Investigation of antiaromatase activity using hepatic microsomes of Nile tilapia (Oreochromis niloticus)

Drug Discov Ther. 2017 May 30;11(2):84-90. doi: 10.5582/ddt.2017.01006. Epub 2017 Mar 19.

Abstract

Microsomal aromatase enzymes of humans and rats have been used in antiaromatase assays, but enzyme activity is species-specific. The current study extracted hepatic microsomes of Nile tilapia (Oreochromis niloticus) to investigate and compare the antiaromatase activity of chrysin, quercetin, and quercitrin. This activity was evaluated using a dibenzylfluorescein (DBF) assay. Results revealed that the age and body weight of Nile tilapia affected the yield of extracted microsomes. Extraction of hepatic microsomes of Nile tilapia was most effective when using a reaction medium with a pH of 8.0. A DBF assay using Nile tilapia microsomes revealed significant differences in levels of antiaromatase activity for chrysin, quercetin, and quercitrin. Chrysin was the most potent aromatase inhibitor, with an IC50 of 0.25 mg/mL. In addition, chrysin is an aromatase inhibitor that also inhibits the proliferation of cancer cells. Hepatic microsomes of Nile tilapia can be used to investigate and compare the antiaromatase activity of different compounds.

Keywords: Aromatase inhibitor; Nile tilapia; chrysin; microsome; pH effect.

MeSH terms

  • Animals
  • Antioxidants / pharmacology*
  • Aromatase Inhibitors / pharmacology*
  • Cell Proliferation / drug effects*
  • Cichlids
  • Flavonoids / pharmacology*
  • Hep G2 Cells
  • Humans
  • Hydrogen-Ion Concentration
  • MCF-7 Cells
  • Microscopy, Electron, Scanning
  • Microsomes, Liver / drug effects*
  • Microsomes, Liver / enzymology
  • Microsomes, Liver / ultrastructure
  • Quercetin / analogs & derivatives*
  • Quercetin / pharmacology*

Substances

  • Antioxidants
  • Aromatase Inhibitors
  • Flavonoids
  • quercitrin
  • chrysin
  • Quercetin