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

<p>Abstract</p> <p>Background</p> <p>The species <it>Himatanthus drasticus </it>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 includin...

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Main Authors: Alves Victor CC, Lopes Amanda A, Leal Luzia, Silva Aline H, Veras Helenicy NH, Bandeira Mary, Lucetti Elaine CP, Lucetti Daniel L, Silva Gabriela S, Brito Gerly, Viana Glauce B
Format: Article
Language:English
Published: BMC 2010-12-01
Series:Journal of Inflammation
Online Access:http://www.journal-inflammation.com/content/7/1/60
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author Alves Victor CC
Lopes Amanda A
Leal Luzia
Silva Aline H
Veras Helenicy NH
Bandeira Mary
Lucetti Elaine CP
Lucetti Daniel L
Silva Gabriela S
Brito Gerly
Viana Glauce B
author_facet Alves Victor CC
Lopes Amanda A
Leal Luzia
Silva Aline H
Veras Helenicy NH
Bandeira Mary
Lucetti Elaine CP
Lucetti Daniel L
Silva Gabriela S
Brito Gerly
Viana Glauce B
author_sort Alves Victor CC
collection DOAJ
description <p>Abstract</p> <p>Background</p> <p>The species <it>Himatanthus drasticus </it>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 <it>in vivo </it>and <it>in vitro </it>the lupeol acetate (LA) isolated from the plant latex, in several models of inflammation.</p> <p>Methods</p> <p>Male 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.</p> <p>Results</p> <p>In the formalin test, LA (10, 25 and 50 mg/kg, i.p.) inhibited both the 1<sup>st </sup>(neurogenic, 0-5 min) and mainly the 2<sup>nd </sup>(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.</p> <p>Conclusions</p> <p>The 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.</p>
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spelling doaj.art-2ea0e7e3f2614df69e26f769a945dbe52022-12-22T01:20:45ZengBMCJournal of Inflammation1476-92552010-12-01716010.1186/1476-9255-7-60Anti-inflammatory effects and possible mechanism of action of lupeol acetate isolated from <it>Himatanthus drasticus </it>(Mart.) PlumelAlves Victor CCLopes Amanda ALeal LuziaSilva Aline HVeras Helenicy NHBandeira MaryLucetti Elaine CPLucetti Daniel LSilva Gabriela SBrito GerlyViana Glauce B<p>Abstract</p> <p>Background</p> <p>The species <it>Himatanthus drasticus </it>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 <it>in vivo </it>and <it>in vitro </it>the lupeol acetate (LA) isolated from the plant latex, in several models of inflammation.</p> <p>Methods</p> <p>Male 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.</p> <p>Results</p> <p>In the formalin test, LA (10, 25 and 50 mg/kg, i.p.) inhibited both the 1<sup>st </sup>(neurogenic, 0-5 min) and mainly the 2<sup>nd </sup>(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.</p> <p>Conclusions</p> <p>The 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.</p>http://www.journal-inflammation.com/content/7/1/60
spellingShingle Alves Victor CC
Lopes Amanda A
Leal Luzia
Silva Aline H
Veras Helenicy NH
Bandeira Mary
Lucetti Elaine CP
Lucetti Daniel L
Silva Gabriela S
Brito Gerly
Viana Glauce B
Anti-inflammatory effects and possible mechanism of action of lupeol acetate isolated from <it>Himatanthus drasticus </it>(Mart.) Plumel
Journal of Inflammation
title Anti-inflammatory effects and possible mechanism of action of lupeol acetate isolated from <it>Himatanthus drasticus </it>(Mart.) Plumel
title_full Anti-inflammatory effects and possible mechanism of action of lupeol acetate isolated from <it>Himatanthus drasticus </it>(Mart.) Plumel
title_fullStr Anti-inflammatory effects and possible mechanism of action of lupeol acetate isolated from <it>Himatanthus drasticus </it>(Mart.) Plumel
title_full_unstemmed Anti-inflammatory effects and possible mechanism of action of lupeol acetate isolated from <it>Himatanthus drasticus </it>(Mart.) Plumel
title_short Anti-inflammatory effects and possible mechanism of action of lupeol acetate isolated from <it>Himatanthus drasticus </it>(Mart.) Plumel
title_sort anti inflammatory effects and possible mechanism of action of lupeol acetate isolated from it himatanthus drasticus it mart plumel
url http://www.journal-inflammation.com/content/7/1/60
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