Studies on Cardiac Principle in Aconite Roots. I. Isolation and Structural Determination of Higenamine

Abstract
Aconite root (Bushi in Japanese) from A. japonicum Thumb. has long been a very important herb in Chinese medicine for use as a heart stimulant, diuretic agent and anodyne. The cardiac principle was water-soluble and fairly unstable, especially in a basic medium. It was tightly adsorbed on charcoal, alumina, silica gel and cellulose powder, indicating that these agents are not useful for separation. Isolation of the material was finally achieved by the limited combination of gel filtration through Sephadex LH-20 and counter current distribution. Colorless plates, mp (melting point) 260.degree., were obtained as HCl salt. This principle stimulates frog heart even 1:10-9 dilution; it was designated as higenamine. Higenamine was identified as dl-demethylcoclaurine from the spectral data and by comparison with synthesized authentic sample.

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