title: Antiulcer and gastric antisecretory effects of dichloromethane fraction and piplartine obtained from fruits of Piper tuberculatum Jacq. in rats.
abstract: BACKGROUND
  Piper tuberculatum Jacq. (Piperaceae) is medicinally used as an analgesic and as a treatment for gastric complaints. Thus, the current study aimed to investigate the gastroprotective and antisecretory properties of the dichloromethane fraction of the fruit of Piper tuberculatum (DFPT) and piplartine, a compound isolated from the DFPT, in rats.
  
  
  METHODS
  Gastric ulcers were induced in fasted rats by oral administration of absolute ethanol and then mucus content and glutathione (GSH) levels were measured. Mechanisms underlying the antisecretory action were studied through gastric H(+),K(+)-ATPase activity of highly purified rabbit gastric microsomes and pylorus ligature method in rats.
  
  
  RESULTS
  In the acute toxicity test the values of estimated LD50 for oral and intraperitoneal administration of DFPT were 1.6266 and 0.2684g/kg, respectively. The DFPT (ED50=29mg/kg, p.o.) and piplartine (4.5mg/kg, p.o.) promoted gastroprotection against acute lesions induced by ethanol, effect that could be related with the maintenance of GSH levels in the gastric mucosa. However, only DFPT stimulated gastric mucus secretion. In vitro, the DFPT and piplartine inhibited the H(+),K(+)-ATPase activity and, in vivo DFPT and piplartine also reduced basal gastric acid secretion, as well as that stimulated by pentagastrin.
  
  
  CONCLUSIONS
  These results demonstrate that DFPT and piplatine cause marked gastroprotective effects accompanied by the increase and maintenance of gastric mucus and GSH levels, as well as a reduction in gastric acid secretion through the gastrinergic pathway.
authors.affiliation: Department of Pharmacology, Sector of Biological Sciences, Federal University of Parana, PO Box 19031, Curitiba 81530-900, PR, Brazil.
authors.forename: Lígia Moura
authors.initials: LM
authors.lastname: Burci
authors.forename: Isabela Tiemy
authors.initials: IT
authors.lastname: Pereira
authors.forename: Luisa Mota
authors.initials: LM
authors.lastname: da Silva
authors.forename: Rosely Valéria
authors.initials: RV
authors.lastname: Rodrigues
authors.forename: Valdir Alves
authors.initials: VA
authors.lastname: Facundo
authors.forename: Júlio Sanches Linhares Teixeira
authors.initials: JS
authors.lastname: Militão
authors.forename: Adair Roberto Soares
authors.initials: AR
authors.lastname: Santos
authors.forename: Maria Consuelo Andrade
authors.initials: MC
authors.lastname: Marques
authors.forename: Cristiane Hatsuko
authors.initials: CH
authors.lastname: Baggio
authors.forename: Maria Fernanda de Paula
authors.initials: MF
authors.lastname: Werner
mesh_terms: D000818:Animals; D000897:Anti-Ulcer Agents / Q000494:pharmacology / Q000627:therapeutic use*; D000431:Ethanol; D005260:Female; D005638:Fruit / Q000737:chemistry; D005744:Gastric Acid / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D005978:Glutathione / Q000378:metabolism; D017506:H(+)-K(+)-Exchanging ATPase / Q000378:metabolism; D008752:Methylene Chloride / Q000737:chemistry; D051379:Mice; D009093:Mucus / Q000378:metabolism; D008517:Phytotherapy; D031701:Piper; D010881:Piperidones / Q000494:pharmacology / Q000627:therapeutic use*; D010936:Plant Extracts / Q000494:pharmacology / Q000627:therapeutic use*; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D012997:Solvents / Q000737:chemistry; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy* / Q000378:metabolism
chemical_list: D000897:Anti-Ulcer Agents; D010881:Piperidones; D010936:Plant Extracts; D012997:Solvents; C498077:piperlongumine; D000431:Ethanol; D008752:Methylene Chloride; D017506:H(+)-K(+)-Exchanging ATPase; D005978:Glutathione