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Fitoterapia ; 82(3): 365-8, 2011 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-21075183

RESUMEN

Processed aconite drugs are widely used in Eastern medicine as painkillers and antirheumatic agents. It is known that the traditional processing of aconite drugs increases the amount of lipo-alkaloids. In order to obtain information about the pharmacological potential of these compounds, semisynthesis of 9 aconitine-derived lipo-alkaloids was carried out and their COX-1, COX-2 and LTB(4) formation inhibitory activities were investigated. It was found that compounds esterified with unsaturated fatty acids demonstrated significant COX-2 inhibitory effects, while in the COX-1 assay only 14-benzoylaconine-8-O-eicosapentaenoate exerted remarkable activity. The inhibition of LTB(4) formation was pronounced in cases of long chain fatty acid derivatives.


Asunto(s)
Aconitina/química , Aconitum/química , Alcaloides/farmacología , Antiinflamatorios no Esteroideos/farmacología , Inhibidores Enzimáticos/farmacología , Ácidos Grasos Insaturados/farmacología , Extractos Vegetales/farmacología , Aconitina/agonistas , Alcaloides/síntesis química , Antiinflamatorios no Esteroideos/síntesis química , Ciclooxigenasa 1/metabolismo , Inhibidores de la Ciclooxigenasa 2/síntesis química , Inhibidores de la Ciclooxigenasa 2/farmacología , Inhibidores Enzimáticos/síntesis química , Esterificación , Leucotrieno B4/antagonistas & inhibidores , Extractos Vegetales/síntesis química
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