Anti-inflammatory effects and possible mechanism of action of lupeol acetate isolated from Himatanthus drasticus (Mart.) Plumel

Journal of Inflammation

Research

Gerly Anne Brito¹  Luzia Kalyne AM Leal²  Mary Anne M Bandeira²  Aline H Silva²  Amanda A Lopes²  Victor CC Alves²  Gabriela S Silva²  Helenicy NH Veras²  Elaine CP Lucetti³  Daniel L Lucetti³  Glauce B Viana⁴ 

[1] Department of Morphology, Federal University of Ceará, Brazil;Department of Pharmacy, Federal University of Ceará, Brazil;Department of Physiology and Pharmacology, Federal University of Ceará, Brazil;Department of Physiology and Pharmacology, Federal University of Ceará, Brazil;Faculty of Medicine of Juazeiro do Norte, Ceará, Brazil;

关键词: Indomethacin;    Naloxone;    Human Neutrophil;    Pentoxifylline;    Neutrophil Migration;   

DOI  :  10.1186/1476-9255-7-60

 received in 2010-05-28, accepted in 2010-12-17,  发布年份 2010

来源: Springer

【 摘 要 】

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.

【 授权许可】

Unknown   
© Lucetti et al; licensee BioMed Central Ltd. 2010. This article is published under license to BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.