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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 anti-Alzheimer’s (AD) neuroprotective components of Valeriana amurensis in order to elucidate the pharmacological basis of the neuroprotective effect of Valeriana amurensis. Methods Various chromatographic methods were used to separate the active components of Valerian anti-AD against chemical constituents. The chemical constituents were identified by physicochemical analysis and spectroscopic data. The compounds with the neuroprotective effect of PC12 were screened by MTT assay. Results A total of 11 compounds were isolated and identified from the active sites of Valeriana officinalis, including 5 bisepoxyignans: (+) - ecdysteroid -4,4’-di-O-β- D-glucopyranoside (1), (+) - lilac-4,4’-di-O-β-D-glucopyranoside (2) (+) - 8,8’-dihydroxy-pinorin-4,4’-di-O-β-D-glucopyranoside (4) Ether Terpenoids: jatamanin A (7), 4-Methoxyhexahydrocyclopenteno [pyrrol-1 (3H) -one -hydroxymethyl-cyclopenten [o] pyran-7-carbaldehyde (8), patriscabroside III (9), jatamanin E (10) and patrinis (11). In vitro activity studies showed that 25,12.5 and 5μmol / L of bis-epoxy lignan compounds can significantly reduce Aβ1-42-induced PC12 cell damage. CONCLUSION Iridoid compounds of 6 to 10 were isolated from this plant for the first time. Dicloxyignans are the basis of some pharmacodynamic substances that protect the effective site of AD from anti-AD.