Investigation of the antimicrobial and anticancer activity of aminonaphthoquinones

Drug Dev Res. 2019 Feb;80(1):138-146. doi: 10.1002/ddr.21477. Epub 2018 Oct 4.

Abstract

In this study, we report on the inhibitory activity of synthesized aminonaphthoquinones against two bacterial and one fungal species to determine their antimicrobial properties. A minimum inhibitory concentration (MIC) of 7.8 μg/mL was obtained against the fungus, Candida albicans, which was better than that of Amphotericin B (MIC = 31.25 μg/mL). Escherichia coli (Gram -), was inhibited at a MIC of 23.4 μg/mL and Staphylococcus aureus (Gram +) at a MIC of 31.3 μg/mL. The aminonaphthoquinones were also screened against HCT116 colon, PC3 prostate and HepG2 liver cancer cell lines to evaluate their cytostatic effects. They had potent activity (GI50 = 5.87-9.90 μM) which was about three-6-fold better than that of parthenolide (GI50 = 25.97 μM) against the prostate cancer cell line. These compounds were generally more selective for cancer cells than for normal human lung fetal fibroblasts (WI-38).

Keywords: aminonaphthoquinones; antibacterial activity; anticancer activity; antifungal activity; minimum inhibitory concentration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Candida albicans / drug effects*
  • Candida albicans / physiology
  • Escherichia coli / drug effects*
  • Escherichia coli / physiology
  • HCT116 Cells
  • Hep G2 Cells
  • Humans
  • Microbial Sensitivity Tests / methods
  • Naphthoquinones / chemistry
  • Naphthoquinones / pharmacology*
  • Staphylococcus aureus / drug effects*
  • Staphylococcus aureus / physiology

Substances

  • Anti-Infective Agents
  • Antineoplastic Agents
  • Naphthoquinones