期刊
MARINE DRUGS
卷 17, 期 9, 页码 -出版社
MDPI
DOI: 10.3390/md17090495
关键词
portimine; Vulcanodinium rugosum; HIV-1; reverse transcriptase
资金
- Japan Society for the Promotion of Science [15K08499, 18k16773]
- Research Program on HIV/AIDS from the Japan Agency for Medical Research and Development [JP18fk0410004]
- Asahi Kasei Medical Co., LTD
- MSD Life Science Foundation, Public Interest Incorporated Foundation
- Grants-in-Aid for Scientific Research [18K16773, 15K08499] Funding Source: KAKEN
In this study, we aimed to find chemicals from lower sea animals with defensive effects against human immunodeficiency virus type 1 (HIV-1). A library of marine natural products consisting of 80 compounds was screened for activity against HIV-1 infection using a luciferase-encoding HIV-1 vector. We identified five compounds that decreased luciferase activity in the vector-inoculated cells. In particular, portimine, isolated from the benthic dinoflagellate Vulcanodinium rugosum, exhibited significant anti-HIV-1 activity. Portimine inhibited viral infection with an 50% inhibitory concentration (IC50) value of 4.1 nM and had no cytotoxic effect on the host cells at concentrations less than 200 nM. Portimine also inhibited vesicular stomatitis virus glycoprotein (VSV-G)-pseudotyped HIV-1 vector infection. This result suggested that portimine mainly targeted HIV-1 Gag or Pol protein. To analyse which replication steps portimine affects, luciferase sequences were amplified by semi-quantitative PCR in total DNA. This analysis revealed that portimine inhibits HIV-1 vector infection before or at the reverse transcription step. Portimine has also been shown to have a direct effect on reverse transcriptase using an in vitro reverse transcriptase assay. Portimine efficiently inhibited HIV-1 replication and is a potent lead compound for developing novel therapeutic drugs against HIV-1-induced diseases.
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