[Shizukaol F: a new structural type inhibitor of HIV-1 reverse transcriptase RNase H].
[Shizukaol F: a new structural type inhibitor of HIV-1 reverse transcriptase RNase H].
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发表时间：
2012-08
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通讯作者：
Ying Yang;Ying-li Cao;Haiyang Liu;Huan Yan;Ying Guo
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作者：
Ying Yang;Ying-li Cao;Haiyang Liu;Huan Yan;Ying Guo
本研究旨在探讨茚满二倍半萜类化合物紫草醇F对HIV-1复制的作用机制。分别采用真实的时间定量PCR、ELISA和荧光法检测HIV-1逆转录过程、RNA依赖的DNA聚合酶活性和RNase H活性。结果表明，shizukaol F抑制HIV-1逆转录的LTR/Gag产生，IC 50为9.11 μ mol × L（-1）。这一结果与其对HIV-1复制的抑制作用一致（IC 50为6.12 μ mol × L（-1））。机理研究表明，化合物Shizukaol F抑制HIV-1 RT-RNase H的IC 50为26.4 μ mol × L（-1），但对HIV-1 RT RNA依赖的DNA聚合酶活性无影响。因此，丁香酚F是一种新结构类型的HIV-1 RNase H抑制剂。这一发现将为新型逆转录酶抑制剂的开发提供线索。
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 micromol x L(-1). This result is consistent with its inhibitory effect on HIV-1 replication (IC50 of 6.12 micromol x L(-1)). Mechanism studies showed that compound shizukaol F inhibited HIV-1 RT-RNase H with IC50 of 26.4 micromol x 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.