Ninety-day toxicity and single-dose toxicokinetics study of alpha-glycosyl isoquercitrin in Sprague-Dawley rats

Food Chem Toxicol. 2016 Nov:97:354-366. doi: 10.1016/j.fct.2016.09.030. Epub 2016 Sep 28.


alpha-Glycosyl isoquercitrin (AGIQ) is highly absorbable and has been shown to possess antioxidative properties. Based on a favorable safety profile, it has been confirmed as generally recognized as safe (GRAS) compound by the FDA. Nevertheless, safety and toxicity information for AGIQ is still sparse. Therefore, the aim of this study was to test the safety and toxicokinetics of AGIQ in a 90-day study in 60 male and 60 female Sprague-Dawley rats at dietary doses up to 5%. All animals survived until scheduled euthanasia with no clinical signs of toxicity in any animal. AGIQ was rapidly absorbed with metabolism to quercetin and quercetin glucuronide at all dose levels. Statistically significant changes were noted in some tissue weights and clinical chemistry analytes, without evidence of systemic toxicity. The most prominent finding was systemic dose dependent yellow discoloration of bones of treated animals. However, no changes were observed microscopically, and this observation was concluded as toxicologically insignificant. The overall lack of adverse clinical signs, changes in body weight, feed consumption, clinical pathology parameters, and histopathological endpoints in animals administered AGIQ supports no observable adverse effect levels (NOAEL) of 5.0% in diet for both male and female rats (3461 mg/kg/day and 3867 mg/kg/day, respectively).

Keywords: AGIQ; Alpha-glycosyl isoquercitrin; EMIQ; Flavonol; Isoquercitrin; Quercetin; Safety; Sprague-Dawley; Toxicity; Toxicokinetics.

MeSH terms

  • Administration, Oral
  • Animals
  • Body Weight / drug effects
  • Dose-Response Relationship, Drug
  • Female
  • Glycosides / chemistry
  • Glycosides / toxicity*
  • Hematologic Tests
  • Male
  • Motor Activity / drug effects
  • Organ Size / drug effects
  • Quercetin / analogs & derivatives*
  • Quercetin / chemistry
  • Quercetin / toxicity
  • Rats
  • Rats, Sprague-Dawley
  • Toxicokinetics


  • Glycosides
  • isoquercitrin
  • Quercetin