Anti-HIV-1 activity of targeted enriched components from Polygonum cuspidatum / 中草药

ABSTRACT

Objective: To investigate the inhibitory effect and targets of enriched components from Polygonum cuspidatum on HIV-1 in vitro. Methods: Four extracts of P. cuspidatum were screened by HIV-1 multi-target screening system based on the surface plasmon resonance. The highly active components were obtained by NHS-activated HiTrap conjugated with integrase. The anti-HIV activity of the sample was determined with TZM-bl infection assay and PBMCs infection assay. The inhibition of HZ60-IN on integrase 3’ processing was detected by fluorescence resonance energy transfer analysis. High-throughput ELISA was used to determine the effect of enriched active ingredients of P. cuspidatum (HZ60-IN) on integrase chain transfer; Effects of HZ60-IN on reverse transcriptase and protease were detected by kit. Results: HZ60-IN displayed higher affinity with integrase. HZ60-IN demonstrated potent antiviral activity against NL4.3 and 1084i strains in TZM-bl cells with the IC50 of (31.94 ± 8.96) and (38.07 ± 11.25) μg/mL, respectively. HZ60-IN showed significant inhibition on HIV-1 NL4.3 strains in PBMCs from two donors. HZ60-IN acted on the integrase with the IC50 of (6.54 ± 1.69) μg/mL for 3’ processing and (2.56 ± 0.97) μg/mL for strand transfer activity. It showed weak effects on the entry stage of HIV infection, with weak inhibitory activity on reverse transcriptase and no effect on protease activity. Conclusion: HZ60-IN showed significant inhibitive effect on HIV-1 replication and might specifically interfere with integrase activities.