INHIBITION OF NITRIC OXIDE SYNTHASE EXPRESSION BY A METHANOLIC EXTRACT OF CRESCENTIA ALATA AND ITS DERIVED FLAVONOLS
| Autor: | Raffaella Sorrentino, Maria Rosaria Lauro, Aldo Pinto, Ugo Sorrentino, Luca Rastrelli, Giuseppina Autore, Stefania Marzocco, Rita Patrizia Aquino |
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| Přispěvatelé: | Autore, G., Rastrelli, L., Lauro, Mr, Marzocco, S., Sorrentino, Raffaella, Sorrentino, U., Pinto, A. AND AQUINO R. |
| Jazyk: | angličtina |
| Rok vydání: | 2001 |
| Předmět: |
Male
Flavonols Rutin Anti-Inflammatory Agents Nitric Oxide Synthase Type II Nitric Oxide General Biochemistry Genetics and Molecular Biology Nitric oxide chemistry.chemical_compound In vivo Animals Edema General Pharmacology Toxicology and Pharmaceutics Enzyme Inhibitors Kaempferols Rats Wistar Cells Cultured chemistry.chemical_classification Flavonoids biology Dose-Response Relationship Drug Plant Extracts Macrophages General Medicine Macrophage Activation Hindlimb Rats Nitric oxide synthase Plant Leaves Aglycone chemistry Biochemistry Bignoniaceae biology.protein Quercetin Medicine Traditional Nitric Oxide Synthase Kaempferol |
| Popis: | In order to validate the use of Crescentia alata (Bignoniaceae) in the traditional medicine of Guatemala as an antiinflammatory remedy, the methanolic (MeOH) extract has been evaluated in vivo for antiinflammatory activity on carrageenin paw edema in rats and in vitro on Escherichia coli lipopolysaccharide- (LPS)-induced nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) expression in J774.A1 macrophage cell line. This extract exerted in vivo a significant anti-inflammatory activity at the highest dose tested. The same extract showed in vitro an inhibitory activity on inducible nitric oxide synthase expression and on NO formation in LPS-primed J774.A1 cells. Subsequent fractionation and analysis of the extract has led to the isolation and characterization as major constituents of two flavonol glycosides: quercetin 3-O-alpha-L-rhamnopyranosyl-(1->6)-beta-D-glucopyranoside (rutin) 1, kaempferol 3-O-alpha-L-rhamnopyranosyl-(1->6)-beta-D-glucopyranoside (kaempferol 3-O-rutinoside) 2, and flavonol aglycone, kaempferol 3. Their structures were elucidated by spectral methods. The bioassay-directed analysis of flavonols 1-3 indicated that kaempferol (3) was the most active compound contained in the MeOH extract because it reduced in vitro both NO production and iNOS expression in LPS-primed J774.A1 cells, whereas rutin (1) and kaempferol 3-O-rutinoside (2) showed no significant activity. The MeOH extract and all of flavonoids tested did not show in vitro significant cytotoxic effect in J774.A1 macrophage cell line. |
| Databáze: | OpenAIRE |
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