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Semisynthesis and pharmacological investigation of lipo-alkaloids prepared from aconitine.

Fitoterapia (2010-11-16)
Botond Borcsa, Ute Widowitz, Dezso Csupor, Peter Forgo, Rudolf Bauer, Judit Hohmann
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Aconitine, ≥95% (HPLC), crystalline
Supelco
cis-5,8,11,14,17-Eicosapentaenoic acid, analytical standard
Supelco
Sephadex® LH-20
Supelco
Linolenic acid, analytical standard