黑水缬草神经保护活性成分研究

Study on neuroprotective active constituents from root and rhizome of Valeriana amurensis

目的对黑水缬草Valeriana amurensis抗阿尔茨海默症（AD）有效部位中具有神经保护活性的成分进行筛选,以阐明黑水缬草发挥神经保护作用的药效物质基础。方法采用各种色谱方法对黑水缬草抗AD有效部位进行化学成分分离,并根据理化分析及波谱数据进行结构鉴定;利用MTT法筛选具有PC12神经保护作用的单体化合物。结果从黑水缬草抗AD有效部位中共分离鉴定了11个化合物,包括5个双环氧木脂素类化合物：（＋）-梣皮树脂醇-4,4′-二-O-β-D-双吡喃葡萄糖苷（1）、（＋）-紫丁香-4,4′-二-O-β-D-吡喃葡萄糖苷（2）、青刺尖木脂醇苷（3）、（＋）-8,8′-二羟基-松脂素-4,4′-二-O-β-D-吡喃葡萄糖苷（4）、青刺尖木脂醇（5）和6个环烯醚萜类化合物：jatamanin A（6）、7-羟基-8-（羟甲基）-4-亚甲基六氢环戊烯[并]吡喃-1（3H）-酮（7）、4-羟甲基-环戊烯[并]吡喃-7-甲醛（8）、patriscabroside III（9）、jatamanin E（10）及败酱苷（11）。对其进行体外活性研究发现25、12.5和5μmol/L的双环氧木脂素类化合物均能明显减轻Aβ1-42所致PC12细胞损伤。结论环烯醚萜类化合物6~10为该植物中首次分离得到,双环氧木脂素类化合物为黑水缬草抗AD有效部位发挥神经保护作用的部分药效物质基础。

Objective To screen the active constituents from the anti-AD active fraction from the roots and rhizomes of Valeriana amurensis and to elucidate the therapeutic basis for the neuroprotective effect of the roots and rhizomes in V.amurensis.Methods The aective fraction of the roots and rhizomes in V.amurensis was separated with various chromatographic processes and the structures of the obtained compounds were identified by physicochemical analysis and various spectra data.The neuroprtective compounds on PC12 cells were screened by MTT assay.Results Eleven compounds were isolated from the roots and rhizomes of V.amurensis,including five bisepoxy lignans of（＋）-medioresinol-4,4′-di-O-β-D-glucopyranoside（1）,（＋）-syringaresinol-4,4′-di-O-β-D-glucopyranoside（2）,prinsepiol-4-O-β-Dglucopyranoside（3）,（＋）-8,8′-dihydroxy-pinoresinol-4,4＇-di-O-β-D-glucopyranoside（4）,prinsepiol（5）,and 6 iridoids of jatamanin A（6）,7-hydroxy-8-（hydroxymethyl）-4-methylenehexahydrocyclopenta [c] pyran-1（3H）-one（7）,4-hydroxymethyl-cyclopenta [c] pyran-7-carboxaldehyde（8）,patriscabroside III（9）,jatamanin E（10）,and patrinoside（11）.The Aβ1-42-induced PC12 cells injuries were alleviated by all the bisepoxy lignans with the concentration of 25,12.5,and 5 μmol/L.Conclusion Iridoids 6—10 are isolated from the roots and rhizomes of V.amurensis for the first time.Bisepoxy lignans are the therapeutic basis of neuroprotective effect in the roots and rhizomes of V.amurensis.