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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9.11μmol·L 1,与HIV-1活病毒感染实验结果 (6.12μmol·L 1)一致;该化合物特异性抑制RNase H的活性,IC50为26.4μmol·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。
Antagonistic effect of the compounds on the HIV-1 replication activity was studied in order to study the mechanism of action of this compound. Real-time fluorescence quantitative PCR, ELISA and fluorescence detection were used to determine the inhibitory effect of the compound against HIV -1 reverse transcription process, reverse transcriptase RNA-dependent DNA polymerase activity, and RNase H activity. The results showed that silver linear alcohol F inhibited the HIV-1 reverse transcription product LTR / Gag generation, IC50 was 9.11μmol·L 1, and HIV-1 live virus infection results (6.12μmol·L 1); the compound specificity Inhibition of RNase H activity, IC50 of 26.4μmol·L 1; reverse transcriptase RNA-dependent DNA polymerase activity had no significant effect. Sildenafil F is a novel structural class of HIV-1 reverse transcriptase inhibitor that acts on RNase H.