Antiulcerogenic activity of extract, fractions,  and some compounds obtained from Polygala cyparissias  St. Hillaire & Moquin (Polygalaceae).
The present study evaluates the gastroprotective properties of acetone extract, chloroform, and methanol fractions, alpha-spinasterol (1); 1,3-dihydroxy-7-methoxyxanthone (2); and 1,7-dihydroxy-2,3-methylenedioxyxanthone (3) obtained from Polygala cyparissias (Polygalaceae). Gastroprotective assays were performed in mice using ethanol/HCl and nonsteroidal anti-inflammatory drug (NSAID)/bethanechol-induced ulcer models. Chloroformic fraction showed no interesting results. On the other hand, in the ethanol/HCl-induced ulcer model, the treatment using doses of 50, 125, and 250 mg/kg promoted ulcer inhibition of 45.19+/-12.93%, 62.99+/-3.49%, and 67.40+/-4.75% for acetone extract and 43.70+/-5.12%, 64.56+/-5.64%, and 74.49+/-6.13% for methanol fraction. In the model of NSAID/bethanechol-induced ulcer, the ulcer inhibitions in the same doses were 28.12+/-12.45%, 60.16+/-6.58%, and 77.86+/-7.18% for the acetone extract and 46.09+/-6.92%, 67.45+/-4.36%, and 75.00+/-2.92% for the methanol fraction. In view of the antiulcer potential of the acetone extract and its high yield and xanthone content, it was submitted to chromatographic procedures, giving compounds 1-3, which were also evaluated in the ethanol-induced ulcer model. The results showed that at a dose of 50 mg/kg, these compounds reduced the percentage of ulcer by around 71.26+/-9.40%, 81.10+/-5.75%, and 86.22+/-3.42%, for compounds 1, 2, and 3, respectively. The antiulcerogenic activity of P. cyparissias may be attributed, at least in part, to these compounds.
Klein
Luiz Carlos
LC
Programa de Mestrado em Ciências Farmacêuticas, Universidade do Vale do Itajaí, UNIVALI, Rua Uruguai, 458, Itajaí, Santa Catarina 88302-202, Brazil.
Gandolfi
Renan Becker
RB
Santin
José Roberto
JR
Lemos
Marivane
M
Cechinel Filho
Valdir
V
de Andrade
Sérgio Faloni
SF
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000897:Anti-Ulcer Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D018723:Bethanechol; D004305:Dose-Response Relationship, Drug; D000431:Ethanol; D006851:Hydrochloric Acid; D051379:Mice; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D029608:Polygalaceae / Q000737:chemistry*; D013265:Stigmasterol / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D013276:Stomach Ulcer / Q000139:chemically induced / Q000517:prevention & control*; D044004:Xanthones / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
C120436:1,7-dihydroxy-2,3-dimethoxyxanthone; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000897:Anti-Ulcer Agents; D010936:Plant Extracts; D044004:Xanthones; D018723:Bethanechol; C031312:spinasterol; D000431:Ethanol; C018087:isogentisin; D013265:Stigmasterol; D006851:Hydrochloric Acid