Natural product sennoside B disrupts liquid-liquid phase separation of SARS-CoV-2 nucleocapsid protein by inhibiting its RNA-binding activity

J Enzyme Inhib Med Chem. 2025 Dec;40(1):2501743. doi: 10.1080/14756366.2025.2501743. Epub 2025 May 15.

Abstract

The nucleocapsid protein (NP) of SARS-CoV-2, an RNA-binding protein, is capable of undergoing liquid-liquid phase separation (LLPS) during viral infection, which plays a crucial role in virus assembly, replication, and immune regulation. In this study, we developed a homogeneous time-resolved fluorescence (HTRF) method for identifying inhibitors of the SARS-CoV-2 NP-RNA interaction. Using this HTRF-based approach, we identified two natural products, sennoside A and sennoside B, as effective blockers of this interaction. Bio-layer interferometry assays confirmed that both sennosides directly bind to the NP, with binding sites located within the C-terminal domain. Additionally, fluorescence recovery after photobleaching (FRAP) experiments revealed that sennoside B significantly inhibited RNA-induced LLPS of the NP, while sennoside A displayed comparatively weaker activity. Thus, the developed HTRF-based assay is a valuable tool for identifying novel compounds that disrupt the RNA-binding activity and LLPS of the SARS-CoV-2 NP. Our findings may facilitate the development of antiviral drugs targeting SARS-CoV-2 NP.

Keywords: HTRF; SARS-CoV-2; liquid-liquid phase separation; nucleocapsid protein; sennoside B.

MeSH terms

  • Antiviral Agents* / chemistry
  • Antiviral Agents* / pharmacology
  • Binding Sites / drug effects
  • Biological Products* / chemistry
  • Biological Products* / pharmacology
  • Coronavirus Nucleocapsid Proteins* / antagonists & inhibitors
  • Coronavirus Nucleocapsid Proteins* / metabolism
  • Dose-Response Relationship, Drug
  • Humans
  • Nucleocapsid Proteins* / antagonists & inhibitors
  • Nucleocapsid Proteins* / metabolism
  • Phase Separation
  • Phosphoproteins
  • Protein Binding / drug effects
  • RNA, Viral / metabolism
  • SARS-CoV-2* / drug effects

Substances

  • Coronavirus Nucleocapsid Proteins
  • Antiviral Agents
  • Nucleocapsid Proteins
  • Biological Products
  • nucleocapsid phosphoprotein, SARS-CoV-2
  • RNA, Viral
  • Phosphoproteins