Chemical Constituents From The Roots And Rhizomes Of Clematis Hexapetala Pall.

The roots and rhizomes of Clematis hexapetala Pall.(Ranunculaceae)have been used as Clematidis Radix Et Rhizoma for expelling wind-damp and warming meridians,which is characterized by salty and pungent flavors,warm in nature,and it can be bladder through to treat rheumatic arthralgia,numbness,spasms and flexion,and negative extension.Using silica,Sephadex LH-20,ODS and preparative HPLC chromatographic methods,66 compounds were purified from the 50%EtOH-H2O elution part of the microporous resin HP-20 column,the 60%EtOH-H2O extract.Structures were elucidated via UV,IR,NMR,MS,followed with a modified Mosher's method and calculated ECD analysis.6 guaianolide sesquiterpenoids(1-3,13-15),5 prenylated 1,2,3,4-tetrasubstituted phenolic or benzyl alcohol glycosides(4-8),41 lignans(9-10,22-60),8 phenylpropanoids(11,17-18,61-65),2 glucogallic acid glucosides(12,16),2 stilbenes(20-21)and 2 phenols(19,66)were gained,and among them were 12 new compounds(1-12),and 14 known compounds(13-17,20,22,35,44-47,65-66)were isolated for the first time from the Clematis,and compounds except 22,30,31 were isolated from the plant for the first time.Compounds 1-3 were confirmed as guaianolide sesquiterpenoids,which were found from the Clematis for the first time.The absolute configurations were ascertained via a modified Mosher's method.Compounds 4-8 were prenylated 1,2,3,4-tetrasubstituted phenolic or benzyl alcohol glycosides,and the prenyl moiety looped with the adjacent phenolic hydroxyl,and formed 6/6 and 6/7 rings.Furthermore,the possible biogenetic pathways for the aglycones of 4-8 were proposed.Compounds 9-10 were new lignan diglucosides.All isolates(10 ?M)were in vitro screened for anti-inflammatory inhibition against TNF-? and NO release in RAW 264.7 macrophages stimulated by LPS.Compounds 15 and 20 exhibited moderate inhibition ratios of 49.46%and 62.50%,and no compounds showed significant inhibition against NO release.Besides,20 showed moderate 86.0%inhibition to PTP1B.Unfortunately,no compounds showed significant cytotoxicity against HCT-116,HepG2,BGC-823,A549 and U251.And no compounds showed significant inhibition to Calpain at 1 mM?10?M.All above enriched the phytochemical studies of C.hexapetala Pall.,and established a pharmacological basis for further researches on active ingredients and provided references for its utilization.