Dose-dependent antihypertensive determination and toxicological studies of tilianin isolated from Agastache mexicana

J Ethnopharmacol. 2013 Mar 7;146(1):187-91. doi: 10.1016/j.jep.2012.12.029. Epub 2012 Dec 28.

Abstract

Ethnopharmacological relevance: Agastache mexicana is used in Mexican traditional medicine for the treatment of hypertension, anxiety and related diseases.

Aim of the study: Current work was developed to establish pharmacological/toxicological parameters of tilianin, a flavone extracted from Agastache mexicana in order to propose it for clinical trials.

Materials and methods: Acute and sub-acute toxicology studies in Imprinting Control Region (ICR) mice and median effective dose (ED50) determination in conscious spontaneously hypertensive rats (SHR) were done.

Results: A median lethal dose (LD50) of 6624 mg/kg (6201, 7076) in mice and significant antihypertensive effect (ED50=53.51 mg/kg) in SHR were determined. Moreover, sub-acute oral administration of tilianin did not alter body weight, clinical chemistry parameters (alanine amino-transferase, aspartate amino-transferase, total cholesterol, high density lipoprotein, low density lipoprotein, triglycerides, glucose and insulin), and also did not induce any toxic or adverse effects on kidney, heart, liver, and lung functions.

Conclusions: We have shown that tilianin, isolated from Agastache mexicana, was not toxic for rodents. Also, its antihypertensive effect was dose-dependent and ED50 (53.51 mg/kg) calculated was lesser than LD50 determined (6624 mg/kg), which suggest a wide range of pharmacology-toxicology patterns. Results support the hypothesis that tilianin must be investigated and developed for clinical trials as antihypertensive drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Agastache*
  • Animals
  • Antihypertensive Agents / therapeutic use*
  • Antihypertensive Agents / toxicity
  • Flavonoids / therapeutic use*
  • Flavonoids / toxicity
  • Glycosides / therapeutic use*
  • Glycosides / toxicity
  • Hypertension / drug therapy*
  • Hypertension / physiopathology
  • Lethal Dose 50
  • Male
  • Mice
  • Mice, Inbred ICR
  • Phytotherapy
  • Rats
  • Rats, Inbred SHR
  • Toxicity Tests, Acute

Substances

  • Antihypertensive Agents
  • Flavonoids
  • Glycosides
  • tilianin