杨 颖, 曹颖莉, 刘海洋, 严 欢, 郭 颖. 银线草醇F: 一种新结构类型HIV-1逆转录酶RNase H活性抑制剂J. 药学学报, 2012,47(8): 1011-1016.
引用本文: 杨 颖, 曹颖莉, 刘海洋, 严 欢, 郭 颖. 银线草醇F: 一种新结构类型HIV-1逆转录酶RNase H活性抑制剂J. 药学学报, 2012,47(8): 1011-1016.
shu
YANG Ying, CAO Ying-li, LIU Hai-yang, YAN Huan, GUO Ying. Shizukaol F: a new structural type inhibitor of HIV-1 reverse transcriptase RNase HJ. 药学学报, 2012,47(8): 1011-1016.
Citation: YANG Ying, CAO Ying-li, LIU Hai-yang, YAN Huan, GUO Ying. Shizukaol F: a new structural type inhibitor of HIV-1 reverse transcriptase RNase HJ. 药学学报, 2012,47(8): 1011-1016.
shu

银线草醇F: 一种新结构类型HIV-1逆转录酶RNase H活性抑制剂

Shizukaol F: a new structural type inhibitor of HIV-1 reverse transcriptase RNase H

    摘要
  • 摘要:

    乌药烷型二聚倍半萜类化合物银线草醇F具有抑制HIV-1复制活性, 为研究该化合物的作用机制,  应用实时荧光定量PCR法、ELISA法及荧光测定法分别测定化合物对HIV-1逆转录进程、逆转录酶RNA-依赖DNA聚合酶活性以及RNase H活性的影响。结果显示, 银线草醇F抑制HIV-1逆转录产物LTR/Gag生成, IC50为9.11 μmol·L−1, 与HIV-1活病毒感染实验结果 (6.12 μmol·L−1) 一致; 该化合物特异性抑制RNase H的活性, IC50为26.4 μmol·L−1; 对逆转录酶的RNA-依赖DNA聚合酶活性无显著影响。银线草醇F是一个作用于RNase H的具有新结构类型的HIV-1逆转录酶抑制剂。

     

    Abstract:

    This study is to investigate the mechanism of action of lindenane disesquiterpenoid shizukaol F on HIV-1 replication.  Real time quantity PCR, ELISA assay and fluorescence methods were used to test HIV-1 reverse transcription process, RNA-dependent DNA polymerase activity, and RNase H activity, respectively.    It showed that shizukaol F inhibited LTR/Gag production of HIV-1 reverse transcription with an IC50 of 9.11 μmol·L−1.  This result is consistent with its inhibitory effect on HIV-1 replication (IC50 of 6.12 μmol·L−1).  Mechanism studies showed that compound shizukaol F inhibited HIV-1 RT-RNase H with IC50 of 26.4 μmol·L−1, but had no effect on HIV-1 RT RNA-dependent DNA polymerase activity.  In conclusion, shizukaol F is a new structural type HIV-1 RNase H inhibitor.  This discovery will provide a clue for new type of reverse transcriptase inhibitors development.

     

    • HTML全文
    • 参考文献(0)
    • 相关文章
    • 施引文献
  • 资源附件(0)

/

返回文章
返回