Abstract
BackgroundThe species Himatanthus drasticus is popularly known in Northeast Brazil as "janaguba" and belongs to the family Apocynaceae. The latex collected from its stem bark is used for several purposes including anti-inflammatory properties and presents among its bioactive constituents the pentacyclic triterpene lupeol. The objective of the present work was to study in vivo and in vitro the lupeol acetate (LA) isolated from the plant latex, in several models of inflammation.MethodsMale Swiss mice (25-30 g, 6-24 animals per group) were administered with LA, 30 min before the test initiation. In the evaluation of analgesic activity the formalin test was used. The anti-inflammatory activity was evaluated by the following tests: paw edema induced by carrageenan and dextran, and the carrageenan-induced neutrophil migration into peritoneal cavities. Furthermore, the effect of LA on the myeloperoxidase release (MPO, an inflammation biomarker) from human neutrophils was also determined, as well as its antioxidant potential by the DPPH assay.ResultsIn the formalin test, LA (10, 25 and 50 mg/kg, i.p.) inhibited both the 1st (neurogenic, 0-5 min) and mainly the 2nd (inflammatory, 20-25 min) phase. Naloxone completely reversed the LA effect, indicating the participation of the opioid system. LA also significantly inhibited carrageenan- and dextran-induced paw edemas, as well as the neutrophil migration to the peritoneal cavity evaluated by the carrageenan-induced pleurisia. In this model, the effect of a very low dose of LA (0.1 mg/kg) was potentiated by the same dose of pentoxifylline (PTX), a known TNF-alpha inhibitor. LA (25 and 50 μg/ml) was also very effective in inhibiting MPO released from stimulated human neutrophils, and significantly decreased the number of cells expressing iNOS activity in the paw of mice submitted to carrageenan-induced edema, suggesting a drug involvement with the NO system.ConclusionsThe anti-inflammatory effect of LA probably involves the opioid system, as indicated by the complete blockade of the opioid antagonist naloxone. Furthermore, the LA effect was potentiated by PTX (a TNF-alpha inhibitor). LA also decreased the number of iNOS cells, suggesting the participation of pro-inflammatory cytokines and the NO system in the drug action.
Highlights
The species Himatanthus drasticus is popularly known in Northeast Brazil as “janaguba” and belongs to the family Apocynaceae
To clarify the lupeol acetate (LA) mechanism of action, we studied the participation of pentoxifylline, a PDE5 and TNF-alpha inhibitor, and morphine, a mu and kappa agonist, on inflammatory processes, and their possible interaction with LA
Formalin test in mice LA (10, 25 and 50 mg/kg, i.p.) reduced both phases of the formalin test, and the results were significant at the two higher doses
Summary
The species Himatanthus drasticus is popularly known in Northeast Brazil as “janaguba” and belongs to the family Apocynaceae. The latex collected from its stem bark is used for several purposes including antiinflammatory properties and presents among its bioactive constituents the pentacyclic triterpene lupeol. The objective of the present work was to study in vivo and in vitro the lupeol acetate (LA) isolated from the plant latex, in several models of inflammation. The species Himatanthus drasticus, popularly known in Northeast Brazil as “janaguba”, belongs to the family Apocynaceae. Its geographical distribution extends from Southeast Brazil to French Guyana, Suriname and Guyana. In Brazil, it occurs in several states, especially from the Northeastern region. The latex from its stem bark is over-exploited without control by local Brazilian communities, for instance in the Northeasterm region of Cariri for medicinal purposes, mainly for the treatment of tumours, inflammatory processes and ulcers [2]
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