Holland L E, Buthod J L, Kowal C D, Antonucci T K
Life Sciences Research Dept., I.I.T. Research Institute, Chicago, IL 60616.
AIDS Res Hum Retroviruses. 1992 Sep;8(9):1717-22. doi: 10.1089/aid.1992.8.1717.
The historical antisyphilis drug oxyphenarsine has been tested for antiviral activity and for cytotoxicity to characterize it as a potential therapy for treatment of HIV infections. These data show that the compound demonstrates marginal antiviral activity against the HTLV-IIIB strain of HIV-1, two clinical isolates of HIV-1 (one sensitive to AZT and one resistant), and the MS strain of HIV-2. However, treatment with concentrations of oxyphenarsine showing optimal anti-HIV activity resulted in significant cytotoxicity. The drug's selectivity index was not significantly improved when tested against H9 cells chronically infected with the HTLV-IIIB strain of HIV-1. Thus, despite a previous report suggesting significant antiviral activity and low cytotoxicity for oxyphenarsine, the data presented here do not provide support for further development of this drug as an anti-HIV agent.
历史上的抗梅毒药物氧苯胂已进行了抗病毒活性和细胞毒性测试,以确定其作为治疗HIV感染的潜在疗法的特性。这些数据表明,该化合物对HIV-1的HTLV-IIIB株、两种HIV-1临床分离株(一种对AZT敏感,一种耐药)以及HIV-2的MS株表现出微弱的抗病毒活性。然而,用显示出最佳抗HIV活性的氧苯胂浓度进行治疗会导致显著的细胞毒性。当针对长期感染HIV-1的HTLV-IIIB株的H9细胞进行测试时,该药物的选择性指数没有显著提高。因此,尽管先前有报告表明氧苯胂具有显著的抗病毒活性和低细胞毒性,但此处提供的数据并不支持将该药物进一步开发为抗HIV药物。