Analgesic and sedative activities of lactucin and some lactucin-like guaianolides in mice.
Lactucin (1) and its derivatives lactucopicrin (2) and 11beta,13-dihydrolactucin (3), which are characteristic bitter sesquiterpene lactones of Lactuca virosa and Cichorium intybus, were evaluated for analgesic and sedative properties in mice. The compounds showed analgesic effects at doses of 15 and 30 mg/kg in the hot plate test similar to that of ibuprofen, used as a standard drug, at a dose of 30 mg/kg. The analgesic activities of the compounds at a dose of 30 mg/kg in the tail-flick test were comparable to that of ibuprofen given at a dose of 60 mg/kg. Lactucopicrin appeared to be the most potent analgetic of the three tested compounds. Lactucin and lactucopicrin, but not 11beta,13-dihydrolactucin, also showed sedative properties in the spontaneous locomotor activity test.
Wesołowska
A
A
Department of New Drugs Research, Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Str., 31-343 Krakow, Poland.
Nikiforuk
A
A
Michalska
K
K
Kisiel
W
W
Chojnacka-Wójcik
E
E
D000700:Analgesics / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D018651:Cichorium intybus / Q000737:chemistry*; D005663:Furans / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D006993:Hypnotics and Sedatives / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D007783:Lactones / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects*; D010146:Pain / Q000188:drug therapy*; D010704:Phorbols; D018515:Plant Leaves / Q000737:chemistry; D018517:Plant Roots / Q000737:chemistry; D012717:Sesquiterpenes / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D045789:Sesquiterpenes, Guaiane / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D013329:Structure-Activity Relationship
D000700:Analgesics; D005663:Furans; D006993:Hypnotics and Sedatives; D007783:Lactones; D010704:Phorbols; D012717:Sesquiterpenes; D045789:Sesquiterpenes, Guaiane; C001458:intybin; C516715:lactucin