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
em Zh
| WPRIM
| ID: wpr-276207
Biblioteca responsável:
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.
Texto completo:
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Índice:
WPRIM
Assunto principal:
Patologia
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Farmacologia
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Fisiologia
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Plantas Medicinais
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Sesquiterpenos
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Replicação Viral
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Medicamentos de Ervas Chinesas
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Estrutura Molecular
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Química
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HIV-1
Limite:
Humans
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2012
Tipo de documento:
Article