title: Gastroprotective effect of diligustilide isolated from roots of Ligusticum porteri coulter & rose (Apiaceae) on ethanol-induced lesions in rats.
abstract: BACKGROUND
  The rhizome of Ligusticum porteri Coulter& Rose (LP) has been traditionally used by the ethnic group Raramuri in the North of México for treatment of diabetes, tuberculosis, stomachaches, diarrhea and ritual healing ceremonies. It is use as antiulcer remedy has been extended to all Mexico.
  
  
  OBJECTIVE
  To evaluate the gastroprotective activity of LP organic extracts and the major natural product diligustilide (DLG),using as experimental model the inhibition of the ethanol-induced lesions in rats.
  
  
  METHODS
  Gastric ulcers were induced by intragastric instillation of absolute ethanol (1 mL). We tested the gastroprotective activity of the organic extracts of LP and the pure compound DLG. The ulcer index (UI) was determined to measure the activity. In order to elucidate the action mechanism of DLG the animals were treated with L-NAME, N-ethylmalemide, Forskolin, 2',5'-dideoxyadenosine, Indomethacin, Glibenclameide, Diazoxide, NaHS and DL-Propargylglycine. The pylorus-ligated rat model was used to measure gastric secretion.
  
  
  RESULTS
  The oral administration of organic extracts of Ligusticum porteri showed gastroprotective effect at 30 mg/Kg on ethanol induced gastric lesions; hexane and dichloromethane extracts were the most active. DLG was the major compound in the hexane extract. This compound at 10 mg/kg prevented significantly the gastric injuries induced by ethanol. The alkylation of endogenous non-protein-SH groups with N-ethylmaleimide abolished the gastroprotective effect of DLG and blocking the formation of endogenous prostaglandins by the pretreatment with indomethacin attenuated the gastroprotective effect of DLG.
  
  
  CONCLUSIONS
  The gastroprotective activity demonstrated in this study tends to support the ethnomedical use of Ligusticum porteri roots. DLG, isolated as major compound of this medicinal plant has a clear gastroprotective effect on the ethanol-induced gastric lesions. The results suggest that the antiulcer activity of DLG depends on the participation of the endogenous non-protein -SH groups and prostaglandins.
authors: Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, Ciudad Universitaria, Coyoacán 04510, México D.F., México.
authors: Josué A
authors: JA
authors: Velázquez-Moyado
authors: Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, Ciudad Universitaria, Coyoacán 04510, México D.F., México.
authors: Alejandro
authors: A
authors: Martínez-González
authors: Instituto de Biología, Universidad Nacional Autónoma de México, Ciudad Universitaria, Coyoacán 04510, México D.F., México.
authors: Edelmira
authors: E
authors: Linares
authors: Instituto de Biología, Universidad Nacional Autónoma de México, Ciudad Universitaria, Coyoacán 04510, México D.F., México.
authors: Robert
authors: R
authors: Bye
authors: Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, Ciudad Universitaria, Coyoacán 04510, México D.F., México.
authors: Rachel
authors: R
authors: Mata
authors: Facultad de Química, Departamento de Farmacia, Universidad Nacional Autónoma de México, Ciudad Universitaria, Coyoacán 04510, México D.F., México. Electronic address: anavarrt@unam.mx.
authors: Andrés
authors: A
authors: Navarrete
mesh_terms: D000478:Alkylation; D000818:Animals; D000897:Anti-Ulcer Agents / Q000302:isolation & purification / Q000627:therapeutic use*; D001572:Benzofurans / Q000302:isolation & purification / Q000627:therapeutic use*; D002492:Central Nervous System Depressants; D004305:Dose-Response Relationship, Drug; D000431:Ethanol; D005753:Gastric Mucosa / Q000187:drug effects / Q000473:pathology; D030004:Ligusticum / Q000737:chemistry*; D008297:Male; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D018517:Plant Roots / Q000737:chemistry; D011453:Prostaglandins / Q000096:biosynthesis / Q000235:genetics; D051381:Rats; D017208:Rats, Wistar; D027343:Rhizome / Q000737:chemistry; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology / Q000517:prevention & control*
chemical_list: D000897:Anti-Ulcer Agents; D001572:Benzofurans; D002492:Central Nervous System Depressants; D010936:Plant Extracts; D011453:Prostaglandins; C523615:levistolide A; D000431:Ethanol
keywords: 2′; 5′-Dideoxyadenosine (PubChem CID: 65166); Carbenexolone (PubChem CID: 636402); Chuchupate; Cimetidine (PubChemCID: 2756); DL-Propargylglycine (PubChem CID: 95575); Diazoxide (Pub ChemCID: 25014811); Diligustilide; Diligustilide (PubChem CID: 70698035); Forskolin (PubChem CID: 47936); Gastroprotection; Glibenclamide (PubChem CID: 3488); Indomethacin (PubChem CID: 3715); Ligusticum porteri; N-ethylmaleimide (PubChemCID: 4362); NaHS (PubChem CID: 16211346); Osha; Phthalides; l-NAME (PubChem CID: 135193)