五味子仁七种成分的一些药理作用比较

从北五味子乙醇提取物中得到七种单一成分,称为五味子甲素、乙素、丙素、醇甲、醇乙、酯甲、酯乙。这些成分能在不同程度上使CCL₄引起的高SGPT降低,其中酯乙与醇乙的作用最强;病理学观察也见到这些成分能或多或少地减轻肝细胞损伤,但与其降酶能力并不平行。进一步研究表明酯乙、醇乙等能明显降低肝组织GPT的活性,其原因可能是对于此酶的暂时性的可逆性抑制。醇乙、甲素、乙素、醇甲能明显促进外源葡萄糖生成肝糖元,此作用以醇乙最强(约与可的松相当)。由于在去肾上腺小鼠仍有此效,故其作用主要不是通过影响体内垂体-肾上腺系统。醇乙、乙素、酯乙对小鼠戊巴比妥睡眠时间有先延长、后抑制的双相性影响,但丙素只有延长作用。从动物实验看来,五味子这些成分的降SGPT作用可能部分地由于对肝内此酶的抑制,因此五味子治疗肝炎的临床效果应根据症状、体征及各种肝功化验综合评价,不宜单从降酶效果来判断。

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.