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

作　　者：Si-wen Han Sheng-ming Shi Yu-xiao Zou Zhi-cheng Wang Yan-qun Wang Lin Shi Ting-cai Yan 

机构地区：[1]College of Food Science,Shenyang Agricultural University,Shenyang 110866,China [2]Tianjin Press of Chinese Herbal Medicines,Tianjin Institute of Pharmaceutical Research,Tianjin 300462,China [3]Dalian Institute for Drug Control,Dalian 116021,China [4]Key Laboratory of Healthy Food Nutrition and Innovative Manufacturing of Liaoning Province,Shenyang Agricultural University,Shenyang 110866,China

出　　处：《Chinese Herbal Medicines》2020年第2期195-199,共5页中草药（英文版）

基　　金：supported by the National Natural Science Foundation of China(No.81602983)。

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.

关 键 词：Panax quinquefolius L total saponins acid hydrolysis hypoglycemic effect 

分 类 号：R285[医药卫生—中药学] R284[医药卫生—中医学]