Mohan P, Schols D, Baba M, De Clercq E
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois, Chicago 60680.
Antiviral Res. 1992 Jun;18(2):139-50. doi: 10.1016/0166-3542(92)90034-3.
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.
已发现四种磺酸聚合物[聚（4-苯乙烯磺酸）（PSS）、聚（茴香脑磺酸）（PAS）、聚（乙烯磺酸）（PVS）、聚（2-丙烯酰胺-2-甲基-1-丙烷磺酸）（PAMPS）]在对宿主细胞无毒的浓度下可抑制HIV-1和HIV-2在MT-4细胞中的细胞病变效应。磺酸聚合物还抑制了MOLT-4细胞与HIV-1或HIV-2感染的HUT-78细胞共培养中的合胞体形成。它们还抑制抗gp120单克隆抗体与HIV-1 gp120的结合，并阻断HIV-1病毒体对MT-4细胞的吸附。PSS和PAS，但不是PVS和PAMPS，干扰了OKT4A/Leu3a与CD4受体的结合。这些聚阴离子化合物的抗HIV活性可归因于对gp120-CD4相互作用的抑制。磺酸聚合物代表了一类抗HIV化合物，值得进一步评估其治疗潜力。
