Sesquiterpenes from Jasonia glutinosa: in vitro anti-inflammatory activity.
Four sesquiterpenes isolated from Jasonia glutinosa D.C. (Asteraceae), namely lucinone, glutinone, 5-epi-kutdtriol and kutdtriol, have been evaluated for their in vitro anti-inflammatory activity in cellular systems generating cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) metabolites. None of the compounds assayed had a significant effect on leukotriene C4 (LTC4)-release from calcium ionophore-stimulated mouse peritoneal cells. However, the release of prostaglandin E2 (PGE2) by mouse peritoneal cells stimulated with calcium ionophore was inhibited by these compounds, although with less potency than the reference drug indomethacin (IC50=0.24 microM). The IC50 values of the active compounds were: lucinone 42.69 microM, glutinone 3.61 microM, 5-epi-kutdtriol 1.28 microM and kutdtriol 39 microM. Of the tested compounds, only glutinone (IC50=24 microM) showed a significant effect on thromboxane B2 (TXB2)-release induced by calcium ionophore in human platelets, although with less potency than the reference drug ibuprofen (IC50=1.27 microM).
Bermejo
Benito Paulina
BP
Department of Pharmacology, Faculty of Pharmacy, University Complutense, Madrid, Spain. naber@farm.ucm.es
Abad
María José
MJ
Díaz
Ana María
AM
Villaescusa
Lucinda
L
González
María Angeles
MA
Silván
Ana María
AM
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000032:analysis* / Q000494:pharmacology*; D019659:Asteraceae / Q000737:chemistry*; D001792:Blood Platelets / Q000187:drug effects; D000001:Calcimycin / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D051545:Cyclooxygenase 1; D016861:Cyclooxygenase Inhibitors / Q000494:pharmacology; D015232:Dinoprostone / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007249:Inflammation / Q000201:enzymology; D007527:Isoenzymes / Q000187:drug effects; D017997:Leukotriene C4 / Q000378:metabolism; D016859:Lipoxygenase Inhibitors / Q000494:pharmacology; D008565:Membrane Proteins; D051379:Mice; D010529:Peritoneal Cavity / Q000166:cytology; D018515:Plant Leaves / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry*; D011451:Prostaglandin-Endoperoxide Synthases / Q000187:drug effects; D012717:Sesquiterpenes / Q000032:analysis* / Q000494:pharmacology*; D013929:Thromboxane B2 / Q000378:metabolism
D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D007527:Isoenzymes; D016859:Lipoxygenase Inhibitors; D008565:Membrane Proteins; D012717:Sesquiterpenes; D017997:Leukotriene C4; D000001:Calcimycin; D013929:Thromboxane B2; D051545:Cyclooxygenase 1; C496511:PTGS1 protein, human; D011451:Prostaglandin-Endoperoxide Synthases; C496512:Ptgs1 protein, mouse; D015232:Dinoprostone