title: Anti-inflammatory activity of two cucurbitacins isolated from Cayaponia tayuya roots.
abstract: Fractionation of an anti-inflammatory extract from Cayaponia tayuya roots yielded two active compounds, identified as 23,24-dihydrocucurbitacin B (1) and cucurbitacin R (2). Both were evaluated for their anti-inflammatory activity on several experimental models of pain and inflammation. In addition, their cytotoxicity and effects on leukotriene B4 (LTB4) formation were evaluated in rat polymorphonuclear leukocytes. Both compounds showed activity in the following models: carrageenan-induced mouse paw oedema (1, 4 mg/kg p.o., 46% inhibition at 3 h), phospholipase A2-induced mouse paw oedema (2, 3 mg/kg i.p., 61% inhibition at 60 min), serotonin-induced mouse paw oedema (1 and 2, 0.5 mg/kg s.c., 73% and 79% inhibition, respectively), 12- O-tetradecanoylphorbol 13-acetate (TPA)-induced acute ear oedema (2, 36% inhibition at 4 mg/kg p.o., and 87% inhibition at 0.1 mg/ear topically). The compounds were also active against the inflammation induced by repeated application of TPA on mouse ears, affecting both the oedema itself (1 and 2 at 0.1 mg/ear, 44% and 56% inhibition, respectively) as well as cell infiltration (68% and 69%, respectively). The activity of both compounds against oedema induced by serotonin was not modified by the glucocorticoid receptor antagonist mifepristone; however, the protein synthesis inhibitor cycloheximide abolished the anti-inflammatory response in both cases. Neither compound modified the production of LTB4 in rat polymorphonuclear leukocytes, nor did they exhibit analgesic properties at the dose assayed.
authors.affiliation: Departament de Farmacologia, Facultat de Farmàcia, Universitat de València, Burjassot, Spain.
authors.forename: M Carmen
authors.initials: MC
authors.lastname: Recio
authors.forename: Maite
authors.initials: M
authors.lastname: Prieto
authors.forename: Marina
authors.initials: M
authors.lastname: Bonucelli
authors.forename: Cecilia
authors.initials: C
authors.lastname: Orsi
authors.forename: Salvador
authors.initials: S
authors.lastname: Máñez
authors.forename: Rosa M
authors.initials: RM
authors.lastname: Giner
authors.forename: M
authors.initials: M
authors.lastname: Cerdá-Nicolás
authors.forename: José-Luis
authors.initials: JL
authors.lastname: Ríos
mesh_terms: D000279:Administration, Cutaneous; D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D002351:Carrageenan; D019662:Cucurbitaceae; D054728:Cucurbitacins; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D007962:Leukocytes / Q000187:drug effects / Q000378:metabolism; D007975:Leukotriene B4 / Q000378:metabolism; D051379:Mice; D010146:Pain / Q000139:chemically induced / Q000517:prevention & control*; D010741:Phospholipases A; D054467:Phospholipases A2; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D018517:Plant Roots; D051381:Rats; D017208:Rats, Wistar; D013755:Tetradecanoylphorbol Acetate; D014315:Triterpenes / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D010936:Plant Extracts; D014315:Triterpenes; D007975:Leukotriene B4; D054728:Cucurbitacins; D002351:Carrageenan; D010741:Phospholipases A; D054467:Phospholipases A2; D013755:Tetradecanoylphorbol Acetate; C478086:23,24-dihydrocucurbitacin B