Lignosulfonic Acid Sodium Salt As A Potential Microbicide For Preventing Sexual Transmission Of HIV

Despite extraordinary advances in the development of prevention and therapeutic strategies against human immunodeficiency virus (HIV) infection, HIV/AIDS continues to spread at an alarming rate worldwide. Heterosexual transmission is the main route to acquire AIDS. Therefore, development of topical microbicides is urgently needed.Lignosulfonic acid sodium salt (LSA) is a sulfated derivative of lignin made up of repeating phenylpropanoid units. In our study, LSA was shown inhibit various HIV-1 isolates, including a number of clinical isolates. Time-of-drug-addition assay and cell-cell fusion inhibition assay showed that LSA was a HIV-1 entry inhibitor. By analyzing the mechanism of action, we conclude that LSA is broad-spectrum HIV entry inhibitors through blocking the gp120-CD4 interaction. By its broad antiviral potency, easy preparation, low production costs, LSA has promising potential to be developed as an anti-HIV microbicide for preventing HIV sexual transmission.LSA used in combination with an reverse transcriptase inhibitors based microbicide for preventing sexual transmission of HIV because the combination may have broad spectrum antiviral activity and reduce the potential toxic effects. These findings might provide a rational basis for testing of microbicides combination in vivo.