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.
Key words
Cayaponia tayuya
- Cucurbitaceae - 23,24-dihydrocucurbitacin B - cucurbitacin R - anti-inflammatory
activity
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A197
Prof. Dr. J.-L. Ríos
Departament de Farmacologia
Facultat de Farmàcia
Universitat de València
Av. Vicent Andrés Estellés s/n
46100 Burjassot
Spain
Telefon: +34-963-544-973
Fax: +34-963-544-973
eMail: riosjl@uv.es