生物化学与生物物理进展
生物化學與生物物理進展
생물화학여생물물리진전
PROGRESS IN BIOCHEMISTRY AND BIOPHYSICS
2002年
2期
211-216
,共6页
HIV-1%大环多胺%凋亡%Docking
HIV-1%大環多胺%凋亡%Docking
HIV-1%대배다알%조망%Docking
HIV-1%macrocyclic polyamines%apoptosis%docking
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.
研究瞭具有抗HIV-1活性的大環多胺類化閤物與RNA的識彆作用,以及其對 cos-7細胞凋亡的影響,以進一步探討其抗HIV-1的作用機理.實驗採用瓊脂糖凝膠電泳方法, 觀察化閤物與RNA的識彆作用;通過流式細胞計數法探討其對cos-7細胞凋亡的影響; 運用計算機分子模型, 從理論上Docking計算化閤物與TAR RNA結閤的可能性.結果錶明, 大環多胺類化閤物MP-1、MP-2和MP-3不僅具有斷裂RNA的作用,併可抑製Tat-RNA的相互作用, 還可影響cos-7細胞亞二倍體的含量; 理論化學計算數據與實驗結果基本一緻.這一結果提示化閤物的抗HIV-1活性可能通過作用于病毒基因組RNA而髮揮作用,是多靶作用的結果.
연구료구유항HIV-1활성적대배다알류화합물여RNA적식별작용,이급기대 cos-7세포조망적영향,이진일보탐토기항HIV-1적작용궤리.실험채용경지당응효전영방법, 관찰화합물여RNA적식별작용;통과류식세포계수법탐토기대cos-7세포조망적영향; 운용계산궤분자모형, 종이론상Docking계산화합물여TAR RNA결합적가능성.결과표명, 대배다알류화합물MP-1、MP-2화MP-3불부구유단렬RNA적작용,병가억제Tat-RNA적상호작용, 환가영향cos-7세포아이배체적함량; 이론화학계산수거여실험결과기본일치.저일결과제시화합물적항HIV-1활성가능통과작용우병독기인조RNA이발휘작용,시다파작용적결과.
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.