Effective Constitutions From Acanthopanax Senticosus(Rupr.&Maxim.)Harms And Their Inhibitory Activity Of PTP1B And NF-κB

OBJECTIVE:The constituents isolated from Acanthopanax senticosus (Rupr.& Maxim.) Harms were studied by bioassay-guided fractionation. The inhibitory acti-vity on protein tyrosine phosphatase 1B (PTP1B) and nuclear factor kappa B (NF-κB) was assayed.METHODS:The potential constituents were isolated from A. senticosus by using silica gel and C18 reverse phase column chromatography, semi-preparative HPLC technology and other separation methods. Their structures were eluci-dated on the basis of spectroscopic(1H-NMR,13C-NMR, HMBC and NOESY)and physico-che-mical analyses.RESULT:The fourteen compounds were isolated from the extraction of A. sent-icosus. The structures of 1-14 were established as 3-[3’-methoxy-4’-(4"-formyl-2",6"-dimethoxy-phenoxy)-phenyl]-propenal (1),3-[3’,5’-dihydroxy-4’-(4"-hydroxymethyl-3 ’,5"-dimethoxy-phenoxy)-phenyl]-propenal (2), sinapaldehyde (3), isovanillin (4),2,6-dimethoxybenzoic acid phenylmethylester (5), gramniphenol A (6), (-)-syringaresin-ol (7), syringin (8), (E)-2,3,5,4’-tetrahydroxystilbene-2-O-β-D-xylosi-de (9), torachr-ysone-8-O-β-D-glucoside (10),3β-hydroxy-28-norolean-12-ene-16-one 3-O-β-D-gluc-opyranoside (11),3β,17β-dihydroxy-28-norolean-12-ene-16-one 3-O-β-D-glucopyran-oside (12),3β-hydroxy-olean-12-ene-16,28-lactone 3-O-β-D-glucopyranoside (13) and eclalbasaponin Ⅱ (14). Five compounds (1-2,11-13) were reported for the first time.CONCLUSION:Inhibitory activity of PTP1B and NF-κB of all the isolates was evaluated. Compounds 1-4 and 6 exhibited significant inhibitory activity of PTP1B. Among them, compounds 1 and 2 showed selectivity of inhibition of PTP1B with IC50 values as 9.2±1.4 and 12.6±1.2μM. Compounds 11-14 inhibited NF-κB with IC50 values ranging from 8.3±0.7μM to 13.5±1.0μM.