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.

Key words

Cayaponia tayuya - Cucurbitaceae - 23,24-dihydrocucurbitacin B - cucurbitacin R - anti-inflammatory activity

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