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 studies demonstrated,1,4-diarylbutane lignans and 8-O-4’ neolignans are characteristic constituents of G.littoralis planted in Laiyang of Shangdong province.These compounds exhibit antioxidant,antihypertensive,estrogen-like effects et al.activities.Besides Laiyang,Chifeng of Inner Mongolia is also a main habitat of G.littoralis.The geographical variation may be influence the constituents of G.littoralis.To illuminate the substantial basis, chemical constituents and bioacctivities of the roots of G.littoralis were investigated.The roots of G.littoralis were extracted with ethanol,and the extract was suspended in water, and then partitioned with pertroleum ether and EtOAc,successively.The EtOAc-soluble fraction was chromatographed on silica gel column,Pre.TLC,repeated Sephadex LH-20 and reverse phase ODS column chromatography to give sixteen compounds.Thirteen compounds’structures were elucidated by physico-chemical properties and spectral analysis.Among them,two new 1,4-diarylbutane lignan glycosides were named Glehlinoside E（1）,Glehlinoside F（3）,and one new 8-O-4’ neolignan glycoside was named Glehlinoside D（2）.Ten known compounds were identified as:Glehlinoside A（4）,panaxynol（5）,falcarindiol（6）,（8E）-1,8-heptadecadiene-4,6-diyne-3,10-diol（7）, xanthotoxin（8）,scopolin（9）,scopoletin（10）,marmesinin（11）,isoquercetin（12）and adenosine（13）.Compound 9 was isolated from this genus for the first time.The protective effect on rat brain acetylcholinesterase（AchE）inhibition induced by free radicals and the prolyl oligopeptidase inhibitory activity of EtOAc-soluble Fr.were investigated. The protective effect of EtOAc-soluble Fr.showed potent activity(EC₅₀=1.41mg/ml),whereas no significant impact on POP inhibitory activity.