Journal
FITOTERAPIA
Volume 82, Issue 3, Pages 365-368Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.fitote.2010.11.001
Keywords
Processed aconite roots; Lipo-alkaloids; COX-1; COX-2; LTB4
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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 LTB4 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 LTB4 formation was pronounced in cases of long chain fatty acid derivatives. (c) 2010 Elsevier B.V. All rights reserved.
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