【摘要】 研究了具有抗HIV 1活性的大环多胺类化合物与RNA的识别作用 ,以及其对cos 7细胞凋亡的影响 ,以进一步探讨其抗HIV 1的作用机理 .实验采用琼脂糖凝胶电泳方法 ,观察化合物与RNA的识别作用 ;通过流式细胞计数法探讨其对cos 7细胞凋亡的影响 ;运用计算机分子模型 ,从理论上Docking计算化合物与TARRNA结合的可能性 .结果表明 ,大环多胺类化合物MP 1、MP 2和MP 3不仅具有断裂RNA的作用 ,并可抑制Tat RNA的相互作用 ,还可影响cos 7细胞亚二倍体的含量 ;理论化学计算数据与实验结果基本一致 .这一结果提示化合物的抗HIV 1活性可能通过作用于病毒基因组RNA而发挥作用 ,是多靶作用的结果 .更多还原

【Abstract】 The molecular recognition of macrocyclic polyamines (MP 1,MP 2 and MP 3) to RNA, and its effects on apoptosis of cos 7 cells were studied in order to explore their mechanism of anti HIV 1 activity. Cleavage of RNA was observed by agarose electrophoresis; and apoptosis was determined by flow cytometry assay. Computer modeling was used to investigate the theoretical possibility of compounds binding to TAR RNA. Results showed that: (1) Compounds MP 1,MP 2 and MP 3 could not only cleave the polyA·polyU and TAR RNA, but also inhibit the interaction of Tat RNA. (2) Compounds could affect the percentage of hypodiploid cell. It is proposed that compounds MP 1,MP 2 and MP 3 could recognize the polyA·polyU and TAR RNA molecules and cleave them, and affect the interaction of Tat RNA. The compounds may affect the apoptosis of cos 7 cells.更多还原