SULFONIC-ACID POLYMERS AS A NEW CLASS OF HUMAN-IMMUNODEFICIENCY-VIRUS INHIBITORS
SULFONIC-ACID POLYMERS AS A NEW CLASS OF HUMAN-IMMUNODEFICIENCY-VIRUS INHIBITORS
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DOI：
10.1016/0166-3542(92)90034-3
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发表时间：
1992-06-01
影响因子：
7.6
通讯作者：
DECLERCQ, E
中科院分区：
文献类型：
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作者：
MOHAN, P;SCHOLS, D;DECLERCQ, E
已发现四种磺酸聚合物[聚(4-苯乙烯磺酸)(PSS)、聚茴香酚磺酸(PAS)、聚(乙烯基磺酸)(PVS)、聚(2-丙烯酰胺-2-甲基-1-丙磺酸)(PAMPS)]在对宿主细胞无毒性的浓度下可抑制HIV-1和HIV-2在MT-4细胞中的细胞病变。磺酸聚合物还抑制了MOLT-4细胞与HIV-1或HIV-2感染的HUT-78细胞共培养中合胞体的形成。它们还抑制了抗gp120单抗与HIV-1 gp120的结合，并阻断了HIV-1病毒粒子对MT-4细胞的吸附。PSS和PAS，而不是PVS和PAMPS，干扰OKT4A/Leu3a与CD4受体的结合。这些多阴离子化合物的抗HIV活性可以归因于抑制gp120-CD4相互作用。磺酸聚合物是一种领先的抗艾滋病毒化合物，值得进一步评估其治疗潜力。
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.