shizukaol-f and Precursor-Cell-Lymphoblastic-Leukemia-Lymphoma

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.

Topics: Cell Line, Tumor; Drugs, Chinese Herbal; HEK293 Cells; HIV Reverse Transcriptase; HIV-1; Humans; Inhibitory Concentration 50; Magnoliopsida; Molecular Structure; Plants, Medicinal; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Reverse Transcriptase Inhibitors; Ribonuclease H; Sesquiterpenes; Virus Replication