大鼠大脑皮层细胞膜色谱法筛选老瓜头镇痛活性成分研究

Screening of Active Components of Cynanchum komarovi Al. Iljinski with Analgesic Effects Using Rat Cerebral Cortex Cell Membrane Chromatography

从老瓜头二氯甲烷、乙酸乙酯萃取层得到4个化合物,分别为新白前酮(1)、邻苯二甲酸二丁酯(2)、华北白前醇(3)、β-谷甾醇(4);正丁醇层得到2个化合物,分别为3-甲氧基-4-羟基苯甲酸(5)、对羟基苯基酸(6);总生物碱中分离到1个化合物,鉴定为7-脱氧基娃儿藤碱(7)。大鼠大脑皮层细胞膜色谱模型上发现乙酸乙酯、正丁醇层在CMC固定相上无保留,二氯甲烷层有弱保留,总生物碱有强保留;化合物1有弱保留,化合物3、7有强保留,保留因子分别为1.5、23.0、20.0。本实验建立的CMC模型可正确反映活性部位、活性成分与细胞膜及膜受体的相互作用,初筛得到3个可能具有镇痛活性的痕量单体化合物,2个为非生物碱,1个为菲骈吲哚里希啶类生物碱,为老瓜头后续研究奠定基础。

In this study, four compounds were isolated and elucidated as hancolupenone （1）, phthalic acid dibutyl ester （2）, hancockinol （3） and fl-sitosteml （ 4 ） from CHCl2 and ethyl acetate fractions. 3 -methoxy-4-hydroxybenzoic acid （ 5 ） and p-hydroxybenzoic acid （6）were obtained from n-butanol fraction. One alkaloid was isolated from crude total alkaloids and was elucidated as 7-demethoxylophorine（7）. The ethyl acetate and n-butanol fractions had no retention on rat cere- bral cortex cell membrane column. The CHCl2 fraction had a weak retention while crude total alkaloid has a strong reten- tion. Compound 1 had a weak retention and compound 3 and 7 had a strong one with retention factor 1.5,23.0 and 20. 0,respectively. The established CMC model correctly reflected the relationship between the cell membrane or mem- brane acceptor and effective parts and compounds. Two non-alkaloid compounds possibly had strong analgesic effects to- gether with a known alkaloid.