Zhang L, Niu X
Institute of Materia Medica, Beijing.
Zhongguo Yi Xue Ke Xue Yuan Xue Bao. 1991 Feb;13(1):13-6.
Schizandrol A (2',3',4',1",2",3"-hexamethoxy-6, 7-dimethyl-1,2,3,4-dibenzo-1,3-cyclooctadien-6-ol) is one of the effective components in the dried fruit of Schizandra chinensis Bail. Previous studies have found that schizandrol A exerts inhibitory effects on the central nervous system (CNS). For the purpose of elucidating the mechanism of inhibition, the concentrations of monoamine neurotransmitters and their metabolites in rat brain and the effects of schizandrol A on some receptors were determined by the ion-pairing reversed-phase liquid chromatography with electrochemical detection method and competitive binding assay. In the neurotransmitter studies, significant elevations of dopamine and its metabolite DOPAC (in striatum) and DA (in hypothalamus) were observed after i.p. administration of 50 mg/kg or 100 mg/kg of schizandrol A. But the receptor binding experiments showed that schizandrol A had no affinity for dopamine D1 and D2 receptors. Serotonin receptors and alpha 1-,alpha 2-adrenergic receptors, and it did not affect the binding of dopamine to dopamine D1 or D2 receptors. These results indicate that the inhibition exerted by schizandrol A on the CNS may be related to the dopamine system, and the increase of dopamine turnover has nothing to do with dopamine receptors. The concentrations of the norepinephrine metabolite MHPG and the serotonin metabolite 5-HIAA showed changes in rat striatum and hypothalamus after schizandrol A treatment, but norepinephrine and serotonin levels were unaffected.
五味子醇甲(2',3',4',1",2",3"-六甲氧基-6,7-二甲基-1,2,3,4-二苯并-1,3-环辛二烯-6-醇)是五味子干燥果实中的有效成分之一。先前的研究发现,五味子醇甲对中枢神经系统(CNS)具有抑制作用。为了阐明其抑制机制,采用离子对反相液相色谱-电化学检测法和竞争性结合试验,测定了大鼠脑中单胺类神经递质及其代谢产物的浓度以及五味子醇甲对某些受体的影响。在神经递质研究中,腹腔注射50mg/kg或100mg/kg五味子醇甲后,观察到多巴胺及其代谢产物DOPAC(在纹状体中)和DA(在下丘脑中)显著升高。但受体结合实验表明,五味子醇甲对多巴胺D1和D2受体无亲和力。血清素受体以及α1-、α2-肾上腺素能受体,并且它不影响多巴胺与多巴胺D1或D2受体的结合。这些结果表明,五味子醇甲对中枢神经系统的抑制作用可能与多巴胺系统有关,多巴胺周转率的增加与多巴胺受体无关。五味子醇甲处理后,大鼠纹状体和下丘脑中去甲肾上腺素代谢产物MHPG和血清素代谢产物5-HIAA的浓度发生了变化,但去甲肾上腺素和血清素水平未受影响。