High Amplification of the Antiviral Activity of Curcumin through Transformation into Carbon Quantum Dots

Small. 2019 Oct;15(41):e1902641. doi: 10.1002/smll.201902641. Epub 2019 Aug 29.

Abstract

It is demonstrated that carbon quantum dots derived from curcumin (Cur-CQDs) through one-step dry heating are effective antiviral agents against enterovirus 71 (EV71). The surface properties of Cur-CQDs, as well as their antiviral activity, are highly dependent on the heating temperature during synthesis. The one-step heating of curcumin at 180 °C preserves many of the moieties of polymeric curcumin on the surfaces of the as-synthesized Cur-CQDs, resulting in superior antiviral characteristics. It is proposed that curcumin undergoes a series of structural changes through dehydration, polymerization, and carbonization to form core-shell CQDs whose surfaces remain a pyrolytic curcumin-like polymer, boosting the antiviral activity. The results reveal that curcumin possesses insignificant inhibitory activity against EV71 infection in RD cells [half-maximal effective concentration (EC50 ) >200 µg mL-1 ] but exhibits high cytotoxicity toward RD cells (half-maximal cytotoxic concentration (CC50 ) <13 µg mL-1 ). The EC50 (0.2 µg mL-1 ) and CC50 (452.2 µg mL-1 ) of Cur-CQDs are >1000-fold lower and >34-fold higher, respectively, than those of curcumin, demonstrating their far superior antiviral capabilities and high biocompatibility. In vivo, intraperitoneal administration of Cur-CQDs significantly decreases mortality and provides protection against virus-induced hind-limb paralysis in new-born mice challenged with a lethal dose of EV71.

Keywords: antiviral agents; carbon quantum dots; curcumin; enterovirus 71; viral infection.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiviral Agents / pharmacology*
  • Brain / virology
  • Carbon / chemistry*
  • Cell Death / drug effects
  • Curcumin / chemistry
  • Curcumin / pharmacology*
  • Enterovirus / drug effects
  • Eukaryotic Initiation Factor-4G / metabolism
  • Female
  • Male
  • Mice, Inbred ICR
  • Muscles / virology
  • Phosphorylation / drug effects
  • Quantum Dots / chemistry*
  • Quantum Dots / ultrastructure
  • Spectrometry, Fluorescence
  • Spectrophotometry, Ultraviolet
  • Virion / drug effects
  • Virion / metabolism
  • X-Ray Diffraction
  • p38 Mitogen-Activated Protein Kinases / metabolism

Substances

  • Antiviral Agents
  • Eukaryotic Initiation Factor-4G
  • Carbon
  • p38 Mitogen-Activated Protein Kinases
  • Curcumin