Antinociceptive properties of caffeic acid derivatives in mice.
Ten ester derivatives from caffeic acid were synthesized, and their antinociceptive properties are evaluated in mice. The most active compound, dodecyl ester derivative, exhibited potent and dose-related activity against the writhing test, with a calculated ID(50) value of 15.1 (11.9-19.1)micromol/kg and MI of 78.8% being several times more active than reference drugs. It was also effective in other experimental models, such as formalin, capsaicin and glutamate-induced pain tests, but was inactive in the hot-plate test. Although the mechanism of action has still not been elucidated, these results appear to support its therapeutic potential against painful diseases.
de Campos Buzzi
Fátima
F
Programa de Mestrado em Ciências Farmacêuticas e Núcleo de Investigações Químico - Farmacêuticas (NIQFAR)/CCS, Universidade do Vale do Itajaí, 88.302-202 Itajaí, SC, Brazil.
Franzoi
Caroline Liandra
CL
Antonini
Graziele
G
Fracasso
Mauricio
M
Cechinel Filho
Valdir
V
Yunes
Rosendo Augusto
RA
Niero
Rivaldo
R
D000700:Analgesics / Q000737:chemistry* / Q000627:therapeutic use*; D000818:Animals; D002109:Caffeic Acids / Q000737:chemistry* / Q000627:therapeutic use*; D051379:Mice; D015394:Molecular Structure; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D000700:Analgesics; D002109:Caffeic Acids; C040048:caffeic acid