title: Evaluation of the gastroprotective activity of the extracts, fractions, and pure compounds obtained from aerial parts of Rubus imperialis in different experimental models.
abstract: Previous phytochemical studies carried out with Rubus imperialis Chum. Schl. (Rosaceae) have demonstrated the presence of triterpenes (niga-ichigoside F1 and 2β,3β,19α-trihydroxyursolic acid) in this species. The literature indicates that triterpenes are closely related to some pharmacological activities, including antiulcer activity. Therefore, in view of the previous promising results with this species, this work extends the phytochemical studies, as well as investigates its gastroprotective action in different models using rodents. The hydroalcoholic extract was tested using the following protocols in mice: ethanol/HCl and nonsteroidal anti-inflammatory drug (NSAID)-induced ulcer, acetic acid-induced chronic ulcer, ligature pylorus model, and free mucus quantification in mucosa. Isolated triterpenes were investigated in the ethanol/HCl-induced ulcer model. The results of this study show that R. imperialis extract (100, 250, or 500 mg) displays gastroprotective activity in the ethanol-induced ulcer model with a percentage of inhibition of gastric lesions of 70, 71, and 86 %, respectively. The extract also significantly reduced the ulcerative lesions in the indomethacin-induced ulcer. In this model, the percentage of inhibition of ulcer was 41, 44, and 70 %, respectively. Regarding the model of gastric secretion, a reduction of gastric juice volume and total acidity was observed, as well as an increase in gastric pH; however, gastric mucus production was not altered by treatment with the extract. It was also observed that the ethyl acetate fraction presented higher activity, leading to the isolation of niga-ichigoside F1 and 2β,3β-19-α-trihydroxyursolic acid, which presented antiulcer activity comparable to that of omeprazole, with an inhibition percentage of 98 and 99 %, respectively. These results demonstrate that R. imperialis extract and isolated compounds (niga-ichigoside F1 and 2β,3β-19-α-trihydroxyursolic acid) produce gastroprotective effects, and this activity seems, at least in part, to be related to antisecretory effects.
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas e Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí - UNIVALI, Rua Uruguai, 458, 88302-202, Itajaí, SC, Brazil.
authors.forename: Priscila Elisabeth
authors.initials: PE
authors.lastname: Berté
authors.forename: Jhonny
authors.initials: J
authors.lastname: da Silva Lopes
authors.forename: Nicole Garbin
authors.initials: NG
authors.lastname: Comandulli
authors.forename: Daniele Wolff
authors.initials: DW
authors.lastname: Rangel
authors.forename: Franco Delle
authors.initials: FD
authors.lastname: Monache
authors.forename: Valdir Cechinel
authors.initials: VC
authors.lastname: Filho
authors.forename: Rivaldo
authors.initials: R
authors.lastname: Niero
authors.forename: Sergio Faloni
authors.initials: SF
authors.lastname: de Andrade
mesh_terms: D019342:Acetic Acid; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000897:Anti-Ulcer Agents / Q000494:pharmacology / Q000627:therapeutic use*; D000431:Ethanol; D007213:Indomethacin; D008297:Male; D051379:Mice; D009093:Mucus / Q000378:metabolism; D008517:Phytotherapy; D035261:Plant Components, Aerial; D010936:Plant Extracts / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats; D017208:Rats, Wistar; D027824:Rosaceae; D012503:Saponins / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy* / Q000378:metabolism; D014315:Triterpenes / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000897:Anti-Ulcer Agents; D010936:Plant Extracts; D012503:Saponins; D014315:Triterpenes; D000431:Ethanol; C090725:niga-ichigoside F1; D019342:Acetic Acid; D007213:Indomethacin