Hibiscus sabdariffa L. and Its Bioactive Constituents Exhibit Antiviral Activity against HSV-2 and Anti-enzymatic Properties against Urease by an ESI-MS Based Assay

Molecules. 2017 Apr 30;22(5):722. doi: 10.3390/molecules22050722.

Abstract

For decades, Hibiscus sabdariffa L. and its phytochemicals have been shown to possess a wide range of pharmacologic properties. In this study, aqueous extract of Hibiscus sabdariffa (AEHS) and its bioactive constituent protocatechuic acid (PCA), have been evaluated in vitro for their antiviral activity against HSV-2 clinical isolates and anti-enzymatic activity against urease. Antiherpetic activity was evaluated by the titer reduction assay in infected Vero cells, and cytotoxicity was evaluated by the neutral red dye-uptake method. Anti-urease activity was determined by a developed Electrospray Ionization-Mass Spectrometry (ESI-MS)-based assay. PCA showed potent anti-HSV-2 activity compared with that of acyclovir, with EC50 values of 0.92 and 1.43 µg∙mL-1, respectively, and selectivity indices > 217 and > 140, respectively. For the first time, AEHS was shown to exert anti-urease inhibition activity, with an IC50 value of 82.4 µg∙mL-1. This, combined with its safety, could facilitate its use in practical applications as a natural urease inhibitor. Our results present Hibiscus sabdariffa L. and its bioactive compound PCA as potential therapeutic agents in the treatment of HSV-2 infection and the treatment of diseases caused by urease-producing bacteria.

Keywords: ESI-mass spectrometry-based assay; Hibiscus sabdariffa L.; anti-HSV-2 activity; bacterial infection; protocatechuic acid; urease inhibitors.

MeSH terms

  • Acyclovir / pharmacology
  • Animals
  • Antiviral Agents / chemistry
  • Antiviral Agents / isolation & purification
  • Antiviral Agents / pharmacology*
  • Chlorocebus aethiops
  • Chromatography, High Pressure Liquid
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / isolation & purification
  • Enzyme Inhibitors / pharmacology
  • Herpesvirus 2, Human / drug effects*
  • Hibiscus / chemistry*
  • Inhibitory Concentration 50
  • Kinetics
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Polyphenols / chemistry
  • Polyphenols / isolation & purification
  • Polyphenols / pharmacology
  • Spectrometry, Mass, Electrospray Ionization
  • Urease / antagonists & inhibitors*
  • Urease / chemistry
  • Vero Cells

Substances

  • Antiviral Agents
  • Enzyme Inhibitors
  • Plant Extracts
  • Polyphenols
  • Urease
  • Acyclovir