CERULENIN AND ZN--HIV-REPLICATION INHIBITORS AS ANTIVIRAL AGENTS

浅蓝素和 ZN--HIV 复制抑制剂作为抗病毒剂

• 批准号: 5200825
• 负责人: M P SELVAM
• 金额: --
• 依托单位: BUREAU OF HEALTH PLANNING AND RESOURCES DEVELOPMENT
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/5200825
• 关键词: antiAIDS agent; antifungal antibiotics; antiviral agents; biological products; combination chemotherapy; divalent cations; dosage; drug screening /evaluation; human immunodeficiency virus 1; human tissue; immunopharmacology; lymphocyte; protease inhibitor; tissue /cell culture; virus replication; zinc

The HIV-proteinase is essential for the proteolytic processing of the viral gag and gag-pol precursor proteins. This has been shown to be structurally and functionally related to aspartyl proteinases. We have studied the inhibition of HIV-replication in lymphocyte cell culture by Cerulenin, a naturally occurring antifungal antibiotic, as well as by Zn2+. We report here for the first time that the combination of Cerulenin and Zn2+ in proper modality, inhibits HIV-replication in C-8166-45 transformed human umbilical cord blood lymphocytes 90%, which is comparable to the potency of inhibition by AZT. We have studied the inhibition of HIV replication by Cerulenin and Zn2+ individually also, in the culture which has very limited activity and toxic too at higher dosages.

HIV 蛋白酶对于 HIV 的蛋白水解过程至关重要 病毒 gag 和 gag-pol 前体蛋白。这已被证明是 在结构和功能上与天冬氨酰蛋白酶相关。我们有 研究了淋巴细胞培养物中 HIV 复制的抑制 Cerulenin，一种天然存在的抗真菌抗生素，以及 锌2+。我们在这里首次报道 Cerulenin 的组合 和 Zn2+ 以适当的方式抑制 C-8166-45 中的 HIV 复制 转化人脐带血淋巴细胞90%，即 与 AZT 的抑制效力相当。我们研究了 Cerulenin 和 Zn2+ 还分别抑制 HIV 复制， 在活性非常有限且在较高浓度下也有毒的培养物中 剂量。