In order to validate the use of Phyllanthus orbicularis (Phyllantaceae) in the traditional medicine of Cuba as an anti-inflammatory remedy, the methanolic (MeOH) extract has been evaluated in vivo for anti-inflammatory activity on 12-O-tetradecanoyl-13-acetate phrobol (TPA) assay in mouse and in vitro for the antioxidant activity on Ferric Reduction Antioxidant Power assay. This extract exerted in vivo a significant anti-inflammatory activity. Subsequent fractionation and analysis of the extract has led to the isolation and characterization as major constituents of apigenin (1), rutin (quercetin 3-O—L-rhamnopyranosyl-(1->6)—D-glucopyranoside) (2) and quercetin (3) and of rutin decaacetate (4) and quercetin pentaacetate (5) from acetylated methanolic extract. Their structures were elucidated by spectral methods. The bioassay-directed analysis of flavonols 1–3 indicated that rutin (2) and quercetin (3) were the most active compounds, whereas apigenin showed no significant activity. The acetylation process increased the anti-inflammatory activity but decreased the antioxidant activity. The MeOH extract and all of flavonoids tested did not show in vitro significant cytotoxic effect in J774.A1 macrophage cell line.

Anti-inflammatory and Antioxidant Activity of a Methanolic Extract of Phyllanthus orbicularisand its Derived Flavonols

RASTRELLI, Luca
2011

Abstract

In order to validate the use of Phyllanthus orbicularis (Phyllantaceae) in the traditional medicine of Cuba as an anti-inflammatory remedy, the methanolic (MeOH) extract has been evaluated in vivo for anti-inflammatory activity on 12-O-tetradecanoyl-13-acetate phrobol (TPA) assay in mouse and in vitro for the antioxidant activity on Ferric Reduction Antioxidant Power assay. This extract exerted in vivo a significant anti-inflammatory activity. Subsequent fractionation and analysis of the extract has led to the isolation and characterization as major constituents of apigenin (1), rutin (quercetin 3-O—L-rhamnopyranosyl-(1->6)—D-glucopyranoside) (2) and quercetin (3) and of rutin decaacetate (4) and quercetin pentaacetate (5) from acetylated methanolic extract. Their structures were elucidated by spectral methods. The bioassay-directed analysis of flavonols 1–3 indicated that rutin (2) and quercetin (3) were the most active compounds, whereas apigenin showed no significant activity. The acetylation process increased the anti-inflammatory activity but decreased the antioxidant activity. The MeOH extract and all of flavonoids tested did not show in vitro significant cytotoxic effect in J774.A1 macrophage cell line.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11386/3884973
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