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Shizukaol F: a new structural type inhibitor of HIV-1 reverse transcriptase RNase H / 药学学报
Acta Pharmaceutica Sinica ; (12): 1011-1016, 2012.
Article in Chinese | WPRIM | ID: wpr-276207
Responsible library: WPRO
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 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.
Subject(s)
Full text: Available Index: WPRIM (Western Pacific) Main subject: Pathology / Pharmacology / Physiology / Plants, Medicinal / Sesquiterpenes / Virus Replication / Humans / Drugs, Chinese Herbal / Molecular Structure / Chemistry Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2012 Type: Article
Full text: Available Index: WPRIM (Western Pacific) Main subject: Pathology / Pharmacology / Physiology / Plants, Medicinal / Sesquiterpenes / Virus Replication / Humans / Drugs, Chinese Herbal / Molecular Structure / Chemistry Language: Chinese Journal: Acta Pharmaceutica Sinica Year: 2012 Type: Article