抗HIV—1活性的大环多胺类化合物与RNA的识别作用及其对细胞凋亡的影响

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TAR RNA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。

Molecular Mechanism of Macrocyclic Polyamines with Anti-HIV-1 Activity to Recognize RNA and Its Effect on Apoptosis

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 stu died in order to explore their mechanism of anti-HIV-1 activity. Cleavage of R NA was observed by agarose electrophoresis; and apoptosis was determined by flow cytometry assay. Computer modeling was used to investigate the theoretical poss ibility 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 al so inhibit the interaction of Tat-RNA. (2) Compounds could affect the percentag e of hypodiploid cell. It is proposed that compounds MP-1,MP-2 and MP-3 cou ld 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 ce lls.