title: Dose-dependent antihypertensive determination and toxicological studies of tilianin isolated from Agastache mexicana.
abstract: BACKGROUND
  Agastache mexicana is used in Mexican traditional medicine for the treatment of hypertension, anxiety and related diseases.
  
  
  OBJECTIVE
  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.
  
  
  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.
authors.affiliation: Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Av. Universidad 1001 Col. Chamilpa, 62209 Cuernavaca, Morelos, Mexico.
authors.forename: Oswaldo
authors.initials: O
authors.lastname: Hernández-Abreu
authors.forename: Mariana
authors.initials: M
authors.lastname: Torres-Piedra
authors.forename: Sara
authors.initials: S
authors.lastname: García-Jiménez
authors.forename: Maximiliano
authors.initials: M
authors.lastname: Ibarra-Barajas
authors.forename: Rafael
authors.initials: R
authors.lastname: Villalobos-Molina
authors.forename: Sergio
authors.initials: S
authors.lastname: Montes
authors.forename: Daniel
authors.initials: D
authors.lastname: Rembao
authors.forename: Samuel
authors.initials: S
authors.lastname: Estrada-Soto
mesh_terms: D031327:Agastache; D000818:Animals; D000959:Antihypertensive Agents / Q000627:therapeutic use* / Q000633:toxicity; D005419:Flavonoids / Q000627:therapeutic use* / Q000633:toxicity; D006027:Glycosides / Q000627:therapeutic use* / Q000633:toxicity; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D008517:Phytotherapy; D051381:Rats; D011918:Rats, Inbred SHR; D023382:Toxicity Tests, Acute
chemical_list: D000959:Antihypertensive Agents; D005419:Flavonoids; D006027:Glycosides; C426884:tilianin