Chemical constituents from acid hydrolyzates of Panax quinquefolius total saponins and their inhibition activity to α-glycosidase and protein tyrosine phosphatase 1B

摘要

Objective:To investigate the hypoglycemic components from the acid hydrolyzates of Panax quinquefolius total saponins,and screen the active compounds by in vitro inhibitory activities toα-glycosidase enzymes and protein tyrosine phosphatase-1 B(PTP1 B).Methods:The hydrolyzates were chromatographed repeatedly over silica gel column,and the structures of the compounds were determined by means of NMR.The in vitro bioassay was performed through the inhibitory effects onα-glucosidase or/and PTP1 B.Results:Eight compounds were isolated,which identified as 20(S)-panaxadiol(1),(20 S,24 R)-dammarane-20,24-epoxy-3β,6α,12β,25-tetraol(2),20(R)-dammarane-3β,12β,20,25-tetraol(3),20(S)-dammarane-3β,6α,12β,20,25-pentol(4),20(R)-dammarane-3β,12β,20,25-tetrahydroxy-3β-O-β-D-glucopyranoside(5),β-sitosterol(6),oleanolic acid(7)and 20(S)-protopanaxadiol(8).Compound 5 was ginseng triterpenoid isolated from the acid hydrolysates of total saponins from P.quinquefolius for the first time.In this paper,the possible in vitro inhibitory activities were investigated.Compound 5 exhibited significantly inhibitory activity againstα-glucosidase,and the IC50 value[(0.22±0.21)μmol/L]was about 43-fold lower than positive control.For the PTP1 B inhibition assay,compound 5 indicated the strongest inhibitory effect with IC50 of(5.91±0.38)μmol/L,followed by compound 4 with IC50 of(6.21±0.21)μmol/L,which were all showed competitive inhibitory pattern by using a Lineweaver-Burk plot.Conclusion:These results supported the potential application of dammaranes from acid hydrolyzates of P.quinquefolius total saponins can be used as ingredients of ancillary anti-diabetic agent or functional factor.