Márcia María de Souza1,2, Fátima de Campos Buzzi2, Valdir Cechinel Filho2, Sarai Hess1,2, Franco Delle Monachè2, Rivaldo Niero3
1Departamento de Farmácia, Universidade do Contestado (UnC), 89.500-900, Campus Caçador, Caçador, SC, Brazil
2Programa de Mestrado em Ciências Farmacêuticas e Núcleo de Investigações Químico-Farmacêuticas (NIQFAR)/CCS, Universidade do Vale do Itajaí (UNIVALI), 88.302-202, Itajaí, SC, Brazil. Fax: ++55(47)3341-76 01. E-mail: [email protected] 3Programa de Mestrado em Ciências Farmacêuticas e Núcleo de Investigações Químico-Farmacêuticas (NIQFAR)/CCS, Universidade do Vale do Itajaí (UNIVALI), 88.302-202, Itajaí, SC, Brazil. Fax: ++55(47)3341-76 01.
Tóm tắt
A mixture of triterpenes named lupeol (1), α-amyrin (2), β-amyrin (3), and β-sitosterol (4) has been isolated from the hexane fraction of Matayba elaeagnoides. In addition, scopoletin (5), umbelliferone (6), 3β-O-d-glycopyranosyl-sitosterol (7) and betulin (8) were isolated
from the chloroform fraction. All the structures were identified by spectroscopic techniques in accordance with literature data. The extracts (hydroalcoholic and methanolic) and some fractions (hexane, chloroform, ethyl acetate and butanol) exerted promising antinociceptive effects in mice. In addition, we have tested the pure compound betulin (8). When analyzed against induced pain using the writhing test (3-10 mg kg-1, i.p.), betulin showed a dosedependent
effect with a calculated ID50 value of 7.74 (6.53-9.17) mg kg-1 [17.5 (14.7-20.7)
μmol kg-1] and a maximal inhibition (MI) of 58.3% in relation to the control group. When
evaluated in the formalin test (3-10 mg kg-1, i.p.), this compound inhibited both phases of
pain (neurogenic and inflammatory pain), with calculated ID50 values of 18.3 (17.7-18.9)
and 8.3 (7.7-8.9) mg kg-1 [41.5 (38.4-42.7) and 18.8 (17.6-19.9) μmol kg-1] and maximal
inhibition of 40.8 and 64.39% for the first and second phases, respectively. Using the same
models, this compound was several times more active than two clinically used drugs, namely
aspirin and paracetamol, suggesting that its main active principle is related to the antinociceptive
effect found for the chloroform fraction of M. elaeagnoids barks
