漢薬の生物活性成分(第3報)枳〓子(Hoveniae Semen Seu Fructus)のアルコール性筋弛緩抑制及び肝保護作用成分 : 新規Dihydroflavonol, Hovenitin I, II, III, の絶対構造

概要

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The methanol-soluble fraction from a Chinese natural medicine Hoveniae Semen Seu Fructus, the seed and fruit of Hovenia dulcis THUNB. (Rhamnaceae) was found to show an inhibitory effect on the alcohol-induced muscular relaxation and a protective activity on the D-galactosamine/lipopolysaccharide or carbon tetrachloride-induced liver injury. Through bioassay-guided separation using a traction performance test, three new dihydrofravonols named hovenitins I, II, and III were isolated from Hoveniae Semen Seu Fructus together with four known flavonoids, (+)-ampelopsin, laricetrin, myricetin, and (+)-gallocatechin. The absolute stereostructures of hovenitins I, II, and III were determined on the basis of chemical and physicochemical evidence to be (2R, 3R)-5,7,4', 5'-tetrahydroxy-3'-methoxydihydroflavonol, (2R, 3S)-5,7,4', 5'-tetrahydroxy-3'-methoxy-dihydroflavonol, and (2R, 3S)-5,7,3', 4', 5'-pentahydroxydihydro-flavonol, respectively. Hovenitin I and (+)-ampelopsin, both of which were principal ingredients of the active fractions from this natural medicine, were found to show an inhibitory activity on the ethanol-induced muscle relaxation in rats. In addition, hovenitin I showed a protective activity on the liver injury induced by D-galactosamine/lipopolysaccharide or carbon tetrachloride in mice.
社団法人日本薬学会の論文
1997-02-25