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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(英)
引用本文:郝美荣,杨铭,卜显和.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(英)[J].生物化学与生物物理进展,2002,29(2):211-216.
作者姓名:郝美荣  杨铭  卜显和
作者单位:北京大学天然药物与仿生药物国家重点实验室, 北京 100083;北京大学天然药物与仿生药物国家重点实验室, 北京 100083;南开大学化学系,天津 300071
基金项目:国家自然科学基金(30171107),北京大学985学科建设基金和国家博士点专项基金(9930)资助项目.
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.

关 键 词:HIV-1,大环多胺,凋亡,Docking
收稿时间:4/9/2001 12:00:00 AM
修稿时间:2001/5/28 0:00:00

Molecular Mechanism of Macrocyclic Polyamines with Anti-HIV-1 Activity to Recognize RNA and Its Effect on Apoptosis
HAO Mei-Rong,YANG Ming and BU Xian-He.Molecular Mechanism of Macrocyclic Polyamines with Anti-HIV-1 Activity to Recognize RNA and Its Effect on Apoptosis[J].Progress In Biochemistry and Biophysics,2002,29(2):211-216.
Authors:HAO Mei-Rong  YANG Ming and BU Xian-He
Institution:National Research Laboratory of Natural & Biomimetic Drugs, Peking University, Beijing 100083, China;National Research Laboratory of Natural & Biomimetic Drugs, Peking University, Beijing 100083, China;Department of Chemistry, Nan Kai University, Tianjin, 300071, China
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.
Keywords:HIV-1  macrocyclic polyamines  apoptosis  docking
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