| Up to now,the most reported β-dihydroagarofuran sesquiterpene polyesters have been isolated and seperated from plants of Celastraceae family,the dihydroagarofuran skeleton with different esters makes their chemical structures complex and diverse,consequently present a wide range of biological activities,such as insecticidal activity,anti-inflammatory activity,antitubercular activity,antitumor activity and cytotoxic activity.Parnassia wightiana W.is a plant from Saxifragaceae family,which have been used as Chinese folk medicine for treating diseases such as rheumatism,lithiasis,hypertension and malaria.In 2012 we began to study the chemical constituents of Parnassia wightiana W.and separated 3β-dihydroagarofuran sesquiterpene polyesters.In this research acaricidal activity analysis and cytotoxic activity of the β-dihydroagarofuran sesquiterpene polyesters from Parnassia wightiana W.were conducted,besides,their structure-activity relationship were elaborated.1.Through established a reasonable and doable method to extract and isolate Parnassia wightiana W.:industrial alcohol as extract solvent,assistant of ultrasonic wave,with moderate heating and circulatory stir;EtOAc-H2O as extraction system,major separation methods include column chromatography,thin-layer chromatography preparation and HPLC preparation,consequently got 9 β-dihydroagarofuran sesquiterpene polyesters and among the compounds,JT(1α,2α,6β,8β,15-pentaacetoxy-9β-benzoyloxydihydro-β-agarofuran)and Y-1(1α,2α,6β,8β,1 5-pentaacetoxy-9β-benzoyloxy-4β-hydroxydihydro-β-agarofuran)were the first time seperated from this plant.2.Preliminary study of acaricidal constituents in Parnassia wightiana W.shows that the EtOH extraction and EtOAc extraction obtained from the plant material which was extracted sequentially by 4 solvents possess mortality 76.7%and 22.5%respectively against acarid when the concentration was 10 mg/mL,which indicates that the polarity of acaricidal constituents distribute between EtOAc and EtOH.3.7 compounds from Parnassia wightiana W.were evaluated for in vitro cytotoxic properties against HL-60,SMMC-7721,A-549,MCF-7 and SW480 cell lines by MTT assays.The compounds 2-5,2-7 and 3-3 exhibited moderate activities with IC50 values ranging from 11.8 to 30.1 μM.Preliminarily structure-activity relationship analyse of 7β-dihydroagarofuran sesquiterpene polyesters showed that introduction of 2-OH or 8-OH were beneficial for the improvement of the activities against most of the cell lines;the combination of 1,8-dihydroxy groups was able to make the higher activities than that of 2,8-dihydroxy groups. |
