Toxicological Research

Korean Society of Toxicology & Korea Environmental Mutagen Society (한국독성학회)
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Oral toxicity and genotoxicity assessment of standardized Echinacea purpurea (L.) extract and the pharmacokinetic profile of its active ingredient chicoric acid

  • Ji‑Soo Jeong (BK21 FOUR Program, College of Veterinary Medicine, Chungnam National University) ;
  • Jeong‑Won Kim (BK21 FOUR Program, College of Veterinary Medicine, Chungnam National University) ;
  • Jin‑Hwa Kim (BK21 FOUR Program, College of Veterinary Medicine, Chungnam National University) ;
  • Eun‑Hye Chung (BK21 FOUR Program, College of Veterinary Medicine, Chungnam National University) ;
  • Dong‑Ryung Lee (Research Institute, NUON Co., Ltd.) ;
  • Bong‑Keun Choi (Research Institute, NUON Co., Ltd.) ;
  • Je‑Won Ko (BK21 FOUR Program, College of Veterinary Medicine, Chungnam National University) ;
  • Tae‑Won Kim (BK21 FOUR Program, College of Veterinary Medicine, Chungnam National University)
  • Received : 2024.01.04
  • Accepted : 2024.04.05
  • Published : 2024.07.15
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Abstract

Echinacea purpurea (L.), a member of Asteraceae family, has traditionally been used in numerous countries to treat and prevent various immune-related diseases. This study confirmed the oral toxicity and genotoxicity profile of standardized E. purpurea extract under good laboratory practice (GLP) conditions and the pharmacokinetic features of chicoric acid, a major ingredient in E. purpurea extract. For the repeated-dose toxicity test, Sprague Dawley (SD) rats were orally administered 500, 1000, and 2000 mg/kg/day of E. purpurea extract continuously for 13 weeks. The genotoxicity of E. purpurea was determined using standard genotoxicity tests, including bacterial reverse mutations, chromosome aberrations, and micronucleus tests. Additionally, a validated LC-MS/MS method was employed to measure chicoric acid levels in rat plasma for pharmacokinetic analysis. The results of this study indicate that during repeated oral administration of E. purpurea, both male and female SD rats showed no abnormal clinical signs. Furthermore, the genotoxicity tests did not reveal any evidence of genotoxicity in E. purpurea. Pharmacokinetic profile of chicoric acid, following the oral administration of highly purified chicoric acid (95%) and standardized E. purpurea extracts containing 2% chicoric acid, revealed the oral bioavailability to be approximately 1.5%. Increasing the dose of standardized E. purpurea extract (equivalent to 20-100 mg/kg of chicoric acid) from 1 to 5 g/kg resulted in a proportional increase in systemic exposure without reaching saturation. In this study, E.purpurea did not cause oral toxicity and genotoxicity. Additionally, the crude formulation was found to have minimal impact on the pharmacokinetics of chicoric acid.

Keywords

References

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