Studies On Chemical Constituents And Bioactivity

Coastal Glehnia Root is the dried root of Glehnia littoralis Fr. Schmidt ex Miq. (Fam. Umbelliferae). It’s used in traditional Chinese medicine as tonic, antiphlogistic, and mucolytic for the treatment of respiratory and gastrointestinal disorders. Previous investigations resulted in the isolation of coumarins, polyacetylenes, lignans, phenolic acids, and nucleotides etc. On the other hand, it has been reported that this crude drug exhibited many pharmacological activities, including antitumor-promotion, antimutation, antitumor, antibacterial and antifungal, analgesicand sedative, inhibition of tyrosinase, and immunosuppressive activities.In this study, chemical constituents of the roots bark of G littoralis and the protective effect on rat brain acetylcholinesterase (AChE) inhibition induced by free radicals and the prolyl oligopeptidase inhibitory activity were investigated.The roots bark of G. littoralis were extracted with ethanol, and the extract was suspended in water, and then partitioned with pertroleum ether and EtOAc. The H2O-soluble fraction was chromatographed on macroreticular resin column, repeated Sephadex LH-20 and reverse phase ODS column chromatography to give eight compounds. The compounds’structures were elucidated by physico-chemical properties and spectral analysis. The compounds were identified as:glehlinoside A (1), (-)-secoisolariciresinol 4-O-β-D-glucopyranoside (2), glehlinoside E (3), glehlinosiden (4), protocatechuic acid methyl ester (5), esculetin (6), baihuaqianhuside (7), xanthotoxol 8-O-β-D-glucopyranoside (8). The EtOAc-soluble fraction was chromatographed on silica gel column, repeated Sephadex LH-20 and reverse phase ODS column chromatography to give six compounds, they were identified as glehlinoside D (9), (-)-secoisolariciresinol (10), ferulic acid (11), caffic acid (12), vanillic acid (13), and syringe (14). Compound 4,5 and 6 were isolated from this genus for the first time.The protective effect on rat brain acetylcholinesterase (AChE) inhibition induced by free radicals of EtOAc-soluble Fr. and H2O-Soluble Fr. were investigated. The protective effect of EtOAc-soluble Fr. and H2O-Soluble Fr. showed potent activity, whereas the POP inhibitory activity. still need further investigation.