A COMPARISON OF THE PHARMACOLOGICAL ACTIONS OF SEVEN CONSTITUENTS ISOLATED FROM FRUCTUS SCHIZANDRAE

From the ethanol extract of dried fruit of Schizandra chinensis Baill.(Fructus Schizandrae) seven constituents have been isolated. All these substances were shown to be active in lowering the high SGPT level to various extents in CCl₄ intoxicated mice. Improvement of histological figure of liver tissue was also observed. The SGPT lowering activities of these compounds may be arranged as follows: Ⅶ>Ⅴ>Ⅲ>Ⅱ>Ⅰ≥Ⅵ≥Ⅳ. Compounds Ⅶ and Ⅴ showed significant SGPT lowering activity at an oral dose of 12.5 mg/kg, whereas compounds Ⅵ and Ⅳ showed such an effect only at a dosage as large as 200 mg/kg.Since the improvement of the histological changes of the liver tissue by these substances did not seem parallel to their activities in lowering the SGPT level, the effectv of these agents on liver GPT(LGPT) level was studied. Compounds Ⅶ, Ⅴ, Ⅲ and Ⅱ were shown to lower the LGPT level. In another experiment it was found that the LGPT level of animals treated with compound Ⅱ 24 hours previously was lower than that of control animals. However, the LGPT level showed a tendency to increase, instead of decrease, if the drug was given 40 hours prior to sacrifice. So it is likely that the inhibition of these constituents on LGPT may be a temporary and reversible process.Glycogenesis was found to be promoted in fasted mice by the administration of compounds Ⅴ, Ⅳ, Ⅱ and Ⅰ, among which compound Ⅴ was the most effective with a potency comparable to that of cortisone. Since such an effect can also be shown in adrenalectomized mice, it is reasonable to presume that the effect of these agents on glycogenesis is not mediated by the pituitary-adrenal system. No effect on glycogenesis was demonstrated for Compounds Ⅲ, Ⅵ and Ⅶ.Compounds Ⅴ, Ⅱ and Ⅶ showed a biphasic effect on pentobarbital sleeping time(PST), i. e., the PST was prolonged when these agents were given one hour prior to the injection of pentobarbital, whereas the PST was shortened when the interval between the administration of the constituents and the hypnotic was 24 hours. Compound Ⅲ exhibited only the prolongation phase, while compound Ⅰ showed no significant effect on PST. This implies that these substances may have very different effects on the hepatic drug metabolizing enzyme system.