syncytium formation in co-cultures of MOLT-4 cells with HIV-1- or HIV-2-infected HUT-78 cells. They also inhibited binding of anti-gp120 mAb to HIV-1 gp120 and blocked adsorption of HIV-1 virions to MT-4 cells. PSS and PAS, but not PVS and PAMPS, interfered with the binding of OKT4A/Leu3a to the CD4 receptor. The anti-HIV activity of these polyanionic compounds can be ascribed to inhibition of the gp120-CD4 interaction. Sulfonic acid polymers represent a lead of anti-HIV compounds that warrant further evaluation of their therapeutic potential.
引用
收藏
页码:139 / 150
页数:12
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