Comparative analysis of the anti-chikungunya virus activity of novel bryostatin analogs confirms the existence of a PKC-independent mechanism

Biochem Pharmacol. 2016 Nov 15:120:15-21. doi: 10.1016/j.bcp.2016.09.020. Epub 2016 Sep 21.

Abstract

Previously, we reported that salicylate-based analogs of bryostatin protect cells from chikungunya virus (CHIKV)-induced cell death. Interestingly, 'capping' the hydroxyl group at C26 of a lead bryostatin analog, a position known to be crucial for binding to and modulation of protein kinase C (PKC), did not abrogate the anti-CHIKV activity of the scaffold, putatively indicating the involvement of a pathway independent of PKC. The work detailed in this study demonstrates that salicylate-derived analog 1 and two capped analogs (2 and 3) are not merely cytoprotective compounds, but act as selective and specific inhibitors of CHIKV replication. Further, a detailed comparative analysis of the effect of the non-capped versus the two capped analogs revealed that compound 1 acts both at early and late stages in the chikungunya virus replication cycle, while the capped analogs only interfere with a later stage process. Co-dosing with the PKC inhibitors sotrastaurin and Gö6976 counteracts the antiviral activity of compound 1 without affecting that of capped analogs 2 and 3, providing further evidence that the latter elicit their anti-CHIKV activity independently of PKC. Remarkably, treatment of CHIKV-infected cells with a combination of compound 1 and a capped analog resulted in a pronounced synergistic antiviral effect. Thus, these salicylate-based bryostatin analogs can inhibit CHIKV replication through a novel, yet still elusive, non-PKC dependent pathway.

Keywords: Bryostatin; Chikungunya virus; Protein kinase C; Salicylate; Sotrastaurin.

Publication types

  • Comparative Study

MeSH terms

  • Acetylation
  • Animals
  • Antiviral Agents / agonists
  • Antiviral Agents / antagonists & inhibitors
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Bryostatins / agonists
  • Bryostatins / antagonists & inhibitors
  • Bryostatins / chemistry
  • Bryostatins / pharmacology*
  • Carbazoles / chemistry
  • Carbazoles / pharmacology
  • Cell Line
  • Chikungunya virus / drug effects*
  • Chikungunya virus / growth & development
  • Chikungunya virus / metabolism
  • Chlorocebus aethiops
  • Drug Design*
  • Drug Synergism
  • Gene Expression Regulation, Viral / drug effects
  • Humans
  • Isoenzymes / antagonists & inhibitors
  • Isoenzymes / chemistry
  • Isoenzymes / metabolism
  • Kinetics
  • Methylation
  • Protein Kinase C / antagonists & inhibitors
  • Protein Kinase C / chemistry
  • Protein Kinase C / genetics
  • Protein Kinase C / metabolism*
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology
  • Pyrroles / chemistry
  • Pyrroles / pharmacology
  • Quinazolines / chemistry
  • Quinazolines / pharmacology
  • Semliki forest virus / drug effects
  • Semliki forest virus / growth & development
  • Semliki forest virus / metabolism
  • Sindbis Virus / drug effects
  • Sindbis Virus / growth & development
  • Sindbis Virus / metabolism
  • Viral Proteins / antagonists & inhibitors
  • Viral Proteins / chemistry
  • Viral Proteins / genetics
  • Viral Proteins / metabolism*
  • Virus Replication / drug effects

Substances

  • Antiviral Agents
  • Bryostatins
  • Carbazoles
  • Isoenzymes
  • Protein Kinase Inhibitors
  • Pyrroles
  • Quinazolines
  • Viral Proteins
  • Go 6976
  • sotrastaurin
  • Protein Kinase C