title: Toxic rather than neuropharmacological effect of Ternstroemia sylvatica fruits and identification of 28-O-[β-l-6-rhamnopyranosyl]-R1-barrigenol as a new compound with toxic effects in mice.
abstract: BACKGROUND
  Fruits of Ternstroemia sylvatica Schltdl. and Cham. (Theaceae) are used in Mexican traditional medicine to alleviate anxiety, sleep disorders and seizures; however, the active principles have not been identified.
  
  
  OBJECTIVE
  To identify the neuroactive principles of T. sylvatica fruits using neuropharmacological tests on mice.
  
  
  METHODS
  The methanol and aqueous extracts of pericarp or seeds of T. sylvatica fruits were intraperitoneally administered (1-562 mg/kg, single doses) to mice. The exploratory cylinder, hole board, open field, Rota-rod and sodium pentobarbital-induced hypnosis tests were used to evaluate the CNS depressant effect after 30 min single administration of extracts. From aqueous seeds extract, triterpene glycoside 28-O-[β-l-6-rhamnopyranosyl]-R1-barrigenol was isolated an active compound.
  
  
  RESULTS
  Crude extracts of T. sylvatica fruits, separated from seed and pericarp, showed sedative effect in mice. The aqueous (ED50 = 4.9 ± 0.8 mg/kg) seed extracts is the most active among them. This extract also decrease locomotor activity and disrupt motor coordination of mice. This extract was also the most toxic extract (LD50 = 5.0 ± 1.4 mg/kg; i.p.). The triterpene glycoside 28-O-[β-l-6-rhamnopyranosyl]-R1-barrigenol was identified in this extract as one of the active sedative compounds (ED50 = 0.12 ± 0.01 mg/kg) also with toxic effect (LD50 = 1.11 ± 0.23 mg/kg).
  
  
  CONCLUSIONS
  The results suggest that T. sylvatica fruits has toxic activity rather than CNS depressant activity in mice and that this effect might be related to the presence of 28-O-[β-l-6-rhamnopyranosyl]-R1-barrigenol, one of the active principles of T. sylvatica fruits with sedative and toxic effect.
authors.affiliation: Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, Ciudad Universitaria , Coyoacán, México D.F. , México and.
authors.forename: José Luis
authors.initials: JL
authors.lastname: Balderas-López
authors.forename: Alejandro
authors.initials: A
authors.lastname: Alfaro-Romero
authors.forename: Amor
authors.initials: A
authors.lastname: Monroy
authors.forename: Ma Edith
authors.initials: ME
authors.lastname: López-Villafranco
authors.forename: José Fausto
authors.initials: JF
authors.lastname: Rivero-Cruz
authors.forename: Andrés
authors.initials: A
authors.lastname: Navarrete
mesh_terms: D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D005638:Fruit; D006993:Hypnotics and Sedatives / Q000008:administration & dosage / Q000737:chemistry / Q000633:toxicity*; D007274:Injections, Intraperitoneal; D007928:Lethal Dose 50; D008297:Male; D000432:Methanol / Q000737:chemistry; D051379:Mice; D008813:Mice, Inbred ICR; D009043:Motor Activity / Q000187:drug effects; D009048:Motor Skills / Q000187:drug effects; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000737:chemistry / Q000633:toxicity*; D010946:Plants, Medicinal; D045442:Rotarod Performance Test; D012503:Saponins / Q000008:administration & dosage / Q000737:chemistry / Q000633:toxicity*; D012639:Seeds; D012890:Sleep / Q000187:drug effects*; D012997:Solvents / Q000737:chemistry; D028242:Theaceae; D013997:Time Factors; D014867:Water / Q000737:chemistry
chemical_list: C000588542:28-O-(6-rhamnopyranosyl)-R1-barrigenol; D006993:Hypnotics and Sedatives; D010936:Plant Extracts; D012503:Saponins; D012997:Solvents; D014867:Water; D000432:Methanol