Antinociception caused by the extract of Hedyosmum brasiliense and its active principle, the sesquiterpene lactone 13-hydroxy-8,9-dehydroshizukanolide.
The hydroalcoholic extract (HE) obtained from stems and leaves of Hedyosmum brasiliense, given i.p., produced significant inhibition of acetic acid-induced abdominal constriction in mice, with a mean ID50 of 12.7 mg/kg. This effect installed rapidly (0.5 h) and lasted for up to 2 h. Given orally up to 1000 mg/kg, the HE was ineffective. When assessed in the formalin response the HE, given i.p., inhibited the first and second phase, with ID50s of 31.1 and 21.7 mg/kg for the first and the second phases, respectively. The HE also inhibited capsaicin-induced neurogenic pain with ID50 of 69.0 mg/kg, but, in contrast to morphine, failed to cause analgesia in either the tail-flick or hot-plate models of pain. In addition, its antinociception was not reversed by naloxone. The sesquiterpene lactone 13-hydroxy-8,9-dehydroshizukanolide, isolated from H. brasiliense and already reported in other plant species (given by i.p., i.t., or i.c.v. routes) exhibited graded antinociception against acetic-acid writhing and capsaicin-induced licking. Additionally, we have corrected some physico-chemical data already reported for this compound. It is concluded that both the extract and the sesquiterpene lactone isolated from H. brasiliense produced marked antinociception in different models of chemical pain. The site of action involved in the antinociception of the 13-hydroxy-8,9-dehydroshizukanolide remains unclear, but the opioid pathway seems unlikely to be involved in its action.
Trentin
A P
AP
Departamento de Farmacologia, Universidade Federal de Santa Catarina, Florianópolis, Brazil.
Santos
A R
AR
Guedes
A
A
Pizzolatti
M G
MG
Yunes
R A
RA
Calixto
J B
JB
D019342:Acetic Acid / Q000633:toxicity; D000700:Analgesics / Q000494:pharmacology*; D000818:Animals; D001938:Brazil; D003251:Constriction, Pathologic; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010146:Pain / Q000188:drug therapy* / Q000209:etiology; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018515:Plant Leaves; D018547:Plant Stems; D010946:Plants, Medicinal; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
C121846:13-hydroxy-8,9-dehydroshizukanolide; D000700:Analgesics; D010936:Plant Extracts; D012717:Sesquiterpenes; D019342:Acetic Acid