Abstract
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.
Highlights
Various therapeutic drugs against human immunodeficiency virus type 1 (HIV-1) have been developed, almost all of these drugs target viral enzymes
Screening of 80 Compounds Extracted from Lower Sea Animals for the Inhibition of HIV-1 Vector Infection
We commercially obtained a library containing 80 compounds extracted from lower sea animals (Figure 1) and measured the impact of each compound on HIV-1 vector infection
Summary
Various therapeutic drugs against human immunodeficiency virus type 1 (HIV-1) have been developed, almost all of these drugs target viral enzymes. Two types of nucleoside reverse transcriptase inhibitors are used in combination with a protease inhibitor, a nonnucleoside reverse transcriptase inhibitor or an integrase inhibitor. All of these drugs suppress HIV-1 enzymes. Because of the high mutation rate of viral replication, viral variants resistant to the drugs appear during drug treatment [1]. To resolve this problem, novel types of drugs are needed
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