title: Semisynthesis and pharmacological investigation of lipo-alkaloids prepared from aconitine.
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 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.
authors.affiliation: Department of Pharmacognosy, University of Szeged, Szeged, Hungary.
authors.forename: Botond
authors.initials: B
authors.lastname: Borcsa
authors.forename: Ute
authors.initials: U
authors.lastname: Widowitz
authors.forename: Dezso
authors.initials: D
authors.lastname: Csupor
authors.forename: Peter
authors.initials: P
authors.lastname: Forgo
authors.forename: Rudolf
authors.initials: R
authors.lastname: Bauer
authors.forename: Judit
authors.initials: J
authors.lastname: Hohmann
mesh_terms: D000157:Aconitine / Q000819:agonists / Q000737:chemistry*; D031841:Aconitum / Q000737:chemistry*; D000470:Alkaloids / Q000138:chemical synthesis / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology*; D051545:Cyclooxygenase 1 / Q000378:metabolism; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D004951:Esterification; D005231:Fatty Acids, Unsaturated / Q000494:pharmacology*; D007975:Leukotriene B4 / Q000037:antagonists & inhibitors; D010936:Plant Extracts / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000470:Alkaloids; D000894:Anti-Inflammatory Agents, Non-Steroidal; D052246:Cyclooxygenase 2 Inhibitors; D004791:Enzyme Inhibitors; D005231:Fatty Acids, Unsaturated; D010936:Plant Extracts; D007975:Leukotriene B4; D051545:Cyclooxygenase 1; D000157:Aconitine