Antinociception Caused by the Extract of Hedyosmum brasiliense and its Active Principle, the Sesquiterpene Lactone 13-Hydroxy-8,9-dehydroshizukanolide

Abstract

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.

Analgesic and sedative activities of lactucin and some lactucin-like guaianolides in mice

“…showed an analgesic effect in the hot plate test in mice (Al-Harbi et al, 1994). The eudesmanolide 13-hydroxy-8,9-dehydroshizukanolide from Hedyosmum brasiliense exhibited a significant anti-nociceptive activity in acetic acid-induced writhing and capsaicin-induced licking tests in mice; the ID 50 values were 14.8 and 20.9 mg/kg, i.p., respectively (Trentin et al, 1999). The pseudoguaianolide helenalin from Balduina angustifolia (also present in Arnica montana) was the most active of sesquiterpene lactones screened by Hall et al (1979) in the writhing test in mice.…”

Chemical composition and antimicrobial activity of Hedyosmum brasiliense Miq., Chloranthaceae, essential oil

“…Despite of these facts, the phytochemistry has not been thoroughly studied and only a single publication concerning the isolation of a lindenanolide sesquiterpene lactone and its antinociceptive activity has appeared (Trentin et al, 1999).…”

Composition of the essential oils from leaves of two Hedyosmum spp. from Bolivia

“…4,5 The leaves of both species are used in folk medicine as an antirheumatic and in cold treatment. 6,7 The phytochemistry of some species of the genus Hedyosmum (H. brasiliense, 8 H. bonplandianum, The oils were obtained by hydrodistillation at atmospheric pressure in Cochabamba (564 mmHg) with a Clevenger-type glass hydrodistillation apparatus 11 immediately after the collection of the plant material. The isolation procedure was continued until the material was exhausted (6 h), and the yield obtained was 0.30 and 0.39 ml/100 g fresh plant material for H. angustifolium and H. scabrum, respectively.…”