Antiulcer and gastric antisecretory effects of dichloromethane fraction and piplartine obtained from fruits of Piper tuberculatum Jacq. in rats

• Published in: Journal of ethnopharmacology Vol. 148; no. 1; pp. 165 - 174
• Main Authors: Burci, Lígia Moura, Pereira, Isabela Tiemy, da Silva, Luisa Mota, Rodrigues, Rosely Valéria, Facundo, Valdir Alves, Militão, Júlio Sanches Linhares Teixeira, Santos, Adair Roberto Soares, Marques, Maria Consuelo Andrade, Baggio, Cristiane Hatsuko, Werner, Maria Fernanda de Paula
• Format: Journal Article
• Language: English
• Published: Ireland Elsevier Ireland Ltd 21.06.2013
• Subjects: acute toxicity; Animals; Anti-secretory; Anti-Ulcer Agents - pharmacology; Anti-Ulcer Agents - therapeutic use; Ethanol; Female; Fruit - chemistry; fruits; gastric acid; Gastric Acid - metabolism; gastric mucosa; Gastric Mucosa - drug effects; Gastric Mucosa - metabolism; Gastrin; Gastroprotection; Glutathione - metabolism; H(+)-K(+)-Exchanging ATPase - metabolism; H+K+-ATPase; intraperitoneal injection; lethal dose 50; methylene chloride; Methylene Chloride - chemistry; Mice; microsomes; mucus; Mucus - metabolism; oral administration; Phytotherapy; Piper; Piper tuberculatum; Piperidones - pharmacology; Piperidones - therapeutic use; Piplartine; Plant Extracts - pharmacology; Plant Extracts - therapeutic use; Rabbits; Rats; Rats, Wistar; secretion; Solvents - chemistry; Stomach Ulcer - chemically induced; Stomach Ulcer - drug therapy; Stomach Ulcer - metabolism; toxicity testing; H+K+-ATPase; Gastroprotection; Piper tuberculatum; Anti-secretory; Piplartine; Gastrin
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2013.04.006

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. 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. 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. 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. [Display omitted]