Anti-Herpetic, Anti-Dengue and Antineoplastic Activities of Simple and Heterocycle-Fused Derivatives of Terpenyl-1,4-Naphthoquinone and 1,4-Anthraquinone

Molecules. 2019 Apr 2;24(7):1279. doi: 10.3390/molecules24071279.

Abstract

Quinones are secondary metabolites of higher plants associated with many biological activities, including antiviral effects and cytotoxicity. In this study, the anti-herpetic and anti-dengue evaluation of 27 terpenyl-1,4-naphthoquinone (NQ), 1,4-anthraquinone (AQ) and heterocycle-fused quinone (HetQ) derivatives was done in vitro against Human Herpesvirus (HHV) type 1 and 2, and Dengue virus serotype 2 (DENV-2). The cytotoxicity on HeLa and Jurkat tumor cell lines was also tested. Using plaque forming unit assays, cell viability assays and molecular docking, we found that NQ 4 was the best antiviral compound, while AQ 11 was the most active and selective molecule on the tested tumor cells. NQ 4 showed a fair antiviral activity against Herpesviruses (EC50: <0.4 µg/mL, <1.28 µM) and DENV-2 (1.6 µg/mL, 5.1 µM) on pre-infective stages. Additionally, NQ 4 disrupted the viral attachment of HHV-1 to Vero cells (EC50: 0.12 µg/mL, 0.38 µM) with a very high selectivity index (SI = 1728). The in silico analysis predicted that this quinone could bind to the prefusion form of the E glycoprotein of DENV-2. These findings demonstrate that NQ 4 is a potent and highly selective antiviral compound, while suggesting its ability to prevent Herpes and Dengue infections. Additionally, AQ 11 can be considered of interest as a leader for the design of new anticancer agents.

Keywords: anthraquinones; antiviral activity; cytotoxicity; dengue virus; herpesvirus; naphthoquinones; terpenylquinones.

MeSH terms

  • Animals
  • Anthraquinones / chemistry*
  • Antiviral Agents / chemistry*
  • Antiviral Agents / pharmacology*
  • Cell Line, Tumor
  • Chlorocebus aethiops
  • Dengue Virus / drug effects
  • HeLa Cells
  • Herpesviridae / drug effects
  • Herpesvirus 1, Human / drug effects
  • Herpesvirus 2, Human / drug effects
  • Humans
  • Molecular Structure
  • Naphthoquinones / chemistry*
  • Vero Cells

Substances

  • Anthraquinones
  • Antiviral Agents
  • Naphthoquinones
  • terpenyl-1,4-naphthoquinone
  • 1,4-anthraquinone