Semisynthesis and pharmacological investigation of lipo-alkaloids prepared from aconitine

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.

Graphical AbstractNine aconitine-derived lipo-alkaloids were prepared by semisynthesis and their COX-1, COX-2 and LTB4 formation inhibitory activities were investigated for the first time.Figure optionsDownload full-size imageDownload as PowerPoint slide