Semisynthesis and pharmacological investigation of lipo-alkaloids prepared from aconitine |
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| Authors: | Borcsa Botond Widowitz Ute Csupor Dezso Forgo Peter Bauer Rudolf Hohmann Judit |
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| Affiliation: | a Department of Pharmacognosy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungaryb Institute of Pharmaceutical Sciences, Department of Pharmacognosy, Karl-Franzens University Graz, Universitätsplatz 4, 8010 Graz, Austria |
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| Abstract: | 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. |
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| Keywords: | COX-1, cyclooxygenase-1 COX-2, cyclooxygenase-2 LTB4, leukotriene B4 |
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